Combo with Pharm Drugs *ALL*
*nitroprusside
This drug is used for hypertensive crises and acute aortic crisis. It can precipitate angina in patients w/CAD due to coronary steal.
Warfarin
Anti-coag Comp (-) Vit K epoxide reductase (factors 9,7,10,2) *Makes WAR with the KKK outside (extrinsic)--long war (chronic) Chronic anti-coag; Watch PT/INR (extrinsic) Tx risk thrombosis & embolism, A fib, prosthetic valves, stents/grafts Teratogenic!!
Rivaroxaban
Anti-coag Direct (-)Xa *Rivarox BANS the X LONG TERM anti-coag Tx DVT and thromboembolitis
Fondaparinux
Anti-coag Induces(-)Xa *Fond of inducing need of a repair in X Rapid anti-coag; watch pTT (intrinsic) Tx Risk thrombosis & embolism, safe in pregnancy
Heparin
Anti-coag Sulfated proteoglycan binds to anti-thrombin; INACTIVATES 12a,11a,9a / 10a & 2a *Heparin: HE pairs with them inside (intrinsic); quick match (acute) Rapid anti-coag; watch pTT Tx risk of thrombois/embolism; safe in pregnancy
Vasodilators
Calcium blocker (dipine, idil, amil): verapamil, nifedipine, felodipine, diltiazem, bepridil, mibefradil **Diping my IDIL in A Milk Nitrates: nitroglycerin, amyl nitrate, isosorbide dinitrate, nitroprusside **NITRO (-)Alpha1: prazosin, doxaxosin, terazosin **LOSIN (loosenin) vessels (-)Beta1,2: Propranolol K arterial relaxants: Diazoxide, hydralazine, minoxidil, pinacidil, nicorandil **OXIDIL, OXIDE, ALAZINE (-)ACE: Captopril (-)AngioRec: Losartan, valsartan, ibesartan, candesartan (-)Renin: Aliskiren (-)Phosphodiesterase 5: Sildenafil (viagra), Vardenafil (levitra), Tadalafil (cialis)
*verapamil
Calcium channel blocker prototype: blocks "L−type" channels; cardiac depressant and vasodilator; used in HTN, angina, and arrhythmias. Tox: AV block, CHF, constipation
*Clopidogrel
Blocks platelet ADP receptors on platelets (ADP binding stimulates insertion of GpIIb/IIIa receptors on platelet membrane). Irreversibly inhibits platelet aggregation. Uses: TIA, prevent strokes, prevent restenosis after placement of coronary stents. Tox: bleeding, neutropenia. Others: Ticlopidine (higher risk of neutropenia and TTP).
*bepridil
CCB that also blocks Na channels in heaert, prolongs QT interval can --> arrhythmias (torsade de pointes - Rx = Mg) used if don't respond to other Antianginals
Clofibrate
Fibrate *Fibrate Inc LPL & catab CM/VLDL, dec VLDL release, inc HDL Tx HyperTG, type III after gemfibrozil
Gemfibrozil
Fibrate - best one *This fibrate is a gem Activate PPAR, inc LPL Decrease: adipose lipolysis, liver TG synth, VLDL secretion Tx: HyperTG
*gemfibrozil
Fibrate antilipemic: activates PPAR-a nuclear receptors; lowers serum triglycerides via stimulation of lipoprotein lipase activity. Used in hypertriglyceridemias and mixed triglyceridemia/hypercholesterolemia. Tox: GI distress, cholelithiasis, skin rashes, increased risk of myopathy when combined with statins or niacin.
Streptokinase
Fibrinolytic Bacterial protein: activates plasminogen *strepto stripped off & copied TPA's play Acute thrombolytic therapy (breaks clot); use with anti-PLT and anti-coag Tx Acute MI, stroke (use within 6-12 hours)
Tissue Plasminogen Activator (TPA)
Fibrinolytic Protease binds fibrin; activate plasminogen *TPA: activates plasmin! Acute thrombolytic therapy (breaks clot); use with anti-PLT and anti-coag Tx Acute MI, stroke (within 6-12 hours)
Urokinase
Fibrinolytic Protease from renal epith: activates plasminogen *Uro from the urine isn't kind to fibrin Naturally in urinary tract. Acute thrombolytic therapy (breaks clot); use with anti-PLT and anti-coag Tx Acute MI, stroke (use within 6-12 hours)
Diazoxide
K arterial relaxant (arteriolar dilatation) *Diazoxide gets the K outside Use with diuretic, B-blocker, and ACE inhib Tx HTN, increase C.O.
*colestipol
bile acid sequestrant / lipid lowering agent (hypercholesterolemia, pruritus r/t elevated bile acids; unlabled: diarrhea r/t elevated bile acids) COLESTID
Cimetidine Ranitidine Famotidine Nizatidine
"-tidine: Table for 2; H2 before you dine" *H2 antagonist; quick 30 min relief Ind: ulcers, zollinger ellison syndrome, GERD *Get ulcer relapse Cimetidine: anti-androgen effects, p450 inh (warfarin, BZD, theophyl, beta blockers, Ca chnnel blockers, phenytoin, carbamazepine, phenobarbital)
Noreethindrone Norgestrel
"19-NOR steroids" Progestins with low androgen activity Ind: Combo contraceptive or ALONE if estrogen CI *if alone: worse lipid effect than progesterone! also androgenic s/e
6-MP 6-TG
"6-Mercaptopurine: puts a cap on purines" *ALL: VM6P; CML "6-Thioguanine: stop thy guanine" *AGL Purine analogs: Hypoxanthine & Guanine *HGPRTase activates it to thiolMP / thioGMP which inh 1st step of purine biosynth *6-TG more readily incorporated into DNA Use: 6MP for ALL & CML; 6TG for AGL Note: Xanthine oxidase breaks down 6-MP (allopurinol inc potency) *NOT with 6-TG
Amantadine Rimantadine
"A man to dine takes off his coat" & "A for infl A" Targets M2 (proton transporter) to prevent uncoating virus Use: 1) Prophylax for Infl A & 2) Parkinson's disease S/E: GI, reversible lCNS effect (dopamine effects--insomnia, anxiety, psychosis
Aprepitant ($)
"A prayer w/ the NKiller penetrating brain" Block NK1 (CTZ, VC) Crosses BBB Ind: Acute-delayed CINV S/E: p450, dizzy, diarrhea, dehydrate, hiccups
Attapulgite
"A tap of clay" Gel forming antidiarrhea Ind: acute diarrhea
Atropine Scopolamine Propantheline Methantheline
"A trip to pine blocks muscarine" "Scope on cruise: look at the line" Anti-chol: block secretion and peristalsis Ind: relief of cramp Negligable effect on diarrhea S/E from antichol (hot as hair...)
Atropine
"A tripe to pine blocks Musc-a-rine" *Life saving tx if organophosphate toxication (malathione eg)
Aztreonam
"AZ tree" Monobactam Very narrow (G- rods - PKS) *use: penicillin allx & renal insuff w/ intolerance to aminoglycosides
Sulfonurea 1st gen: Tolbutamide, tolazamide, chlorpropamide
"Amide told Chlora to get her BUT into gear" Block K channel in Beta cell; trigger insulin release Only T2DM S/E of sulfonureas: weight gain common, dec iodine uptake, GI anorexia & n/v/d *1st gen: disulfiram like effect *Tolbutamide: CV deaths *Chlorpropamide: ADH-like effect (don't use with elderly) DI: NSAID, salicylates, warfarin/dicoumarol
Deferoxamine
"Amine for a little time"-acute Fe & Al Bind Fe3+; no removal of Fe from Hb, Mb, cytochromes Use: ACUTE Fe poisoning (some Al) Tox: hypoTN (quick passing), flush, abd pain, rash
Streptomycin Gentamycin (Tobramycin, amikacin, neomycin)
"Aminoglycoside pic" & buy AT 30 Use: Gram (-) rods & enterics *Gentamycin: DOC for severe sepsis & pneumonia *Neomycin: bowel sx *use w/ b-lactam for synergy S/E pic (nephro, ototoxic, teratogen)
Amphetamine Diethylpropion Phentermine
"Amp up DANE" Decrease appetite (anorexogenic" Ind: obesity CI: CV disease/HTN & pregx Dependance issue Amphetamine: CNS stimulation; get tolerance to weight loss fast *Other 2 less CNS effect; but phentermine has insomnia
Amphotericin B
"Ampho tears holes at ergosterol" DOC: serious systemic mycoses *only if life threatening due to s/e S/E: binds cholesterole: *nephrotoxicity 100% (K/Mg wasting) *anemia, IV phlebitis, shake & bake, hypoTN
Anastrozole Exemestane
"Ana take a stroll and ex aromatase" Tx: breast cx S/E: hot flashes, severe long term effects on bone & cholesterol (no estrogen: no bone, high LDL)
Antilymphocyte & Anti-thymocyte Globulin (ALG & ATG)
"Anti-thymocyte= anti-Tcell" Immunosuppressive Ab Only block ADAPTIVE cellular immunity (no effect on humoral) *ALG/ATG binds tcells and activate complement Use: REVERSE allograft rejection Tox: over immunosupp->opportunistic infxn, type3hypersens *unwanted antibodies->serum sick, glomerulonephritis, granulocytopenia
*Ticlodipine
"Antiplatelet Agent" ADP Receptor Antagonists Brand name: Ticlid -inhibits ADP activation of platelets and thrombus formation -arterial thromboembolism,MI, stroke prevention -acute coronary syndromes STEMI,NSTEMI,UA
Ticarcillin Piperacillin Carbenicillin
"Antipseudo picture" Penicillinase sensitive (not for staph aureus or e. faecalis) IV only
Atovaquone + proguanil
"At any moment vanish-last minute travel" Antimalarial Atov: block plasmodium mitoch Proguanil: block plasmodium DHFR Tx: for chloroquine resistant areas (1-2 days prior)
Atropine, propantheline, isopropamide
"Atropine blocks muscarine" Block ACh stim & motility S/E: Blind as a bat... (dry mouth, constipated)-intolerable
Azathioprine
"Aza is a 6MP & 6TG precursor) Cytotoxic agent *block DNA synth (in lymphoid cells) Use: organ allograft & solid organ transplants Tox: bone marrow suppression (severe leukopenia), hepatoxicity
IFN alpha2a Lamivudine/entacavir + Adefovir/tenofovir
"B has Both Lamiv + tenofovir" Use: Hep B SQ Tox: flu like, CNS (depress), hem Combo thx: Adeofovir/tenofovir + lamibudine or entecavir
Dacarbazine
"BVDD"-hodgkins and soft tissue "D for diazomethane metabolite" Mech: alkylate *inhibit RNA/protein synth Use: hodg/soft tissue, Malignant melanoma Tox: moderate myelosuppression, flu-like Activation: liver (diazomethane) *carbonium ion and alkylate DNA
Testosterone Methyl-testosteron Oxandrolone/Nandrolone
"Become like an ox w/ androgens" Tx: hypogonad, libido, anemia 2nd line, muscle/bone wasting *ANABOLIC S/E: virilization, smaller testis, CV, oily skin/acne *Methyl-test: jaundice, liver tox & cx
Albendazole & Mebendazole
"Bendazole for bendy worms" "Azoles are a**holes--steel all the beta tubulin" Anti-helminths Bind free beta-tubulin (no tubulin polymerization) Albend DOC: larval tapeworms and adult tapeworms Mebend DOC: ascaris, hookworm, pinworm, whipworm (larval and adult) Mebendazole has better thx index
Benzodiazepines
"Benzos slow the CNS" +GABA Chloride channel, hyperpolarize cells **Zepams and Zolams Alprazolam: short trip to alps Lorzaepam: Lorry and the bedtime story Oxazepam: pulse ox after seizure Tirazolam: try falling asleep Chlordiazepoxide: clings onto pills Diazepam: all day covererd everything Flurazepam: flury keeps the furry outside Temazepam: team is trying to fall asleep Midazolam: in my days we used a pendulum Chlorazepate: gastric juice Clonazepam & fenoldopam: panic, HTN, anti-convulsant Estazolam Quzepam Prazepam
Bethamethasone Dexamethasone
"Beth stays days" (36-54 hrs) Prednisolone deriv w/ 16beta/alpha methyl group Dexamethasone Suppression test *pituitary cushing's will drop ACTH Unbound to albumin
Bevacizumab
"Beverly hates Vegetables" Antibody inh VEGF Use: colon cancer
Bismuth subsalicylate Bismuthane
"Bismuth business to build mucus" Subsalicylate inhibit COX (dec PG) Anti-diarrhea Ind: traveler's diarrhea (prevent/tx) S/E: tongue & stool black; salicylate toxicity
Bleomycin
"Blow in free radicals" DNA fragmentor *BEC & BVC (testicular cx), BVDD (hodg/lymphoma) Mech: Copper chelating glycopeptides-chelates iron->free radicals (dna frag/break) *Resistance: hydrolase (low in skin and lung) Cell cycle: G2 Don't use with sarcomas (high hydrolase) Tox: B for lungs (pulm fibrosis) *O2 will exacerbate *VERY LITTLE myelosuppression (combo thx)
Busulfan
"Bus full of grains - CGL" "B for lung diagram"-fibrosis Aklyl sulfate: Same mech as nitrog mustard Use: CGL Tox: myelosuppressive (only granulocytes - why use for grains CGL), Busulfan lung Less reactive than mustards Excreted as methan and sulfonic acid
Cisplatin/Carboplatin
"C for ears and kidneys" "BEC & BVC use in testicular cx" Mech: Cs for low Cl areas (intracell activation) *alkylate guanine OR proteins Use: testicular, ovarian cx Tox: kidney and ototoxic
Peggylated IFN alpha2a + Ribavirin
"C those ribs..." IFN: antiviral, antiprolif Use: Hep C SQ admin Tox: flu-like, CNS (depress), hematologic
Dronabinol (Nabilone)
"Cannibol" - a cannabinoid Unk MOA Ind: cancer chemo (CINV) *NOT motion sickness S/E: sedation, dry, ortho hypoTN, munchies, abuse
Caspofungin
"Casper the fungal wall" Inh beta glucan synthesis for cell wall Tx: deep candidiasis, invasive aspergillosis s/e: GI & flushing
Chloroquine
"Claire has malaria-give Chloroquine" Antimalarial Block plasmodium heme polymerase DOC: P falciparum (acute, not resistant) *chemoprophylax in non-res areas s/e: retinopathy, visual disturb
Clindamycin
"Cleaning mice" Use: severe anaerobic infxn, penetrating wound to abd/gut (use with amino or ceph), prophylaxis BE if penicillin allx S/E: AAC
Clonidine
"Clony gives neg feedback at dinner" Alpha 2 agonist Dec secretion/diarrhea Ind: HTN
Clomiphene
"Come ovulate!" SERM Dec estrogen feedback inhibition (enhance FSH)--occupies the estrogen receptor S/E: limited; hot flashes
Cyclophosphamide
"Cycle of CD and CM high fives on breast" "Cycle through shirts due to mustard stains" **most used nitrogenous mustard Nitrog Mustard (cross link DNA) *Guanine (at N-7) in monoalkylated-pair with thymidine Use: CA5, CM5 (breast) Tox: breakdown acrolein (hem cystitis), marrow suppression (but less that mechlor), alopecia *tx: mesna or N-acetylcystein & fluid *bioactivation in liver...
Acyclovir Valacyclovir (intestines hydrolyze this to acyclo)
"Cycle of cars during NA dinner" & "hsv and zvz pic" Block DNA polymerase and chain term Guanosine analog-viral thymidine kinase does firstphosphorylation Use: VZV & HSV PO or IV (valacyclovir is only PO)
Cyclophosphamide
"Cycle through those mustard shirts" Cytotoxic Agent - nitrogen mustard *alkylate DNA (kill activated Tcells) Use: severe autoimmune (SLE, scleroderma) Tox: pancytopenia, hemorrhagic cystitis (CY)
Cyclosporine
"Cyclo cycled to the store and stole CyPA" Immunophilin ligand *bind cyclophillin (CyPA)-> CsA/CyPA complex blocks CaN (can't activate NFAT and NO IL2 production) *NFAT normal activated from TCR ligation on APC Use: solid organ transplant, GVHD, RA... Tox: NEPHROTOXIC, deadly herpes (and other viral infxns) *common S/E: neurotoxic, hirsutism, moobs, gingival hyperplasia, hyperK, HTN, DM
Cyclosporine
"Cyclosporine is last cycle" UC flare ups: last resort Immunosuppressive
Daclizumab
"Dac binds IL-Dos R" Immunosup antibodies *Bind IL-2 Receptor (not Tcell prolif) Use: prevent renal transplant rejection Tox: infxn, lymphoma, hypersensitivity
Chenodeoxycholic acid Chenodiol
"Deoxycholic = deGallstone" "Chenodiol is cholesterol die all" *HMG-CoA reductase inh S/E: diarrhe 40%, liver dysfunction, inc LDL
Ursodiol Ursodeoxycholic acid
"Deoxycholic = deGallstone" Ursodiol: "bile chol & lipid sec die all" Does NOT affect CYP7A (won't effect cholesterol metabolism CI: chronic liver disease or allx to bile acid
Dimenhydrinate Diphenhydramine Meclizine Promethazone
"Dimen Divers Make Pros HISS" Anti-histamine w/ antimuscarinic (VC) Ind: motion sick, post-op n/v *careful: pregx Ind: vertigo (give meclizine) S/E: antimusc (dry as a..)
Etidronate
"Dronate: drone attack on osteoclast" "Eti is akin to dronates: non-amino" Binds hydroxyapatite crystal; osteoclast apoptosis Tx: Pagets, malignant hypercalcemia, osteoporosis S/E: esoph irritation, GI bleed *long term: osteomalacia
Alendronate Ibandronate
"Dronate: drone attack on osteoclast" 2nd gen amino-bisphosphonate Block farnesyl disphosphate synthase (impair osteoclast post-translation modifications Ras,Rho,Rac) *osteoclast death Tx: pagets, Ca malignancy, osteoporosis S/E: osteonecrosis of jaw; NO reflux, no osteomalacia
Erythromycin
"Earth keeps on movin - motilin" Binds nerve and musc motlin R Ind: diabetic gastroparesis S/E: abd cramps
Edetate (Ca EDTA)
"Edetate is on/off date" Chelates extracellular Fe *also some Zn, Mn, Ca (give Ca salt) Use: Pb in adults *Chronic: use on/off schedule (Pb redistrib)
NNRTI: Efavirenz Nevirapine Delavirdine
"Elfs Never Deliver" Bind RT at allosteric site; also inh DNA dep DNA polym Efavirenz: 1st line combo thx *CNS sx, avoid if px Nevirapine: hepatoxicity Delavirdine: Rash DI due to p450
Imipenem + Cilastatin Meropenem
"Emmy penny" Carbapenem BROADEST beta-lactam (G+/-, anaerobes..) *GSW & mixed infxns Crosss allergenicity w/ penicillin Resistant: E faecium, MRSA, c diff
Anti-TNF-alpha Monoclonal antibodies
"Etanercept intercepts TNF" Immunosuppressive antibodies *Anti-TNFalpha antibody (neutralize alpha/beta) *prevent IL1,6 response (no leukocyte activ) Use: Arthritis, UC, Chronic plaque psoriasis, akylosing spondylitis Tox: swell/red, inc lymphoma (tumor necrosis factor...)
Methyl ter-butyl ether
"Ether lipid solvent"-GB Direct injxn into GB for small stones
Ethionamide
"Ethio blocks myco" 2nd line antiTB Rarely used
Exenatide
"Ex for ex copies: GLP-1 analog" Stimulates glucose-dep insulin secretion, inh glucagon, promote satiety, less gastric emptying Weight loss, dec HbA1C S/E: GI n/v/d, teratogenic
Imatinib mesylate (Gleevac)
"Eye mat & CML" Tyrosine Kinase inhibitor CML: philadelphia chromosome; Bcr-Abl oncoprotein *Inh Bcr-Abl = apoptosis/remission Use: CML and some others Resistance: mutations in Abl kinase
Foscarnet
"Fast Cars at dinner" "Fast car used to catch all runaway resistant viruses" Block DNA polym & chain term PPi (pyrophosphate) analog "FOScarnet = pyroFOSphate analog" Use: acyclovir-res HSV, VSV & gangciclovir-res CMV S/E: nephrotoxic (pyrophosphate)
Anastrozole
"Fat Ana says no more estrogen!" Inh aromatase (testosterone->estrogen) Use: breast cx
Fenfluramine (w/ phetemine: Fen-Phen)
"Fen says I'm full - 5HT" Promotes satiety Ind: obesity S/E: sedation, mild euphoria *rebound depression *off market now because of toxic effect: heart valve, pulm HTN "it's also full of S/E"
Fenastride
"Finally stop staring at baldy" 5-alpha reductase inhib Tx: BPH & male pattern baldness
Fludrocotisone Acetate
"Flood for aldosterone effects" Mineralocorticoid Use: Addisons (must use), congenital adrenal hyperplasia (CAH)
Fluoroquinolones (moxi/levo/gatifloxacin)
"Fluoro pic" 2nd line antiTB Ind: M tub, MAC, M foruitum
Flutamide
"Flutes turn off the androgen receptor" *Androgen R antag Use: prostate carcinoma Note: if used along, neg feedback inc testosterone! (need coadmin w/ leuprolide)
Flutamide Leuprolide
"Flutes turn off the androgen receptors" "Lube for GnRH analog neg feedback" Tx: BPH, Prostate cx
Flucytosine
"Fly away cytosine" *inhibit DNA synth by conversion to 5-FU Crypto meningitis in AIDS: Flucytosine + Ampho s/e: bone marrow tox
Nitrofurantoin
"Furantoin feeds on flavoprotein activation" Toxic intermediate--ribosomal, DNA, pyruvate attacks 1 wk tx for UTI resistant TMP or fluoroquinolone *3rd line antiseptic UTI
Meglitinides: Repaglinide, Nateglinide
"G line copied the Sulfonurea" K block S/E: weight gain common *LESS hypoglycemia than sulfonureas
Sulfonurea 2nd gen Glyburide, glipizide
"GLY lies about being lazy" Block K channel - insulin release Only T2DM Use in 2nd stage (L + M + S) S/E: hypoglycemia (so does chlorpropamide) *Chlorpropamide and Glyburide: high risk of hypoglycemia (CI in elderly)
Griseofulvin
"Greesy block of microtubules" Use: skin, hair, nail infx & ring\worm Has been replaced by itraconazole, terbenafine
Transtuzumab (Herceptin)
"Herceptin intercepts HER2 receptor" *HER2: altered EGF receptor (Antitumor antibody) 25-40% of breast tumors overexpress HER2 (1st line tx; use in combo thx)
Hydroxyurea
"Hydroxyurea affects uracil" *Inh ribonucleotide reductase Use: Myeloprolif d/o (incl CGL) *radiotherapy
Infliximab Adalimumab Certolizumab
"INFliximab = TNF alpha Ab" Anti-inflamm: Crohns Ind: refractory Crohns S/E: serum sickness, delayed hypersens, Tb reactivation, Lupus, non-Hodgkins, CNS demyel
Isoniazid
"Ice knight picture" "iso blocks myco" & INH: "injures neurons, hepatocytes" 1st line anti-tb use: extra & intracellular; NOT granuloma neurotoxicity: give vitB6
Furosemide
"In a fury lose Ca" Loop diarrhetic *Remember thiazides: inc Ca Tx: ACUTE hyperCa
Anti-ectoparasite agent: Permethrin
"Insect neurons have no permission" Anti scabies/mites (sarcoptes scabei)
Ipodate sodium Iopanoic acid
"Iodine effect AND p for peripheral effect" Adjunct in thyroid storm Non toxic but avoid in pregx
Iodoquinol (+/- metronidazole)
"Iodo for tropho In Intestine" Anit-Protozoa Tx only luminal/intestinal tropho *DOC: dientamoeba fragilis *entamoeba, giardia
Paclitaxel Docetaxel
"It is taxing to stay polymerized" Stabilize microtubule from disassembly New drug - use for ovarian and breast cx, non-small cell lung cx
Ivermectin
"Iver for river blindness-onycho.." & "strong man over river" & "Iver releases a river of GABA" Anti-helminth Inappropriate GABA release DOC: strongyloides stercoralis Mazzotti reaction No BBB penetration
Dapsone
"Leprosy pic" Other anti-mycobact Inh folate synth (like sulfonamides--PABA analogue) *watch for sulfa allx Use: m leprae (prevent resistance use Dapsone, Rifampin, Clofazamine) S/E: hemolysis w/ methemoglobinemia
Sitagliptin Linagliptin
"Liptin says lips don't degrade" block DPP-4 protease of GLP-1
Orlistat
"Listat stops the lipase" Inh pancreatic & intestinal lipase (prevent fat abs) Ind: obesity S/E: FLATULENCE, STEATORRHEA, FECAL LEAKAGE *liver damage *supplement ADEK
Thiazidolinediones (TZD): Pioglitazone, rosiglitazone
"Litazones light up the sensitivity zone" Inc number of periph glucose transporters (PPAR-gamma binding on adipose) *T2DM S/E: weight gain, edema, bone fractures, liver tox, CHF PROBLEMS: *troglitazone removed (hepatoxicity) *rosiglitazone: increased CHF & MI
Loraserin
"Lora brings serotonin" (+)5HT-2c: satiety, CNS, diabetic, drop blood sugar Ind: obesity
Lubiprostone
"Lubi pro lubricator" Activate Cl channels Ind: idiopathic chronic constipation (only drug), off label IBS
Mycophenolate mofetil (MM)
"MMs block the gMp" Proliferation signal inh Metabolized to mycophenolic acid *inh IMP DH (no GMP prod) *potent INH of T&B cell; kills only lymphocytes (only attacks de novo purine synth) Use: solid organ transplant, GVHD, autimmune (RA, SLE) *alternate to CsA, Tacro Tox: mild myelosupp **More lymphoid specific and less S/E than AZA
Macrolides (clarithromycin, azithromycin)
"Mac light pic" Other anti-mycobacterial Use: MAC complex, rapid growers, m leprae
Maraviroc
"Make CCR5 like a rock" CCR5 chemokine receptor antagonist S/E: muscle & joint pain, diarrhea, sleep dist *DI due to CYP3A4 (watch if given w/ ritanovir)
Fomiversen
"Make early foamy protein shake full of CMV eyeballs" Block early protein synth *Antisense CMV oligonucleotide Use: CMV retinitis in AIDS (effect on systemic)
Zanamazir Oseltamavir
"Mazir says you NEVER are leaving!" Neuraminidase inhitor Prophylax for Infl A/B (36-48 hrs of sx)
Mechlorethamine
"Mechlor says Hodgkins in MVPP" Nitrog Mustard (cross link DNA) *Guanine (at N-7) in monoalkylated-pair with thymidine Use MVPP: hodgkin and other lymphomas Tox: dose limited low WBC and PLT Tx extravasation: thiosulfate
Melphalan and Chlorambucil
"Melphalan has mouth full of M&Ms" Nitrog Mustard (cross link DNA) *Guanine (at N-7) in monoalkylated-pair with thymidine Use: Melphalan for MM, chlormabuicl for CLL & waldernstrom's macroglobinemia Tox: marrow suppress, no alopecia Note: more stable than mechlor
Metformin
"Met is meant for T2DM" Inc insulin sensitivity; dec hepatic gluconeogenesis *no risk of hypoglycemia, weight gain 1st line drug for T2DM (L + M) S/E: lactic acidosis, GI, dec B12 absorption
Methenamine
"Meth makes formaldehyde" UTI antiseptic; LONG TERM antiseptic Formaldehyde cross links bacteria Use: chronic UTI
Metoclopramide Prochloperazine
"Meto says NO to dopamide" "Prochlo is a pro: does 2-D2 & M1" Dopaminergic antag (and M1 antag)-CTZ(&VC) Ind: cx chemo, irradiation, postop n/v, pregx *NOT for motion sickness (need H/M for that) S/E: extrapyramidal (no dopamine)-restless, anxiety, dystonia *M1 block: sedation, diarrhea
Metoclopramide
"Meto says No to dopamide" Prokinetic Dopamine antag (neuron D2 receptor inhibits ACh release) *result: more ACh release Increase LES tone, esoph clearance, gastric empty Ind: GERD, gastric stasis, diabetic gastroparesis S/E: Parkinson-type tremors, tardive dyskinesia, somnolence, nervous, prolactinemia DI: digoxin, diabetic agents, CI w/ bowel obstruction
Metronidazole
"Metro knight picture" & GET GAP on the Metro Active only in ANAEROBES Use: giardia, entamoeba, trichomona, gardneralle, anaerobes (c diff, bacterioids), h pyloria DOC: B fragilis, C difficile S/E: disulfram rxn, peripheral neuropathy if long term
Metronidazole
"Metro: can't breath area - smelly diarrhea" Anti-protozoa Ferrodoxin activates this Tx: extra intestinal E histolytica, giardia, trichomonas
Metronomic therapy
"Metronome of tubulin doesn't stop - block endoth" *Destroy epithelial cells & angiogenesis: very low nontoxic dose over time: target tubulin and retard tumor angiogenesis
Vinblastine Vincristine
"Microtubules are vine of cells"-blast away Microtubule inhibitor (spindle poisons) (bind tubulin heterodimers (block M phase) Use: Vinblast-BVC, BVDD & solid tumors; Vincristine-VM6P (ALL), MVPP Tox: Vinblast: leukopenia (blasts the bone) & caution w/ obst jaundice Vincrist: periph neuropathy/severe constip. Note: vinblast has a wide blast radius (large Vd); Vincristine IDEAL for combo thx
Mifepristone (RU-486)
"Mife cuts baby like a knife" Progesteron antagonist: medical abortion Detachment of blastocyst & inc contractions *use w/ prostaglandins to enhance contractions
Mitomycin
"Mighty GA alkylator & single strand breaks" Potentiates doxorubicin cardiotoxicity (D for heart and CD5...) Extravasation: can cause severe local injury
Carmustine, Lomustine, Semustine
"Mustines are the nitro mustangs - power through bbb) Nitrosureas: alkylate DNA same as mustards AND caramylation of proteins Use: broad spectrum; CNS TUMORS!!! Tox: CUMULITIVE myelosuppression; long term: renal failure
Natalizumab
"Natalie integrates a FORE!!" Anti-inflamm: Crohns Integrin-a4 receptor antibody S/E: progressive multifocal leukoenceph, risk UTI/vag/GI/herpes, hepatox, hypersensitivity
Protease inhibitor: Saquinavir, indinavir, nelfinavir, amprenavir/fomasprenavir *Lopinivir Ritonavir, Tipranavir
"Navir say NEVER have a late protein shake" Inh HIV aspartic protease Only in combo thx (esp lopinavir) Peptides (poor BBB penetration) All: GI problems; DM, lypodystrophy Ritonavir: Rids CYP4A3 fxn (boost to other protease inh) Tipranavir: Not a peptide, NO lipodystrophy
Neostigmine
"Nife into AChE" Prokinetic ACh on M3: smooth muscle contraction rarely used S/E: SLUDS (salivation, lacrimation, urination, diarrhea"
Nitazoxanide
"Night time crib: Tx cryptosporidium" Anti-protozoa Inhibits pyruvate (ferredoxin oxidoreductase)
Nitrogen Oxides
"Nitro: think car exhaust" Auto exhaust fumes, cigar and gas stoves Penetrates alveoli: interstitial edema & epith cell proliferation *high exposure: pulm fibrosis and emphys Nitric and nitrous acids
Enfuvirtide
"No en fusion" Binds gp41 (inhibits fusion to host cell)
H pylori triple thx
"O + A + C" omeprazole, amoxicillin, clindamycin *amox allx: use metronidazole
Octreotide
"Octagon stop sign of somatostatin" Anti-diarrheal Somatostatin analog: DEC gastrin, GIP, motilin, VIP, insulin, glucagon, GH, splanchnic blood flow Ind: severe secretory diarrhea, carcinoid syndrome & VIPoma *AIDS pt, portal HTN Polypeptide: no PO use (SQ or IV)
CINV: chemo induced N/V
"Oh Day ; Pray ; Dex & Loraz" Block 5HT3 (acute): odansetron Block NK1 (acute/delay): aprepitant Corticosteroid (delayed): Dexamethasone (Possible: Lorazepam for anticipatory)
Doxercalciferol Paricalcitol
"Pair of doxers box out PTH" No effect on Ca/PO4 levels Ind: hyperPTH secondary to renal failure (Bones, stones, groans)
Erythromycin
"Pic" DOC: cornybacterial infxn, pneumonia (pneumococcus, mycoplasma, legionella) S/E: pic (GI irritation #1), p450...
Omeprazole Lansoprazole (Rabeprazole, pantoprazole, esomeprazole-nexium)
"Prazole: pray my stomach acid stops" - PPI Block parietal H/K ATPase Trapped in secretory canaliculi: low pH activates sulfur group-covalent bond to K transport site *Loses effectiveness @ night; H2 is better @ night Ind: GERD, Peptic ulcer (H pylori = O+A+C), Z-E syndrome, gastrinoma, NSAID associated ulcer S/E: resp/GI infxns, osteoporosis (Ca malab), acid rebound CI: pregnant using clopidogrel
Praziquantel
"Preeze let me leave" & "Prazi has a calcium breeze" Anti-helminth Inc Ca permeability (tetany) DOC: schistosomiasis (blood fluke)
Primaquine
"Prima prevents relapse" Antimalarial ONLY drugs that killsl hypnozoite (vivax & ovale)
Streptogramin:
"Pristine strip club at the P site" B: Quinipristin (30%) A: Dalfpristin (70%) Use: G+ (except E faecium), MRSA, VRSA
Leuprolide
"Proglide that GnRH: down reg Receptors" *Dec LH/FSH release Use: Prostate carcinoma (use with flutamide)
Anti-ectoparasite: Pyrethrin + piperonyl butoxide
"Pyrethrin like permethrin: no neuronal" **DDT like "Piper keeps pyrethrin in the pipes" **p450 inhibitor Head lice (peduculus humanus) & pubic lice (phthiris pubis
Quinine + tetracycline
"Quinine for the quiting chloroquine" Antimalarial Tx: chloroq resistant Falciparum & vivax S/E: cinchonism (tinnitus, HA,..) Clindamycin (not tetra) in child
Rifampin (Rifobutin for HAART, Rifapentine)
"Ref amp picture" 1st line antiTB RNA polymerase inh, orange secretion, p450 (OCP) *CI in HIV on protease or NNRTI (use rifabtuin) Use: Extra, Intra, granuloma Leprosy: use Rifampin & Dapsone
Methotrexate
"Remember sulfamethoxazole (SMX)-similar methotrexate" Immunosuppression: Crohns DHFR inhibor (inh purine & thymidine synth) *T lymph apoptosis Ind: Crohn's remission maintenance S/E bone marrow
Ribavirin
"Rib dinner at NA dinner" & "Riba for RSV" Block DNA/RNA synth *Guanosine analog Use: RSV pneumonitis, Hep C (w/peg IFN)
Rimonabant
"Rimon reverse Simon (CB1)" Cannabinoid CB1 block: blocks munchies Ind: obesity S/E: SEVERE DEPRESSION, improved short term memory *not FDA approved
Raloxifene
"Rolex of postmenopause tx" SERM; +bone/liver & -uterus/brain Dec rate of bone loss; dec LDL Inc bone mass Tx: osteoporosis S/E: hot flashes, procoag
Raloxifene
"Rolex of the post menopausal" SERM + bone; -breast/endomet/BRAIN Tx: osteoporosis *protective: breast & endometrial cx S/E: hot flash, VTE
Scopolamine
"Sea sick scope: M1 for motion sickness" Anti-chol (M1) - vestibular DOC: motion sickness CI: glaucoma, BPH (antichol) Transdermal: less s/e, less effective S/E: dry as a...
Sibutramine
"See butt: inc NE & 5HT -> satiety" *similar to mazindol Ind: obesity S/E: HTN, tachyC, dry mouth, insomnia *OFF market: CV events (MI, CVA)
Cisapride
"Serotonin pride" Prokinetic: 5HT4 agonist *mainly upper GI Ind: GERD, intestinal obstruction, diabetic gast S/E: fatal cardiac arrythmia (off market now)
Ondansetron ($) (Granisetron)
"Setron sits down the serotonin" 5-HT3 antag (CTZ, VC, GI) DOC: Acute CINV, postop N/V, pregx S/E: HA, diarrhea, constipation
Cinacalcet
"Sinner steals calcium's identity for PTH feedback" Stimulates CaR->dec PTH release Tx: hyperCa
Sirolimus (SRL)
"Siro has zero mTOR" Proliferation signal inh SRL binds FKbp-but not CaN rxn *SRL/FKbp binds mTOR -> inh T cell Use: GVHD and solid organ transplant (combo w/ prednisone) Tox: myelosuppression (plt,wbc), liver, hyperTG, diarrhea *LESS NEPHROTOXIC than CsA/Tac
Deferasirox
"Sirox for lots of time"-chronic *High affinity for Fe; low for Zn/Cu Use: CHRONIC Fe Few s/e
Ampicillin (sulbactam) Amoxicillin (clavulanic acid)
"Soldiers like amps; cleavers for oxen" "Aminopenicillin pic" & "HELPSS pic" "Pros Listen to the Amp" Amp: DOC proteus mirabilis (kidney stones, nosocomial wound infxn, sepsis, pneumonia) & DOC Listeria (synergy with aminoglycoside) Amox: DOC bacterial endocarditis prophylax *Amoxicillin NOT affected with food intake
Sulcralfate
"Stop sulking; improve fate with sulcrafate" Bind exposed protein in ulcer; stimulate PG, inhib pepsin; suppress H pylori Ind: ulcers (esp stress) S/E: constipation (no systemic-not absorbed)
Strontium Ranelate
"Strontium for strong bones" Divalent metal ion: stim bone formation Tx: post menopause, osteoporosis
Succimer
"Sucks your kid had Pb paint" Use: Pb poisoning in kids Infreq s/e: n/v/d, hypersensitivity
Sulfonamides: sulfamethaxaole (SMX), sulfadiazine, sulfadoxine, sulfasalazine
"Sulfa match fondu" PABA analogy (block Dihydropterogate synthase) Use: UTI, nocardia *SMX: UTI *sulfasalazine: UC, GI enteritis, IBD S/E: G6PD, nephrotoxic, photosensitivity, steven johnson *not good in pregx (BBB)
Sulfur Oxides:
"Sulfur think fossils" Combustion (fossil fuel, petroleum, coal) Inorganic gas Increasing exposure: first bronchospasm, goblet cell inc, pulm edema Sulfuric acid (acid rain)
Mazindol
"TCA for the maze" TCA like (DANE,5HT reuptake block) Dec appetite Less dependance and less CNS s/e CI: severe CV disease, pregx, antidepressants
TMP-SMX
"TMP pic" & "TMP treats marrow poorly" Blocks DHP synthase & DHFR Use *TMP: UTI *salmonella, shigella, PCP in AIDS, URI, MRSA
Tacrolimus (FK506)
"Tac steps on tack says FK" Immunophilin ligand *Bacterial product - binds FK506bp (blocks CaN) = no NFAT and no IL2 Use: GVHD, transplant, autimmune... *topical for atopic dermatitis, psoriasis Tox: Nephro AND neurotoxic (can't feel Tac), HTN, hyperGLY, hyperK *NO SX: of hirsutism, gingival hyperplasia, moobs
Tamoxifen
"Tamox turns off the estrogen" SERM: +bone/lipid, -brain (hot flash), +endomet (cx), +clotting (VTE) Tx: breast cx (if estrogen sensitive) S/E: from lack of estrogen (hot flash, cx, vte)
Vancomycin
"Tank mice" (also pic of toxicity) Glycopeptide Gram + only (c diff, staph, gram +) *G(-) are intrinsically resistnat SLOW IV infusion; oral for AAC oly S/E picture (especially red man syndrome & histamine)
Telithromycin
"Tell this line if macrolide resistant" Ketolide Higher 50S affinity, less efflux than macrolides
Terbenafine
"TerbeNaFine: The skin, nails, fat" "Terpentine like squalene epoxide"-squeel w/ terpentine Tx: onychomycosis (expensive, ineffective...)
Cytosine Arabinoside
"The Arab Sea: araCMP" *activated to araCMP by deoxycytidine kinase DNA incorp: mistacking bases (inh DNA synth) *note: give drug slowly (need cells in S phase) Use: AML (a cyte to sine (site or seen) of monkeys) Toxic: potent myelosupp Resist: dec deoxyctidine kinase, inc CTP Note: inactivation by cytidine deaminase to AraU (liver,blood, etc)
Tegaserod (prescription)
"Tickles serotonin" Pre-synaptic 5HT-4 partial agonist Promote gastric and small bowell transit Ind: constipation Withdrawn: Cardiac adverse events
Tenofovir
"Tiny favorite" - nucleoTide analog (already has P) Adenosine Nucleotide 1st line in combo thx Few S/E; don't give w/ didanosine
Denosumab
"Tis enough bone loss! Ab vs RANK-L" Tx: osteoporosis for risk of frax S/E: infxn, hypoCa, rash, joint pain, osteonecrosis of jaw
Etoposide Teniposide
"Toposides and posides block topo II" Eto: BEC Inh topo: nicks/breaks -> fragment Cell cycle: G2 Use: Etoposide (BEC, SmCC lung), Teniposide (refactory ALL) Note: teniposide can be given with impaired renal fxn!! Tox: leukopenia dose limiting
Triamcinolone Paramethasone
"Tram and Para are the transition" 36 hr intermed acting glucocorticoid
Rifaximin
"Traveler on the river" Non-abs Abx Anti-diarrhea Effective prevention/tx of traveler's diarrhea *Also IBD
Idoxuridine Trifluridine
"Uridine is your a dine during NA dinner" Thymidine analog Use: TOPICAL HSV keratitis *Phophorylated by cell and viral TK (too toxic for systemic)
NRTI *Zidovudine (AZT/ZDV) *Lamivudine, emtricitibine Also didanosine, zalcitabine, stavudine, abacavir, tenofovir
"Vudine while watching tv" & citibine for C" Must be phosph (thymidine kinase) Inhibit rev transcript & dna chain term Zidovudine: T *S/E-hematologic, liver, avoid DI (stavudine, gangcic, rib) Didanosine: A *S/E-pancreatitis (esp drunks), periph neuropathy; avoid DI (AZT, stavudine) Zalcitabine: C *S/E: periph neuropathy in 20%, pancreatitis Stavudine: T *s/e: periph neuropathy, lipodystrophy, liver toxic Lamivudine, emtricitibine: C; 1st line in combo thx *S/E: few; 15% kids pancreatitis *Combivir = lamivudine + AZT Abacavir: G (abba is G)
PIrenzepine/Telezepine
"Zepine zips up M1-ECL cells" *Dec histamine/acid Fewer S/E
Linezolid
"Zolid against resistant bacteria: Use only with: MRSA, VRSA, VRE Hematologic toxicity (thrombocytopenia, neutropenia)
Aminoglycosides Top line: streptomycin Middle: amikacin Bottom: Capreomycin
"amino glider pic" Use: extraceular Tb
Artemesnin (+- lumefantrine)
"ancient art--used in 3rd world Antimalarial Inhibit parasite Ca ATPase
Tetracycline Doxycycline Minocycline
"buy AT 30" DOC (pic): rickettsia, chlamydia, mycoplasma, spirochetes (and also pneumoniae, vibrio cholera) Don't take with milk, antacids, Mg/Fe S/E: GI, teeth, bone, photo (esp doxy), blue gums (minocyc) Doxy: fecal excretion
Ganiciclovir (Valganciclovir prodrug)
"cycle of cars during NA dinner" Block DNA polym & chain term Guanosine analog Use: life threatening CMV disease (retinitis, pneumonitis) S/E: Hemato suppress (lueko, neutro, thrombocyto-penia)-additive with zidovudine; renal tox *"Gangs up on bone marrow & kidney"
Famciclovir (prodrug for penciclovir) Penciclovir
"cycle of cars during na dinner" Inhibits DNA polym only Guanosine analog Penciclovir: poor absorption (use for herpes labialis)
Fluoroquinolone: norfloxacin, ciprofloxacin, levofloxacin
"flower queen pic" Inh topoisomerase DOC anthrax: Ciprofloxacin *use: UTI, neisseria, pseudo, gram neg *not for anaerobes S/E picture
Raltegravir
"integration like gravy" Pyrimidinone analog: rev inhibit viral integrase
Clofazamine
"leprosy pic" Other anti-mycobact Pheanzine dye (alter DNA fxn) Use: m leprae s/e: red-black discoloration of skin
Nystatin
"nice thrush..." Binds ergosterol Tx: oral candidiasis (oral thrush), diaper rash candidasis *topical (due to toxicity)
Pyrazinamide
"peaks inside"-for only intracellular 1st line antiTB Nicotinamide analog S/E: hepatitis, hyperuricemia
Plicamycin
"plica has plight of toxicities" *similar to dactinomycin though DNA intercalator... Low dose tx: blocks osteoclast resorption to drop Ca Tox: severe hemorrhagic d/o (impair clotting)-most hepatotoxic agent in use
Azothioprine 6-Mercaptopurine
"prines and purines are anti-metabolites" Block lymphocytic prolif Ind: remission of IBD s/e: bone marrow suppress
Ethambutol
"thumb butt picture" 1st line antiTB Block arabinsyl transferase, RG colorblind (don't give to <8yo) Use: extra, intra, granuloma
Calcitonin
"tones down the Calcium" Release by thyroid parafollicular cells Kidney (excrete Ca, Phos, Mg/Cl/K) Bone: high dose dec both form & resorp Ind: Paget's disease, hyperPTH, osteoporosis, osteolytic bone malignancy Salmon calcitonin more potent
Ipecac
"vomit a cat" Emetic Emetine: stimulates vagal periph afferents & CTZ Ind: acute poisoning S/E: large dose heart tox
Linezolid
"zolid for drug resistant"--drug resistant Tb 2nd line antiTB Bind 23S rRNA For intracellular s/e: hematoligc, GI, serotonin syndrome, bone marrow suppression
Amphetamine *Methamphetamine *Methylphenidate **Phenteramine
(+) DA/NE release in CNS; (-)MAO "Amps up the amines--DANE" "Meth amps up the amines--DANE" "Meth scheduled regularly with prescribed dates"--Ritalin "Phenteramine" Stimulant **** Met: plasma&liver cholinesterase-->benzoylecgonine & ecgonine methylester *Thx: ADHD Acute: euphoria, sympath stim (w/insom, anxiety), sexual arousal & dysfunction Chronic: tolerance & dependance, anxiety, insomnia; CVA, seizure, coronary vasospasm, MI, psychosis, nasal perf *(+)necrotizing arteritis Crash: anxiety/fatigue/hypersomnia, hung Withdraw: drug crave, anhedonia, depress, dysphoria
Adenosine
(+) K efflux out of cell (hyperpolarize) *A done sign: won't depolarize Class other: dec AV node conduction Tx PAT
Terpin hydrate
(+) secretory cells in resp tract "Hydrate your resp after drinking terpin tine" Expectorant *Tx cough
Iodides
(+) secretory glands "Iodides rid the cough's cries" Expectorant *Tx cough Comp: hypersens to iodides; potential thyroid suppression
Dopamine
(+)A1,B1,D1 "I don't mind if the kindey's stay a mine" Hemodynamic: Renal vasodilator Inc blood flow, GFR; DEC counter current exchange Tx post-MI (w/dobutamine)
Clonidine
(+)A2 "Cloni dines with us to give neg feedback" Inhib release of NE, vasodilate Dec BP Tx HTN, opioid withdrawal, diarrhea Comp: don't abruptly stop (rebound HTN), hypotension, dry mouth, sedation
Clonidine
(+)A2, CNS adrenolytic "While Cloni dines, she gives some neg feedback" Antagonize stretch receptors: dec renin release Ind: HTN Comp: effective only when serum renin is high
Nicotine
(+)ACh Nic: mimic "Nicotine on nicotinic receptors" Stimulant; (+) Adrenal E/NE; (+)CNS: ACh,NE/DA/5HT; Dec MAO Metab: liver CYP2A6; also lung, kidneys Thx: patch/gum/inhalant for nic depend Acute: stim motor/cogn/BP&HR, N&V; dec GI and appetite Chronic: CANCER, tolerance, dependance Tx: nicotinic tx, behavioral thx, antidepressants (bupriopion, varenicline)
Fludrocortisone
(+)Aldosterone agonist "Flood on core with sodium" Tx adrenal insufficiency *mineralcorticoid; give w/ glucocorticoid PO
COA (deoxocorticosterone)
(+)Aldosterone agonist "corticosterone given with adrenal insuff" Tx adrenal insufficiency *mineralcorticoid; give w/ glucocorticoid IV or IM (in oil)
Epinephrine *Oxymetazoline *Phenlephrine *Xylometazoline *Cocaine
(+)Alpha agonist "Epi & zolines let's your breath and smell febreeze" "Cocaine: inhibit reuptake of NE/E" Vasoconstriction Tx Rhinitis *topical, rapid onset Comp: few systemic; rebound congestion, rhinitis medicamentosa, tachyphylaxis
Pseudoephedrine
(+)Alpha1 "Pseudo like ephedrine" Like ephedrine but... *PO (not topical) *slow onset, longer acting *Comp: dizzy, termor, insomnia, irritable, palpitations, HTN *less potential for dependance
Ropinirole Pramipexole (Bromocriptine) (Apomorphine)
(+)D2 receptor "Pray we can Rope in this D2 receptor" Ropinirole Pramipexole: D3 preferential (Bromocriptine) (Apomorphine): temporary relief (for 2 hrs) Adm: not as long lasting as L-dopa *not as long lasting: desensitization of receptors Comp: similar to L-dopa *LESS: incidence of response fluctuations & dyskinesias *MORE: severity of behavioral disturb *Pedal edema, severe hypoTN
Hydralazine
(+)NO "Hydra hides how he releases N.O." arterial relaxant, mechanism not fully understood Dec BP and afterload Tx HTN, CHF Comp: headache, flushing, slow acetylators *LUPUS LIKE SYNDROME
ADH
(+)V1a: smooth muscle/vascular, brain--PIP hydrolysis (+)V1b: pituitary--PIP hydrolysis (+)V2: basolateral kidney tubular cells of CD and DCT--cAMP, aquaporin II; also in endothelial cells "Vasopressin presses out the water from urine" Effects: vasoconstrict at high concen, thirst/salt appetite, coag VIII prod, V1a: dec medullary blood flow to enhance concentration ability, V1b: ACTH release, V2: aquaporin
Desmopressin
(+)V2: DCT and CD (aquaporins) "Desmopressin is long Duration Vasopressin" Tx: pituitary diabetes insip, GI bleed (esoph, divertic) - chronic **treat vWB disease and factor VIII deficiency!! Intranasal, Inhale, PO, inject, 14-20hours Comp: DI w/ clofibrate & chlorpropamide
Pentazocine
(+)kappa, (- weak)mu "Pentacostals at the zoo speak kappa and mu" Mixed agonist/antag Ind: detox and maintenance thx, some moderate pain Comp: dysphoria, hallucinations, depersonalization; MUCH LESS DEPENDENCE; minimal sedation/resp depression Resists naloxone reversal
LSD *psilocybin
(+)partial 5-HT (2a) receptor "LSD let's serotonin deliver" - ACID Shrooms Indoleamine, halluncinogen Acute: symp (pupils, bp, HR) Good trip: aLOC, euphoria, inc sensory, introspection Bad trip: anxiety, agitated, panic, psychosis, hallucinate Chronic: tolerance; cross-tol w/psilocybin & mescaline Tx: BZ & therapy
Buprenorphine (Butorphanol) (Nalbuphine)
(+partial)kappa "Bu is prayin to get off morphine" Mixed agonist/antag Ind: detox and maintenance thx, some moderate pain Time: long duration, less severe withdrawal Comp: dysphoria, hallucinations, depersonalization; MUCH LESS DEPENDENCE; minimal sedation/resp depression Resists naloxone reversal
Zileuton
(-) 5-Lipoxygenase (less LT biosynth) "Zeus stops leukotriene synthesis" Ind: mild/persistent asthma (esp if sensitive to aspirin) *PO Note: inhibits many p450s *DI w/ terfenadine, theophilline
Zileuton
(-) 5-lipoxygenase "Silly zileuton blocks leukocyte's lipoxy for a short while" Anti-leukotriene Long term: attenuate bronchospasm and inflamm response *slow onset Tx: asthma, rhinitis **PO, SHORT acting Complications: inc liver enzymes (contraind if liver disease); interfere w/ drug metabolism of warfarin, propranolol, theophyline
Trazadone Nefazodone
(-) 5HT2 receptors "zadones and zodones are used if there's too much serotones" Atypical Comp: *Trazadone: severe sedation, N&V, hypoTN, priapism, safer than TCA in OD *Nefazodone: moderate sedation
Theophylline *Caffeine *Aminophylline *Theobromine
(-) Adenosine receptor: (x) cAMP PDE & alters Ca intracell **similar B2 agonist effect: increase cAMP by preventing degredation (B2 increases synth via AC) "Theo files into his cAMPing tent--like B2" Tx ashtma, chronic bronchitis, emphysema *IV, PO *variable time course Comp: headache, insomnia, anxiet, behav/learning problems, N/V, heartburn, ulcers, tremor, convulsions, arrhythmias Good oral bioavail, crosses BBB, placenta
Amiloride
(-) Aldosterone "AMY can't pass Na through this" Site 4 (CT) Inhibits Na channel influx; dissipates transepith potential PO Comp: hyperK, inc Li reabs, elevates urate
Triamterene
(-) Aldosterone "Gynecomastic guy riding the TRAM" Site 4 (CT) Inhibits Na channel influx; dissipates transepith potential PO Comp: rare nephrotoxicity w/ indomethacin
Amiloride
(-) Aldosterone (physiological antag) "Amy love - proposed on tram" Comp: DO NOT use with ACE (-)
Triamterene
(-) Aldosterone (physiological antag) "Gynecomastia on tram" Comp: DO NOT use with Ace (-)
Spironolactone
(-) Aldosterone Receptor "Saw my breasts spiral out, and Na spiral down the toilet bowl" Site 4 (CT) Blocks aldosterone Na/K exchange (inh K loss) Tx K+ protection from diuretic, hyperaldosteronism, CHF,cirrhosis *slight Na excretion and diuresis PO w/ food Steroid: slow on/off Comp: hyperK (bad in DM or low GFR), gynecomastia, impotence, menstrual irreg
Flumazenil
(-) BZ receptor (comp antag) "Flumaze blocks the Z's: zopli, zaleplon, eszopli, BZ" Blocks action of zolpidem/zaleplon/eszoplicone NOT buspirone Ind: manage BZ overdose (resp), anesthetic & diag procedure recovery Time: short duration (freq admin) Comp: precipitate withdrawal symtpoms
dl-Sotalol
(-) Beta blocker & (-) K *Alol=beta blocker. "Sot" hurts the POTassium Class II/III; LONG TERM; suppress atrial re-entry Tx: V tach/fib, A flutter/fib, AICD (v tach/fib)
Entacapone (Tolcapone)
(-) COMT "COME put that CAP on the PD patient" Act: selective periph COMT inhibitor (block metab l-dopa) *give to patients with fluctuation dopa responses *adjunct thx Comp: dyskinesia, nausea, confusion, sleep disturbances, ortho hypoTN, abd pain, diarrhea, orange urine *Tolcapone: hepatoxicity (why entacapone preferred)
Ketorolac
(-) COX "Lack oral admin? Keto can go in" NSAID acetic acid Rapid onset analgesic *Only parenteral NSAID *serious GI effects
Diclofenac
(-) COX2 > COX1 (5-10 fold) *All those dicks in Europe use this Fenac NSAID acetic acid Most commonly used in Europe
Etodolac
(-) COX2>COX1 (3x) Protein binding w/o warfarin effects Sustained release w/ 7hr half life; one day dose
Verapamil
(-) Ca *Diltiazem: VERY helpful PAM for my ILL Class IV: ACUTE; decrease AV node Tx: A flutter/fib (rate); PAT
Diltiazem
(-) Ca *Diltiazem: VERY helpful PAM for my ILL Class IV: CHRONIC; dec AV node Tx: A flutter/fib (rate); PAT
Nifedipine
(-) Ca channel; cario sparing "Nife dipped in the milk" Dec vascular tone; less heart
Methadone (Levomethadyl actate)
(-) Ca presyn channel; (+) K channel: hyperpol "Methadone turns down need for morphine" (detox) Strong opioid Ind: detox/maintenance thx; cancer & neuropathic pain Adm: high oral : parenteral potency ratio Time: long duration (less withdrawal)
Imipramine Amitriptyline (Doxepin, trimipramine) Nortriptyline Desipramine (Protriptyline)
(-) Catechol reuptake into presyn nerve "Pramine, ptylines" - the Praying Tilers ride Tricycles TCA Ind: MDD, bipolar affective d/o, ADHD Time: 1-2 days Comp: *sedation, confusion, delirium, memory dys *mania, seizures, tremor (tx propranolol) *postural HTN, tachycard, dry mouth, blurred vision, constipation, difficult urination, narrow angle glaucoma *weight gain, sex dys *rebound effects DI: CNS depressants, clonidine, alpha-methyldopa, anti-Chol drugs, MAOIs (serotonin syndrome)
Cocaine
(-) DA transport (reuptake of NE/DA) "Cocaine keeps DA,NE in the main" Stimulant Met: plasma&liver cholinesterase-->benzoylecgonine & ecgonine methylester Thx: topical anesthesia (vasoconstrict) Acute: euphoria, sympath stim (w/insom, anxiety), sexual arousal & dysfunction Chronic: tolerance & dependance, anxiety, insomnia; CVA, seizure, coronary vasospasm, MI, psychosis, nasal perf Crash: anxiety/fatigue/hypersomnia, hung Withdraw: drug crave, anhedonia, depress, dysphoria
Buproprion (Maprotiline)
(-) DA/NE reuptakes "Bupro likes his coco" (acts like cocaine) (Mapro blocks NE reuptake) Atypical Ind: depression, smoking cessation Comp: Agitated, insomnia, weight -, seizure (more than TCA), low sedative, antiChol, hypoTN, less sex dys
Disulfiram
(-) EtOH aldehyde DH "Disulfir given to the a.m. drinker" Ethanol--(alc DH)--> Acetaldehyde --(Ald DH)--> ACETATE Tx: alcoholism
(Tiagabine)
(-) GABA uptake New AED Ind: adjunct for refractive partial & tonic clonic seizures Comp: dizzy, nervous, tremor, difficult to concentrate
Anakinra
(-) IL-1 receptor, competitive antag Ind: RA *SubQ, short half life
Budenoside
(-) Inflamm mediator synthesis (+) number of B2 adrenergic receptors (relaxation) "Buden is putting those mediators aside with the Tide" Tx Asthma, Rhinitis *emergency or long term *NEBULIZER*--think about the guy on hitch putting his nebulizer aside (budenoside) rapid systemic metabolism Comp: high lipid solubility *Promotes oropharyn candidiasis, dysphonia, suppress adrenal axis in children, bone loss?
Ciclesonide
(-) Inflamm mediator synthesis (+) number of B2 adrenergic receptors (relaxation) "Cycles the Tide away" **prodrug Tx Asthma, Rhinitis *emergency or long term Inhalatin (chronic) or IV (acute) *Rhinitis: topical *rapid systemic metabolism Comp: high lipid solubility *Promotes oropharyn candidiasis, dysphonia, suppress adrenal axis in children, bone loss?
Methylprednisolone
(-) Inflamm mediator synthesis (+) number of B2 adrenergic receptors (relaxation) "Methyl is meant to be use Pretty quick" Tx ASTHMA *EMERGENCY IV (acute) *rapid systemic metabolism Comp: high lipid solubility *Promotes oropharyn candidiasis, dysphonia, suppress adrenal axis in children, bone loss?
Flunisolide *Triamcinolone *Fluticasone
(-) Inflamm mediator synthesis (+) number of B2 adrenergic receptors (relaxation) *"Flunis uses Tide to slide away these mediators" "Triam is trying to make those mediators sin alone" "Flut played is flute until the mediators were cast alone" Tx Asthma, Rhinitis *emergency or long term Inhalatin (chronic) or IV (acute) *Rhinitis: topical *rapid systemic metabolism Comp: high lipid solubility *Promotes oropharyn candidiasis, dysphonia, suppress adrenal axis in children, bone loss?
Beclomethasone
(-) Inflamm mediator synthesis (+) number of B2 adrenergic receptors (relaxation) FAMILY: with the use of -TIDE, washed away the mediators so that they are al-ONE. "Beclo tones down the asthma by ridding the mediators" **first of class Tx Asthma, Rhinitis *emergency or long term Inhalatin (chronic) or IV (acute) *Rhinitis: topical *rapid systemic metabolism Comp: high lipid solubility *Promotes oropharyn candidiasis, dysphonia, suppress adrenal axis in children, bone loss?
Dofetilide
(-) K blocker *Come here banana! jk I LIED Class III: Acute cardioversion; Inc atrial refractoriness Tx: A flutter/fib (cariovers, suppress)
Ibutilide
(-) K blocker *Kick my butt-I lied again. Or take my banana. Class III: Acute cardioversion; Inc atrial refractoriness Tx: A flutter/fib
Amiodarone
(-) K channel *Amio my love--I dare you to block the banana Class III; ACUTE&CHRONIC Tx: V tach/fib, A flutter/fib (cardioversion)
Levodopa/Carbidopa = Sinemet
(-) L-AminoAcid decarboxylase "Carbidopa is like giving a car ride for dopa straight into CNS" Act: blocks decarboxylase in periphery (can't pass BBB)--dec L-dopa periph effects Ind: PD *admin w/ levodopa
Verapamil
(-) L-type Ca channel "Very important Pam: hand those pills with the milk" Dec calcium influx: dec vascular tone & dec HR (counter: baroreceptor reflex) Tx: HTN, angina from spasm Comp: headache, flushing, constipation, premature labor, peripheral edema *NOT in CHF, heart block, WPW
Montelukast
(-) LTD4 Receptor "Puts a mountain in front of the Leukotriene" Leukotriene modfiier Ind: mild persistent asthma *PO Comp: HA, elev hepatic enzymes
Montelukast *Zafirlukast
(-) Leukotriene receptor "Puts a mountain in front of the leukotrien receptor" "Zafir says the furr is blocking the lukotriene receptor" Anti-leukotriene Long term: attenuate bronchospasm and inflamm response *slow onset Tx: asthma, rhinitis **PO, LONG acting Excreted in bile Comp: montelukast elevates liver enzymes (liver injury)
Selegiline Rasagiline
(-) MAO-B (at low doses selective) "Gilines are gills that let DOPA keep swimming" Act: dec DOPA and L-DOPA metab in CNS Ind: PD *adjunct to L-DOPA thx DI: meperidine or SSRI (serotonin syndrome)
Phenelzine (Tranylcypromine)
(-) MAO-a&b; Irrev (inhib NE breakdown) "Nelzine adds the NE time (and 5HT, DA)" Ind: if don't respond to TCA, SSRI *Short half life in plasma, long bioeffect (irrev) Comp: CNS stim--hypoTN, HA, dry mouth, sex dys, weight+ DI: indirect/direct sympathomimetic amines, SSRI, TCA, opioids, CNS stim
Atropine
(-) Muscarinic *A trip to pine blocks muscarine Class other: dec vagal, increase HR Tx bradycardia
Acamprosate
(-) NMDA glu receptor "A camping--and drinking pros took this to subside effects" EtOH antagonist tx: alcoholism
Phencyclidine
(-) NMDA glut receptor "Phun cycling through hallucinations with enterohepatic circ"- PCP Anesthetic, hallucinagen Metab: long half life (enterohepatic circ) Acute: euphoria, personality dissoc, poor judge, aggression, psychosis / hallucinate, seizures, resp depress, coma / renal failure, rhabdomyolysis Tx: induce vomit, resp support, BZ seizure control, reduce sensory stim
(Felbamate)
(-) NMDA glycine receptor "Amates are a mate to the old AED" New AED Ind: adjunct for partial and atonic seizures in patients w/ lenox-gastuat syndrome Comp: anaplastic anemia, liver failure Interact: significant
Digoxin/digitalis
(-) Na/K pump *Dig in with the toxin Class other: ACUTE or CHRONIC; incrase vagal, decrease AV node Tx: A fib/flutter (rate, suppress), PAT
Dextromethorphan
(-) cough reflex at cough center "morphine's morphan is dextromethorphan" Non-Opioid Ind: cough Comp: less constipation; no analgesia or depend *SE: dizzy, nausea, drowsy
Lithium
(-) inositol monophosphatase (deplete PIP2 available for PLC) *Lithium's liter burns up the inositol monophosphatase" Ind: acute/prophylactic tx of mania or bipolar Mood stabilizer *Onset: takes 2-3 weeks! Comp: low therapeutic index *N/V, diarrhea, fine tremor, lethargy *impair concentration *polyuria/dyspsea/water intake, weight gain, rash, thyroid enlarged/hypothyroidism *fetal malformations (Ebstein's anomaly) *HIGH DOSE: confused, memory loss, drowsy, dizzy, ataxia, severe tremors, clonus, seizures, arrythmia, circ collapse, coma DI: Na depletion results in toxicity risk, NSAIDs dec renal clearnace, theophylline & caffeine lower levels *Clearance inc during pregnancy
Magnesium
(-) ion flow (Na, Cl, K) *Magnesium ion blocks other ions Class other; suppress early after-depolarization Tx Tourades de Pointes
(Mirtazapine)
(-) receptors: alpha2, 5-HT2&3, H1 Remember Amoxapine? zaps the DA and NE Mirta only zaps Norepi Comp: sedation, weight+, fewer s/e than SSRIs *no therapeutic adv over TCA
Cocaine
(-) voltage gated Na channels (neuronal) "Cocaine can block the Na's maine" Thx: local anesthesia Ind: topical anesthesia Comp: CNS stimulant, CVS stimulant **Schedule II controlled substance
Lidocaine (Mepivacaine, etidocaine, prilocaine, ropivacaine, levobupivacaine)
(-) voltage gated Na channels (neuronal) "LAMIDE blocks the Na's maine; L = liver metabolism" Thx: Local anesthesia *Amide Ind: local pain control; epidural/subdural injection *blockage of sympathetic fibers *tx neuropathic pain syndromes, cardiac dysrhythmias Time: Metabolized by HEPATIC MECHANISM, excrete both metab/unchanged forms in kidney DI: CYP3A4 compet inhibition (cimetidine, alfentanil, midazolam) *Dec hepatic blood flow (propranolol, halothane) Comp: *CNS tox: inititial depression of cortical inhib centers--nystagmus, muscle twitch & tonic-clonic sz; followed by general CNS depression *Local neurotox *CV tox: ECG alterations, myocard depression, periph vasodilation & eventual CV collapse Note: admin epinephrine-->vasoconstriction-->reduces systemic absorption + enhances neuronal uptakes + prolonged duration
Procaine (Tetracaine, Benzocaine)
(-) voltage gated Na channels (neuronal) from cytoplasm side "Procaine PESTER blocks the Na's maine" Thx: Local anesthesia *Ester Ind: local pain control; epidural/subdural injection *blockage of sympathetic fibers *tx neuropathic pain syndromes, cardiac dysrhythmias Time: metabolizes fast--butrylcholinesterase; urine excretion Comp: *CNS tox: inititial depression of cortical inhib centers--nystagmus, muscle twitch & tonic-clonic sz; followed by general CNS depression *Local neurotox *CV tox: ECG alterations, myocard depression, periph vasodilation & eventual CV collapse *Esters: more associated with allergy
Clomipramine
(-)5HT reuptake "The Pramine that Closes ONLY 5HT reuptake" Tertiary TCA Ind: OCD Comp: moderate sedation, hypotension, anti-Chol, GI effects, sexual dys, weight gain, seizures *caution w/ heart problesm, elderly *lethal in OD DI: CNS depressants, clonidine, alpha-methyldopa, anti-Chol, MAOI (serotonin syndrome)
Fluoxetine Sertraline Paroxetine (Fluvoxamine, escitalopram, citalopram"
(-)5HT reuptake Xetines + Sertralines: "increase the amount of Sero time" *Fluoxetine: Prozac = 14 day half life SSRI Ind: MDD, bipolar affective *Anxiety, OCD, PTSD, social anxiety, panic d/o, GAD, prement dysphoritic disorder, bulemia Comp: HA, sex dys/red libido/delayed ejac, nausea, heartburn, weight +/- (sig gain with sertraline), anxiety/excitation, apathy *rebound discontinuation effects *suicidal ideation <24 yrs DI: serotonin syndrome (agitated, sweat, diarrhea, fever, hyperreflex, incoordiation, myoclonus, *severe: convulsions, coma, death esp w/ MAOIs *Fluoxetine (-) liver enzymes (potentiate other drgs); also is LEAST specific of SSRI
Olanzapine
(-)5HT2>D2 (-) Hist & musc "Oh lance you're just another apine" Atypical Ind: schizophrenia, shizoaffective, mania, MDD w/psychosis -improves POS & NEG symptoms **SE: no agranulocytosis, no hyperPROL **Comp: somnolence, dry mouth, appetite, tremor, constipation, dysphagia -DM devo, lower seizure threshold **DI: CNS depressants, carbamazine
Quetiapine Ziprasidone Aripiprazole
(-)5HT2>D2 (-) Hist & musc More Atypicals: Apines and Idones Ind: schizophrenia, shizoaffective, mania, MDD w/psychosis -improves POS & NEG symptoms Quetiapine: little EPS, weight+, no hyperPROL -comp: sedation, hypotension -DI w/ CNS depress Ziprasidone: little weight+, less EPS -comp: QT inc, toursades de pointes -avoid other QT+, carbamazepine dec Aripiprazole: antag DA if high -less antichol effects, akithesia
Risperidone *Paliperidone
(-)5HT2>D2 (-) Hist (not musc!!) "Peridones pair up to attack seritone" "Risper's metabolite is his Pal" Atypical Ind: schizophrenia, shizoaffective, mania, MDD w/psychosis -improves POS & NEG symptoms **SE: neuroleptic malignancy, tardive dysk?, no agranulocytosis **Comp: Sedation, weight+, hyperProl, hyperkin, nausea, ED, anxiety -High dose: extrapyramidal sympt, postural hypoTN **Comp of Pal: QT prolong, HA, akathesia, dizzy, dystonia, tremor, drool, weight+, somnolence **DI: carbamazepine, phenytoin, rifampin, phenobarbital, other CYP3A4: incr metab
Clozapine
(-)5HT2>D2 (-) Hist, musc (side effects!) "Closes zerotonin, and Dz" Atypical Ind: schizophrenia, shizoaffective, mania, MDD w/psychosis -improves POS & NEG symptoms SE: agranulocytosis (rev/fatal), seizures, sedation, inc HR Comp: agranulocytosis, weight gain, postural hypoTN, sedation, impotence, tachycard, antichol, seizures
Prazosin
(-)A1 "Preeze losin the arterioles" Relax smooth muscle, vasodilate Tx: BPH, HTN, HF Comp: ortho hypotension, inhibits ejaculation, little reflex tachycardia 3 hours, does not block A2
Carvedilol
(-)A1, B1/2 "Carves out the HF receptors" Dec cardiac, arterial, and kidney effects of NE actions on B1/2; A1: vasodilate with drop BP *antioxidant Tx: CHF *Use w/ ACE(-) and diuretics
Enalapril
(-)ACE "Enalapril is our ACE: she laps everyone" Dec BP, afterload Vasodilate, dec aldosterone Tx CHF, HTN, MI, angina Comp: cough (bradykinin and ACE), ortho hypotension, hyperK, NOT IN PREGNANCY
Captopril
(-)ACE *Enalapril has Capped the victory Arteries>veins, dec BP/afterload, kidney sparing
Captopril
(-)ACE (Peptidyldipeptidase) "Winner's cap, but it smells like sulfur" Block AngII formation (increase renin release) Tx HTN (w/DM nephropathy), CHF, angina, post MI *Dec bp & aldosterone secretion PO w/o food Comp: hypoglyc w/ insulin (sulfr), proteinuria, hypogustia, hypersens, cough, neutropenia **contraind w/ triamterene or amiloride--hyperkalemia
Enalapril
(-)ACE (Peptidyldipeptidase); has carboxyl "Our true ace that laps everyone" Block AngII formation (increase renin release) Tx HTN (w/DM nephropathy), CHF, angina, post MI *Dec bp & aldosterone secretion PO w/ or w/o food Comp: fewer side effects
Guanethidine
(-)Adrenergic (non-receptor) "Guan makes you yawn" Dec catecholamine release Comp: ortho hypotension
Eplerenone
(-)Aldosterone (compet antag) "Epimer like spironolactone" More specific mineralcorticoid antagonist Tx HTN, post-MI
Spironolactone
(-)Aldosterone (compet antag) "breasts and Na spiral out" Binds to mineralocorticoid, androgen, and progestin receptors Tx HTN, CHF Comp: weakly diuretic
Eplerenone
(-)Aldosterone action "Epimer of spironolactone" K retention, Na excretion Dec vascular volume Tx: *CHF, cirrhosis Comp: hyperK w/ ACE(-) or ARB; gynecomastia, GI upset, mental confusion
Spironolactone
(-)Aldosterone action "Na spirals down toilet, breasts spiral out" K retention, Na excretion Dec vascular volume Tx: *CHF, cirrhosis Comp: hyperK w/ ACE(-) or ARB; gynecomastia, GI upset, mental confusion
Candesartan
(-)Angiotensin Receptor *The loser can't find the angiotensin receptor! (Losartan: Valsartan, Ibesartan, Candesartan--losers get a TAN, at least they look good) Decrease BP (dec afterload) Tx HTN
Ibesartan
(-)Angiotensin Receptor *The loser can't find the angiotensin receptor! (Losartan: Valsartan, Ibesartan, Candesartan--losers get a TAN, at least they look good) Decrease BP (dec afterload) Tx HTN
Losartan
(-)Angiotensin Receptor *The loser can't find the angiotensin receptor! (Losartan: Valsartan, Ibesartan, Candesartan--losers get a TAN, at least they look good) Decrease BP (dec afterload) Tx HTN
Valsartan
(-)Angiotensin Receptor *The loser can't find the angiotensin receptor! (Losartan: Valsartan, Ibesartan, Candesartan--losers get a TAN, at least they look good) Decrease BP (dec afterload) Tx HTN
Propranolol
(-)B "Propran is a pan beta blocker" Blocks NE/E: dec CO, rennin/angio (less O2 demand), crosses BBB Tx: HTN, arrhythmia, angina, migraine prophylaxis, anxiety, tremor Comp: HF, worsen asthma/COPD/emph (block B2), hypoglycemia, allergy comp Abrupt cessation: angina, sudden death Lipophillic/BBB, PO poor bioavail, 3-4hours
Atenolol
(-)B1 "I'll give a A TEN if you B#1" Dec BP and afterload; dec CO, dec rennin Tx: HTN Comp: less bronchial constriction, careful w/ CHF, asthma, COPD, heart blocks Longer half life than metoprolol
Propranolol
(-)B1,2 "Pro pran is a pan beta blocker" Antagonize stretch receptors: dec renin release Ind: HTN, tremor Comp: effective only when serum renin is high
Naproxen
(-)COX1/2 reversible "like an oxen: keeps workin 15 hours straight" NSAID proprionic acid Ind: RA, analgesia (w/in 30in) *sodium salt absorbed more rapid *15 hours (twice daily admin)
Ibuprofen
(-)COX1/2, non-covalent "Ibuprofen..." NSAID proprionic acid Ind: RA, analgesia *PO, 2-4hrs, rapid urine excretion Note: high protein binding, rare anti-coag events
Diltiazem
(-)Ca channel *DIL me TIA some of ZEM pills (dropped in milk) Dec contractility etc.
Meperidine
(-)Ca presyn channel; (+) K channel: hyperpol "Pregnant meper is fine using meperidine" Strong Opioid Ind: more common in obstetrics (less resp depression in fetus); no effect on cough reflex Time: shorter duration of action than morphine Comp: overdose:CNS excitation/seizure, weak antiChol activity (mydriasis, tachycard, dry mouth, blurred vision) **less constipation, not used for diarrhea DI: SSRI or MAOIs-->serotonin syndrome (fever, seizure, coma) *w/MAOI: severe restlessness, excitement
Fentanyl
(-)Ca presyn channel; (+) K channel: hyperpol "Watch the vents w/ fentanyl during anesthesia" Strong Opioid Ind: anesthetic (pre/supp), combo w/ neuroleptanalgesia (allow wakeful state) Adm: parenteral, patch, lozenge Time: shorter duration of action than morphine Comp: muscle rigid (watch ventilation) **minimal cardiac depression
Morphine
(-)Ca presyn channel; (+) K channel: hyperpol Prototype Opioid Ind: pre/post operative pain, terminal illness, relieve MI pain, acute pulmonary edema dyspnea, anesthesia supp *also: anxiolytic, venodilateor (post MI) Adm: oral, rectal, pareteral, special admin *high first pass metab: morph-6-glucuronide alagesic, morph-3-gluc is neuroexcitatory Comp: resp depression, sedation, n/v, tolerance, psycho/phys dependance, pneumonia, miosis, post hypoTN, constipation, urine retention&pain, pain from biliary spasm, pruritis DI: resp depression drgus, serotonin syndrome (hyperpyrexia, coma) if w/SSRI or MAOI
Acetazolamide
(-)Carbonic anhydrase "I see tat hole: H build up" Site 1 (prox tubule) Block Na/H antiporter by increasing proton buildup in lumen (can't reabs Na) Tx Glaucoma, epilepsy, acute mnt sickness **Dec CSF and intraocular volume Comp: alkalinized urine-->hyperchloremic metabolic acidosis **DI w/ memantine
Haloperidol
(-)D1/2 (-) weak H1, musc "Halts the D y'all" High oral potency (50x thorzaine-aka chlorpromazine) Slow release depot form available
Thiothixene Loxapine Molindone
(-)D1/2 (-) weak H1, musc Thio: high potency Lox & Mol: intermediate -intermediate potency but no clear adv over haldol or PTZ
Chlorpromazine
(-)D2 (mesolimbic & mesocortical) (-) H1 (cns), musc (pns), alpha-adre (pns) "Clear that maze inside your head" Aliphatic Phenothiazine (PTZ) Ind: shizophrenia, schizoaffective, mania, tourette's, antiemetic, delusional, depression w/ psychosis, borderline personality, agitation/violence, delerium, dementia **improves POSITIVE symptoms SE: agranulocytosis, cholestatic jaundice, photosensitive Comp: impotence, ortho hypoTN (alpha-ad), weight gain (H1), antichol, seizures, hyperPROL, withdrawal syndrome (n/v, insomnia, headache), neuroleptic malignant syndrome DI: additive effect w/ CNS depress, levodopa, antichol *antiacids decrease absorption *smoking increases metab
Triflupromazine Trifluoperazine Perphenazine
(-)D2 (mesolimbic & mesocortical) (-) H1 (cns), musc (pns), alpha-adre (pns) "Maze is gone per this group of Triflu" "Rids the maze but flood of complications: tardive dysk etc" Piperazine PTZ *High Oral Potency Ind: shizophrenia, schizoaffective, mania, tourette's, antiemetic, delusional, depression w/ psychosis, borderline personality, agitation/violence, delerium, dementia -->improves POSITIVE symptoms Hydroxyzine potentiates toxicity (pipers...)
Fluphenazine
(-)D2 (mesolimbic & mesocortical) (-) H1 (cns), musc (pns), alpha-adre (pns) "Rids the maze but flood of complications: tardive dysk etc" Piperazine PTZ *High Oral Potency Ind: shizophrenia, schizoaffective, mania, tourette's, antiemetic, delusional, depression w/ psychosis, borderline personality, agitation/violence, delerium, dementia -->improves POSITIVE symptoms **Comp: extrapyram syndromes (acute dystonia, akthisia, parkinson like); tardive dyskinesia (irreversible); neuroleptic malignant syndrome (rigid+fever, can be fatal) **Slow-release depot available **DI: hydroxyzine potentiates toxicity
Thioridazine
(-)D2 (mesolimbic & mesocortical) (-) H1 (cns), musc (pns), alpha-adre (pns) "Rids the maze but thy eyes and heart..." Piperidine PTZ *Low Oral Potency Ind: shizophrenia, schizoaffective, mania, tourette's, antiemetic, delusional, depression w/ psychosis, borderline personality, agitation/violence, delerium, dementia **improves POSITIVE symptoms **SE: inc QT, arrythmia, priapism, retrograde ejac **Comp: cardiotoxic-sudden death; retinal pigmentation & blindness **DI: hydroxyzine potentiates toxicity
Antipsychotics
(-)D2, H1/Musc/aADR : PTZ (phenothiazides) "mazines rid the maze" *Chlorpromazine: clears the maze *Thioridazine: rids maze but thy eyes and heart *Fluphenazine: maze is gone but flood of comp *Triflupromazine: maze gone w/ triflu *Trifluoperazine *Perphenazine (-)D1/2, weak H1/Musc *Thiothixene *Haloperidol: halt the D y'all *Loxapine *Molindone (-)5HT (each drug varies here) - ATYPICALS "apines & idones attack the dopaMINES and seratONES" *Clozapine: cloze zeratonin *Risperidone: peridones attack the serotone *Paliperidone: risperidone's pal (metabolite) *Olanzapine: another atypical (D2, 5HT) *Quetiapine: quiet comp *Ziprasidone *Aripiprazole
Amoxapine
(-)DA receptor, (-)NE reuptake Xapine zaps the DA receptor, and acts like a TCA Atypical but tx same TCA indications Ind: MDD, bipolar affective d/o, ADHD Comp: movement d/o (EPS, tardive dyskinesia), hyperPROL DI: CNS depressants, clonidine, alpha-methyldopa, anti-Chol, MAOIs (serotonin syndrome)
Drugs of Hemostasis
(-)Glycoprotein IIb:IIIa **Abciximab, Eptifibatide (-)COX **Acetylsalicylic Acid (aspirin) (-)PLT aggregation **Ticlopidine, Clopidogrel Fibrinolytic **TPA, streptokinase, urokinase Anti-coag **Heparin, fondaparinux, rivaroxaban, warfarin
Loratadine - claritan *Desloratidine - clarinex *Azelastine *Fexofenadine - allegra *Cetirizine - zyrtec
(-)H1 receptor "The --tadines tick off the hista-mines" Second generation H1 receptor antagonists-->DO NOT cross BBB Longer half life; no crossing BBB, no sedation/no antiChol action Comp: abs altered with grapefruit juice; arrhythmias
Rhinitis & Cough Drugs 1
(-)H1 receptor (1st gen) *Diphenhydramine, clemastine, pyrilamine *Clorpheniramine, brompheniramine *Cyproheptadine, meclizine, hydroxyzine *Promethazine --"Hydramines, astines, pheniramines, and izines block the histamines and muscarines" --Hydralisks are Asses, it's Phunny don't I Zink? (-)H1 receptor (2nd gen) *Loratadine, desloratidine, azelastine, fexofenadine, cetirizine --"The tadines, astines, & izines block the histamines and muscarines" --No more Hydralisks and Phunny-Ta da! (+)alpha1 *Epinephrine, oxymetazoline, phenylephrine, xylometazoline, cocaine --"Epi & zolines let's you breath and smell Febreeze" *Pseudoephedrine "sort of like epi"
Chlorpheniramine *Brompherniramine
(-)H1 receptor (1st gen), (-)Musc --"Hydramines, astines, pheniramines, and izines block the histamines and muscarines" --Hydralisks are Asses, it's Phunny don't I Zink? --alkylamine Tx rhinitis, induce sedation, motion sickness, common cold prophylaxis *PO *onset 30 min; max effect 1-2 hours Comp: sedation, anti-chol, hypersens, tolerance, CNS stim in children *careful giving to asthmatics: H1 block can thicken bronchial secretions (more obstruction) Crosses BBB & placenta
Diphenhydramine (benadryl) *Clemastine *Pyrilamine
(-)H1 receptor (1st gen), (-)Musc --"Hydramines, astines, pheniramines, and izines block the histamines and muscarines" --Hydralisks are Asses, it's Phunny don't I Zink? --ethanolamine Tx rhinitis, induce sedation, motion sickness, common cold prophylaxis *PO *onset 30 min; max effect 1-2 hours Comp: sedation, anti-chol, hypersens, tolerance, CNS stim in children *careful giving to asthmatics: H1 block can thicken bronchial secretions (more obstruction) Crosses BBB & placenta
Cyproheptadine *Meclizine *Hydroxyzine *Promethazine
(-)H1 receptor (1st gen), (-)Musc --"Hydramines, astines, pheniramines, and izines block the histamines and muscarines" --Hydralisks are Asses, it's Phunny don't I Zink? --piperazine Tx: hydroxyzine used for conscious sedation *PO *onset 30 min; max effect 1-2 hours Comp: sedation, anti-chol, hypersens, tolerance, CNS stim in children Crosses BBB & placenta
Receptor blockage side effects
(-)H1: Sedation, weight+, hypotension, potentiate CNS depressants (-)Muscarinic: dry mouth, blurred vision, urinary retention, constipation, memory dys, tachy -Blind as a bat, mad as a hatter, red as a beet, hot as a hare, dry as a bone, the bowel and bladder lose their tone, and the heart runs alone. (-)alpha1-adre Postural hypotension, reflex tachy (-)alpha2-adr Block anti-hypertensive effects of clonidine, alpha-methyldopa (-)5-HT2 Ejac dysfunction
Venlafaxine (Desvenlavaxine) Duloxetine
(-)NE/5HT reuptake Dulox is the delux duo: blocks NE&5HT reuptake -Send the fax (venlafax) Atypical/SNRI Ind: neuropathic pain, if don't respond to SSRI, anxiety (+GAD) Comp: most likely due to discontinuation, high dose-seizures
Furosemide
(-)NKCC at asc limb Loop diuretic Dec vascular volume, TPR Tx: *CHF, pulm edema (acute/rapid) Comp: OTOTOXICITY, hypoK, hypoMagn, hypoVol, gout
Bumetanide
(-)NKCC2; high ceiling "loop" "Bums in a Fury" Site 2 (asc limb) Block N/K/2Cl-4x potency Tx Diabetics (less hyperglyc) or those allergic to furosemide **diuresis, vasodilator PO or SubQ Comp: less hyperglycemia than furosemide **OH DANG (ototoxic, hypoK, dehydration, allergy-sulfa, nephritis, gout) **DI: COX inh, propranolol, org acids, albumin
Ethacrynic Acid
(-)NKCC2; high ceiling "loop" "Ethan is in a Fury about his sulfa allergy." Site 2 (asc limb) Block N/K/2Cl-w/o sulfonamide Tx patients w/ sulfa allergy **diuresis, vasodilator PO or SubQ Comp: more GI problems, less hyperglyc **OH DANG (ototoxic, hypoK, dehydration, allergy-sulfa, nephritis, gout) **DI: COX inh, propranolol, org acids, albumin
Furosemide
(-)NKCC2; high ceiling "loop" "In a fury lose N,K,Cl,Cl" *N,K,C,C (also Na, K, Cl, ... but also Ca) Site 2 (asc limb) Block N/K/2Cl--tubular side; inc renal blood flow Tx Edema (acute/pulmonary), inc Ca, HTN in pts with dec renal blood flow **diuresis, vasodilator PO or SubQ Comp: OH DANG (ototoxic, hypoK, dehydration, allergy-sulfa, nephritis, gout) **DI: COX inh, propranolol, org acids, albumin
Torsemide
(-)NKCC2; high ceiling "loop" "Unlike furosemide, tore its way to the receptor" Site 2 (asc limb) Block N/K/2Cl-2x greater bioavailability QD dose: long half life Comp: **OH DANG (ototoxic, hypoK, dehydration, allergy-sulfa, nephritis, gout) **DI: COX inh, propranolol, org acids, albumin
Chlorothiazide
(-)Na/Cl cotransport (thiazide) "Chloride blocking thiazide" Site 3 (DCT) HyperOsm urine Tx HTN, CHF, hyperCa, mild edema, Diab Insipid **Long term therapy PO, long half life Comp: hypoK, hypoNa, orthostatic hypo, Inc Ca, Inc glucose, Inc lipid, hypersens, lithium buildup, metabolic alkalosis **digitalis toxicity (hypokalemia) **dec renal BF **phosphaturia Not useful if GFR<30 mL/min
Hydrochlorothiazide
(-)Na/Cl cotransport (thiazide) - POTENT "Hydro is hyper chlorothiazide" Site 3 (DCT) HyperOsm urine; MORE POTENT Tx HTN, CHF, hyperCa, mild edema, Diab Insipid **Long term therapy PO, long half life Comp: hypoK, hypoNa, orthostatic hypo, Inc Ca, Inc glucose, Inc lipid, hypersens, lithium buildup, metabolic alkalosis **digitalis toxicity (hypokalemia) **dec renal BF **phosphaturia Not useful if GFR<30 mL/min
Hydrochlorothiazide (HCTZ)
(-)Na/Cl transport at DCT "Thiazide!" Thiazide diuretic Dec Reab Na; loss of Cl, K, Mg, water Dec vascular volume & TPR Tx: HTN, *CHF, hypercalciuria, diabetes ins Comp: hypoK, hypoNa, gout, volume depleted
Vardenafil
(-)PDE 5 *Varden can't A FIL his level garden Levitra Tx ED
Tadalafil
(-)PDE 5-more specific *Tadal taled that we saw the Cialis commercial Cialis Tx ED
Acetaminophen (tylenol)
(-)PG biosynth - more CNS (neuron COX??) "A C for acting more on CNS" Non-opiate analgesic Ind: analgesia, antipyretic (acts centrally) *Use IF: hx ulcer, blood abnormality, ASA hypersensitive Dose: 2-3 hours, PO Comp: renal tox w/ long term dose, hep tox w/ above therapeutic dose *alcohol exacerbates - uses GSH; NAPQI bad Note: red pep ulcers, no affect on TXA2, safe pregnancy, NOT anti-inflamm
Sildenafil
(-)Phosphodiesterase 5 (PDE 5 inhibit), inhib breakdown of cGMP *Sild had a wild night, but couldn't A FIL his cavernosa Viagra Tx ED, pulmonary HTN
Amiloride
(-)Physiological Aldosterone antagonist "Amy my love--proposing on Tram with gynecomastia" Electrogenic, fast acting physiological antag of aldosterone; (-)Na channel influx, dissipates transepithelial potential
Aliskiren
(-)Renin (inhibit peptidase) *Alis cures Renin overdrive Tx HTN
Aliskiren
(-)Rennin peptidase activity "Alice cures our kidney from rennin" Reduces angioII: Vasodilation Tx HTN Comp: hyperK; greater rennin rebound than others
Conivaptan
(-)V1a/V2 "Vaptan evaporates vasopressin effects; Coni likes both" Tx: hyponatremia **also SIADH, CHF, cirrosis, hyponatremia, (euvolaemic hypoNa therapy) Comp: thirst, dry mouth, polyuria
Tolvaptan
(-)V2 "Vaptan evaporates vasopressin effects; Told you 2" Tx: cirrosis, CHF *also SIADH, CHF, cirrosis, hyponatremia Comp: thirst, dry mouth, polyuria
Lixivaptan
(-)V2 "Vaptan" Tx CHF but clinical trials haven't shown improved morbidity/mortality
Codeine
(-)cough reflex via cough center "The coughing dean is in a lot of pain" Weak agonist Ind: moderate pain, antitussive, diarrhea Adm: high oral:parenteral *10% converts to morphine *Vicodin = codeine + acetomenophin Comp: OD-seizures, less likely abused, less likely to cause resp depression
Oxycodone (Dihydrocodeine) (Hdrocodone)
(-)cough reflex via cough center Weak agonist Ind: mod pain, antitussive, diarrhea Adm: oral sustained release *Percocet = oxycodone + acetamenophin Comp: OD-seizures, resp dep & abuse less likely
Allopurinol
(-)xanthine oxidase "All the purinol metabolites are Fee Buxed (stopped)" Inhibits biosynthesis of uric acid (comp antag) Long term therapy Indication: chronic, tophagous gout (high urate, imparied renal, hypersensitive to uricosuric agents) **use if hypersensitive to uricosuric agents PO Complication: may precipitate gout attack on therapy initiation; GI sx, skin rash, hypersens Drug interactions: Increases half life of: azothiaprine, mercaptopurine, dideoxyadenosine, warfarin **activatees anticancer agent 5FU
Febuxostate
(-)xanthine oxidase (more specific) ""All the purinol metabolites are Fee Buxed (stopped)" Inh biosynthesis of uric acid (more specific) Indication: reduced freq of hypersensitivity (comp to allopurinol) Complications: CV adverse effects and similar drug interactions to allopurinol
*terazosin
(Hytrin). An alpha-1 blocker that relaxes smooth muscles of arteries, prostate, and bladder neck. Lowers b/p & allows those w/enlarge prostates to pee.
Philocarpine
(M1-5) *"PILE on the sweat and tears" Closed/narrow (pupillary sphincter) and open angle glaucoma (ciliary muscle)
Bethanechol
(M1-5) *Beth mixed methane/carbachol "Beth Anne, call me if you want to activate your bowels and bladder" urine or fecal retention
Methacholine
(M1-5) *Methal: attacks Muscarinic-like ACh; add meth L esophageal sphincter response; Also challenge test to diagnose asthma
Muscarine
(M1-5) *muscarine=muscarinic receptors not used as drug; found in drugs
Carbachol
(NN, NM) *carbachol keeps it all (Carbamate increases half life) Open-angle glaucoma
Nicotine
(NN, NM) *nicotinic smoking
Acetylcholine
(NN, NM, M1-5)
Donepezil
(Nic/Musc) -revers AChEI *It's a done puzzle--delay Delay Alzheimers
Neostigmine
(Nic/Musc) -revers AChEI *Neo had myesthesia gravis AND atony "NEO CNS = NO CNS" Non obstructive GI/GU atony; myesthasia gravis
Edrophonium
(Nic/Musc) -revers AChEI *does EDRO have myesthasia? yes: then let's PHONe HIM Diagnose myesthasia gravis (very short half life)
Physostigmine
(Nic/Musc) -revers AChEI *physo (physics shows permeability to CNS) stigmine (stick it in AChE) "PHYS is for the EYES" Acute glaucoma, atropine poisoning, Alzheimers
pirenzipine*
* Cholinergic Antagonist: Muscarinic Agonist * Selective for M1, low side effects • Reduction in vagally stimulated gastric acid secretion • Peptic ulcer disease • CANADA & EUROPE
Barbituates
**barbital Amobarbital Pentobarbital: pento stops the vent yo Secobarbital Thiopental: sleep in thi pent house Phenobarbital: convulsing aint Phunny Mephobarbital
Cholinesterase inhibitor poisoning
*DUMBBELSS Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation of skel muscle & CNS, lacrimation, sweating, and salivation ANTIDOTE: atropine + pralidoxime
Local Anesthesia
*Procaine: P-ESTER blocks Na's maine (Tetracaine, benzocaine) (Cocaine): can also block the Na's maine *Lidocaine: L-AMIDE blocks the Na's maine; L=liver metab (Mepivacaine, bupivacaine, etidocaine) *Prilocaine EMLA=Priolocaine + Lidocaine
Buspirone
+5HT1A-receptor (partial agonist) "Buspi is slow as a BUS but aint Sleepy" Azaperone Ind: chronic GAD (gen anxiety d/o), week antidepressant Time: short onset (up to 1 week) Comp: HA, nausea, dizzy, insomnia, nervous, restless, dysphoria, tachycardia **Note: no interaction with EtOH, no dependence/hypnosis/sedation
Dopamine
+A1,B1 *I don't a mind if my kidney stays mine Increase renal perfusion while increasing BP, HR, contractility Tx acute failure IV drip
Dobutamine
+B1 *Dough butt B #1 Increase contractility Tx Acute failure IV drip; cardiogenic shock
Metaproterenol Pirbuterol Albuterol Levalbuterol Salmeterol Formoterol
+B2 adren "Met a pro: now breath..."--rapid onset, Inh "Pretty butt-get excited, keep breathing" "Albuterol, Lev-albuterol"--intermed onset, PO/Inh "Motors all day long"--long onset, Inh (LONG ACTING) Inhibits mast cell release, inc mucociliary clearance, relaxes airway (smooth muscle B2) Tx Asthma Levalbuterol: R enantomer of albuterol *more active, fewer CV side effects *Contraind: CV disorders, hyperthyroid, DM Salmeterol NOT used alone: increased CV deaths (use with corticosteroids)
Zolpidem Zaleplon Eszoplicone
+GABAa (bind alpha1 subunity)--> Cl conductance "Zaleplon plans on saling non-BZ" Zolpidem, eszoplicone **non-BZ hypnotic / SAFER!!! Ind: insomnia (short term) -little muscle relaxant and anticonvuls effect Time: rapid onset, short duration Comp: ph dependence, less withdrawal symp, safer than BZ note: CYP3A4 metab, minimal tolerance, less amnesia, less daytime sedation
Ramelton
+MT1 & MT2 in brain (superchiasm nuc) "Rame plays the game where he makes you fall asleep without touching the GABA receptor" Melatonin Receptor Agonist Ind: insomnia (induction) Comp: dizzy, lethargy, endocrine changes
Chlordiazepoxide
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Chlordi clings onto her pillies"-depedance Benzodiazepine **Ind: physical dependance/withdrawal **Time: half life>50hrs Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors Note: low lipid solubility
Diazepam
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Dia lives her days doing everything" Benzodiazepine **Ind: status epilepticus, drug/toxin induces seizures, skel muscle spasticity, physical dependance **Time: long >50hrs Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors **Note: *HIGH lipid solubility (short action duration)
Flurazepam *Temazapm
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Flury keeps the furry outside while you're warm and tucked in bed inside" Benzodiazepine Ind: insomnia (maintenance) Time: short-intermediate Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors Note: low lipid solubility
Midazolam
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "In MY DAYS we hypnotized with a pendulum watch, not MIDAZ-olam" Benzodiazepine **Ind: Pre-anesthetic, hypnosis, anxiety **Time: rapid onset, shorter activating Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors
Lorazepam
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Lory's pills are like a bedtime story & gets rid of her seizures in a hurry" Benzodiazepine **Ind: insomnia (induction), status epilepticus, drug/tox induced seizures Time: short-intermediate Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors Note: low lipid solubility
Oxazepam
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Lory's pills are like a bedtime story & gets rid of her seizures in a hurry" **Ox: get her ox sat during seizure Benzodiazepine ** Time: short-intermediate Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors Note: low lipid solubility
Alprazolam
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Short trip to the alps makes one calm down" Benzodiazepine **Ind: Short term anxiety management, agoraphobia, acute mania/bipolar Time: short-intermediate Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors **Note: physical dependance more common w/ short acting BZ
Triazolam
+allosteric inc opening of GABA stim Cl channels (hyperpolarize cell) "Try falling asleep one more time" Benzodiazepine **Ind: insomnia (induction) Time: short-intermediate Comp: sedation, drowsiness, ataxia, confusion, impair judgment, anterograde amnesia, resp depression w/COPD, elderly more vulnerable DI: CNS depressants and CYP3A4 inhibitors **Note: *HIGH lipid solubility
Entacapone & Tolcapone
- COMT *hard to put a CAP on ONEs head with parkinson's. Maybe COMpanion can help increase dopamine duraction Tx parkinson's
Clorgyline
- MOA-A Increase 5HT duration
Selegiline
- MOA-B *At the MOA, selling parkin' passes increase dopamine duration Tx parkinson's
alpha-Methyltyrosine
- Tyrosine hydroxylase inhibits NE synthesis
Diltiazem
-(Ca channel) *DIL me TIA some of ZEM pills; my heart is killing me Dec contractility and O2 demand Tx angina
Nifedipine
-(Ca channel) *Knife cuts through bone (calcium) Dec contractility and O2 demand Tx angina
Atropine
-(M1-5) *A trip to pine BLOCKS musca-rine "Blocks DUMBBELSS" Optho exam: Produce mydriasis & cyclopegia Also decrease Parkinson secretions
Propantheline
-(M1-5) *Drank some propane--ulcer Tx Peptic ulcer
Ipratropium
-(M1-5) *I PRAY i can breath soon Tx reversible airway disease (asthma, COPD)
Tiotropium
-(M1-5) *Ipratropium's uncle (tio) Tx reversible airway disease
Scopolamine
-(M1-5) *on cruise ship, looking through SCOPE makes you seasick Tx motion sickness, preanesthetic
Carvediol
-(a1/b1&2) Carve it all out: except A2 Decrease NE: dec TPR & HR Tx CHF step 2
Atenolol
-(b1) *I ate all that? need to calm down and B1 with myself Decrease BP & afterload Tx CHF step 2
Metoprolol
-(b1) *Riding the Metro: calm down heart (don't confuse with metaproterenol) Beta antagonist: enerol Beta blocker: olol Decrease Cardiac output & renin Tx CHF step 2
DOXAZOSIN
-A1 *Losin ability to pee a Z: Prazosin, doxazosin, terazosin Tx BPH, HTN
Terazosin
-A1 *Losin ability to pee a Z: Prazosin, doxazosin, terazosin Tx BPH, HTN
PRAZOSIN
-A1 *Preeze give me some A1 sauce *LOSIN ability to pee a Z: Prazosin, doxazosin, terazosin Tx benign prostate hypertrophy, HTN, heart failure
Carvedilol
-A1 & -B1,2 *Carve out that dilated heart: CHF *no A2 feedback but all others Alpha: decrease vasoconstriction/BP Beta: decrease cardiac and kidney effect Tx CHF
Phenoxybenzamine
-A1,2 (Irrev) *Phentol told TOLAZ and PHENOXY his secret Tx pheochromocytoma & ED
PHENTOLAMINE
-A1,2 (rev) *No reason to VENT, no longer have ED (it's A ok - both A1/2) Reduce periph resistance from NE/E Tx pheochromocytoma and male ED
Tolazoline
-A1,2 (rev) *Phentol told TOLAZ and PHENOXY his secret (work similar) Tx pheochrom & ED
YOHIMBINE
-A2 (rev) *Yo Him! don't stop Him (negative feedback A2) Increase NE release (block neg feedback) Tx diabetic neuropathy and ED; depression
Atenolol
-B1 *I ATE all that? help me calm down so I can B 1 with myself Tx HTN
Metroprolol
-B1 *Riding the METRO: need to decrease HR Decrease Cardiac Output and Renin Tx HTN, angina, hyperthyroidism
Metoprolol
-B1 *Riding the METRO: need to decrease HR Class II: Decrease Cardiac Output and Renin; Dec contractility/HR/AV Tx: V tach/fib, A flutter/fib (rate control)
PROPRANOLOL
-B1,2 *A PRO on a PLAN takes this to reduce anxiety *Like propanol, pran 2B Block NE/Epi Tx HTN, angina, arrythmia, anxiety
TIMOLOL
-B1,2 *Tim you have LOTs of aqueous humor in 1 eye... no 2 eyes (b1,2) Decrease aqueous humor prod (B1) Tx HTN, open angle glaucoma
Propranolol
-B1,2 *A PRO on a PLAN takes this to reduce anxiety *Like propanol, pran 2B Class II: Block NE/Epi; Dec contractility/HR/AV Tx: V tach/fib, A flutter/fib (rate control), PAT
Pindolol
-B1,2 partial *Pin down BP problem without affecting HR Decrease BP (smaller effect: HR) Tx HTN with bradycardia
Pirenzipine
-M1 *Pirenzip says don't take a SIP of acid Decreases acid secretion
Tolterodine
-M3 *TOLD HER not to pee her pants at the DINEing table Inhibits bladder contractions
Atracurium
-NM *A track: help relax OR muscle relaxation
d-Tubocurarine
-NM (AChR) *Turbo cure: relax OR muscle relaxation or myasthenia gravis
Succinylcholine
-NM (depolarizing nicotinic) *Suck: I can't repolarize no CNS, prevent repolarization
Hexamethonium
-NN (ganglion) *TRIED METH to put a HEX / against NICK "Put a HEX on smokers to help them quit" (trimethaphan & hexamethonium: INHIBIT nicotinic) HTN crisis
Trimethaphan
-NN (ganglion) *TRIED METH to put a HEX / against NICK (trimethaphan & hexamethonium: INHIBIT nicotinic) HTN crisis; IV
Lisinopril Quinapril Benazepril
-april = ACE inhibitors Lisinopril: no plasma binding Quinapril Benazepril: most potent PDP inh *our Mercedes Benz of the group
Drug development
1 Preclinical (animal studies, tissue culture) 2. Clinical -phase 1: safe dose (1/10 rodent LD to MTD=max tolerated dosage) -phase 2: efficacy @ 80%MTD; 15% response -phase 3: compare to gold standard *Group C status 3. Approved process: FDA (new drug app)
TX review for viral 1. HSV1&2, VZV 2. CMV 3. EBV 4. HSV 6/8 5. RSV 6. INFL A 7. INFL A&B
1. Acyclo/famciclovir (res: foscarnet; keratitis: idoxuride) 2. Gangciclovir, cidofovir (res: foscar; aids: fomivirsen) 3. 4. 5. Ribavirin (also for Hep C) 6. Amantadine (A for infl A) 7. Zanamazir/oseltamivir
Osteoporosis Tx
1. Ca supp (Ca Citrate) & VitD supplement 2. Estrogen 3. Teriparatide (synth PTH) 4. Alendronate (aminobisph)
Tx plans: 1. serious systemic 2. histo/blasto (Non CNS) 3. crypto meningitis
1. amphotericin B 2. itraconazole 3. fluconazole (fluco C)
Parasite treatments: 1. P falciparum 2. P falc (res) & P vivax 3. Larval tapeworms 4. Ascaris, hookworm, pinworm, whipworm 5. Strongyloides 6. Schistosoma
1. chloroquine 2. quinine + tetracycline 3. albendazole 4. mebendazole 5. ivermectin 6. praziquantel
16**Upper GI Drugs**(cont)
1.Contact Protection Sulcrafate: "stop sulking; improve fate with sulcrafate" 2.Mucus: "business to mucus up: bismuth" Rebamipide, Carbenoxylone, Bismuth compounds (Pepto Bismol) ** Prokinetic Agents Neostigmine: nife into AChE Metoclopramide: Metoclo say NO to dopamide Cisapride: Serotonin pride Erythromycin: earth keeps movin (motilin) ** Gallstone dissolution: "Deoxycholic = deGallstone" Chenodeoxycholic acid & Chenodiol: block chol secretion Ursodiol & ursodeoxycholic acid: urso dec bile and lipid secretion Methyl tert-butyl ether: ether injection GB Monoctanoin: vegetable oil injection BD
2**Cephalosporin Antibiotics**
1st gen: "Chef flex" & PEcK Cephalexin Cefazolin ** 2nd gen: "oxen, fox, apple" & HENS PEcK Cefaclor Cefoxitin Cefuroxime ** 3rd gen: "ceph 3 tree" Cefixime Cefotaxime Ceftaxidime ** 4th gen: "pine tree" Cefepime
5**Anti-Mycobacterial Agents**
1st line Anti-Tb: "RIPE" Isoniazide: "iso blocks myco" Rifampin: "Ref amp pic blocks RNA poly" *Rifobutin if on haart Ethambutol: "pic-blocks arabinsyl transferase" Pyrazinamide: "peaks inside-intracellular nicotamide" ** 2nd line anti-Tb: "Amino, fluoro..." Aminoglycosides (streptomycin, amikacin, capreomycin) Ethionamide: "ethio blocks myco" (Para-aminosalicylic acid) Fluoroquinolones (moxi/levo/gatifloxacin) (Cycloserine, linezolid) ** Other: Macrolides: clarithro, azithro Dapsone Clofazamine
Q: HTN, asthma
1st use diuretic Alpha 1 blocker could work but risky
Air toxin 1,3 butadiene Sick building syndrome
200+ chemicals (cig, de-gasing) 1,3 but: rubber product synth (E. Houston) *Carcinogen (lung, hematologic, other) Sick building syn: HA, fatigue, nasal congest, dry skin
Lead (Pb)
2MC metal poisoning Kids have higher GI abs Pb binds Hgb or membranes; redistribute to bone and soft tissues (20yrs bone) Acute: CNS paresthesia, weak, generalized pain & hemolysis *SLAP Lead - ALAD and ferrochelatase Chronic: Kids get lead encephalopathy, lose appetite/constipation, anemia, renal fibrosis & nephrosclerosis, HTN, stillbirth Tx: EDTA (on/off because of bone reserv); dimercaprol is alternative *Succimer for child
HAART
2NRTI + NRTI/NNRTI/PI: 1. Lamivudine/emtericitabine 2. Zidovudine (AZT) "vudines while you dine-lame side" + 3a. Efavirenz (elfs never deliver) 3b. Lopinivir (never have late protein shake)
Para-aminosalicylic acid (PAS)
2nd line anti-TB Inhibit folate (similar to PABA)
Zolendronic acid
3rd gen bisphosphanate Like bisphosponate: ATP analog induces osteoclast apoptosis Tx: reduce hip/wrist/vert fracture
5-FU
5 fluorouracil: block thymidilate(dTMP) synth Breast: CM5,CA5 Mech: inhibit thym.synthase (FdUMP) Use: breast (cm5,ca5), GI CA (w/leucovorin) *topical: BCC & premalignant keratoses Tox: myelosupp NOT reversible with leuco *stomatitis, diarrhea (indicate proper dose) Resist: dec conversion to FdUMP, alter thym.synthase Note: penetrates into all tissue (inc CNS)
Maintenance Dose
= Elimination Rate/F =CL x [D] / F Again note: Loading dose = Vd x [D] but... Maintenance dose = CL x [D]!!!
Elimination Rate Constant k
= slope of ln[D] curve *k = 0.7/half life
acetylcholine*
A neurotransmitter used by neurons in the peripheral and central nervous systems in the control of functions ranging from muscle contraction and heart rate to digestion and memory.
*Lidocaine
A patient on your unit is being treated for symptomatic preventricle contractions begins to complain about double vision, which drug might the patient be having an adverse reaction to?
Epinephrine
A/B adrenergic Agonist "EPI let's you breath" Inhibits mast cell release, inc mucociliary clearance, relaxes airway (smooth muscle B2) Tx Asthma *Long term control; PRN for acute symptoms *Inhale, SubQ (emergency) *Immediate, short duration Comp: vasoconstriction, cardiac stim, skeletal tremor, refractoriness (counter with corticosteroid), mask progression of disease
PHENYLEPHRINE
A1 *topical to nasal mucous or eye: "feels PHUNNY"-so funny he's #1 Vasoconstrict, less mucous, mydriasis, bp Tx decongest, hypotension, atrial tachy
DOPAMINE
A1, B1, D1 *Dopamine: I don't mind if the kidney stays mine Low dose: D1 renal perfusion High dose: contractility/HR; highest: BP Tx hypotensive shock AND protect kidney
NOREPINEPHRINE
A1,2 & B1 *NO effect on B2; rest same as EPI (has NO methyl) local anesthesia, hemorrhage, hypotension/shock(rare)
EPINEPHRIN
A1,2 & B1,2 *Epi Pen Tx Asthma attack, anaphylaxis, cardiac arrest, open angle glaucoma
AMPHETAMINE
A1,2 (direct/indirect) *Amp up your CNS/bp/hr - amped and fed up with NE CNS stimulant, bp, hr Tx ADHD, narcolepsy
EPHEDRINE
A1,2 (indirect/indirect) *ephedrine: is FED up with NE (kicks it out--release of NE) Bronchial relaxation, nasal vasoconstrict Tx decongestant, asthma, hypotension
Pseudoephedrine
A1,2? *like ephedrine vasoconstriction, contraction, decongest Tx decongestant, stress incontinence
Clonidine
A2 *CLONE says TONE it down (A2 negative feed back decrease BP Tx hypertension; opioid withdrawal; diarrhea
Q: HTN, CHF
ACE (-)
Enalapril
ACE inhibitor *Ena laps everyone--she's our ACE Decrease BP (dec afterload) Tx CHF step 1
*enalapril
ACE inhibitor / antihypertensive (HTN, HF, slow progression of LVD; unlabled: proteinuria in steroid resistant nephrotic syndrome) VASOTEC
*captopril
ACE inhibitor prototype: used in HTN, diabetic renal disease, and CHF. Tox: hyperkalemia, fetal renal damage, cough ("sore throat")
Q: HTN, type2 DM, dec clearance
ACE(-) or ARB
Q: poor kidney function, HTN, hypoK
ACE(-) or ARB
Q: Elderly, P.A.T., est accessory track
ACE, ARB Cautious with Beta-blocker; NOT verapamil (calcium block)
Pralidoxime
AChE REACTIVATOR *PRAY it will detox in time Treat NMJ effects of Cholinergics; cannot cross BBB
Neostigmine
AChE inhibitor "Put a stick in it, inhibitor" Use: avoid residual paralysis, reverse blockage Disadv: incomplete effectiveness *CV side effects
Lysine vasopressin
ADH agonist (+V1a,V1b, V2) "Lysine is like Tannin but is Longer acting" IV or intranasal, more stable than Tannin *** Tx: pituitary diabetes insip, **GI bleed (esoph, divertic) - chronic DI w/ clofibrate & chlorpropramide
Tannin Vasopressin
ADH agonist (+V1a,V1b, V2) "Tannin for a short time" parenteral, short acting *** Tx: pituitary diabetes insip, **GI bleed (esoph, divertic) - chronic (better than desmo because desmopressin only does V2) DI w/ clofibrate & chlorpropramide
Lithium
ADH antagonist "Lit up the fire and burned out the cAMP" Decreases AC activity Higher risk of toxicity compared to others
Demeclocycline
ADH antagonist "The kidney demon is cycling all the water back" (-)water peremeability caused by ADH (NOT AFFECTING cAMP) Unpredictable time course Tx: SIADH, hyponatremia Effectively causes nephrogenic diabetes insipidus
What chemo drugs cross BBB?
ALKYLATING: Nitrosureas (-mustines) Procarbazine (MOPP) Anti-metab: 5-FU
Chemo Drug Combo (cont)
ALL: VM6P (All say VM and 6 pee) Vincristine, Methotrexate, 6-MP, Prednisolone Breast: CD5, CM5 (California & Camera high 5 breast) Cyclophosphamide, Doxorubicin, 5-FU Cyclophosphamide, methotrexate, 5-FU
Losartan
ARB "Losers can't find receptor; get a tan instead" Dec BP, afterload Vasodilate Tx HTN, CHF comp: ortho hypotension, hyperK, NOT IN PREGNANCY
Losartan
ARB "loser can't find the angiotensin receptor" Block AT-1 receptors from AngII Tx: alone or w/HCTZ PO Comp: dizziness, hyperkalemia *excreted in ble
Valsartan
ARB "losers all get -a tan" Block AT-1 receptors from AngII Tx: alone or w/HCTZ PO w/o food
Losartan
ARB *The loser can't find the angiotensin receptor! Decrease BP (dec afterload) Tx CHF step 1
Q: Elderly, HTN, dizzy
ARB Diuretics would work but cause increased urination
Vitamin C
Abscorbic acid: "Viking C = sea" Cofactor but not B vitamin Protein hydroxylation, anti-ox, Fe absorp "Tea & toast" diet *Def: perifollicular hemorrhage, impaired wound heal, swollen gums Tx: *high dose: false + urine glucose & suppresses hemoccult (miss colon CA) *megadose: diarrhea, renal damage (oxalate stones)
NSAIDS
Acetic Acid: olacs and fenacs *Indomethacin: "block Indo that mit" *Diclofenac: "dicks in Europe use this fenac" *Ketorolac: only parenteral NSAID (Sulfindac): renal insuff *Etodolac: COX2>1 Propionic Acid *Ibuprofen: duh *Naproxen: "like an oxen--works 15 hour" Salicylate "Aspirin! ASA" Fenamate (meclofenamic acid, mefenamic acid): fair weather fanatics Oxicam (prioxicam, meloxicam): camps out 45 hrs COX2 Specific *Celecoxib: "only cox2 still selling" (Rofecoxib, valdecoxib)
pralidoxime*
Acetylcholinesterase regenerator (antidote for organophosphate poisoning): very high affinity for phosphorus in organophosphates. Tox: neuromuscular weakness.
(Zonisamide)
Acts on volt-dep Na channels Possibly acts on voltage-dependent T-type Ca channel New AED Ind: partial and generalized tonic-clonic in resistant patients, BROADER SPECTRUM Comp: CNS-related--drowsy, cogn impaired *kidney stones, weight loss
Iron (Fe)
Acute & Young child: think Fe tablets Chronic: transfusion, hemachrom, miner 3 phases: GI (2hrs), recovery, relapse (12-48hrs)-metabolic acidosis/shock/death Tox: heart, liver, pancreas Tx: Decontaminate (get sh*t out) *Acute: Defiroxamine *Chronic: Deferasirox *Hemochrom: phlebotomy
Tx Emphysema, Chronic Bronchitis, COPD
Acute: B agonist (albuterol), anti-Chol (iprtroprium) Chronic: long acting B agonist (salmeterol), anti-Chol (tiotropium), Methylxanthine (theophylline) Severe airway obstruction: inhaled corticosteroids
Cortisone
Addison's disease, 21-OH deficiency Adrenocorticoal insuff, rheum, derm, optho, allx Most potent of ALL glucocorticoids S/E: INC: stomach acid, PTH, Ca excretion Block: Ca abs
dobutamine*
Agent which stimulates cardiac contractile force more than rate with little effect on total peripheral resistance
Aliphatic alcohols & glycols: Methanol (wood alcohol)
Alcohol dehydrogenase: methanol to formaldehyde & formic acid Retinal cells: blindness Formic acid: systemic acidosis CNS depress (like EtOH) Tx: hemodialysis, ethanol, VitB1 & B6
Spironolactone
Aldosterone antagonist (K sparing) *Men see their breasts SPIRAL out and start LACTATING--only to get their sodium to SPIRAL down the toilet K retention, Na excretion Tx CHF step 1
Pesticides & Herbicides (cont)
Aliphatic hydrocarbon solvent/vapor *methane, ethane, propane, butane, hexane ---- Aliphatic alcohols & glycols *Methanol: formic acid *Ethylene glycol & Propylene glycol ---- Halogenated aliphatic hydrocarbon solvents *Dichloromethane, chloroform, carbon tetrachloride, halothane - (free radicals...) Aromatic hydrocarbon solvents:DNA adducts *Benzen, toluene Polychlorinated & polyhydroxylated hydrocarbons: *PCB (polychlorin. biphenyl), PBB (bromin)
Drugs that treat Gout
Allopurinol: all the purinol metabolites are fee buxed Febuxostate: same (all the purinol...) Pegloticase: peg this in case others don't work (uricase) Colchicine: leukocytes run cold Probenecid: prohibits gout transport Sulfinpyrazone: so fillin the holes
Q: LDL high
Alpha 1 antagonist (doxazosin)
phenylephrine*
Alpha agonist used to produce mydriasis and reduce conjunctival itching and congestion caused by irritation or allergy, it does not cause cycloplegia
phentolamine*
Alpha blocker. Hypertension caused by pheochromocytoma. Causes postural hypotension. Phen=pheochromocytoma
(Gabapentin)
Alter GABA activity New AED Ind: adjunct for partial & tonic/clinic seizures; post herpetic neuralgia Comp: dizzy, ataxia, tremor Comment: dose dependent bioavailability
donepezil*
Alzheimers drug. Acetylcholinesterase inhibitors. Tox: Nausea, vomiting, insomnia.
MAC complex
Amikacin, Fluoroquinolone, Macrolide, Rifabutin
Tx rapid growing mycobacterium (m fortuitum, m chelonae)
Amikacin, cephalosporin, imipenem
4**Other antibiotics** Aminoglycoside, fluoroquinolone, metronidazole, sulfonamide, UT antiseptics
Aminoglycosides: "amino glider pic" Streptomycin & Gentamycin (Also tobramycin, amikacin, neomycin) ** Sulfonamide: "Sulfur match fondu" Sulfmethaxazole (SMX), Sulfadizine, sulfadoxine, sulfasalazine Trimethoprim-SMZ (TMP-SMZ): "picture of TMP tampon" ** Fluoroquinolone: "Flower queen pic & floxacins" Norfloxacin, ciprofloxacin, levofloxacin ** Metronidazole: "metro pic" & GET GAP on the metro ** UT antiseptic: Methenamine Nitrofurantoin
Thx indications
Analgesia: Morphine and other strong opioids Diarrhea: codeine, diphenoxylate, loperamide (resp dep or abuse less likely) Dypnea (pulm edema): morphine (venodilate, dec resp, relax) Cough: codeine, dextromethorphan Anesthesia: fentanyl (short duration) Phys Dependance: methadone, buprenorphine (detox/maintenance thx)
Aspirin Acetaminophen Ibuprofen
Analgesic Act: Block COX (PG can't potentiate pain) Thx: acute, abortive thx; initial line of def *for mild to moderate migraine pain *effervescent most effective Comp: GI dys (n/v, dyspepsia, ulcer) *CI: active ulcer disease
Migraine
Analgesic: Aspirin Acetaminophen Ibuprofen Ergot derivatives: Ergotamine: "E for epi, go for seroto, amine for DA--receptor +" Dihyrdoergotamine: cross BBB Triptans: "trips are soothing (serotonin rec)" Sumatriptan: "like summer-come and go" Zolitriptan: "Zoli makes the CNS his homi" (Naratriptan, rizatriptan, eletriptan, frovatriptan) Beta blocker Propanolol: "pan beta blocker" (Timolol, atenolol) TCA Amitriptyline: "The praying ptylers on tricylces" (Nortriptyline, doxepin) Ca blocker Verapamil: "very important pam: take pills with milk"
Benzonatate
Anesthetize stretch/cough receptors "Benzon stops the tension of stretch receptors" Anesthetic
Angiostatin Endostatin
Angiogenesis inh (block vascularization) *angiostatin: plasminogen(angio) fragment *endostatin: collagen(endo) fragment No toxicity/resistance in models
*Losartan
Angiotensin AT1 receptor blocker prototype: used in HTN. Effects and toxicity similar to those of ACE inhibitors but causes less cough. Other AT1 blockers: candesartan, eprosartan, irbesartan, olmisartan, telmisartan, and valsartan.
18**Emetics, Antiemetics, Anorexogenics**(cont)
Anorexogenics: Amphetamine: Amps up DANE Diethylpropion Phentermine Mazindol: TCA for the maze Rimonabant: Rimon reversed Simon (inh CB1) Fenfluramine: 5HT says I'm full (w/ phetermine is Fen-Phen) Sibutramine "see butt->NE,5HT->satiety Orlistat: "listat stops the lipase" ** Others Loraserin: 5HT2c, satiety Topiramate: anti=-ep
Sodium Bicarb Calcium Carbonate Mg OH Al OH3
Antacid (weak base) *all antacids can cause hypokalemia Ind: GERD, ulcers, heartburn, dyspepsia NaBicarb: not for long term *systemic alkalosis / fluid retention (CI: HTN) -- CaCarb: acid rebound, milk alkali syndrome *CI renal impairment -- Mg OH: "magical diarrhea," nonsystemic Al OH3: "minimum feces" nonsystemic, binds PO4 in lumen *Both Mg/Al: reduce bioavailability of drugs *Chelation: tetracycline, digoxin
16**Upper GI Drugs**
Antacids Sodium bicarbonate Calcium carbonate (tums) Magnesium OH - "magical diarrhea" Aluminum OH3 - "Al: minimum feces" ** Muscarinic Antagonist Atropine, Propantheline, Isopropramide Pirenzepine/Telezepine: "Zepines zip up M1 - the ECL cell" ** H2 antagonist: "-tidine: H2 before you dine" Cimetidine Ranitidine (Zantac) Famotidine: "Fam is Nize = no p450" Nizatidine ** PGE1 Misoprostol: "Misopro = more prostaglandin" Arthrotec = Miso + Diclofenac(NSAID) ** PPI: "-prazole: pray stomach acid stops" Omeprazole, lansoprazole (Rabeprazole, pantoprazole, esomeprazole-Nexium)
COPD Drugs 1
Anti-IgE: *Omalizumab: Omali says the IgE is yummy Corticosteroid: -TIDE washes away the mediators to be alone (-ONE) (tx astham/rhinitis) *beclomethasone, flunisolide, triamcinolone, fluticasone, ciclesonide, budesonide (puttine nebulizer aside), methyprednisolone (meant to be use pretty soon) NOTE: triamcinolone and methylprednisone not used to treat rhinitis Cromone *Cromlyn: taunting mast cell: "come on" release those mediators *Nedocromil: stuck mast cell with needle, can't move Anti-leukotriene *Zileuton: "Silly zileuton blocks leukocyte's lipoxy for a short while" *Montelukast: "puts a mountain in front of the leuko recept -Zafirlukast: "the fir is blocking the leuko receptor"
7**Anti-Parasite**(cont)
Anti-Protozoics Iodoquinol (+/- metronidazole): Iodo for tropho Metronidazole: "pic" extraintestinal e hist, giardia, trich Azithromycin, paromomycin Nitazoxanide: nitazox inhibits pyruvate's socks "Night crib for cryptosporidium" ** Anti-Helminths: "bendazole for bendy worms Albendazole Mebendazole Ivermectin: "iver for river blindness & strongyloides" Praziquantel
Adalimumab
Anti-TNFa antibody (human) DMAARD Ind: RA Adm: subQ QO every week Comp: infxn (TB and injection site); immunogenicity, lymphoma
Infliximab
Anti-TNFa antibody (murine/human) "Use this antibody on the autoimmune disease inflicting my friend" DMAARD (drug modifying anti-arth drug) Ind: RA, crohn's, autoimmune disease Adm: IV every 2 weeks Comp: infxn (TB and injection site); immunogenicity, lymphoma
*amiodarone
Anti-arrythmic (Type 3). Potassium channel blockers with some anti-adrenergic activity. Prolongs QT= torsade risk. Blue-grey skin discoloration.
Corticosteroids
Anti-diarrhea Stim active Na abs (Na/K ATPase in J/I/colon) Ind: chronic refractory diarrhea, IBD S/E: Cushings
Topiramate
Anti-epileptic drug Unk MOA Ind: obesity S/E: parasthesia, change taste, dizzy
Sulfasalazine Mesalamine Olsalazine (mesa dimer)
Anti-inflamm: UC tx Colonic bacteria convert to 5-ASA *inh COX & LOX *prevent PMN prod of LT-B4 *scavenge O2 free radicals Sulfa: acute exacerbations UC Mesalamine: retention enema for active UC Olsalazine: PO for UC "O for PO" Sulfa many S/E; Olsa few *N/V, anorexia, ABD discomfort, HA, malaise, arthralgia, folate def, sulfa allx
Hydrocortisone Prednisone Prenisolone Budenoside
Anti-inflamm: UC/C Ind: mod to severe IBD *more chronic dx Cushing rxn
7**Anti-Parasite**
Anti-malaria: "Aquine & aquone for malaria you know" Chloroquine: "Claire has malaria, give this in time" Quinine+Tetracycline:"Quinine for the quiting chloroqine" Atovaquone+Proguanil: "last minute travel-at any vanishing minute" Primaquine: "Prevent relapse-hypnozoite" Artemesinin (+lumefantrine): ancient art (3rd world tx) ** Anti-malaria & others Tetracycline: "cycline combo w/ quinine" Sulfonamide Pyrimethamine TMP + SMX
Hydroxychloroquine
Anti-malarial Cytotoxic agent; may suppress APC Use: occasional SLE & RA Tox: long term: ocular toxicity (reversible cornea, irrev macular degen)
Paramomycin, azithromycin
Anti-protozo Only luminal parasites
Amantadine
Anti-viral: potentiates dopamine CNS action "A man invites DOPA to dine" Ind: early stage Parkinsonism; rabbit syndrome *Thx effect may dec in few weeks DI: MAOIs, stimulants CI: sz, renal disease (watch renal function to prevent toxicity) Caution: CV disease Comp: HA, confusion, hallucinations, skin discoloration (livedo reticularis), periph edema, urinary retention, CHF OD: toxic psychosis & convulsions
Benzotropine Trihexphenidyl Diphenhydramine
Anticholinergic (diphen also antihistamine) "Try HEX on that BENZ--blind as a bat, mad as a hatter..." Act: suppress over-active cholinergic neurons in Basal Ganglia Ind: initial stages of PD *adjunct to L-dopa thx *Little effect on bradykinesia & postural reflexes; 25% effective DI: DRAs, TCAs, tetracyclic antidepressants CI: BPH, paralytic ileus, narrow angle glauc Comp: restless, sedation, confusion, mood changes, dry mouth, mydriasis, constipation, tachy & arrhyth, postural hypoTN, urinary retention *Abuse potential
ORT
Antidiarrheal Dextrose/Na Ind: pediatric and child field (diarrheal dehydration) 10tsp sugar + 1tsp salt + 1L water
17**Lower GI Drugs**(cont)
Antidiarrheal: Bismuth subsalicylate & bismuthane: "business to inc mucus" Corticosteroid Octreotide: "octagon stop sign - somatostatin" ORT: dextrose/Na ** Anti-inflamm: "salazine/salamine - sialic acid" (USE: UC) Sulfasalazine Mesalamine Olsalazine (dimer with less mess) ** Anti-inflamm: UC & Crohns Hydrocortisone, prednisone, prednisolone, Budenoside **Anti-inflamm: Crohn's Infliximab "INF = TNF Ab," (Adalimumab, Certolizumab) Natalizumab: "Integrin-a4 receptor antibody" Azothioprine, 6-Mercaptopurine (prines & purine are anti-met) Methotrexate (DHFR -block purine&thymidine) ** Cyclosporine: UC flare up
Ethylene glycol
Antifreeze Acute: renal injury (metabolic acidosis & oxalate deposition) *necrosis of putamen, claustra, retina gang Tx: ethanol, formepizole
*hydralazine
Antihypertensive. Arteriolar vasodilator, orally active. Uses: Severe HTN, CHF, HTN in preg (with Methyldopa). Metabolized by Acetylation. Tox: Tachycardia, Salt and H2O retention, Lupus like syndrome.
reserpine*
Antihypertensive: selective inhibitor of vesicle catecholamine/H+ antiporter; used in HTN, causes depletion of catecholamines and 5−HT from their stores. Tox: severe depression, suicide, ulcers
Tetracycline or doxy
Antimalarial Combo with Quinine "(for the quiting chloroquine)" Doxy: Thailand (MDR P falciparum) Tetra: dientamoeba fragilis Good for last minute travel
Sulfonamide
Antimalarial PABA analog (folic acid) Ind: malaria, cyclosporiasis, toxoplasmosis S/E: agranulocytosis TMP/SMX combo
TMP + SMX
Antimalarial SMX: block DHPS (synthase) TMP: block DHFR Tx: toxoplasmosis in immunocompro or pregx
Tx Cough
Antitussives (codeine, dextromethorphan) Expectorants (Guaifenesin, terpin hydrate, iodides) Mucolytics (Acetylcysteine, bromhexine) Anesthetics (benzonatate)
Lorazepam Diazepam
Anxiolytic Ind: anticipatory CINV, vertigo *Not for motion sickness S/E: amnesia, mental change
Heavy Metal Poisoning
Arsenic: groundwater, industrial *AsO4 sim PPi, arsenite blocks pyruvate DH Lead: paint, batteries, ammo *Hgb or membrane fragile, bone accum Cadmium: mining, shellfish, battery *compete w/Zn, renal complexes Iron: NO RESP abs; iron supplments, transfus *GI,recovery,relapse; heart liver pancreas Mercury: -Elemental: bbb; neuro *tremor, neuropsych, giviostomatitis -Ionic/Merc salts: no bbb, GI and nephro -Organomercurials: fish/shellfish, pollution *bbb; neuro (parasthesia, ataxia, hearing, speech, visual) Others: Al, Cu, Zn, Ag, Co, Cr
TCCD/Dioxin/Ah Receptor
Aryl hydrocarbon (Ah) genetic locus: receptor for polycyclic aromatic hydrocarbons *TCCD: high affinity *polymorphism: different sensitivity
General Anesthesia: NM relaxation
Atropine Tubocurarine - put a tube in the AChR Pancuronium Succinylcholine - suck, all depol and can't repol Neostigmine - put a stick in it, inhib Sugammadex - sugar, sugar this will get the AChR workin
Cholinergic antagonists
Atropine/scopolamine: high doses cause disorientation, dilusion, etc Anticholinergic, hallucinagen
Antidepressants (2)
Atypical: *(Trazadone, nefazodone): "Zadones and zodones for times with too much serotones"-block 5HT receptor *Buproprion, (Maprotiline): Bupro likes coco *(Mirtazpine: like amoxapine, mirta zaps on norepi) Atypical/SNRI: (-) NE&5HT reuptake *Duloxetine, Venlafaxine, (Desvenlavaxine) "The duo delux, vend the fax!" Atypical/herbal *Hypericum: "Hyper about icky herbals" MAO-I *Phenelzine, (tranylcypromine) "Nelzine adds the NE time" Mood stabilizer *Lithium: lites up the inositol phophatase *(Carbamazepine, valproic acid, lamotrigene)
MDMA *MDA *Mescaline
Augment 5-HT release; release DA "MD missing in action: on ectasy"-ectasy Phenethylamine, Hallucinogen Acute: degen of 5-HT nerve cells/axons
Neuroleptic malignant syndrome
Autonomic instability, rigid, diaphoresis, hyperthermia, aLOC, death Generally weeks, high mortality Disc drug thx; bromocriptine, dizepam, dantrolene -cooling blankets, IV fluids
*nesiritide
B- Natriuretic peptide -- used in treatment of acute decompensation. decreases preload, afterload as well as removing excess fluid and salt. useful for short term vasodilating actions (decreases aldosterone, Ang II, endothelin and NE)
DOBUTAMINE
B1 *Dough Butt BE #1 CHF (beta blockers are better); caution in a-fib
ISOPROTERENOL
B1,2 *I'm such a pro: only touch the beta Tx heart block, asthma, cardiac arrest
Vitamins: B series C & ADEK Fe
B1,2,3,6,9,12 C, ADEK Iron
METAPROTERENOL
B2 *Meet a pro and have an asthma attack Bronchial relaxation Tx asthma, COPD
Ritodrine
B2 *Rito makes sure you don't RID YO' baby. Can't B2 careful Relax uterine muscle Tx premature contractions
FORMOTEROL
B2 *Salmeterol & formoterol MOTOR all day long Bronchial relaxation Tx asthma prophylaxis
ALBUTEROL
B2 *albuterol inhaler--keep it with you (can't B 2 careful) bronchial relaxation Tx acute asthma
TERBUTALINE
B2 *terbut is 2 Butts (B2) bronchial relaxation and relax uterine muscle Tx acute asthma
SALMETEROL
B2 partial *Salmeterol & formoterol MOTOR all day long bronchial relaxation Tx asthma prophylaxis/nocturnal asthma
Benzodiazepine
BZ "Benzo slows the CNS"
Vitamin B3
Bee 3 tree: Niacin "Nice Sun" Prec: NAD, NADP Def: Pellagra (3D: dementia, diarrhea, dermatitis/glossitis) Tx: oral replacement *too much->pruritis/flushing/HA
Polychlorinated & polybrominated biphenyls (PCB & PBB)
Beef, dairy, milk, chicken... Plastics, solvents, burning wood Dioxin/Agent Organce = TCDD (tetrachlorodibenzo-p-dioxin) Not nearly as lethal in humans (vs guinea pig) Acute: chloracne, porphyria, psych, CNS Chronic: leukemia/non-hodg... *ADHD like sx Extreme resistance to degradation
terbutaline*
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
Propanolol (Timolol, Atenolol)
Beta Blocker "Pan beta blocker" Thx: prophylaxis/prevent; HTN, tremor Comp: hypoTN, asthma worsens, CHF, AV block, depression, Raynaud's
Isoproterenol
Beta adren agonist "I'm such a pro: only B1/2 +" Inhibits mast cell release, inc mucociliary clearance, relaxes airway (smooth muscle B2) Tx Asthma *Long term control; PRN for acute symptoms *Inhale, parentally *Immediate, short duration Comp: vasoconstriction, cardiac stim, skeletal tremor, refractoriness (counter with corticosteroid), mask progression of disease
CHF step 2
Beta blockers (with ACE inhibit + diuretic) A1/B1/B2: carvediol B1: metoproplol B1: atenolol pan B: propranolol
metroprolol*
Beta-1, cardioselective noncatecholamine adrenergic antagonist. Used to treat angina, high BP, and prevention of heart failure. (Toprol XL or Lopressor)
isoproterenol*
Beta1, beta2 agonist catecholamine prototype: bronchodilator, cardiac stimulant. Always causes tachycardia because both direct and reflex actions increase HR. Tox: arrhythmias, angina
atenolol*
Beta1−selective blocker: low lipid solubility, less CNS effect; used for HTN. (Note mnemonic for beta1−selective blockers: their names start with A through M. [Exceptions: carteolol & labetalol are not selective])
*cholestyramine
Bile acid-binding resin: sequesters bile acids in gut and diverts more cholesterol from the liver to bile acids instead of circulating lipoproteins. Tox: constipation, bloating; interferes with absorption of some drugs. Colestipol is similar
Pentobarbital *amobarbital *secobarbital
Bind GABAa: allosteric & mimetic "Pento in the middle / barbital" Barbituate: short/med 6-8 hours Metab: liver oxidation & conjugation; excrete w/ acidic urine Thx: preanesthesia, regional anesthesia ****** Acute: drowsy, resp depress, induce hepatic delta-aminolevulinic acid synth; inc steroid hormone metab Chronic: tolerance and dependance Withdraw: anxiety, insomnia, anorexia, autnomic hyperactive (like EtOH) Tx: resp support, gastric lavage, hemodialysis and osmotic diuretic Comment: cross-tol w/ other sedatives = hypnotics
Omalizumab
Bind IgE "Omali's yummy IgE" Tx asthma, allergic rhinitis *Long-term\ *does not treat acute rxns SubQ every 2-4 weeks Comp: not all patients respond, anaphylaxia
Drugs of Hyperlipidemia
Bind bile acid in intestine: *choles- coalesc in the GI (cholestyramine, colestipol, colesevelam) (neomycin) Inhibit lipolysis (HSL): Niacin, nicotinic acid Inhibit oxidation of LDL: probucol Inhibit HMG-CoA reductase *statins (Lovastatin, simvastatin, pravastatin, *atorvastatin*, rosuvastatin, pitavastatin, fluvastatin, cerivastatin) Inhibit cholesterol uptake: ezetimibe Fibrate: -fibrate (Clofibrate, gemfibrozil, fenofibrate) Omega-3 fatty acids: Marine Oils
6**Antifungal Agents**
Bind ergosterol -> holes Amphotericin "ampho tears holes" Nystatin: "nice thrush" ** Inhibit ergosterol synth (CONAZOLES): "con as*holes block ergosterol synth" Ketoconoazole Itraconazole: "itra is it" Fluconazole Voriconazole Posaconazole: "possa for all possibilities" Clotrimazole (lotrimin): "clotri for OTC" Miconazole ** TerbiNaFine: "The skin, Nails, Fat" & "terpentine likes squalene epoxide" Flucytosine: "fly away cytosine" Griseofulvin: "greasy block of microtubules" Caspsofungin: "casper fungeal wall"
Cholestyramine
Bind intestine bile acid (bile resin) *choles tears out the bile to lower cholesterol Often combo with statin/niacin Tx: lower LDL, inc VLDL
Colestipol
Bind intestine bile acid (resin) *choles tears out the bile to lower cholesterol Often combo with statin/niacin Tx: lower LDL
Ethanol
Binds GABAa Receptor "Ethanol is alcohol" Opens Cl channels@GABA; inhibit NMDA glut rec EtOH DH (MEOS)-->aldehyde DH--> acetate (makes NADH and NADPH) Therapeutic: methanol toxicity Acute: CNS depression, diuresis, vasodilate Chronic: cirrhosis, pancreatitis, PUD, malnutrition, FAS, thymine def Withdraw: anxiety, insomnia, anorexic, hyper sympathetic, delerium, seizures Tx OD: supportive/prev aspirations *rehab, thiamine *BZ for seizure, hladol, clinidine ContraInd: durgs irritating GI
Corticosteroids
Binds cytosolic receptor & GRE *Block cytokinetic genes (IL2,3,6; TNFalph/beta & IFN-gamma) *inh lymphoid cell proliferation Tx: autoimmune d/o *combo with AZA +/- CsA Tox: short term few *long term: cushing, infxn, etc
Neomycin
Binds intestine bile acid (NON-resin) *Neomycin: NOT resin, but still says MY bile
Cyanide (CN)
Bitter almond smell! Byproduct of nitroprusside; Electroplating; plastics Tox: bright red venous blood + smell of bitter almonds *Binds cytochrome oxiidase **Lactic acidosis, CNS, CV, rapid death Treat FAST!!! *Met-Hgb grabs cyanide (give amyl nitrite[inhale] followed by sodium nitrite [iv]) *Sodium thiosulfate (CN to SCN->less toxic and urine)
Botulinum toxin
Block ACh release
Tramadol (Ziconotide, Tapentadol)
Block NE/5HT reuptake -weak mu-receptor activity "Tram the doll is about to ball (cry)" Ind: moderate pain (esp neuropathic) Comp: seizures (CI: epilepsy), anaphylaxis DI: MAOI; partially reversed by naloxone
Flecainide
Block Na and K *It's a Cain. Flec goes FOREVER Class I--LONG TERM. Increase refractory period. Tx: V tach, A flutter/fib (suppress)
Procainamide
Block Na channel *It's a Cain, and PRO--does v tach and A fib & flutter Class I--ACUTE. Increase refractory period & suppress repolarization Tx: V tach, A fib & flutter, PAT in WPW
Lidocaine
Block Na channel *It's a Cain; LIed-can't do DOS (only v tach) Class I--NO VAGAL/NODAL EFFECT. Increase effective refratory period Tx arrythmia after AMI (no increase survival)
Oxcarbazepine
Block Na channel in inactive state-prolong refractoriness "Cars and azepines: in a car with a seizure; azepines are a zip shut in the sodium channel" Ind: complex partial & tonic clonic *Also pain syndromes (trig neuralgia) & bipolar Adm: PO *Prodrug is more expensive than carbamazepine ------------ **Comp: *Improved adverse effect profile. MEOS induction is less, hypoNa more frequent, rashes **Interactions: *Dec oral contraceptive bioavail *High dose: inhib MEOS and inc phenytoin *Enzyme inducing drugs inc its clearance
Carbamazepine
Block Na channel in inactive state-prolong refractoriness "Cars and azepines: in a car with a seizure; azepines are a zip shut in the sodium channel" Ind: complex partial & tonic clonic *Also pain syndromes (trig neuralgia) & bipolar Adm: PO ------------ **Comp: *n/v, occasionally hypoNa *visual disturbances (diplopia, nystag), ataxia, sedation at high dose *RARE: idiosyncratic rxns (severe rash, blood dyscrasias) **Interactions: *autoinduction, inc metab of other anticonvulsants (phenytoin, valproic acid) *Cimetidine dec metabolism
Fosphenytoin (Mephenytoin, Ethotoin)
Block Na channels in inactive state-prolong cell refractory "Enytoins stop the sodi's in what they're doin" *Ind: status epilepticus *Adm: IV or IM *fosphenytoin: less irritating than phenytoin ------ Comp: Low Therapeutic Index: *N/V, rash, gingival hyperplasia (kids), hirsutism *visual dist, ataxial, mental confusion RARE: megaloblastic anemia, coarsen facial features, osteomalacia, idiosyncratic rxns (blood dycrasias--agranulocyt--& severe rash--exfoliative dermatitis, Stevens-Johnson syndrome), fetal malformations Interactions: *inc metab: oral contrac, anticoag, AEP *Carbamazine & phenobarbital inc metabol *Cimetidine dec metabolism Metab: liver microsomal enzymes; saturated at high doses
Phenytoin
Block Na channels in inactive state-prolong cell refractory "Enytoins stops the Sodi's in what they're doin" *Ind: complex partial & tonic clonic *Adm: PO *slowly absorbed is formulation dependent ------ Comp: Low Therapeutic Index: *N/V, rash, gingival hyperplasia (kids), hirsutism *visual dist, ataxial, mental confusion RARE: megaloblastic anemia, coarsen facial features, osteomalacia, idiosyncratic rxns (blood dycrasias--agranulocyt--& severe rash--exfoliative dermatitis, Stevens-Johnson syndrome), fetal malformations Interactions: *inc metab: oral contrac, anticoag, AEP *Carbamazine & phenobarbital inc metabol *Cimetidine dec metabolism Metab: liver microsomal enzymes; saturated at high doses
Alpha2 adreno block adverse effects
Block anti-hypertensive action of clonidine, alpha-methyldopa
Cocaine/tricyclic antidepressent
Block neuronal membrane transport uptake of NE
OTHER anti-myco drugs: R207910 (sirturo or bedquilone)
Block proton pump (ATP synthase) *use in combo *10x more effective than INH & rifampin *blackbox: arrythmia
PTU (propylthiouracil) Methimazole
Block thyroperoxidase (block T3/4 synth) *PTU: also block peripheral T3 conversion (P for periphery) S/E: itch, rash, agranulocytosis, cross placenta (less with PTU) *Use PTU for Pregnancy (p for pregnant) Give 2-3 weeks to take effect
(Topiramate)
Block volt-dep Na channels Potentiates GABA at non-BZ site New AED "A mates are a mate to the old AED" Ind: adjunct for partial and tonic-clonic seizures Comp: dizzy, parathesia, problem memory/word finding, confusion, fatigue, nervous, weight loss, myopia & glaucoma *nephrolithiasis inc 2-4x
Hemicholinium
Blocks Ch transport
Lamotrigene
Blocks voltage and use dependent Na channels "Lamo makes the voltage dep & use dep Na channels lame" New AED Ind: partial seizures; maybe absence & myoclonic seizures Comp: dizzy, HA, dipolipia, nausea, drowsy, skin rash *Rare: S-J syndrome & toxic epidermal necrosis Interactions: *phenytoin & carbamzepine reduce half life 50% *valproic acid inhibits clearance
Bromhexine
Break down mucopolysacc fibers in mucus "Bros break down the hex of fibers" Mucolytic *Inhalation
(Bupivacaine) (Prilocaine)
Bupivacaine = "Bupi the vampire is toxic for the heart" **cardiotoxicity: high affinity for Na channels, dec cAMP, long AP duration Prilocaine: metabolized to o-toluidine, can result in methemoglobinemia
Newer Hypnotics
Buspirone: buspi is busy with GAD Zolpidem Zaleplon: plans to have a sale of non-BZ Eszoplicone Ramelton: Rame plays the game to make you fall asleep without touching GABA Receptor *Flumazenil: Flumaze fights the Zs
Q: HTN, pregnant
CAN'T use ACE(-) or ARB; Ca block mess up myometrium Use Diuretic
Anti-CD3 monoclonal antibodies
CD3 on T cell surface Immunosuppressive Ab *Block cells from interacting with Tcell (block fxn) Use: REVERSE kidney allograft rejection Tox: good for only first 2 doses (get rxn due to foreign proteins) *first 2 doses: flu like (rigors, chills, n/v/d..)
Pharmacokinetic Factors
CHF: dec Vd Pregx, cirrhosis: inc Vd Dec CL, but t1/2 can stay same (if Vd dec): t1/2 = 0.7 / k = 0.7 / (CL/Vd) **Liver disease: Vd inc, CL dec (t1/2 INC) **CHF: Vd dec, CL dec (t1/2 same) Note: Maint dose = CL x [D] =CL x dose/Vd =CL/Vd x dose =k x dose
Methyldopa
CNS adrenolytic (inh adrenergic) "Makes a meth of the CNS system. dope!" Antagonize stretch receptors: dec renin release Ind: HTN Comp: effective only when serum renin is high
Opioid Adverse Effects
CNS: resp depression, sedation/drowsy, n/v, tolerance: psycho & phys, pneumonia, miosis (edinger-westphal) CV:postural hypoTN GI, Kidney, Gallbladder: constipation, urine retention/pain, pain from biliary spasm Other: pruritis
Celecoxib (Rofecoxib) (Valdecoxib)
COX2 > 1 (10x) "Celecox is only specific COX2 still selling" Ind: osteoarth, RA, hx ulcers CI: asthma, hep/renal insuff, late pregnancy, CV disease?? Metab: oral abs, distrib to all tissue, liver p450, excrete urine/feces *11 hours Comp: edema, HA, indigestion, URI, diarrhea, sinus inflamm, gastric pain, nausea Note: reduced gastroduod erosion *DI: cidofovir, Li, ACE inhib, fluconazole, lasix
(piroxicam) (meloxicam)
COX2 > 1 (2x) "Oxicam camp out 45 hours" NSAID oxicam Metab: absorb NOT affected by food *enterohepatic circulation *45 hours!! Comp: tox in 11-45%; lower peptic ulcer
Chemoreceptor Trigger Zone Vomiting Center (brain stem)
CTZ (area postrema) D2, NK1 (killer trigger), serotonin (5HT3) Vomiting center (brain stem): H1/M1, NK1, serotonin Vestibular: H1/M1 *Vs have the H1/M1 (hmmm..) GI: mechano, chemo, 5HT3 CNS
Verapamil
Ca blocker "Very important pam: take pills with milk" Action: causes vasodilation Thx: coexisting prinzmetal's angina or Raynaud's *controversial Comp: constipation CI: hypotension, heart block
*diltiazem
Calcium channel (L−type) blocker prototype: like verapamil, has more depressant effect on heart than dihydropyridines (eg, nifedipine). Tox: AV block, CHF, edema, constipation
Drugs of Abuse (2)
Cannabinoid: Marijuana Dronabinol: drove into bin--marijuana Hallucinogens: LSD: acid-let serotonin deliver psilocybin: shrooms phenylcyclidine: phorever, cycles (PCP) MDMA: ectacy (MD missing in action) *MDA *Mescaline Cholinergic antagonist: atropine, scopolamine Solvent, aersol: benzen, NO Benzodiazapine Opioid: heroin, morphine
norepinephrin*
Causes blood vessels to constrict, -Regulation of BP, stimulates secretion of histamine, increase HCl secretion
Chlorazepate Clonazepam Fenoldopam Estazolam Quazepam Prazepam
Chlora: >50hrs, decarbox in gastric juice Clonazepam: *early relief while titrating SSRI Fenoldopam: auto accidents (car fenolded) *both: anticonvulsant, panic d/o, acute HTN Estazolam Quazepam Prazepam: >50hrs
Pesticides & Herbicides: Insecticides & Weed killer
Chlorinated insecticides: reduce repolarize Organochlorine insect: DDT Chlorinated cyclodienes Organochlorine insect: Lindane, Kepone Organophosphate Insect: -athion (AChE) *Malathion, parathion... Carbamates: CAN be hydrolyzed! Pyrethroid insect: *RAID (deltamethrin), pyrethrin... Chlorophenoxy Herbicides (weed killer) *2,4-D(dichlorophenoxyacetic acid), 2,4,5-T Bipyridyl Herbicides: free radical generation *Roundup (Diquat) & Paraquat
Chlorthalidone Metolazone Quinethazone Indapamide
Chlorthalidone: long half life "This chlorothiazide: I aint done" Metolazone: use low GFR (high dose) "Met this drug in the danger zone: RF" Indapamide: use w/ GFR (high dose) "Indented GFR, pay for this drug" Quinethazone
Vitamin D
Cholecalciferol: "Viking Daisy","Locked up", and "Toxic green glow" Hormone like (like vit A); Calcium and bone metab
Atropine
Cholinergic Antago "A trip to pine blocks muscarine" Dec secretions
neostigmine*
Cholinesterase inhibitor. Increase endogenous ACh. Little CNS effect. Uses: Postoperative ileus and urinary retention, MG, reversal of neuromuscular blockade. DON'T ENTER CNS
pilocarpine*
Cholinomimetic. Contracts ciliary muscle of eye (open angle), pupillary sphincter (narrow angle). Resistant to AChE. Uses: Glaucoma, Sjoren, Stimulator of tears, sweat, and saliva.
9b**Interferon Drugs**
Chronic Hep C: Peggylated IFN (alpha2a) + ribavirin ** Hep B: INF (alpha2a) OR Lamivudine/entecavir + Adefovir/tenofovir
Common chemotoxicities
Cisplatin/carboplatin: (C) for ear -(acoutic nerve damage and nephrotoxic) Vincristine: (V) peripheral neuropathy Bleomycin/busulfan: (B) pulm fibrosis Doxorubicin & Trastuzumab (T inside D): -cardiotoxicity Cisplatin/Carboplatin: (C) for kidney Cyclophosphamide (CY): hem cystitis 5-FU/6-MP, methotrexate (56M): -myelosuppression
Anti-arryhythmic drugs
Class I: block Na (the caines) *Procainamide, Licocaine, Flecainide Class II: B-blocker (-olol) *Metoprolol, propranolo *fusion II/III: dl-Sotalol Class III: Block K (K love I dare you), atrial refraction (-ilide) *Amiodarone *Dofetilide, ibutilide Class IV: Block Ca *Diltiazem, verapamil Others: *Digoxin/digitalis, Magnesium (Na/K/Ca), AICD, Adenosine (K), Atropine (ACh)
*sotalol
Class III antiarrhythmic w/ non-selective beta-block -Prolongs repolarization and duration of action potential (via block of rapid outward potassium current(delayed rectifier)) -Block sympathetic tone, decrease conduction and increase refractoriness
*pinacidil
Class: K+ channel blocker MOA: activation of potassium channels, increasing potassium efflux and inducing hyperpolarisation of smooth muscle membrane. When the memebrane is hyperpolarised, calcium influx is inhibited and the arteriolar smooth muscle relaxes. Effects: causes relaxation of resistance (arterioles) vessels rather then capacitance vessels(veins).Reflex tachycardia and renin stimulation (subsequent fluid overload) therefore coadmin with BB and diuretic. S/E: tachycardia, fluid retention, congestive heart failure, hypertrichosis
Vitamin B12
Cobalamin: "Dozen viking Bees" & "12 Viking Bees Burning Up" Cause: malab *Binding factor, IF, ileum, transcobalamin *pernicious anemia, gastrectomy, ileal insuf **(TX: SQ or IM) Result: macrocytic megaloblastic anemia/hyperseg neutrophils, severe neuro damage *myelin problem: subacute combined degen (paresthias, no DTR, confusion, psych, dementia) Synth: soil/eneterics 1-C transfer rxns: homocystein to methionine & SAM Def: DNA synth/dec RBC maturation/nuc:cyt
CNS stimulants
Cocaine Amphetamines/methamph/methylphenidate Nicotine Bupropion Varenicline euphoria, self-confidence, dependance
Vitamins: Cofactors Hormone Precursors Anti-oxidants
Cofactors: BCK Hormone Precursor: A,D Anti-ox: E
*acetylsalicylic acid
Commonly known as aspirin; often used as an analgesic (against minor pains), antipyretic (against fever), and anti-inflammatory; irreversibly blocks formation of thromboxane A2 in platelets, producing an inhibitory effect on platelet aggregation.
Naloxone
Compet (-) opioid receptor "is the One that Locks into the opioid recept" Opioid antagonist Ind: precipitate withdrawals; opioid OD/tox Adm: IV *short duration (1-2hrs)-watch recurrence of resp depression/coma DI: precipitated withdrawal
Naltrexone
Compet (-) opioid receptor "the ones that Reck the opioid receptor" Opioid antagonist Ind: red alcohol cravings Adm: oral but high first pass *longer duration
Methylnaltrexone (Nalmfene, Alvimopan"
Compet (-) opioid receptor "the ones that Reck the opioid receptor" -methyl: in the mouth but not coming out the anus Opioid antagonist Ind: constipation in late-stage advanced illness
Tubocurarine (Pancuronium)
Competitive ACh receptor blocker "Tube stuck in ACh receptor" Muscle relax/immobility
Calc Clearance
Constant infusion (when D1=D2...) Or withdraw infusion ER = (change in [D])xVd/time *CL = ER / [D]avg = ER / (AUC/time) **area under curve
17**Lower GI Drugs**
Constipation: 1) Bulk-forming laxative: psyllium, methylcellulose, polycarbophil, bran 2) Saline lax: Mg salt, Na Phophates 3) Mild irritants (secretory): Bisacodyl, phenolphthalein (exlax), Anthraquinone deriv, Castor oil 4) Osmotic lax: Docusate, Lactulose, Sorbitol 5) Prescriptions: Tegaserod (tickles serotonin), Lubiprostone (Lubi is pro lubricator) ** Opoioid anti-diarrhea Natural: Opium tincture, codeine, morphine Synthetic: Diphenoxylate (diphen dives through bbb-give w/ atropine), Loperamide ** Anticholinergic anti-diarrhe: atropine, scopolamine, propantheline, methatheline ** Clonidine: Cloney dines - gives neg feedback Rifaximin: traveler on river Attapulgite: "a tap of clay" gel forming anti-diarrhea
Rebamipide - Asia Carbenoxylone - Europe Bismuth compound (pepto bismol)
Contact protective Stimulate mucus secretion *Bismuth: also adherence & antibacterial Ind: ulcer healing & travel prophylaxis
Medroxyprogesterone acetate
Contraceptive Hypothalamus feedback: block ovulation (less LH) S/E: menstrual irregularities Very effective OCP (95%); also depo form
Dexamethasone ($ big gun)
Coritcosteroid Inh PG & cytokines Ind: Delayed CINV *often give with Odansetron (5HT antag-acute) S/E: dec mental fxn
Immunosuppressive Agents
Corticosteroids: block cytokine genes Cytotoxic agents: Azathioprine: AZA is a precursor to 6mp,6tg Cyclophosphamide: cycle through the mustard shirts Hydroxychloroquine: anti-malarial Immunophilin Ligands: Cyclosporine (CsA): sporine went to the store and stole CyPA Tacrolimus: "Tac FK!" binds FKbp Proliferation signal inh: Sirolimus: Siro has zero mTOR Mycophenolate mofetil (MM): M's block GMP
Alkylation
Cross link Guanine: chlorinated region of alkylated guanine Hypersensitivity if no excision repair (xeroderma pigmentosum) Cell cycle non-specific but MUST have proliferation to see damage S/E: alkylating agents are mutagenic (secondary cancer and leukemia or sterility)
Interleukin 2
Cytokine produced by T cells *Activates B & T cell prolif; stim lymphokine acdtivated killer cells (LAK) Use: Adoptive immunothx (culture and activate pt lymphocytes) OR cloncal expansion of tumor infiltrate lymphocytes *renal cell CA Tox: fever, fluid retention, hypoTN, nausea
Interferon
Cytokine-induced by dsRNA! Leukocyte (IFN-alpha) &Fibroblast (IFN-beta) *INC MHC-I and stim NK cells (cytotoxicity) T-cells (IFN-gamm) *INC MHC-II; stim tumoricidal macrophages Use: Hairy cell leukemia, CML (chronic phase), HepB&C, Kaposi sarcoma Tox: fever, flu like
Organochlorine Insecticide Chlorinated Cyclodienes Organochlorine Insecticide
DDT, methoxychlor *low acute tox Aldrin, dieldrin, heptachlor, chlordane *high dermal absorption; severe acute tox Lindane (kwell), kepone, mirex, toxaphen *Lindane: lice shampoo Very lipophilic; induce p450 Reduce repolarization *neuro: CN5 parasthesia, seizures Tx: Barb/BZ for sz; cholestyramine (fecal excretion)
Antitumor Antibiotics, Hormones, Etc.
DNA intercalator (local unwinding at GC base pairs) - Rubicin & Mycins Doxorubicin Daunorubicin Dactinomycin Plicamycin: plight of s/e DNA fragmentor: Bleomycin "blow in free radicals" Topo II Inhibitor: "toposides mess up topo" Etoposide, Teniposide Microtubule Inhibitor: "Microtubules are vine of cells --vinblastine, vincristine "It's taxing to stay polymerized" --Paclitaxel, docetaxel
Renin-Angio-Aldosterone
Dec Renin production: *Propranolol: pan beta block *Clonidine: while dining negative feedback *Methyldopa: makes a meth of adren (-)ACE *Captopril: winners cup w/ sulfur *Enalapril: true ace that laps all *Lisinopril: no plasma binding *Quinapril: -april *Benazepril: mercedes benz of potency ARB *Losartan K: loser can't find angio Rec *Valsartan: all losers get a tan (-)Renin *Aliskiren: alice will cure our kidney (+)Aldosterone agonist *Fludrucortisone: flood the core with Na *DOCA: corticoid for adrenal insuff (same) (-)Aldosterone Spironolactone: breasts and Na spiral out Eplerenone: epimer more specific than spir Triamterene: gynecomastia on TRAM Amiloride: amy my love-propose on TRAM
Iron
Def: diet, demand, malabsorption (deod/jej) *ferrous salts tx Poisoning: chelation etc *Hemochromatosis & HFE gene (Phlebotomy) *Chronic hemolytic anemia (Fe chelator desforaxamine) States: absorb 2+, store 3+, 2+ for O2
Anti-metabolites
Def: interphere with S-phase (DNA synth) Methotrexate: antifolate like TMP 5-FU: block thymidilate synthase Cytosine Arabinoside (araC): araCMP 6-MP,6-TG: mercaptoPURINE (cap on purine) Hydroxyurea: affects uracil
succinylcholine*
Depolarizing neuromuscular relaxant. Short duration (5 min) if patient has normal plasma cholinesterase (genetically determined). No antidote. Implicated in malignant hyperthermia.
Succinylcholine
Depolarizing nicotinic AGONIST "Suck, it would let go and all our Na is gone" Use: OR anesth, ortho, intub, electroshock thx *IV drip, 2-3 min onset Adv: musc relax, prevent repolarization *NO CNS Comp: more prolonged action if gene defect, liver disease, hypothermia, or AChEI * w/ halothane = malig hyperthermia (gene mutation) * apnea if drop in plasma AChE
AICD
Device *A...I...See...D! Class other: immediate elctrocardioversion (need surgery) Tx: V tach/fib
Long Acting BZ
Diazepam Chlordiazepoxide Prazepam Flurazepam Clonazepam
Heavy Metal Chelators
Dimercaprol: Ionic Hg (& As) Deferoxamine: Fe (& Al) *Amine for in short time = acute Deferasirox: Fe "sirox for lots of times" Edetate (EDTA): Pb ("detate is on/off date schedule") Succimer: Pb ("sucks your kid had Pb paint") Unithiol: Ionic Hg (&As) *note: As use the Di or Uni (dimercaprol or unithiol)
muscarine*
Directly acting cholinomimetic - alkaloid used as muscarinic agonist - side effects SLUDGE
Saline laxative: Magnesium salts Sodium phosphates
Distend bowel to stimulate contraction Ind: constipation S/E: get toxic [Mg] in renal failure; phophate cells -> excess Na in CHF patients
Pediatric tx of anti-myco
Don't use ethambutol (RG colorblind)
Levodopa
Dopaminergic Agent "Levo is leaving to become DOPA" Act: Decarbox to dopamine *(+)D2Rec and adenylate cyclase *Location: prejunctional SN axons & postjunctional striatal neurons Ind: Parkinson's disease Admin: GI tract (abs slowed by food, influ by pH), transport from GI to CNS via aromatic amino acid transport system *95% metab in periphery (high dose needed unless given with carbidopa) DI--Dec absorption/action: *antipsychotics/antiemetics that block DA receptors; TCA (anticholinergics), natural aromatic AA *NOT used w/ selective MAOIs *VitB6 (pyroxidine): dec periph levels of L-dopa CI: psychosis, angle-closure glaucoma, peptic ulcer disease, melanoma Comp: *dyskinesia, akinesia (wearing off, on-off) *anxiety, insomnia, depression, dream alter, visual hallucination, psychoses *PERIPH: n/v, postural hypotension, arrhyth, mydrisasis-->acute angle glauc
PARKINSON'S DRUGS
Dopaminergic Agent Levodopa: "leaving to become dopa" Carbidopa: "like a car escort to the CNS" (+)D2 Receptor Ropinirole: "Pray we can Rope in this D2 receptor" Pramipexole: D3 affinity (Bromocriptine) (Apomorphine): temporary 2hr relief (-)MAO-B Selegiline: "gilines like gills let dopa keep swimming through mayo" Rasagiline: "gillines..." Anticholinergic: "TRY putting a HEX on the BENZ" Benztropine Trihexphenidyl Diphenhydramine (-)COMT Entacapone: "COME put a CAP on the PD patient" (Tolcapone) Antiviral Amantadine: "a man invited DOPA to dine"
ritodrine*
Drug used to reduce premature uterine contractions. Binds B2 only.
*nicorandil
Dual mode of action: NO releaser and K channel opener. Leads to cell depolarization and smooth muscle relaxation. Problem: It causes flushing, tachycardia, oral and anal ulcers.
D2 receptor: adverse effects
EPS (acute dystonia, akathisia, Parkinson synd); tardive dyskinesia HyperPROL (dec libido/impotence) Inhib of L-dopa activity (parkinson's)
OTHER anti-myco drugs: PA-824
Effective vs LATENT Tb (works under anaerobic conditions
Serotonin 5HT2 block adverse effects
Ejac dysfunction
PTH Teriparatide (synth PTH)
Elev Ca, Red Phosph (+)AC-cAMP Bone (freq dep), Kidney, Intestine (indirect via VitD) *pulsatilve causes bone formation Ind: osteoporosis S/E: nausea, dizzy, cramps; post hypoTN at initiation Teriparatide CI: osteosarcoma risk, skeletal irradiation planned, kids w/ unclosed epiphyses
18**Emetics, Antiemetics, Anorexogenics**
Emetic: Ipecac "vomit a cat" ** Antichol: Scopolamine (M1) "M for motion" ** H1 antagonist: "Dimen Divers Make Pros Hiss" Dimenhydrinate Diphenhydramine Meclizine Promethazine ** Dopaminergic antag Metoclopramide: "meto says NO to dopamide" Prochloperazine: also blocks M1 (CTZ & VC) ** Cannabinoid: Dronabinol: cannibol Nabilone ** Corticosteroid: Dexamethasone Anxiolytic: Lorazepam & Diazepam ** Big Guns: Ondasetron: "setron sits down serotonin" *Granisetron Aprepitant: "A prayer if see NK" (penetrate brain)
Q: second degree heart block stage 2, HTN:
Enalapril Furosemide might be too strong
Valproic Acid (Trimethadone: absence seizures)
Enhance GABA in CNS "Val keep GABAing (Jabbering) on about these absent seizures" Ind: absence & myoclonic seizures Comp: *GI distress: severe n/v, abd pain, heatburn (USE DIVALPROEX SODIUM TO ALLEVIATE) *Weight gain, hair loss, ataxia, tremor *High dose: sedation *Rare: polycystic ovarian syndrome, fetal malform (spina bif), idiosyncratic hepatotoxicity Interactions: inhibit carbamazepine and phenytoin metabolism
8**Anti-Virals**
Enter: "Enters Maravinoc, a Pal & Doc" Enfurvirtide (T20-HIV) Maraviroc (CCR5-HIV) Docosanol (HSV) Palivizumab (RSV) ** Interference after through door: IFN-alpha (HBV, HCV) ** Takes off coat: Amantadine Rimantadine (Influenza) ** Makes a early foamy protein shake with owel eyeballs: Fomiversen (CMV retinitis)
Q: HTN, digitalis
Eplerenone Losartan can work (may retain too much K though)
Dihydroergotamine
Ergot derivative: (+) serot, Epi, DA receptors "Ergo adds to E-epi, Ergo: seroto's, admine--DA" Act: (+)5HT1A/1D receptor, (+)alpha adren, (+)DA *suppress neurogenic inflamm, inhibit vasodilation, dec CN V pain *Thx: abortive migraine or cluster HA attack Spec: crosses BBB (low recurrence) *admin: IM, IV, nasal (ER) *extensive first pass Comp: N/V (use anti-emetic) Note: binds dorsal raphe nucleus neurons
Ergotamine
Ergot derivative: (+) serot, Epi, DA receptors "Ergo adds to E-epi, Ergo: seroto's, admine--DA" Act: (+)5HT1A/1D receptor, (+)alpha adren, (+)DA *suppress neurogenic inflamm, inhibit vasodilation, dec CN V pain Thx: acute abortive Spec: vasoconstriction (long, cumulates), admin w/ caffeine (inc absorption) *Admin: oral/rectal *max 8 tx/month Comp: N/V, epigastric distress, diarrhea, rebound HA *Ergotism: parasthesia, vasospasm, periph vascular insuff, gangrene CI: obstructive vascular dis, collagen dis, pregnant, HTN, angina, peptic ulcer
Estradiol Estrone
Estrogen Tx hot flashes (HRT), vaginal atrophy, prevent colon cx S/E: endometrial cx, breast cx, stroke, VTE, GB, migraine *inc HDL; dec LDL & TG CI: smokers, HTN
14.15**Sex Hormones**
Estrogen: Estradiol (from testosterone) Estrone (from androstendione) Ethinyl estradiol - in contraceptives *Mestranol (prodrug for ethinyl..) ** SERM: xifens... Tamoxifen: tamox turns off the estrogen Clomiphene: Come ovulate! (block feedback inh) Raloxifene: Rolex of post-menopause Fasolodex: pure estrogen antago ** Aromatase inhibitor: "Ana... take a stroll & ex-aromatase" Anastrozole Exemestane
CNS depressants
Ethanol, Methanol, Ethyl glycol, Fomepizole Barbiturates Benzodiaepines Opioids withdrawal excitation
Drugs of Abuse (1)
Ethanol: +GABAa, -NMDA *Disulfiram: treat the AM drinker *Naltrexone: Na don't want a beer trick *acamprosate: camping beer drinking pros Methanol Ethylene glycol BARBITUATES: +GABAa Thiopental: thy pent house I shall sleep (methohexital & thiamylal) Pentobarbital: pento in the middle (amobarbital, secobarbital) Phenobarbital: barb forever (mephobarbital) Release the DANE: Cocaine: keeps the DANE in the main Amphetamine: Amp up DANE release *Methamphetamine *methylphenidate: meth taken on reg dates *phenteramine Nicotine: nicotinic receptors
Aliphatic alcohols & glycols: Ethylene glycol, Propylene glycol
Ethylene glycol: anti-freeze, nail polish Tox: general CNS depress *metabolites of ethylene glycol: Met acidosis & renal toxicity (oxalate stones) Propylene glycol: 30x less toxic
alpha-latrotoxin
Excess ACh release Black widow
Phenobarbital (Primidone, Mephobarbital)
Facilitate GABA hyperpolarization (Cl channel) "Barbituates: GABA and Cl hyperpol" Ind: febrile sz, status epilepticus Comp: *Kids/elderly: paradox. hyperactive, shorten attention span *Chronic use: sedation, ataxia, nystagmus *If abrupt withdrawal: seizures Interactions: liver microenzymes upreg (other drugs metab quicker)
Fenofibrate
Fibrate *Fibrate Tx HyperTG
HTN: Diuretics and Kidney
First step therapy for prevention HF *Hydrochlorothiazide: thiazide! *Furosemide: in a fury, NaKClCl swift away *Spironolactone: Na and breast spiral *Eplerenone: epimer of spirono *Amiloride: on TRAM my love; phys antag
Azoles
Fluconazole: "Fluco C's: crypto, coccidio" & "Fluco flies across BBB" *DOC: cryptococcal meningitis (esp in AIDS), coccidiodomycosis meningitis (can cross BBB) Voriconazole: "v for visual disturbances" Posaconazole: broad spec "posa for all possibilities" *zygomycosis, mucormycosis; PO w/ fatty meal Clotrimazole: "cloti for OTC" & Miconazole *superficial skin (candida, ringworm)
Vitamin B9
Folate: "Be cry if B9 is missing if pregnant" Def: alcoholics Gestational: spina bifida/anenceph Cofactors for 1-c metab (eg DHF) **form homocystein to methionine (thf-ch3 to thf; also req vitB12) Synth: soil/enteric microorg Absorbed in duedeum (sprue/sx); enterohepatic circ (blocked by EtOH) B12 def can cause folate def (SOME features of B12 are found in folate def) *megaloblastic anemia *folate: also get spinal cord & cortical damage *folate deficiency can mask b12 def!! (give folate with b12 - IM)
Bipyridyl herbicides *Paraquat, Diquat (roundup)
Free radical generation ("it would be radical selling roundup for free") *pulm tox: fibroblast; don't give O2 Farms and accidental poisonings
Clarithromycin Azithromycin (Z-pak)
G+/- (some more gram neg) MAC in AIDS & BE Clarithro: less GI irritation Azithro: no drug interactions
Diazepam Lorazepam (Clonazepam, Clorazepate)
GABA facilitation (Cl and hyperpol) "Benzos slow the CNS" Diaz ind: status epilepticus immediate tx Loraz ind: status epilepticus Clonaz: absence seizures Comp: Rapid tolerance develops, some children will get sedation and paradoxical hyperactivity Comment: NOT for chronic use
Thiopental *methohexital *thiamylal
GABAa bind: allosteric and mimetic "Thy pent hous: where I take drugs to sleep" Methohexital: meth house drugs to sleep Thiamylal: mylal in the thiopental Barbituate: ultrashort Lipid soluble Therapy: IV general anesthesia Acute: drowsy, resp depress, induce hepatic delta-aminolevulinic acid synth; inc steroid hormone metab Chronic: tolerance and dependance Withdraw: anxiety, insomnia, anorexia, autnomic hyperactive (like EtOH) Tx: resp support, gastric lavage, hemodialysis and osmotic diuretic Comment: cross-tol w/ other sedatives = hypnotics
Phenobarbital *Mephobarbital
GABAa rec bind: allosteric and mimetic "Pheno is forever; barbital" Long acting >8hrs Metab: liver oxidation & conjugation Thx: epilepsy, w/draw from sedative **** Acute: drowsy, resp depress, induce hepatic delta-aminolevulinic acid synth; inc steroid hormone metab Chronic: tolerance and dependance Withdraw: anxiety, insomnia, anorexia, autnomic hyperactive (like EtOH) Tx: resp support, gastric lavage, hemodialysis and osmotic diuretic; +alkanize the urine (25% excreted uncharged) Comment: cross-tol w/ other sedatives = hypnotics
Granulocyte Colony Stimulating Factor
GCSF - produced by macro/fibro,endoth cell *Expand and enhance granulocytes Use: prevent neutropenia Tox: bone pain; well tolerated
Granulocyte Macrophage Colony Stimulating Factor
GMCST - produced by macro/fibro/endoth AND Tcells! *Acts earlier in stem cell differentiation (remember myeloid stem cell can go to myeloblast/granulocytes & monoblast/monocytes) Use: prevent neutropenia in chemo; also use in bone marrow transplant Tox: fever, bone pain, myalgia
Abciximab
Glycoprotein IIb:IIIa inhib Fab: Binds IIb/IIIa--fibrinogen can't bind PLT *Ab (Fab fragment) doesn't let PLT stick (CIX) Acute inhibition of PLT aggregation, arterial side Tx PCI, ACS
Eptifibatide
Glycoprotein IIb:IIIa inhib Peptide: Binds IIb/IIIa--fibrinogen can't bind PLT *Fibrinogen: "F!" blocked by the peptide eptifibatide Acute inhibition of PLT aggregation, arterial side Tx PCI, ACS
*procainamide
Group IA antiarrhythmic drug: short half−life; similar to quinidine but may cause lupus erythematosus
*Flecainide
Group IC antiarrhythmic prototype: used in ventricular tachycardia and rapid atrial arrhythmias with Wolff−Parkinson−White syndrome. Tox: arrhythmogenic, CNS excitation
Levothyroxine
HRT Thyroxine: T4 Ind: hypothyroid S/E: hyperthyroid effects-angina, arryth DI: cholestyramine dec absorption; barbiturates inc metab *displace NSAIDs from binding Special: myxedema coma & pediatric needs
19**Thyroid Agents**
HRT Hypothyroid Levothyroxine (thyroxine=T4) Liothyronine, dessicated thyroid, liotrix ** Hyperthyroid Methimazole PTU (propylthiouracil): P for peripheral too Potassium Iodide Ipodate sodium, lopanoic acid (iodine effect & p for peripheral effect) Radioactive iodide Propanolol (counter thyroid storm sx) Thyroid storm: use PTU, KI, propranolol
Hydrocortisone (cortisol)
HRT: adrenocorticol insuff (primary/secondary) Rheumatic, dermatologic, opthal, allx states S/E: Inc gluconeogenesis and lipolysis
Progesterone
HRT: use w/ estrogen Progesteron alone: dec HDL, inc LDL, inc TG (OPPOSITE of estrogen effects)
Diuretics (2)
Hemodynamic *Dopamine: keeps the kidney mine *Caffeine: keeps it lean via x adenosine Osmotic *Mannitol: man sucks it all in *Isosorbide: sucks it in for the eyes *Glycerol: glycerol sucks it all in
Caffeine
Hemodynamic: vasa recta "Caffeine make the diameter lean by preventing adenosine" Constricts blood vessels to the brain and prevents adenosine from inhibiting the release of dopamine and acetylcholine
Opioids
Heroin, morphine High lipid solubility: rush/orgasm like feeling, then euphoria / then period of sedation Dependance Withdrawal: lacrimation, rhinorrhea, yawn, sweating, weak, chills, N/V, termor, hyperpnea *tx w/ methadone (long acting), taper off, and sedatives & clonidine (auton blocker)
Retinoids
High dose: induce PML cells to differentiate *PML: t15:17->RARalpha-PML gene fusion **RAR=retinoic acid receptor Promyelocytic Leukemia (PML): normally rapidly progressive, chemo fails
Bulk forming lax: Psyllium Methylcellulose Polycarbophil Bran
Hydrophillic colloids: absorb water/bulk Ind: constipation
Nitrites & Nitrates
Hypoxia: oxidize ferrous(II) to ferric(III) *methemoglobin (dec binding) Tx: methylene blue *causes false transient dec in pulse ox
Benzathine penicillin G Procaine penicillin G
IM only Long duration
TB meningitis
IPE (just not rifampin)
(Remifentanil)
IV analgesia: Opiate Receptor Agonist "Fentaly needs the ventil" Use: Sedation, combined for general anesthesia *rapid, ultrashort acting (ester linkage--rapid hydrol) Adv: no accumulation *syndergy w/ hypnotic drugs (propofol) & volatile anesthetics - reduce other drug dose Disadv (all opiates): Dose related resp depression, need controlled vent
Fentanyl (Sulfentanyl)
IV analgesia: Opiate Receptor Agonist "Fentaly needs the ventil" Use: analgesia-combine w/ muscle relaxants and inhalation anesthetics *Combo: fentanyl + droperidol + N2O = neuroleptanesthesia *rapid onset & redistribution *low dose: short duration; high dose: long duration Adv: CV stable, profound analgesia Disadv (all opiates): Dose related resp depression, need controlled vent Comp: repeated injection accumulation, prolonged recovery
Morphine (Alfentanil)
IV analgesia: Opiate Receptor Agonist "Morphine! More Please!" Adv: min cardiac depression, dec vascular resistance *Low dose: Intermediate duration *High dose: prolonged duration of action Disadv (all opiates): Dose related resp depression, need controlled vent Comp: skel muscule rigidity, vomit, constipation, urinary retention, pruritis *Histamine release
Thiopental (methohexital, thiamylal)
IV hypnosis/amnesia: Barbituate (GABA) "The BARBer in your pent house puts me to sleep" Use: anesthesia induction, short procedures w/ little pain *30-40 sec onset; 12 hour elimination Adv: rapid pleasant induction/fast recovery (single dose); little post-anesth excitement & vomit Disadv: very alkaline (tissue irritation); poor analgesia; low TI *dec cardiac contraact & resp depression *laryngospams & bronchospasm Comp: cardiopulm depression, hangover and accumul Note: redistribution (not metab) terminates single dose; also protein bound (liver failure will inc potency)
Diazepam
IV hypnosis/amnesia: Benzodiazepine (GABA) "Diaz: BZ will make your days seem happy' Use: Sedation, reduce anxiety; use w/ opiate in cardiac patients *Slow onset, plasma prolonged in cirrhosis Adv: safer, anterograde amnesia Disadv: unpredictable dose-response Comp: min cardiovascular depression; irritates veins (phlebitis)
Midazolam (Lorazepam)
IV hypnosis/amnesia: Benzodiazepine (GABA) "In MI DAZE, hypnosis was done with a watch" Use: pre-anesthetic sedation; supplement or induce anesthesia *3-5 min onset *Most widely BZ anesthetic drug Adv: min cardiopulmonary depression, excellent amnesia, more predictable dose response Disadv: NOT an analgesic
Ketamine
IV hypnosis/amnesia: Dissociative "Low BP? Keep this in mind" Use: asthmatics (BRONCHODILATES); good analgesia (superficial pain) & amnesia *sympathetic: use in trauma or low BP *Rapid onset, long lasting Adv: cardiorespiratory stability (sympathetic) Disadv: CNS stimulant... Comp: associative anesthesia: hallucinate, terrifying dreams, delirium upon emergence *Inc ICP (cerebral blood flow)--CI with head trauma Similar structure to LSD
Etomidate
IV hypnosis/amnesia: Misc "Are you intimidated with low BP or MI risk? use Etomidate" Use: Induce patients at risk of low BP or MI *Rapid onset, short duration; rapid liver metabolism Adv: min cariorespirator depression; CV stability after induction Disadv: pain on injection; myoclonic activity Comp: *Adrenocortical suppression (less cortisol); N/V
Propofol
IV hypnosis/amnesia: Misc "MJ drug--drug caused this pro to fall" Use: induction w/ balanced anesthesia; induction & maintenance w/ outpatient sx **Short duration of action; after prolong infusion recovery NOT delayed! **Note: Most widely use IV anesthetic; protein bound Adv: smooth/rapid induction; swift clear headed recover in 2-8 min; anti-emetic Disadv: min cardiovascular and resp depression Comp: pain on injection; hypotension; high apnea incidence
Rho-D Immune Globulin
Immunosup. Antibodies Prevents formation of anti-D abs *Immunize if Rh- mother gives birth to Rh+ baby (give w/in 3 days after birth; also next baby give at 28 weeks) Tox: swell/redness
Immunosupp Agents (cont)
Immunosupp Antibodies: Antilymphocyte & Anti-thymocyte globulin (ALG & ATG): anti-THYMOCITE (T cell block) Anti-CD3 monoclonal Ab: block Tcell Rho-D Immune Globin Anti-TNFalpha (prevent inflamm response for leuko activation) Daclizumab: Bind IL2-R (Dac blocks Dos)
Colchicine
Impair chemotaxis of granulocytes to gouty joints (tubulin activity) "Make the granulocytes run COLD" Acute therapy or + probenecid Indication: acute gout attacks Complications: nausea, vomiting
Cholecalciferol (vitD3) Ergocalciferol (vitD2) Dihydrotachysterol (DHT) Calcifidiol (25)-liver Calcitriol (1,25)-kidney
Inc Ca & PO4, #of osteoclast Bone (PTH like), Intestine *1,25 on kidney: inc Ca & PO4, dec FGF23 Ind: Chronic hypocalcemia
Multidrug Resistance
Inc P-glycoprotein expression (export pump) *Antitumor antibx: VIN, TAXI, TOPOISOMER. **NOT bleomycin, alkyl High in adrenal/kidney, colon/liver/pancreas Verapamil inh Pgp (but requires too high dose) Pgp into viruses to infect marrow cells (reduce S/E in cx from VIN/TAXI/TOPOIS
Carbon Monoxide
Incomplete combustion Most freq cause of death from poisoning Tox: HA, flush, weak, dizzy, dim vision, n/v, collapse, syncope, coma, death Tissue hypoxia (due to hypoxemia) *Carboxyhemoglobin%: 15 ha, 40 flush, 50-60 resp, 70 death Tx: hyperbaric O2 (get below 10%), ABC, metabolic acidosis tx *incorrect pulse ox
Particulates
Incomplete combustion - sooty cities Tox: CV disorders/Heart Failure!! *CHF, ischemic heart disease, arrhythmia *inc hospital admission in ALL but injury
ephedrine*
Increases NE release from terminal. This was included in many diet pills, but was removed due to increase heart/BP conditions. Nasal Decongestion, Urinary Incontinence, hypotension.
Potassium iodide
Ind: hyperthyroid Inhib T3/4 synth Rapid effect Crosses placenta Short term only (thyroid escape)
endophonium*
Indirect acting agonists, acetylcholinesterase Inhibitor: Diagnosis of Myasthenia gravis
tyramine*
Indirectly acting sympathomimetic prototype: releases or displaces norepinephrine from stores in nerve endings. Usually inactive by the oral route because of high first pass effect but will cause potentially lethal hypertensive responses in patients taking MAO inhibitors
Carbamates *Carbaryl, aldecarb
Inh AChE (REVERSIBLE with hydrolysis) Tox: Muscarinic storm (SLUDGE/DUMBELLS) *Nicotonic stim then blockade (HTN,fasc,tremor THEN weak) *CNS: restless, ataxia, confused, sz Tx: atropine (no pralidoxime) *excess atropine (antichol): confuse,sz,death Note: don't accumulate in environ
Organophophate Insecticides *Malathion, parathion, diazinon
Inh AChE (complex can age - irrev) Tox: Muscarinic storm (SLUDGE/DUMBELLS) *Nicotonic stim then blockade (HTN,fasc,tremor THEN weak) *CNS: restless, ataxia, confused, sz Tx: atropine and pralidoxime *pralidoxime can bind Ca (muscle spasm) Note: don't accumulate in environ
Corticosteroids: prednisone and prednisolone
Inh tumor growth Use: VM6P (ALL), Hodgkin (MVPP) Tox: cushings syndrome
Solvent, aerosol
Inhalant--benzenes, Nit oxide "aerosols" Acute: euphoria, delirium, altMS, anesthesia, arrhythmia, bone marrow depress, cerebral degen, asphyxia, aspiration, death
Nitrous Oxide
Inhalation general anesthesia; +GABA, -NMDA, K+ *Fast acting (NO, Desflurane, Sevoflurane)--"DesServe Nitrous oxide" "Is this going to hurt? NO if we use NO" Use: minor surgery *can combine with more potent anesth for general anesthesia - 2nd gas effect (2nd gas more potent, don't need as much) Adv: rapid induction & recover; no odor; minimal cardiopulm depression; good analgesia Disadv: weak anesthetic Comp: post-op N/V; recovery hypoxia; chronic exposure vitB12 def Toxic effects of inhalation anesth: increased ICP (blood flow inc), spont abortion, teratogenic
Desflurane
Inhalation general anesthesia; +GABA, -NMDA, K+ *Fast acting: outpatient "DesServe N.O.--fast (outpaitent) Use: outpatient Adv: rapid onset & recovery; potent; min metabolism Disadv: cardiopulmonary depression Comp: Malignant hyperthermia; very pungent; airway irritation--laryngospasms; tachycardia *not good for induction
Sevoflurane
Inhalation general anesthesia; +GABA, -NMDA, K+ *Fast acting: outpatient for KIDS "DesServe N.O.--fast (outpaitent)" "Outpatient for kids: kids always want to be served" Use: outpatient Adv: fast induction & recovery; potent; min nonirritating vapor Disadv: cardiopulmonary depression, very pungent & expensive Comp: Malignant hyperthermia, nephrotoxic *unstable when exposed to CO2 (anesthetic machinery absorbents)
Isoflurane (Methoxyflurane)
Inhalation general anesthesia; +GABA, -NMDA, K+ *Slow acting "Adults are all the same: ISO" Use: anesthesia maintenance *uterine relaxant (fetal manipulations) Adv: stable cardiac rhythm, rapid onset & emergence; minimal metab; muscle relax Disadv: cardiopulmonary depression, pungent odor Comp: Malignant hyperthermia; airway irritant--coughing, laryngospasms *CI: asthmatics
Halothane
Inhalation general anesthesia; +GABA, -NMDA, K+ *Slow acting "Asthmatic children with HALOs" Use: anesth maintenance *ASTHMA patients & pediatrics *uterine relaxant (fetal manipulations) Adv: pleasant odor, bronchodilator Disadv: SLOW induction/recovery; high metab side effects; cardiopulmonary depression Comp: Malignant hyperthermia; myocardium sensitized to arrhythmic effects from catecholamines; fatal hepatotoxicity (metab) **may inc postpartum bleeding
(Enflurane)
Inhalation general anesthesia; +GABA, -NMDA, K+ *Slow acting Use: anesthesia maintenance, uterine relax Adv: Pleasant odor Disadv: cardiopulm depressn, significant metabolism Comp: BP depression, seizures; metab-renal toxicity **Not longer used much
Pyrimethamine (+sulfadoxine)
Inhibit DHFR Antimalarial Malaria (won't kill schizonts), cyclosporiasis, toxo *all 4 malarial forms S/E: severe anemia
Cidofovir
Inhibit DNA poly only Nucleotide analog DOES NOT require viral kinase Use: CMV retinitis S/E: nephrotoxic *coadminister w/ probenecid to reduce
Guanetidine
Inhibit NE vesicle fusion Tx HTN
Furosemide
Inhibit Na/K/Cl cotransport *In a fury, see my Na/K/Cl get washed away Loop diuretic Tx CHF step 1, pulmonary edema; otoxicity!
Cycloserine
Inhibit cell wall synth 2nd line anti-TB "cyclo for psycho"-CNS problems
Azoles
Inhibit fungal ergosterol synth: "CONAZOLES are con as*holes who inhibit the synth" *STATIC (not for life threatening *don't give antacids for keto and itraconazole (need acid for stomach absorption) Ketoconazole: inhibits adrenal/gonad hormone synth *PCOS (rev hirsuitism); s/e gynecomastia Itraconazole: "itra is it" *DOC: Histo, blasto, sporotrichosis *No CNS penetration
Nedocromil
Inhibit mast cell activation and chemotaxis and inhibits bronchoconstrict (does not cause dilation) *cromolyn does not inhibit release of LTb4 and PAF! "Nedo pokes the mast cell with a needle; now he's taunting them like Cromo" Long term; inhibit early and late response *prior to exercise or known exposure Tx: asthma (antigen, cold, or exercise induced) Tx: rhinitis Inhalation: prior to exposure/exercise *also nasal spray, optic solution 3-4 days to be effective
hemicholinium*
Inhibits Choline transport into a vessicle via a Na-symporter.
*vardenafil
Inhibits phosphodiesterase (PDE) 5, preventing breakdown of cGMP, which promotes vascular vasodilation. Use: erectile dysfunction. Tox: Life-threatening hypotension when combined with nitrates, impaired blue-green color vision.
Air Pollution
Inorganic Gases: Sulfur Oxides: "sulfur = fossil fuel, coal" Nitrogen Oxides: "nitro - think car exhaust" Ozone: urban smog Air toxins: 1,3-butadiene Sick building syndrome Particulates: sooty cities and incompl comb. CO: incompl combustion Nitrites & Nitrates: inhal or PO Cyanide: nitroprusside, metal processing, plastic combustion, plants Hydrogen sulfide: rotten egg smell, natural sources (similar to CN)
Dimercaprol
Inorganic/ionic Hg & As Tox: HTN, tachy, n/v, fever, pain at injxn DO NOT use for: methyl-mercury (increases bbb transport), Fe or Cd (complexes)
BZ indications: Insomnia Status epilepticus Pre-anesthesia Skel Musc spasticity Phys Dependance Acute Mania
Insomnia: flurazepam, temazepam, triazolam, zolpidem/zaleplon/eszoplicone Status epil: lorazepam, diazepam Preanesthetic: midazolam (induce anesthesia) Skel Musc spasticity: diazepam, baclofen (Gaba B analog) Phys dependence: chlordiazepoxide, diazepam Acute mania: diazepam, lorazepam
Insulin: Insulin LAG (liptin, aspart, glulisine) or inhaled Humilin Insulin isophane (NPH), insulin zinc (lente) Ultralente insulin, insulin determir, glargine
Insulin: DM Bind tyrosine kinase (liver, muscle, fat) S/E: hypoglyc, hypokalemia, lipodystrophy Rapid: give before a meal Long: give at bedtime
11**Diabetes Drugs**
Insulin: DM Rapid: insulin lispro/aspart/glulisine "LAG has no lag", inhaled insulin Short: humulin "humiliating being short" Interm: insulin isophane (NPH)/zinc(lente) Long: Ultralente, insulin glargine/determir "Determined to gargle for LONG time" ** Sulfonurea: T2DM 1st gen: T2DM "amide told you to get your butt in gear" Tolbutamide, tolazamide, chlorpropamide 2nd gen: Glyburide, glipizide "GLY lies about being lazy" ** Meglitinides (glinides): like sulfonylurea Repaglinide, nateglinide
Ezetimibe
Interfere gut cholesterol absorption *Be Eazy this time on the cholesterol absorption Use in combo with statin; lower LDL Tx hyperchol, phytosterolemia
Pyrethroid insecticides *Pyrtethrin, cypermethrin, deltamethrin (RAID)
Interfere neurotransmission (Na, GAB, Ca) Low acute tox in humans Long persistence in environ
New Direction in Chemo Thx
Interleukin (IL2): produced by T cells; T/B prolif Interferon: alpha(Leuk) & beta(fibro) INC MHCI and NK cells; gamma(Tcell) INC MHCII (macrophage) GCSF & GMCSF: colonsy stimulating factor Retinoids: differentiation in PML (AML) Herceptin/Transtuzumab: Bind HER2 Imatinib (Gleevec): Tyrosine kinase inh Angiostatin: plasminogen fragment; inh angio Endostatin: collagen fragment: inh angiogen Bevacizumab: "Beverly hates vegetables" Metronomic thx: tubulin metronome (endothelial/angiogen blocked)
Coagulation
Intrinsic pathway (pTT measures)-12,11,9,8 12 (hageman), 11, 9 (t8)-->10 Extrinsic pathway (pT measures)-7,9 Tissue injury, thromboplastin, 7,9-->10 Common pathway (10-5-2) 10, (t5), 2-->Fibrin (t13)-->fibrin cross link (plasmin breaks down) **Vit K dependent (Warfarin KILLS these): 7, 9, 10--2 9, 10--2
Akathisia
Irresistible compulsion to be in motion (like mania) 1st two weeks of tx Tx: same as acute dystonia; also central beta block (eg propranolol)
Echothiophate
Irrev AChEI *Echo helps aqueous flow Open angle glaucoma (topical)
Malathion
Irrev AChEI *Mal = bad (spiders and insects are bad...) Insecticide; causes SLUDS
Sarin
Irrev AChEI *Sarin when y'all are war'in Military nerve gas (cross BBB)
Radioactive Iodide (I-131)
Irrev destruction of thyroid Contra: pregx Most become hypothyroid Stop PTU before ablation
Echothiophate
Irrevers AChEI *Echo through eternity: the phate of death for AChE Constrict? Inc flow of aqueous Tx open angle glaucoma
Aspirin (ASA)
Irrevers acetyl COX1/2 "Aspirin!" NSAID - salicylate Ind: analgesia, antipyresis *mod dose: uncouples phosph oxidation *high dose: pyretic and neuro effects CI: bleeding d/o, asthma, head trauma, hypersensitivity, aplastic anemia, agranulocytosis, pancytopenia, peptic ulcer Metab: 15-30hrs; stomach & plasma: de-acetyl; liver: conjugation; kidney: excretion *Zero order @ high dose (liver conjugation limiting) Comp: GI ulcer, hep/renal toxicity, bleeding, Reye's syndrome (viral infxn conseq) Tox: tinnitus, n/v, HA, hyperventilate, confusion, rash, bronchoconstriction
Nicorandil
K arterial relaxant (ateriolar dilatation) *Diazoxide's cousin: LAZY, LIDDLE, AND ILL (HydraLAZINE, Minoxidil, Pinacidil, Nicorandil)
Pinacidil
K arterial relaxant (ateriolar dilatation) *Diazoxide's cousin: LAZY, LIDDLE, AND ILL (HydraLAZINE, Minoxidil, Pinacidil, Nicorandil) Use w/ diurhetic, B-block, and ACE inhib Tx HTN
Hydralazine
K arterial relaxant (ateriolar dilatation) *Diazoxide's cousin: LAZY, LIDDLE, AND ILL (HydraLAZINE, Minoxidil, Pinacidil, Nicorandil) Use w/ diurhetic, B-block, and ACE inhib Tx HTN, CHF
Minoxidil
K arterial relaxant (ateriolar dilatation) *Diazoxide's cousin: LAZY, LIDDLE, AND ILL (HydraLAZINE, Minoxidil, Pinacidil, Nicorandil) Use w/ diurhetic, B-block, and ACE inhib ROGAINE Tx HTN, Baldness
*diazoxide
K channel opener used to relax smooth muscle in treating severe hypertension. Side effects include reflex tachycardia, angina, hypertrichosis. Also used topically to regrow hair. Diazoxide acts on pancreas and can cause hypoinsulinemia (not used).
Minoxidil
K+ arterial relaxant "Minox Kocks up the hair with K" Dec BP, afterload Tx HTN, baldness Comp: headache, flushing, hypertrichosis
*minoxidil
K+ channel opener that hyperpolarizes and relaxes vascular smooth muscle. Uses: Severe HTN, baldness. Tox: Hypertrychosis, Pericadial effusion, Reflex tachy, Angina, Salt retention.
Non-linear pharmacokinetics
Km = [S] when 1/2 Vmax Vmax = max rate Ex: phenytoin ER = CL x [drug] = Vmax x [Drug] / (Km + [Drug] **CL = Vmax / (Km + [Drug]) MD = CL x [drug] = above insert
Aliphatic hydrocarbon solvents/vapor *Methane, ethane, propane, butane, hexane
LOW MW: act as asphyxiants HIGH MW: CNS depression Hexane & MBK (methyl n-butyl ketone): polyneuropathy (2,5-hexanedione metab) High hexane exposure (glue sniffing): distal neuropathy (neurofilament aggregates in distal axon) *Stocking and glove sensory loss, THEN more proximal sensory and motor
Amobarbital **Phentobarbital Secobarbital **Thiopental **Phenobarbital Mephobarbital
LOW: prolong GABA induced opening of Cl HIGH: open Cl independent of GABA *hyperpolarize cell Amobarbital *Phentobarbital: phento stops the vent yo Secobarbital *Thiopental: anesthesia "thy pent house I sleep" *Phenobarbital: anticonvulsant "it's not funny she's convulsing" Mephobarbital Barbituate Ind: non-selective, dose dep CNS depression Comp: sedation, decreased cogn & motor, rapid tolerance, DI, abuse, resp depression/lethal Note: less freq sedative/hypnotics, usually supplanted by BZ (tx anxiety/sleep d/o)
Hallucinogens
LSD: acid Phencyclidine: PCP, angel dust MDMA: ectasy MDA, mescaline, psilocybin Marijuana (THC) Dronabinol impaired judgment, reckless, CVA
BInding proteins
Lidocaine binds AAG (alpha1 acidic glycop) *labs measure both bound/unbound *AAG: phys stress protein Albumin: bind anionic (-) drugs AAG (alpha acidic glycoprotein): stress protein, bind NON-anionic drugs
Hypericum (St. John's Wort)
Like TCA: (-) catechol reuptake "Some people are hyper about icky herbals" Atypical/herbal Ind: mild depression Comp: affect liver metab pathways (drugs used for heart dx, depression, seizures, HIV, transplants) *Not FDA regulated
Methotrexate
Like TMP: antifolate ALL (VM6P) & breast (CM5) Block DHFR (FH2->FH4): deplete N5,10methyleneTHF (needed for dUMP to T) Use: osteogenic sarcoma (high dose w/ leucovorin), child ALL (VM6P), chorioCA, leukemic meningitis, breast (CM5) *also for bad psoriasis and RA Tox: myelosupp (use leucovorin rescue *worse if dec excretion (weak acids, nephro) *GI: mucositis *higher doses: inc 7-hydroxyMTX (inc renal failure) Resistance: dec uptake #1 (less if high dose w/ leucovorin = folinic acid)
salmeterol*
Longer acting Beta 2 agonist is recommended for prophylaxis of asthma
*furosemide
Loop diuretic prototype: blocks Na+/K+/2Cl_ transporter in thick ascending limb; high efficacy; used in acute pulmonary edema, refractory edematous states, hypercalcemia. Tox: ototoxicity, K+ wasting, hypovolemia, increased serum uric acid. Ethacrynic acid is similar but has less effect on uric acid.
Chlorophenoxy Herbicides (weed kill) *2,4-D(dichlorphenoxyacetic acid), 2,4,5-T
Low dose: neurotoxic High dose: Vfib death Production workers: chloracne & dermatitis Used in agent orange; 2,4,5-T was contaminated with TCCD *low acute tox, low environ persistance
Selective B2 agonist
MAST: Metaproterenol & Albuterol--acute asthma Salmeterol--long term Terbutaline--reduce premature uterine contractions
Arsenic
MC metal poisoning Groundwater (wells in west), pesticide/herbicide industrial Abs: resp & GI Liver: As+5 ->As+3 (arsenite binds SH groups and inactivates pyruvate DH AsO4 mimics PPi *AsO4 + ADP -> energy wasting Arsine gas (AsH#) triad: massive hemolysis, abd pain, hematuria w/ nephrotoxicity (gas kills Hb & RBC) Tx: Dimercaprol or unithiol *supportive for diarrhea/shock
pseudoephedrine*
MECH: indirect sympathomimetic (amplify EPI and norEPI release) and directly activates adrenergic receptors, causing vasocontrictions and cardiac stimulation USE: decongestant TOX/Other: OTC cold-relief
tiotropium*
Maintenance treatment of bronchospasm associated with COPD; reduction of COPD exacerbations
Hormone Therapy
Mammary cancer: androgens (SE hirsutism) Endometrial cancer: progestins after sx/rad Androgen dep prostate: Estrogens (s/e GI sx, inc ECF, gynecomastia)
Cockcroft-Gault
Measure clearance CL = (140-age) x Kg (0.85 if female) / (SCr x 72)
Other Sedative/Hypnotic Agents
Meprobamate Chloral hydrate Hydroxyzine Parahaldehyde
Other sedative hypnotic agents
Meprobamate Chloral hydrate Hydroxyzine Parahaldehyde
11**Diabetes Drugs**(cont)
Metformin (T2DM 1st line) - Biguanide class ** Thiazidolinediones (TZD): "diones are litazones that light up the sensitivity zone" - T2DM Pioglitazone Rosiglitazone ** GLP affects: T2DM Exenatide - analog (ex copies) Sitagliptin, Linagliptin - liptin says lips don't degrade
Organomercurials
Methyl and alkyl mercury Fish/shellfish 90% absorption in GI! *enterohepatic recycling-slow clearing *concentrate in RBC *Methylmercury: Bind cysteine (mimc methionine and cross bbb & placenta) NEURO poisoning: parasthesia, ataxia, hearing, dysarthria, visual
Secretory laxatives: Bisacodyl Phenolphthalein (Ex lax) Anthraquinone deriv Castor oil
Mild irritant Ind: constipation Ex-lax had carcinogenic potential (phenolpthalein aint that funny) Castor oil: less ADEK abs
Eplerenone
Mineralcorticoid receptor antag (specific) "Epimer like spironolactone" Site 4 (CT) Tx HTN, post MI, K protection **combo with site 3 diuretics Comp: hyperkalemia
Cadmium (Cd)
Mining, smelting, shellfish, batteries *More often respiratory Toxicity usually due to chronic exposure *chelator therapy causes nephrotoxicity *chronic: respiratory (fibrosis, emphysema), renal toxicity (metallothionen-Cd & RTN)
Alkylating Agents (cont)
Misc: Cisplatin/Carboplatin: C for ears and kidneys -Carbazine: Cars racing through DNA/RNA/protein now in the da bin (Dacarbazine, Procarbazine) Mitomycin: Mighty GA
Misoprostol Athrotoec = Miso + diclofenac(NSAID)
Misopro = more prostaglandin *PGE1 derivative Inhibits AC: less histamine stim Stim gastric mucosa & HCO3 Ind: high risk ulcer patients taking NSAID S/E: freq bloating&diarrhea *PG:uterine contractions (CI preg) & patent DA
**Monobactam, carbapenem, glycopeptide**
Monobactam: Aztreonam "AZ tree" ** Carbapenem: Imipenem (w/cilastatin) & meropenem "Emmy penny" ** Glycopeptide: Vancomycin: "Tank mice"
(Carbamepine) (Valproic Acid) (Lamotrigene)
Mood stabilizers (like Lithium) *tx of mania/bipolar Carb: unknown MOA *comp: drowsy, dizzy, slurr speech, transient rash, incoordination, leucopenia, aplastic anemia, rare-thrombocytopenia, teratogenic *dec contraceptive effectiveness Valproic: +GABA levels in CNS *comp: GI, sedation, tremor, thrombocytopenia, polycycstic ovarian syndrome, teratogenic Lamotrigene: (-)Na channels *comp: Stevens-Johnson syndrome, fulminant rash
General Anesthesia: IV Analgesia
Morphine: "More Please!" (Alfentanil) Fentanil: "Needs a ventil." (Sulfentanyl) (Remifentanil)--synergy, ester rapid hydrol
Methylprednisolone
Most anti-inflamm of all SHORT acting (but short acting the leaset anti-inflamm of all) CI: DM, GI ulcers, Tb hx, HTN, infxn, psychoses
Tiotroprium
Musc & Cholinergic Antag "Ipratroprium's tio (uncle) blocks Chol as well" "Tio blocks Two: Musc & Chol" -atropine blocks muscarine -otropine also blocks Chol Bronchodilation, reduce secretion Tx Chronic Bronchitis, emphysema *Long acting
COPD DRUGS 2
Musc antagonist *Ipratroprium: "I pray I can breath soon" *Tiotroprium: "Ipra's uncle but can also do Chol block" *Atropine: the root of Ipratroprium; blocks muscarine Adrenergic Agonist *A/B: epinephrine: EPI let's you Breath *B: isoproterenol: I'm such a pro *B2: metapro (now breeeathe), pirbuterol (pro with a pretty butt), albuterol & lev-albuterol, salmeterol & formoterol (motor all day long) Methylxanthine *Theophylline: "phylline blocks adenosine; filing cabinets add up" -caffeine, aminophylline, theobromine Others: Alpha1 proteinase inhibitor: "emphysema" DNAse: "emphysema, break up mucus"
Ipratroprium
Muscaranic Antag (block receptor: block cGMP formation) "I pray I can breath soon" Bronchodilation, reduce secretion *2x more potent than atropine *not as potent as B2 agonist Tx asthma (intolerant to B agonist), Rhinitis *SLOW ONSET, LONG DURATION Comp: local irritation Contraind: closed angle glaucoma
scopolamine*
Muscarinic Antagonist. Used as a patch. Affects the CNS and used in Motion sickness and anti-nausea end of life care.
iptratropium*
Muscarinic antagonist *Organ system*: respiratory *Application*: asthma, COPD ("I PRAY I can breathe soon")
propantheline*
Muscarinic antagonists. Block M1 receptors on ECL cells and M3 on parietal cells. Reduce gastric acid secretion. Uses: PUD (rarely used) Tox: Tachycardia, dry mouth, difficulty focusing eyes.
9**HIV**
NRTI: "vudine" *Zidovudine: "T analog: tv while dining" Didanosine: "A analog" Zalcitabine: "C analog: cita for c" Stavudine: "T analog: tv.." *Lamivudine, emtricitibine: "C analog: cita for c" Abacavir: "G analog: g movie in cave" *Tenofovir: "tiny favorite" nuceloTIDE adenosine analog" ** NNRTI: "Elfs Never Deliver" Efavirenz Nevirapine Delavirdine **Protease Inhibitor: "Navir say NEVER have late p. shake" Saquinavir, indinavir, nelfinavir, amprenavir/fosamprenavir, lopinivir, ritonavir, tipranavir ** Others- Enfuvirtide: "No en fusion-fusion inhibitor" Maraviroc: "CCR5 receptor like a rock" Raltegravir: "integrase like gravy"
(Sulfindac)
NSAID acetic acid In patients w/ renal insufficiency 1/2 as potent as indomethacin Active form is created in liver metab
Nesiritide
Natriuretic Peptide *Like some Na SIR? Increase FGR, dec Na retention / dec afterload Tx Acute L failure
Opium tincture Codeine Morphine
Natural opioid anti-diarrhea CNS/enterics: Delay gastric empty, absorp water/electrolytes, inhibit secretions and propulsion Ind: analgesia, diarrhea *most effective against neurogenic secretory diarrhea
*dopamine
Neurotransmitter and agonist drug at dopamine receptors: used in shock to increase renal blood flow (low dose) and positive inotropic effects (moderate dose).
hexamethonium*
Nicotinic antagonist (blocks para and sympathetic). Uses: Ganglionic blocker. In experimental models, prevents vagal reflex responses to changes in blood pressure - prevents reflex brady.
Alkylating Agents
Nitrogen mustards: *Mechlo cycles* through shirts with all the mustard stains Mechloretamine: Mechlor says Hodgins is the MVPP Cyclophosphamide: Cycle of CD & CM high five breasts (Melphalan: mouth full of M&Ms, Chlorambucil) Alkyl Sulfonates: Busulfan: Bus full of grains (CGL) Nitrosureas: (nitro mustangs: all end in -mustine); mustangs through bbb (Carmustine, Lomustine, Semustine)
Osmotic lax: Docusate Lactulose Sorbitol
Non-abs carbohydrates Ind: constipaion
(meclofenamic acid) (mefenamic acid)
Non-covalent inhib of COX1/2 "Fenamics are fair weather fanatics--block only for some time" NSAID fenamate Met: liver oxidation, urine excretion (70%), feces (30%) *2hr Act central and peripheral
Other
Non-opiate analgesic *Acetaminophen: "A C for acting more CNS" Leukotriene Modifier *Montelukast: "throw a mountain in front of the Leuk receptor" *Zileuton: "Zeus stops leuko synthesis" DMAARD *Inflixamab: anti-body to TNF (Adalimumab) (Etanercept): fusion TNFa receptor / IgG Anti-IL-1 & others (anakinra) (Chloroquine) (Gold compounds)
phenoxybenzamine*
Non-selective, irreversible alpha blocker. Used in Pheochromocytoma. Toxicity is Orthostatic Hypotension and reflex tachycardia.
propranolol*
Nonselective beta−blocker prototype: local anesthetic action but no partial agonist effect. Used in HTN, angina, arrhythmias, migraine, hyperthyroidism, tremor. Tox: asthma, AV block, CHF
carbachol*
Nonselective muscarinic and nicotinic agonist: choline ester with good resistance to cholinesterase; used for glaucoma (not a first−line drug)
Calcipotriene:
Not used to treat Ca d/o Tx psoriasis (hyperprol of keratinocytes)
8**Anti-Virals**(cont)
Nuclear dinner synthesis: NA acid synth "Rib dinner, enter cave watching Fast cars on Nascar & Indy do cycles" Ribavirin (RSV) Entecavir (HBV) Foscarnet (CMV) NRTI, NNRTI (HIV) Idoxuridine (HSV kerat) Cyclovirs (HSV, VZV) ** Protease inh: "Never have post dinner protein shake" Ritonavir, Indinivir (HIV) Note-Raltegravir: "gravy slow transition to late protein" ** Neuraminidase inhibitor: Nuram is leaving Zanamazir & Oseltamivir (Inf)
General Anesthesia: Inhale
Old Drugs: Diethyl Ether, chloroform, cyclopropane "Flurane flow through ane the nostrils" Fast acting: Nitrous Oxide: "will this hurt? NO with NO" Desflurane: "DesServe to have N.O." Sevoflurane: "DesServe..." and "Kids..want..served" Slow acting: Halothane: "Asthmatic child with the Halo" (enflurane) Isoflurane: "All adults are the same: ISO" (Methoxyflurane)
Rhinitis & Cough Drugs 2
Opioid (antitussive) *Codeine: "for the coughing dean" *Dextromethorphan: "codeine made right" Secretory (expectorant) *Guaifenesin: "guai, guaia,... clear throat" *Terpin hydrate: "hydrate resp after terpin" *Iodides: "iodides treat the cough's cries" Reduce viscosity (mucolytics) *Acetylcystein: "cyst like viscosity no more" Bromhexine: "Bros break down the hex of fibers" Anesthetic *Benzonatate: "Benzon stops the tension of stretch receptors"
Opioids (2)
Opioid Antag: "rexones are the ones that reck teh opoid receptor" *Naloxone: locks on to the opioid *Naltrexone: recks opioid; alcohol cravings *Methylnaltrexone: recks opioid; constipation (Malmfene, Alvimopan) Opioid Antidiarrheal Agents *Diphenoxylate: diphen had some oxylate... *Loperamide: so he won't be a loser w/ diarrh (Dilfenoxin) Non-opioid antitussive *Dextromethorphan: morphine's morphan is dextromethorphan
Diphenoxylate Loperamide (Difenoxin)
Opioid Antidiarrheal agents "Diphen had some Oxylate so he's not a Loper loser w/ diarrhea" Ind: diarrhea Diphenoxylate: *use w/ atropine; high insolubility Loperamide: *doesn't cross BBB Comp: abuse and resp dep less likely
Naltrexone
Opioid antag "Na! I don't want a beer--play a trick on you" Reduces EtOH craving tx: alcoholism
Codeine
Opoioid analgesic "Co-deen for the Coughing Dean" Antitussive: Decreases cough center sensitivity *Antitussive action at lower doses than those required for analgesia
Dextromethorphan
Opoioid sterioisomer "Codeine made right (dextro)--no addictive or analgesic effect" Antitussive: Decreases cough center sensitivity *tx cough *No analgesic or addictive effect
malathion*
Organophosphate insecticide cholinesterase inhibitor: pro−drug converted to malaoxon. Less toxic in mammals and birds because metabolized to inactive products
Tardive dyskinesia
Oro-facio-lingual movements (tics) but occasionally also dystonic trunk movements Months to years Tx: may be irrev; discont tx and replace with quetiapine or clozapine *Antichol may predispose
Glycerol
Osmotic-plasma compartment "Glycerol sucks it all in" Countercurrent washout *inert, osm active, filtered not reabs, not metabolized *prevent water reabsorption Tx cerebral edema, glaucoma, prophylax ARF IV, PO Comp: rebound excess CSF: HA, nausea, vomit *contraind: anuria, peripheral edema, CHF, dehydration
Mannitol
Osmotic-plasma compartment "Mann sucks it all in" Countercurrent washout *inert, osm active, filtered not reabs, not metabolized *prevent water reabsorption Tx cerebral edema, glaucoma, prophylax ARF IV Comp: rebound excess CSF: HA, nausea, vomit *contraind: anuria, peripheral edema, CHF, dehydration
Isosorbide
Osmotic-plasma compartment "isosorbide: sucks it in for the eyes" Countercurrent washout *inert, osm active, filtered not reabs, not metabolized *prevent water reabsorption Tx cerebral edema, glaucoma, prophylax ARF *EYE SURGERY IV, PO Comp: rebound excess CSF: HA, nausea, vomit *contraind: anuria, peripheral edema, CHF, dehydration
Liothyronine Dessicated thyroid Liotrix
Other drugs to tx hypothyroid
Elemental Mercury
Ouccupation or pollution exposure Inhalation (volatile), bbb, no GI abs ACUTE: Resp-pneumonitis, pulm edema *gingivostomatitis CHRONIC: triad (tremor, neuropsych, gingivostomatitis) Tx: remove source *note: elemental can be oxidized to ionic
Short Acting BZ
Oxazepam Lorazpem Temazepam Aplazolam Triazolam
CI in pregnancy with anti-myco tx
PAFE: pyrazinamide, aminoglycoside, fluoroquinolone, ethiomide *use RI*E instead
Iloprost
PGE, PGI2 "I for Ilo, and E before I" Ind: severe pulmonary HTN *nasal spray
Misoprostol
PGE1 synthetic analog "Miso make MY stomache hurt" Protect against NSAID-induce gastric & peptic ulcers
Epoprostenol
PGE1, PGI2 "Prost: E for epo, I for Inol" Act: vasodilator, platelet inhibitor *IV Ind: *periph vasc disease (Raynaud, arteriosclerosis obliterans) *pulmonary HTN, MI, cerebral ischemia *Heparin replacement in dialysis Note: limited by desensitization
Aloprostadil
PGE1: relax smooth musc (PDA, ED) "Prost: make a dil pickle straight; oh and keeps the PDA straight sailing" Action: maintain patent ductus arteriosus; erection if inject into corpus cavernosus *continuous infusion for PDA Ind: PDA need, Erectile Dysfunction Comp: apnea in 10-12% of neonates w/ CHD
Dinoprostone
PGE2 "Dino gets that dino out" Action: uterine contractions, induce term labor, ripen cervical opening *Vaginal admin Ind: 1st and 2nd trimester abortions, term labor induction *Alternative to oxytocin or give before oxy Comp: vomit, diarrhea, teratogenic Notes: 96% effective w/ abortions (more so w/ mifepristone, methotrexate)
Eicosanoids
PGE: -prost+adil/ol/one/enol *Alprostadil: "a dil pickle becomes straight" *Misoprostol: "my stomache hurts" *Dinoprostone: "dino gets the dino out" PGE/PGI: *epoprostenol: E for Epo, I for Inol *iloprost: I for Ilo, I before E PGF: -prost *Latan: "rids the HA from Satan" *Carbaprost tromethamine": "Carbon rid"
Carboprost tromethamine
PGF2 alpha "Carbo gets that carbon out" Act: stim uterine contraction Ind: 1st/2nd trimester abortion; persistent postpartum hemorrhage *IM Comp: vomit, diarrhea, teratogenic Note: 69% effective
Latanoprost
PGF2 alpha "Latan decreases the headache from Satan" Act: (+) FP receptors--inc aq humor outflow Ind: intraocular pressure *opthalamic solution
Penicillin V
PO - take on empty stomach
Ionic Mercury salts
PO uptake, no bbb, kidney concentrate ACUTE: corrosive *hemorrhagic gastroenteritis; pain, vomit, melena, shock CHRONIC: GI injury and nephrotoxic (NO neuro) Tx: Dimercaprol *supportive O2 and flush for renal
Seizure Type - Tx
Partial Seizures: *Carbamazepine, Phenytoin Tonic-Clonic Generalized *Carbamazepine, Phenytoin, Valproic Acid, Lamotrigine Atonic: *Valproic acid; lamotrigine, clonazepam Myoclonic: *Valproic acid Absence: *if w/ tonic-clonic: valproic acid *ethosuximide, clonazepam Febrile: *Phenobarbital, diazepam Status Epilepticus *Diazepam/Lorazepam + fophenytoin *(also phenobarbital)
Natural penicillin
Penicillin G (gold standard) *take on empty stomach Cell wall synth inhibitor (penicillin, cephalosporin, carbapenems) *Binds to transpeptidase (PBP) DOC for G+cocci/bacilli All Penicillin S/E: hypersensitivity, anaphylaxis, serum sickness, rash, oral lesion, resp distress, n/v/d, oral contraceptives
1**Penicillin Antibiotics**
Penicillin: "Pencil Villain" Natural Penicillin (Penicillin G)--oral Benzathine/Procaine Penicillicin G-- "B for group B strep" Penicillin V-- "V for via stomach" ** Penicillinse resistant-"oxen with knives don't need cleavers" Oxacillin Nafcillin "naf for staph" Methicillin ** Extended spectrum: "Aminopenicillin: amigo pencil" Ampicillin--"pros listen to the amp" Amoxicillin--"o for oral bioavailable" Clavulinic w/ amox & sulbactam w/ampicillin ** Antipseudomonals: "rainbow w/ pseumo picture" Ticarcillin Piperacillin Carbenicillin
Oxacillin Nafcillin (Methicillin)
Penicillinase resistant "oxen with knives don't need cleavers" *"Naph for staph" Use: penicillinase producing staph (naf for staph) Oxacillin and Naf both have bile excretion (okay for renal impaired; **Naf has both bile and renal) Methicillin: only susc testing
Dactinomycin
Phenoxazone right intercalates between GC "Dactin mice do a Phunny act" *Very potent RNA synth inhibitor DNA intercalator - affects all phases Use: Rhabdomyosarcoma, Wilm's tumor (kids) Tox: no cardiac affects!!
Vitamin K
Phytonadione: "Viking King", "Koagulation vitamin" Def: inadeq supply/abs, Coumadin Made: plants/enterics Role: cofactor carboxylation of glutamate w/ 2,7,9,10 C&S Def: inc PT, pTT (antibiotics thx, malab, newborns, coumadin) *prophylax: give newborns vitK Tx: IM vit K, phytonadione
Alpha1 adrenoreceptor block adverse effects
Postural hypotension/dizzy Reflex tachy Sexual dysfunction
*Ibutilide
Potassium channel blocker (Type III anti arrhythmics). Prolongs QT so watch for torsade. Come here potassium, jk I lied! (ilide), get out of here. Blocking K supposedly is prolonging phase 3 (repolarization)
*dofetilide
Potassium channel blocker (Type III anti arrhythmics). Prolongs QT so watch for torsade. Come here potassium, jk I lied! (ilide), get out of here. Blocking K supposedly is prolonging phase 3 (repolarization)
Indomethacin
Potent (-)Cox1/2, competitive antag "Indo puts one heck of a block in the mit(receiver)" NSAID-acetic acid Ind: acute gout, actue RA flare, pericarditis *Ankylosing spondylosis: drug of choice **PO, rapid, 2-4 hrs, enterohepatic cycle Comp (acetic acids): intolerance, ulcers *HA, dizzy, confusion *neutropenia, thrombocytopenia DI: Probenecid inc concen, antagonizes lasix, interferes thiazide (anti-HTN) *rare nephrotoxicity w/ triamterene
Cromolyn
Prevent mast cell release of mediators, prevent bronchoconstriction "Cromo is taunting them: Come on! Release your mediators!" "Cromo has a long chronology--takes long time to take effect" Long term; inhibit early and late response *prior to exercise or known exposure Tx: asthma (antigen, cold, or exercise induced) Tx: rhinitis -no bronchodilator activity (just inhibit brochoconstrict) Inhalation: prior to exposure/exercise *also nasal spray, optic solution Does not work for acute attack
EMLA
Prilocaine + Lidocaine Skin anesthetic in pediatrics
12**Calcium Metabolism**
Primary agents: PTH *Teriparatide: "synthetic PTH" Calcitonin ** VitD derivatives Calciferol "says calcium for all" 1) Cholecalciferol d3, ergocalciferol d2, dihyrdotachysterol, calcifidiol 25OH, calcitriol 1,25OH 2) Doxercalciferol, paricalcitol: "pair of doxers box out PTH 3) calcipotriene: psoriasis ** DRONATES: "drone attack on osteoclasts" Non-amino bisphosphonate: Etidronate (binds hydroxyappetite crystal) 2nd gen amino bisph: Alendronate, Ibandronate "Alan and Iban block farnesyl disphosphate" Zolendroic acid
Q: Low Renin Activity
Probably salt sensitive, Ca channel blocker OR diuretics
Uricosuric Agents
Probenecid: prohibits gout transport Sulfinpyrazone: Sulfin is fillin those holes
14.15**Sex Hormones**(cont)
Progesterone - HRT Medroxyprogesterone Acetate-contracep. inh ovlulation ** 19-nor steroids: low androgen progestin (like testost) Norethindrone Norgestrel ** Progesterone Antag Mifepristone: mife cuts baby like a knife ** Testosterone Methyl-testosterone Oxandrolone/Nandrolone "become like an ox: androlone" ** Flutamide: "flutes turn off androgen receptor" Leuprolide: "lube for GnRH analog" Fenastride: "Finally stop staring - dec DHT"
Anti-Epileptic Drugs (1)
Prolong cell refractory (block Na in inactive state) *Phenytoin: enytoins stop the sodi's in what they're doin" *Fosphenytoin" (Mephenytoin, Ethotoin) *Carbamazepine: in car w/seizure; azepines zips the sodi's shut (Oxcarbazepine) Reduce threshold of T-type Ca current; enhance GABA: *Ethosuximide: Ca current is sucky (Methsuximide) *Valproic Acid: Val's GABA (jabber) and seizures (Trimethadione: absence seizures) *Phenobarbital: GABA facilitated (Cl hyperpol) (Premidone, mephobarbital) *Diazepam *Lorazepam (Clonazepam, Chlorazepate)
labetalol*
Properties: - α1 and β-antagonists (more β) Action: - ↓BP in hypertensives - α1 block leads to vasodilation (upright position) - β1 blockade blocks reflex sympathetic stimulation of heart Use: - chronic HTN (oral) - HTN emergencies (IV) Adverse Effects: - orthostatic hypotension - dizziness - hepatic injury (limited)
yohimbine*
Properties: - α2 antagonist Use: - erectile dysfunction (replaced) - reverse anti-hypertensive affects of α2 receptor agonists such as clonidine
Opioids (1)
Prototype opioid: close Ca, open K *Morphine: opioid (Hydromorphone, oxymorphone, heroin, levorphanol) Meperidine: pregnant mepers can use this fine *Fentanyl: watch vents during anesth *Methadone: turns down need for opioids Weak opioid agonist: *Codeine: the coughing dean in lots of pain *Oxycode: oxy-oral sustained release (Dihydrocodeine, hydrocodone) Misc: *Tramadol: tram the doll is about to ball (Ziconotide, tapentadol) Mixed agon/antag: *Pentazocine: pentacostals at zoo speak kappa & mu *Buprenorphine: Bu is praying to get off morphi (Butorphanol, Nalbuphine)
Fasolodex
Pure antiestrogen SERM Tx: breast cx
Vitamin B6
Pyridoxine: "Bee sax" INH can predispose to deficiency Precursor to pyridoxal phosphate (trasaminiation and AA metabolism); stimulate L-dopa metabolism!! Def: dermatitis, neuritis, sideroblastic anemia
Sugammadex
REVERSE ACh blockade - 10x faster recovery "Sugar sugar--this will get your AChR working again" Note: binds steroidal nondepolarizaing NM blockers in plasma. In EU only
Glucocorticoids
Reduce intestine Ca absorption Tx: hyperCa
Ethosuximide (methsuximide)
Reduce low threshold of T-type Ca current "Ca current is sucky" Ind: absence seizures Comp: n/v, fatigue, dizzy *Rare: severe rashes, blood dyscrasias Note: Ca channels provide thalamus pacemaker
Severe HTN
Reduce no more than 25% of BP in 1st hour, but not too slow Prefer: Fenoldopam (D1 agonist) Other: Nitroprusside (accumulates thiocyanate toxicity) Other: Nifedipine and other oral meds
Estrogen
Reduce resorption NO increase in bone mass tx: osteoporosis
Acetylcysteine
Reduce sputum viscosity "cyst like viscosity no more" Mucolytic *Inhalation
Assess for renal/hepatic dysfunction
Renal: 24h creatinine (endog), 125-iothionate, inulin, 99-techneticum (exog) **Dose adjust: CrCL / 120 **MD x DA = new dose (unless other organs eliminate, factor in %) Hepatic: bilirubin (damage/fxn), tranaminase (damage)
Aliskiren
Renin inhibitor (non peptide) "Alice will cure our kidney by inhib Renin" Blocks production PO, poor bioavailability Comp: diarrhea, hyperkalemia **does not inhibit kinins
Vitamin A
Retinoids: "Viking Apple Castle" & "Viking Apple with excess apples" Visual transduction and ligand for nuclear hormone receptors Retinol->retinaldehyde (+opsin)-> rhodopsin (visual pigment) *Vit A necessary for cis to trans rhodopsin *childhood blindness worlwide Retinol -> retinoic acid (hormon like molec) *epithelial differentiation DEF: night blindness, xeropthalmia, measles risk of death HYPER: teratogen, peeling skin, cheilosis, cerebral edema, bone toxicity (irrev) Tx: psoriasis, acne, keratinization d/o, wrinkle cream, leukemia (APL/AML), suppress luekoplakia
Vitamin B2
Ribaflavin: "Viking with B tutus; Ribs on flavin flav" Def: malnourished Precursor: FAD, FMN Def: dermatitis & neuritis (w/o clinically distinctive features) *cheilosis, corneal vascularization Tx: oral replacement
Doxorubicin & Daunorubicin
Ruby heart & urine rubs topoisomerase wrong *DNA intercalator - GC unwinding and topoisomerase II inhibition *affects ALL phases Doxo: BVDD (hodg/soft) & CD5 (breast) Dauno: ALL, AGL Tox: cardiotox (dilated) *myofibrillar dropout irreversible; cumulative *don't tx with digitalis! (use iron chelator dexrazoxane) Doxorubicin (adriamycin): MC drug in cx chemo
Tamoxifen
SERM-"turns off breast estrogen"; turns on endometrium though... Use: mammary CA w/ estro R Tox: hyperCa in osteolytic mets
12**Calcium Metabolism**(cont)
SERM: Raloxifene "Rolex of post menopausal" Estrogen ** Denosumab: "Tis enough! Ab vs RANKL" ** Fluoride Strontium Ranelate "strontium makes strong bones" ** HYPERcalcemia tx: Glucocorticoids: dec intestinal Ca absorption Furosemide: loop diuretic "in a fury lose Ca" Cinacalcet: "Sinner stole Ca identity-mimics Ca in PTH feedback"
Labetalol
SR mix: -A1 (rev) RR mix: -B1,2 *SR? RR? what does the LABEL say? A 1.... or a B1,2 Peripheral vasodilation Tx HTN (pregnancy, crisi)
H1 receptor block adverse effects
Sedation, drowsy Weight gain CNS depressants potentiate
albuterol*
Short acting Beta 2 agonists that is drug of choice in treatment of acute asthma but not recommended for prophylaxis
10**Glucocorticoids**
Short to medium acting glucocorticoids: Cortisol (hydrocortisone) Cortisone: most potent of all Prednisone Prednisolone Methyprednisolone: most anti-inflamm of short acting ** Intermed acting: "tram and para are the transition" Triamcinolone Paramethasone ** Long-acting: "Breaks into days" Betamethasone Dexamethasone ** Mineralocorticoid: Fludrocortisone acetate: "flood for aldosterone/fluid affects"
Diuretics
Site 1 (prox tubule): CA *acetazolamide: Acetazol is the hydrogen wall Site 2 (asc limb): NKCC2 (loop-high ceiling) *Furosemide: in a fury rid Na/K/Cl *Bumetanide: furosemide looks like a bumb *Ethacrynic Acid: Edem ethan stop crying-S *Torsemide: unlike furosemide tore its way Site 3 (DCT): NaCl cotransport (thiazide) *Chlorothiazide: Chloride/Na blocking thiaz *Hydrochlorothiazide: hyper chlorothiaz *Chlorthalidone: chlorthiaz 'I aint done' *Metolazone: met this drug in danger zone *Indapamide: indented GFR *Quinethazone Site 4 (CT): Aldosterone inh (K sparing) *Spironolactone: Na and breast spiraling *Eplerenone: epimer like spironolactone *Triamterene: gynecomastic riding TRAM *Amiloride: AMY can't pass Na through
Dantrolene
Skel muscle relaxant: Block SR Ca release "Dan could become lean if we don't give him this drug" Prevent/tx for Malignant Hyperthermia & neuroleptic malignant syndrome
Gold compounds
Slow acting Ind: second line in RA *IM; 50% gold weekly for life *concentrates in synovium Comp: tox in 30% w/ blood abnorm, GI issues CI: pregnant, impaired liver/renal
*Digitalis
Slows and strengthens contractions of the heart muscle by increasing the amount of Ca2+ that enters cardiac muscle cells and by prolonging the action potentials' refractory period.
Hydrogen sulfide (HS)
Smell like rotten eggs Natural sources and petrochemicals Similar to CN + CONJUNCTIVITIS & PULM EDEMA Potent (-) of cytochrome oxidase Tx: don't use thiosulfate but use nitrite (methemoglob reacts w/ HS->sulfmethoglobin)
Aromatic Hydrocarbon solvents *Benzene, toluene
Solvents *Free radicals and DNA adducts Acute tox: CNS Long term: leukemia, aplastic anemia
Halogenated aliphatic hydrocarbon solvents *Dichlormethane, Chloroform, Carbon tetrachloride, Halothane
Solvents & cleaning compounds *Generate free radicals and p450 rxns Tox: general CNS depression, renal tox *CCl4: fatty, necrotic, or cirrhotic liver *Chloroform/Halothane: arrythmia
L-asparaginase
Some tumors can't synth L-asparagine *removes from blood... Use: ALL Tox: hemorrhage (dec clotting factors), liver/pancreas toxicity, hypersensitivity (bacterial enzyme!!)
Antitumor Antibiotics, Hormones, other (cont)
Steroid: Prednisone (VM6P, MVPP) SERM: Tamoxifen (turns off estrogen at breast) Aromatase Inh: Anastrozole "Fat Ana says enough estrogen!!" Leuprolide: GnRH agonist (down regulate receptors) Flutamide: "flutes antagonize androgen receptors)-prostate cx **use together L-Asparaginase: some tumors can't synth asp
Guaifenesin
Stim secretion; reduce mucus viscosity "Guai, gaui, gaui fenesin - clear your throat" Expectorant *Tx cough Comp: triggers vagal reflex--near emetic doses required
(Hydromorphone) (Oxymorphone) (Heroin) (Levorphanol)
Strong Opioid agonist Same action as morphine hydro: oxymorphone: little antitussive heroin: no clinical use, more lipid sol (fast act) levo:
Diphenoxylate Loperamide
Synthetic opioid anti-diarrhea "Diphen dives through BBB" CNS/enterics: Delay gastric empty, absorp water/electrolytes, inhibit secretions and propulsion Ind: OTC diarrhea *most effective against neurogenic secretory diarrhea S/E: diphen used w/ atropine (abuse)
Amitriptyline (Nortriptyline, Doxepin)
TCA: block catechol reuptake "Prayin ptylers on their tricycles" Thx: prophylaxis; fibromyalgia, depression *takes 2-3 weeks Comp: sedation, weight gain, dry mouth CI: glaucoma, urinary retention, CV disease, asthma
Marijuana *Dronabinol
THC receptor: Gi protein CB1 (motor/cogn), CB2 (immune) "Mary is like a cannabi (cannabinoid)" "Drove into a bin: all this marijuana spilled out" Marinol Cannabinoid Metab: lung absorption to CNS Thx: treat N&V from chemo, appetite stim in AIDS, glaucoma (dec pressure), neuropathic pain Acute: euphoric, inc appetite, relax, tachy/red eyes, laughter, inattention, tremulosness, dec short term memory Chronic: lung damage and cogn impairment No demonstrated phys dependance
Tx plan of T2DM
TIER 1 Step 1: LIfestyle + Metformin Step 2a: L + M + Sulfonurea Step 2b: L + M + Basal Insulin Step 3: L + M + Intensive insulin TIER 2 Step 1: L + M Step 2: L + M + (pioglitazone / GLP-1 agonist) Step 3: L + M + (Sulfonurea / Basal insulin)
Etanercept
TNFa receptor fused to IgG Fc Admin: SubQ weekly
Chemo Drug Combo
Testicular Cancer: BEC & BVC (BEC got his in the testicles with BVC) Bleomycin, etoposide, cisplatin Bleomycin, vinblastine, cisplatin Hodgkin & other lymphoma: MVPP (Hodgkin is our MVP) Mechlorethamine, vincristine, procarbazine, prednisone Hodgkin & soft tissue lymphoma: BVDD (it's soft-it aint BVC today) Bleomycin, Vinblastine, Dacarbazine, Doxorubicin
3**Other Antibiotics** Tetracyclines, macrolides, ketolides, clindamycin, linezolid, streptogramin
Tetracycline: "tetris cycles picture" Tetracycline/Doxycycline/Minocycline Tigecycline ** Macrolide: "Macaroni Lights Pic" (x2) Erythromycin Clarithromycin Azithromycin ** Ketolide: "For macrolide resistant: Tell this helper" Telithromycin ** Clindamycin: "Cleaning mice pic" same MOA as macrolides ** Linezolid: "This line of antibiotics is Zolid against MRSA, VRSA, VRE" ** Streptogramin: "Pristins @ the P site" B: Quinipristin A: Dalfpristin
carvedilol*
The alpha 1 receptor blockade results in vasodilation; the beta 1 blockade prevents a reflex sympathetic increase in heart rate. These effects combine to decrease blood pressure. Also used in treatment of heart failure # Clinical benefit in HF through volume reduction (↓afterload) via ↓ renin production and vasodilation (↓preload) . # contraindicated in severe HF
Intro to toxicology
Therapeutic index = TD50/ED50 or LD50/ED50 MOS = TD1/ED99 (over 1 is safe) MOS = NOEL / Human exposure ADI = NOEL / 1000 (human variation, interspecies, lack chronic data)
Vitamin B1
Thiamine: "The thigh man", "Berries", and "worm mickey corset cop" MC deficiency in routine practice TPP (thiamine pyrophosphate): *ATP and enzymes (branched chain DH etc) *Inc need TPP: glucose infusion, hyperthyroid, pregx Cause: inc demand (pregx), dec abs (elder/alcoholics/polished rice diets) Wet Beri-beri (edema/arteriolar dilatation & dec heart fxn) Dry beri-beri (polyneuritis, muscle wasting) *Wernicke (MOAN), Korsakoff Thx: thiamine (IV/IM), VitB
Q: HTN, reduced to 90 w/ enalapril, ADD:
Thiazide ACE(-) + Thiazide = Ace Thiazide of Beauty (a thing of beauty)
Combination therapy
Thiazide +..... *adrenergic antag *RAS inhibitor *Ca channel antag *Central Alpha2 agonist *Non-receptor sympatholytics *arterial vasodilators
Hydrochlorothiazide
Thiazide diurhetic *Thiazide diuretic: lose hydro (water) chloro (Cl)... as well as Na/K/Mg Block Na reabsorption; loss of Cl, K, Mg, water Tx CHF step 1
Risky Patients due to HTN
Thiazide: first choice of treatment Thiazides & B-blocker: data shows decreased mortality and morbidity
General Anesthesia: IV Amnesia
Thiopental: "BARBer- thy pent house puts me to sleep" (Methohexital, thiamylal) Diazepam: "Makes your DAYZ sure seem happy" Midazolam: "In MI DAYZ, used a watch for hypnosis" (Lorazepam) Ketamine: "Low bp: keep this in mind" Etomidate: "Intimidated by low bp and MI risk?" Propofol: "MJ: drug made this pro to fall"
bethanechol*
This agent has greater affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
timolol*
This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
sarin*
This organophosphate nerve gas is a suicide inhibitor of AChE and can be reversed with pralidoxime.
Principle of Cancer Chemo
Tobacco and Diet: 65% of causes of cx Colon cx: APC, K-RAS, DCC, p53, others Protoconcogenes 10^8 xray, 10^9 palpate, 10^12 (1kg) Fast growth: burkitt, choriocarc, ALL, hodgkin, testicular Slow: colon, lung Growth fraction S phase: anti-metabolites G2 phase: topoisomerase & bleomycin
tolterodine*
Tolterodine is used to relieve urinary difficulties, including frequent urination and inability to control urination. Tolterodine is in a class of medications called antimuscarinics. It works by preventing bladder contraction.
Inhalants
Toluene Nitrous Oxide Amyl Nitrate euphoria, LOC and impaired judgement, (benzene,toluene): bone marrow depression, periph nerve, liver, kidney damage
Serotonin
Tones down your worries
echothiphate*
Trade Name: Phospholine Half-life: very long Mechanism: Irreversible AChE inhibitor Elimination: unkown Rx: Open angle glaucoma
Drug Resistance
Transport: MTX, melphalan, nitro mustard, cARA MTX: transport, inc dhfr, dec affinity, dec polyglutamation
metaprterenol*
Treat asthma, COPD
physostigmine*
Treatment of atropine overdose and glaucoma (because lipid soluable). Enters the CNS rapidly and has a stimulant effect, which may lead to convulsions
Parkinsonism
Tremor, bradykinesia, rigid 5 days to several weeks Tx: As for acute dystonia
Antidepressants (1)
Tricyclic: pramine, tyline = "prayin for the ptiline" - prayin tilers riding tricycles *Imipramine, amitriptyline, Nortriptyline, (droxepin, trimipramine), Desipramine, (protriptyline) *Amoxapine: zaps DA receptor/NE reuptake *Clomipramine: pramine closes only 5HT SSRI: "the xetines and sertralines increase the amount of Sero time" *Fuoxetine, Sertraline, Paroxetine *(Fluvoxamine, escitalopram, citalopram"
Sumatriptan Zolmitriptan (Naratriptan, rizatriptan, eletriptan, frovatriptan)
Triptan: (+) 5HT1B/1D receptor "Trips are soothing--serotonin" "Suma is like a summer season--comes and goes" "Zolmi makes the CNS his homi" Action: contracts carotids, blocks pain registration Thx: acute abortive tx Suma: HA reoccurs 40% in 24 hrs Zolmi: cross BBB; dorsal raphe nuc central action Admin: tablet, sc, nasal *6 tx days/mo. or 2/wk *short half life Comp: triptan sensation (paresthesia, flushing, throat +/- chest tightness) CI: vascular disease, HTN
HTN: Adrenergic blockers
Tx HTN, CHF *Atenolol: give you a ten if you -B#1 *Propranolol: pan beta blocker *Prazosin: preeze losin arterials (-A1) *Carvedilol: carves out -A1, B1/2 *Clonidine: Cloni dines to give neg feedback (+A2) Guanethidine: Guan makes you yawn (- adren)
HTN: RAAS
Tx HTN, CHF / Comp: hyperK and watch pregnancy *Enalapril: is our ACE (laps everyone) *Losartan: ARB--losers can't find receptor *Aliskiren: cures our kidney from rennin
HTN: Ca Blocker and arterial relaxants
Tx HTN, CHF, (baldness) *Verapamil: very important Pam: heart/art *Nifedipine: dip nife in milk *Hydralazine: hides how release N.O. *Minoxidil: minox Kocks up the hair
ADH Antagonists
Tx SIADH, hyponatremia Conivaptan: evaporates vasopressin effect; Coni likes both Tolvaptan: evap vaso effect, told you 2 Demeclocycline: Demon kidney cycles all the water back Lithium: lit up the fire and burned away cAMP
Alpha 1 proteinase inhibitor DNAse (break up mucus)
Tx emphysema
ADH Agonists
Tx pit diabetes inspidus, GI bleed (esoph, divert), nocturnal enuresis DI w/ clofibrate & chlorpropamide Desmopressin: Vaso for long Duration Tannin Vasopressin: Tannin for short time Lysine vasopressin: Like tannin, Long durat
Propanolol
Tx thyroid storm sx (HR, tachyC, tremor) Contra in pregx
N/V in Preg
Tx: Vit B6 Block H1 (diphenhydramine) Block D2 (metaclopromaide) Block 5HT3
Ethinyl estradiol Mestranol (its prodrug)
Tx: Contraceptives, dysmenorrhea, anemia *suppress FSH Same estrogen effects (HDL etc.) & CI Combo w/ progesterone for effectiveness
Thyroid storm
Tx: You're gonna PPP! PTU, Potassium Iodide, Propanolol *also glucocorticoids (block peripheral prod & general support) *don't give NSAIDs (can displace T3/4)
(Levetiracetam)
Unknown MOA New AED Ind: adjunct in refractory partial seizures Comp: mild adverse rxns
Ozone (O3)
Urban smog (NO2 + O2 + uv) Chronic: inflamm, edema, bronchial constriction, pulm vascular changes *asthma incidence
Pegloticase
Uricase recombinant "Uricase: in case other drugs don't break down urate" Exogenous enzyme oxidizes uric acid to alltoin (highly water soluble) Therapy: acute reduction of serum urate Ind: treat gout if unresponsive to other tx IV infusion Side fx: infusion related effect (urticaria to erythema)
Sulfinpyrazone
Uricosuric: (-) urate transport "Sulfin is fillin those holes: no urate enters the zone" Metabolite of phenylbutazone, strong acid Inc urate excretion Ind: chronic gout w/ hypersensitivity to probenecid Comp: more GI, but less hypersensitivity **antithrombotic properties
Probenecid
Uricosuric: (-) urate transport (low dose: more effect on secretion; high dose: no reabsorption) "Probene prohibits urate transport" High dose: increase urate excretion (dec reabsorption) Low dose: decrease excretion Long term therapy Ind: chronic gout or 1-shot treatment of umcomplicated gonococcal + long acting penicillin (blocks pen. secretion) PO Comp: GI, kidney stones, hypersensitive **Low dose: paradoxical effect (dec excret) **aspirin prevents actions on urate **additive effect with sulfinpyrazone **antag diuretics
Procarbazine
Use in MVPP: Hodg/Non hodg lymphoma Same as Dacarbazine (diazomethane, alkylate) Pro because it penetrates CSF & because no cross resistance with other alkylating agents Tox: inhibits MAO (avoid tyramine)-HTN
Unithiol
Use: Acute Inorg Hg and As Water soluble form of dimercaprol Infreq s/e: hypersensitivity *rapid IV: vasodilate & hypoTN
Prednisone Prednisolone (11betaOH converts Pred to this)
Use: pituitary ACTH def, Cushing's disease, replacement thx LIver 11-betaOH: prednisone to prednisolone Use: arthritis, allx, MS, lupus, cx S/E: aldosterone like effects, gluconeogenic effects, HPA suppression, iatrogenic Cushings Withdraw: tired, dec appretite, weak, nausea
Tigecycline
VERY broad Use: MRSA, VRE (& tetracycline resistant bacteria) IV only Safe for renal dysfxn
Clinical Pharmacokinetics
Vd = dose(mg) / concentration(mg/L) *when two compartment, Co is theoretical -- ln[D] = f(t) Loading dose = [Drug] x Vd / F CL = elimination rate / [Drug]plasma *gives amount of fluid completely cleared
Monoctanoin
Vegetable oil, common bile duct direct injxn for small stones
Q: HTN, anginal attacks
Verapamil (heart and sm muscle Ca blocker)
Q: mild ischemia, HTN, dec CO & BP
Verapamil (heart and vasc Ca channel blocker)
*sildenafil
Viagra. Blocks phosphodiesterase that splits cGMP; enhanced smooth muscle relaxation causes erection. Important interaction with nitrates.
Vitamin D
Vit D3 (Cholecalciferol) 25-OH Vit D3 (Calcifidiol) 1,25-OH2 Vit D3 (Calcitrol)
New AED
Voltage/use dep Na blockade Lamotrigene: makes the used Na lame (Gabapentin, topriamate, felbamate, tiagabine, leveitracetam, zonisamide)
Fluoride
With Ca: stim bone formation Dec frax by 35% Tx osteoporosis Bone has less strength (but more mass) than normal bone
Methanol
Wood alcohol "Methanol is mal alcohol" MetOH--> OH DH-->formaldehyde--> formate Acute: blur vision/blind, seizure/coma, acidosis *necrosis: putamine, claustra, retinal ganglion cells Tx: supportive, EtOH
Atropine*
a poisonous crystalline alkaloid extracted from the nightshade family, Muscarinic cholinoceptor blocker prototype: lipid-soluble, CNS effects. Tox: "red as a beet, dry as a bone, blind as a bat, mad as a hatter," urinary retention, mydriasis.
epinephrin*
adrenalin; increases heart rate and blood pressure, dilates bronchial tubes Increased HR, Greater Cardiac Muscle Contractility and diverts blood to skeletal Muscles
Vitamin E
alpha tocopherol: "Viking Electric" Anti-ox (along w/ E,C,beta carotene); prevent atherosclerosis **prevent oxidation of unsat lipids & block oxidation of cholesterol (to oxy-sterols) Prevent hemolysis and neural damage!!
Adrenergic Receptors
alpha1: smooth muscle contraction Gq alpha2: inhibit neurotrans & cardiac Gi beta 1: heart contraction Gs beta2: smooth muscle relaxation Gs D1: Gs D2: Gi
*losartan
angiotensin 2 receptor blocker / antihypertensive (HTN, diabetic nephropathy in DM 2, prev of CVA in HTN w/ LVH) COZAAR
Muscarinic block receptor
atropine overdose is: "hot as a hare, blind as a bat, dry as a bone, red as a beet, and mad as a hatter" (opposite of SLUDGE); urinary retention, constipation, memory dysfunction, tachycardia, narrow-angle glaucoma
alpha-latrotoxin*
black widow spider venom - enters nerve terminal and interferes with exocytosis to promote massive irreversible release and depletion of Ach - initial contractions followed by paralysis
*spironolactone
blocks aldosterone receptors; binds with receptors for some steroid hormones; used for hypertension and heart failure; is potassium sparing--does not deplete potassium like most Adverse Effects: hyperkalemia, gynecomastia, menstrual irregularities, impotence, hirsutism, and deepening of the voice.
*diltiazem
calcium channel blocker / antihypertensive / antiangina / antiarrhythmic (HTN, angina pectoris, vasospastic angina, A-fib, A-flutter)
CHF step 1
decrease afterload: ACE inhibitor + ARB + Aldosterone Inh + diuretics ACE: enalapril AngRB: losartan Aldosterone: Spironolactone Loop diuretic: Furosemide Thiazide diuretic: hydrochlorozthiazide
RESERPINE
deplete NE *Sorry, this is no longer RESERVED for amines no amine transport system for high NE Tx HTN
*hyrdochlorothiazide
diuretic that works in the distal tubule short acting
amphetamine*
drugs that stimulate neural activity, causing speeded-up body functions and associated energy and mood changes
botulinum toxin*
enters nerve terminal and interferes with docking of synaptic vesicles and inhibits exocytosis irreversibly - failure of Ach release causes paralysis. Can be used for reduction of saliva in Parkinson's, for pain relief, spasticity hemifacial spasm, focal dystonia
*tadalafil
erectile disfunction agent / vasodilator (CIALIS: ED, BPH; ADCIRCA: PAH)
Acute dystonia
exaggerated posture of head/neck/jaw 1st week of therapy Tx: reduce dose; central acting anticholinergics (benztropine, biperdien, diphenhydramine), benzodiazapine
TYRAMINE
indirect A1,2 *Tyson tore off some of mine cheese; now tearing due to hypertensive crisis Increase NE release; in cheese and wine
Digoxin/Digitalis
inhibit Na/K ATPase *Dig in with this toxin Decrease Ca efflux; incrase contractility Tx CHF step 3 (add digoxin) -toxic if patient is hypokalemic OR hypercalcemic -careful with diuretics, calcium channel blockers, beta blockers
formoterol*
long acting B2 agonist
Q: HTN, edema
loop diuretic (eg metolazone)
d-tubocurarine*
non-depolarizing neuromuscular blocker from plant alkaloid ("arrow poison")
pindolol*
nonselective beta blockerPartial agonist (ISA): means less change in cardiac output and heart rate (less loss of exercise tolerance)ISA- inhibits endogenous response in high levels of neurotransmitter, but creates a response in low levels of endogenous neurotransmitter
*rivaroxaban
oral drug that directly blocks Xa - does not require monitoring - not effected by food or drugs - dosing stable across age groups * just as good/better than LMWH in DVT prevention WITHOUT increased risk of bleeding - effective in stroke prevention in a-fib and therapy of DVT
Propranolol
pan beta blocker *Pro on a plan takes this to reduce anxiety Dec BP & afterload Tx CHF step 2
*doxazosin
peripherally acting antiadrenergic / antihypertensive (HTN; outflow obstruction r/t BPH) CARDURA
tolazoline*
reversible alpha antagonist- vasodilator
Chloroquine
slow acting; dec chemotaxis *free radical trap Ind: RA,lupus, unresponsive NSAIDs
nicotine*
the addictive drug found in tobacco that speeds the heartbeat, raises blood pressure, and causes dizziness and upset stomach
*nitroglycerine
vasodilator used for chest pain; mechanism is a quick reduction in preload and afterload which reduces cardiac workload
Review
x
prazosin*
• Adrenergic antagonist • Alpha1-selective • Competitive • Used to treat HTN and urinary obstruction due to BPH • Highly selective for A1, so little tachycardia results from treatment • Orally-effective • Duration = 12 hrs
doxazosin*
• Adrenergic antagonist • Alpha1-selective • Used to treat urinary obstruction due to BPH
terazosin*
• Adrenergic antagonist • Alpha1-selective • Used to treat urinary obstruction due to BPH
methacholine*
• Cholinergic agonist (synthetic choline ester) • CH3 group decreases N receptor activity • Used to test function of muscarinic receptors, to slow HR, and to test for bronchial hyperreactivity • Decreases arterial pressure • T 1/2 = 10-15 min
trimethaphan*
• Cholinergic antagonist with a positively-charged sulfur group • Nicotinic-selective (ganglionic blockage) • Non-depolarizing (competitive) • Administered IV in the OR to decrease bleeding • Adverse effects: excess hypotension (antagonizes vasopressor action of nicotine), possible brain anoxia • Duration = minutes
atracurium*
• Cholinergic antagonist, benzylisoquinoline • NM blockade • Non-depolarizing (competitive) • No effect on M or N1 receptors • Some histamine release
Epinephrine
(+)A/B *Epi (-) aq humor secretion & (+) trabecular outflow Tx open angle glaucoma
Drugs for Open-angle glaucoma
(+)A/B: epinephrine (-)Carb Anh: dorzolamide Prostamide: Bimatoprost Prostaglandin: Latanoprost (-)B: Timolol (+)A: Brimonidine +NN, NM, M1-5: carbachol Irrev AChEI: Echothiophate
Brimonidine
(+)A2 *Bri attract the alpha male w/ money to dine less sympathetic--constrict? (-) secretion; (+) uveoscleral outflow Tx open angle
Cerivastatin
(-)HMG-CoA reductase *Statin; no long in Cervice Removed from market Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol, CAD
*nifedipine
Calcium channel blocker prototype: vasoselective (less cardiac depression); used in angina, HTN. Tox: constipation, headache
*ezetimibe
This drug inhibits intestinal cholesterol absorption by jejunal enterocytes by targeting NPC1L1 to decrease total cholesterol and LDL
*fenofibrate
Tricor Hyperlipidemia Enhances clearance of triglyceride-rich particles
*colesvelam
bile acid sequestrant dyslipidemia drug
*tissue plasminogen activator
converts PLASMINOGEN to PLASMIN in the presence of fibrin ,may lose fibrin specificity at high doses which disolves clots(Like in the case of a heart attck) and bleeding is common
*prazosin
• Adrenergic antagonist • Alpha1-selective • Competitive • Used to treat HTN and urinary obstruction due to BPH • Highly selective for A1, so little tachycardia results from treatment • Orally-effective • Duration = 12 hrs
*propranolol
Nonselective beta−blocker prototype: local anesthetic action but no partial agonist effect. Used in HTN, angina, arrhythmias, migraine, hyperthyroidism, tremor. Tox: asthma, AV block, CHF
*Warfarin
Oral anticoagulant prototype: causes synthesis of nonfunctional versions of the vitamin K− dependent clotting factors (II, VII, IX, X). Tox: bleeding, teratogenic. Antidote: vitamin K, fresh plasma
Mannitol
Osmotic agent *Man absorbs it all--even from the eye Reduce aq humor Tx acute glaucoma (IV)
Glycerin
Osmotic agent *glyc you're in--brings it all in Reduce aq humor Tx acute glaucoma (PO)
Nitroprusside
Nitrates *Nitrate used in pressing times--HTN crisis Potent vasodilator Tx HTN crisis and acute HF
Isosorbide Dinitrate
Nitrates (sugar) *Don't die with nitrates in hand--take prophylaxis Dec pre and afterload Tx angina prophylaxis, CHF
Mibefradil
(-)T/L Ca channel; Ca & Na antagonist *Riddle me this: MAYBE you can't Vasodilate (periph and coronary)--MAYBE both Tx HTN, angina
*eptifibatide
Reversible GPIIb-IIIa inhibitor, peptide inhibition of platelet aggregation, used in treatment of acute MI Cyclic heptapeptide designed from pit viper venom peptide, barbourin Potential for major increased bleeding
Colesevelam
Bind intestine bile acid (resin) *choles tears out the bile to lower cholesterol Often combo with statin/niacin Tx: lower LDL, inc HDL
Drugs for Acute glaucoma (closed angle)
**Acute: hurts--I have to go PP Osmotic agent: mannitol, glycerin (-)AChE: physostigmine (+)M3: pilocarpine
Pilocarpine
(+)M3 *Pile on the tears Constrict pupil Inc aq humor trabecular OUTFLOW Tx acute glaucoma, limited open angle
Carbachol
(+)NN, NM, M1-5 *Carbachol keeps it all (ACh longer lasting) Dec intraocular pressure Tx open-angle glaucoma
Niacin, Nicotinic Acid
(-) lipolysis & liver TG synth *Nice to sin eating 10 cheeseburgers a day--but need to block the lipolysis Dec LDL/VLDL, Inc HDL Tx hyperchol, hyperlip, hyperTG
Probucol
(-) oxidation of LDL & uptake to macrophage *Pro BUCK off the LDL Lower LDL, lower HDL Tx after other drugs--hyperchol, hyperlipid
Physostigmine
(-)AChE *Sticks it to AChE; phizzles through BBB Pupillary constriction Inc aq hum trabecular OUTFLOW Tx acute glaucoma (last resort)
Propranolol
(-)B1&2 *-olol (beta block) Pro on a plan takes this to reduce anxiety Lower BP by dec C.O. Tx HTN, arrhythmia, angina, tremor, migraine prophylaxis
Timolol
(-)B1/2 *-olol (beta antag) Inh aq humor secretion (adrenergic response) Tx open angle glaucoma; prevent loss of retinal cells
Acetylsalicylic acid
(-)COX irreversible block PLT produced TXA2 (no real effect on endothelial PGI2) *Aspirin: blocks the COX Chronic inhib of PLT aggregation, arterial side Tx CAD, risk MI/TIA/CVA, damaged endothelial, arterial prsthesis
Felodipine
(-)Ca channel, cardio sparing *Dip my knife and fellow in milk (cut the calcium) Tx HTN, agina (spasm)
Nifedipine
(-)Ca channel; cardio sparing *Dip my knife in milk (cut the calcium) Dec vascular tone (less heart effect) Tx HTN, angina (spasm)
Dorzolamide
(-)Carbonic anhydrase *Doors close on the aq humor secretion (-) aq humor secretion Tx open angle glaucoma
Fluvastatin
(-)HMG-CoA reductase *Statin Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol, CAD
Pravastatin
(-)HMG-CoA reductase *Statin Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol, CAD
Simvastatin
(-)HMG-CoA reductase *Statin Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol/CAD; single daily dose
Lovastatin
(-)HMG-CoA reductase *Statin Increase LDL catabolism, block mevalonate production (dec LDL, inc HDL) Tx hypercholesterol, CAD
Atorvastatin
(-)HMG-CoA reductase *Statin Most commonly prescribed Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol, CAD
Pitavastatin
(-)HMG-CoA reductase / superstatin *Statin / superstatin: Pitava! Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol, CAD
Rosuvastatin
(-)HMG-CoA reductase / superstatin *Statin; superstatin: makes it to the Rose bowl Increase LDL catabolism, block mevalonate production (dec LDL) Tx hypercholesterol, CAD
Verapamil
(-)L-type Ca channel *Very important PAM: DIL me TIA some of ZEM pills Decrease vascular tone & HR (but get baroreceptor reflex) Tx HTN, angina (spasm)
Clopidogrel
(-)PLT aggreg (-)ADP induction of GpIIb:IIIa receptor (block PLT aggreg) *Clopi blocks the GpIIb via blocking ADP *Plavix Chronic inhib of PLT aggreg, areterial side Tx thrombosis prophylaxis during PCI, stroke prophylaxis, MI, ACS
Ticlopidine
(-)PLT aggreg (-)ADP induction of GpIIb:IIIa receptor (block PLT aggreg) *Tickled away the ADP (pee'd away the receptor) Chronic inhib of PLT aggregation, arterial side Tx TIA, stroke
Bepridil
(-)T/L Ca channel; Ca & Na antagonist *Riddle me this Bepril: a lil' Ca & Na? Vasodilate, increase refractoriness (Be=make it BE late) Tx Angina, arrhythmia
Prazosin
(-)alpha1 *Preeze loosin your arterial (Prazosin, Doxazosin, Terazosin) Arterial>venous dilatation Tx HTN, BPH
Terazosin
(-)alpha1 *Preeze loosin your arterial (Prazosin, Doxazosin, Terazosin) Arterial>venous dilation Tx HTN, LONG ACTING
Doxazosin
(-)alpha1 *Preeze loosin your arterial (Prazosin, Doxazosin, Terazosin) *Does Losin AND drop LDL Arterial>venous dilation Tx HTN, BPH, lower LDL
*marine oils
-EPA and DHA (take place of arachidonic acid) *EPA is converted to TxA3 (a weaker platelet aggregator and activator) -the TxA2:PGI2 balance is tipped toward PGI2 (vasodilation and inhibition of platelet activation) Lipoxins, Resolvins, Protectins, and Maresins = all marine oil-derived mediators that possess potent anti-inflammatory and pro-resolving actions
*mibefradil
A calcium channel blocker that was briefly introduced as an agent that blocked the "T"-type channel, in addition to "L"-type block. The "T"-type is in high level in the SA node. It tended to cause excess bradycardia (and other problems) and was removed from the market quickly. The utility of a "T"-type blocker is now in question.
*heparin
Anticoagulant: large polymeric molecule with activity against thrombin and factor X. Rapid onset, in vitro and in vivo anticoagulation. Tox: bleeding. Antidote: protamine. See also Enoxaparin.
*lovastatin
Antilipemic HMG−CoA reductase inhibitor prototype: acts in liver to reduce synthesis of cholesterol. Other statins: atorvastatin, fluvastatin, pravastatin, simvastatin. Tox: liver damage (elevated enzymes), muscle damage
*niacin
Antilipemic: reduces release of VLDL from liver into circulation. Lowers LDL cholesterol and triglycerides and raises HDL cholesterol. Tox: flushing, pruritus, liver dysfunction, increased risk of myopathy when combined with statins.
*clofibrate
Cholesterol-lowering agent (fibric acid) • Use: clears chylomicrons and VLDL quickly, lowers triglycerides (VLDL) and raises HDL cholesteral • Mech: increases the activity of lipoprotein lipase • SFX: GI (nausea, hepatic, myositis; worse with gemfibrozil and lovastatin)
*probucol
Cholesterol-lowering agent (fibric acid) • Use: modest cholesterol reduction • Mech: increases LDL catabolism and blocks LDL oxidation • SFX: prolongs QT interval (ventricular arrhythmias) and lowers HDL
Marine Oils
Compete with arachidonate for COX, lipooxygenase; inhibit hepatic TG synth *Marine oils on the COAST like COX; block TG synth (hepatic) Decrease TG Tx Type IV
*urokinase
MOA: human thrombolytic enzyme synthesized by kidney -> directly converts plasminogen to plasmin (non-fibrin selective) 1: lyse already-formed clots AE: bleeding (especially when there are physiologically appropriate fibrin clots USE: treat acute MI when angioplasty (PCI) is not readily available, approved for lysis of pulmonary emboli
*abciximab
Monoclonal antibody to the platelet glycoprotein IIb/IIIa receptor that binds fibrin. Used to prevent clotting after coronary angioplasty and in acute coronary syndrome. Eptifibatide and tirofiban act similarly
*amyl nitrate
NO donor. Used to treat anginas and cyanide poisoning by inducing formation of methemoglobin which sequesters cyanide. Also used as illegal inhalant drug that produces a brief euphoria.
Amyl nitrate
Nitrate *Does Amy need nitrates (quick inhale test) Dx angina, murmur
Nitroglycerine
Nitrate *NITRO lets the blood FLOW Vasodilate, dec preload, dec O2 demand/Cardiac Output, coronary artery Tx angina
Latanoprost
Prostaglandin analog *O-prost opens the outflow *-Prost = prostaglandin INC uveoslceral outflow (remodel ciliary body)
Bimatoprost
Prostamide (prostanoid F2a analog) *O-prost opens the outflow *-prost is a mide because it's bi (does two outflow tracks) INC trabecular and oveoscleral outlfow Tx open angle glaucoma
*streptokinase
Thrombolytic. Protein from streptococci that accelerates plasminogen-to-plasmin conversion. Increase pT and pTT. Uses: Early MI, stroke. Tox: bleeding, allergy. Tox treated with Aminocaproic acid.
*felodipine
Vasoselective Ca blockers • Use: hypertension esp. low renin • Mech: - Block voltage sensitive L type Ca2+ channels (SM relaxes) - Relax VSM and decrease peripheral resistance - Decrease MAP-reflex increase sympathetic discharge and HR - Negative chronotropic • Toxicity: - Contraindicated in heart failure (edema) - Depresses A-V conduction and contractility - Headache
*isosorbide dinitrate
angina prophylaxis
*fondaparinux
anticoagulant (prevention of DVT & PE; SQ, short acting within minutes, more predictable dosing = blood tests (platelet count) needed less frequently than heparin, home tx ok) ARIXTRA