Pharmacology test 2: units 3&4: chapters (18,19,20,21)(22,23,24,25,26,27,29)

detrol

(Tolterodine) Urinary bladder modifier -leaky bladder

Methyldopa (Aldomet)

*alpha 2 agonists* *side effects*: -drowsiness; -dizziness; -bradycardia; -hemolytic anemia; -fever; -orthostatic hypotension

adrenergic drugs adverse effects

*restlessness, excitement, headache, insomnia, euphoria* CV: chest pain, vasoconstriction, hypertension, reflexive bradicardia, palpitation, dysrhythmias -anorexia, dry mouth, vomiting

Cholinergic Blocking Drugs Cardiac effects:

Increases heart rate in bradycardia Meds: Atropine

Enalapril (Vasotec)

Only ACE inhibitor available in both oral and parenteral preparations. Enalapril intravenous (IV) does not require cardiac monitoring Oral enalapril: prodrug Improves patient's chances of survival after an MI Reduces the incidence of HF

Norepinephrine (levophed)

Stimulates alpha-adrenergic receptors Causes vasoconstriction Direct-stimulating beta-adrenergic effects on the heart (beta1-adrenergic receptors) No stimulation to beta2-adrenergic receptors of the lung Treatment of hypotension and shock Administered by continuous infusion

cholinergic Drugs:

These drugs change the genetic make up of a cell by allowing Ca+ and Na+ to flow into cell and it then depolarizes and stimulates organ

Adrenergic Blocking Drugs beta Blockers Adverse effects:

cardiovascular: atrioventricular block, bradycardia, heart failure -central nervous: dizziness, depression, fatigue, drowsiness, unusual dreams -gastrointestinal: nausea, vomiting, constipation, diarrhea -Hematologic: agranulocytosis, thrombocytopenia -metabolic: delayed hypoglycemia recovery, masked symptoms of hypoglycemia, hyperlipdemia -Other: impotence, alopecia, bronchospasm, wheezing, dry mouth

Adrenergic Blocking Drugs Alpha Blockers Adverse effects:

cardiovascular: palpitations, orthostatic hypertension, tachycardia, edema, chest pain -Central nervous: dizziness, headache, anxiety, depression, weakness, numbness, fatigue -Gastrointestinal: nausea, vomiting, diarrhea, constipation, abdominal pain -other adverse effects: incontinence, dry mouth, pharyngitis.

what do high doses of epinephrine do?

causes vasoconstriction elevates blood pressure

clonidine (catapres)

centrally acting adrenergic drug-alpha 2 agonist decreases blood pressure -helps with opioid withdrawal -many routes of admin -dont discontinue quickly

angina pectoris

chest pain resulting from a low supply of blood oxygen to the heart. -heart muscles ache

Atropine

cholinergic antagonist antimuscarinic -causes increased heart rate, also used as an antidote to treat bradycardia and ventricular asystole --reduce salivation and GI secretions -contraindicated in those with angle closure glaucoma, advanced hepatic/renal dysfunction, hiatal hernia associated with reflux esophagitis, intestinal atony, obstructive GI or GU conditions and severe ulcerative colitis -injectible, oral, ophthalmic forms

Pyridostigmine (Mestinon)

cholinergic drug increase acetylcholine -improve muscle strength and symptomatic treatment of myasthenia gravis -contraindications: drug allergy, asthma, gangrene, hyperthyroidism, cardiovascular disease, mechanical destruction of GI or GU tract -Adverse effects: increased salvation, GI upset -oral and injectable forms

cholinergic adverse effects:

consequence of overstimulation of the PSNS. CV effects: bradycardia or tachycardia, hypotension or hypertension, syncope, conduction abnormalities -headache, dizziness, convulsions, ataxia -GI: cramps, *increased secretions*, vomiting, diarrhea, nausea respiratory: *increased bronchial secretions*, bronchospasm -*other: lacrimation, sweating, salivations*

Scopolamine

prevent motion sickness -transdermal patch -may cause drowsiness, dry mouth, and blurred vision -dont use with CNS depressants, alcohol due to increased sedation -can be given sub cut, IM, IV, ocular, oral - same contraindications as atropine

nasal decongestants drugs:

reduce blood flow and decrease congestion -ephedrine (nose spray)

*Cholinergic Blocking Drugs GI effects

reduce gastric secretions -Meds:Glycopyrrolate/Robinul

*Adrenergic Blocking Drugs* Bladder::

reduce smooth muscle contraction -Meds: Tamsulosin (prostate enlargement), urinary blockage-may be used to help with kidney stones

peripheral nervous system

somatic nervous system (skeletal muscles) autonomic Nervous sytem -connects the central nervous system to every part of the body

BiDil

specifically indicated as an adjunct for treatment of HF in african american patients

centrally acting adrenergic drugs MOA alpha 2 agonist

stimulate alpha 2 adrenergic receptors in the brain, which are unique in that they reduce sympathetic outflow and reduce blood pressure -alpha 2 decrease sympathetic stimulation and norepinephrine -reduce renin activity in the kidneys -results in a decreased bp

nitrates and nitrites

sublingual*, IV*, transligual sprays*, chewable tablets, transdermal patches*, oral capsules/tablets, ointments * bypass the liver and the first pass effect -these drugs cause vasodilation because of relaxation of smooth muscles, they have a potent dialing effect on the coronary arteries -results in giving O2 to ischemic myocardial tissues

oxybutine (ditropan)

synthetic antimuscarinic drug used for the treatment of an overactive bladder -antispasmodic for neurogenic bladder associated with spina bifida and spinal cord injuries -contraindications: drug allergy, urinary or gastric retention, and uncontrolled angle closure glaucoma -oral use, patch

contraindications of beta blockers

systolic HF serious conduction disturbances -use caution with bronchial asthma, diabetes mellitus, peripheral vascular disease

cholinergic drugs work on what nervous system/

the Parasympathetic nervous system INCREASE SECRETIONS

parasympathetic (cholinergic) ACh and Sympathetic (adrenergic) NE are a part of what nervous system?

the autonomic nervous system

sympathetic nervous system (adrenergic)

the division of the autonomic nervous system that arouses the body, mobilizing its energy in stressful situations -FIGHT OR FLIGHT RESPONSE

parasympathetic nervous system (cholinergic)

the division of the autonomic nervous system that calms the body, conserving its energy -digestion, urination, defecation, sexual arousal, salvation, tear production -REST AND DIGEST

cholinergic drugs stimulate:

the intestine an bladder which result in increased gastric secretions, GI motility and urinary frequency

Sodium Nitroprusside and IV diazoxide is only used for

the management of hypertensive emergencies

cholinergic drugs work on

the parasympathetic nervous system -stimulates saliva, slows heart beat, constrict bronchi, stimulates peristalsis and secretion, stimulates release of bile, contracts bladder

adrenergic drugs work on

the sympathetic nervous system -they stimulate the SNS -dilates pupils, accelerates heart rate, dilates bronchi (take in more o2), inhibits peristalsis, conversion of glycogen to glucose (more energy), secretion of adrenaline and noradrenaline, inhibits bladder constriction

Adrenergic Blocking Drugs (adrenergic Antagonist)

these drugs INTERRUPT stimulation of the SNS -adrenergic blockade leads to vasodilation, reduced blood pressure, pupillary constriction and smooth muscle tone in the organs such as bladder and prostate.

CHOLINERGIC CRISIS

too much medication -watch out for fertilizers Monitor cholinergic drugs closely to prevent cholinergic crisis from over medication -Abdominal cramping -Flushing of skin -Nausea/Vomiting -Salivation progressing to circulatory hypotension -Hypotension -Cardiac Arrest

Calcium channel blockers

treatment of hypertension and angina -causes smooth muscle relaxation by blocking the binding of calcium to its receptors thereby preventing contraction and lowering BP -used with angina, dysrhythmias, hypertension, migraine, raynauds, present the cerebral artery spasms after subarachnoid hemorrhage

Cholinergic Blocking Drugs near effects:

treats parkinson's tremors and muscle rigidity

cardiovascular adrenergic drugs:

vasoconstricts heart during shock -meds: dobutamine, dopamine, epinephrine (allergic reactions), norepinephrine, phenylephrine.

ARBs

well tolerated -no dry cough -primarily affect vascular smooth muscle and the adrenal gland -slectively bock the binding of A II to the type 1 A II receptors in the tissues -ARBs block vasoconstriction and the secretion of aldosterone

can centrally acting adrenergic drugs be used with pregnancy?

yes

Dual-action alpha1 and beta receptor blockers

~Reduce heart rate (beta1 receptor blockade) ~Cause vasodilation (alpha1 receptor blockade) carvedilol (Coreg) and labetalol ~Result in decreased blood pressure -widely used -used in hypertension, HF in conjunction with digoxin, diuretics, and ACE inhibitors

Acetylcholine

is a neurotransmitter (a chemical released by nerve cells to send signals to other cells) and it is used in the autonomic nervous system

Cholinergic drug effects on musculoskeletal: ex drugs

improve muscle strength like in myasthenia gravis (chewing, smiling) Drugs include: pyridostigmine (mestinon)

Cholinergic drugs effects on neruo

increase acetylcholine (alzheimers pts. have decreased levels of acetylcholine so it may help with alzheimers)

cholinergic (parasympathetic) SLUDGE

increased Salivation and sweating increased Lacrimation increased Urinary incontinence increased Diarrhea increased GI cramps increased Emesis

cholinergic drug effects on the bladder: ex drugs:

increases bladder tone and motility: drugs: Bethanechol (Urecholine)-helps you urinate

cholinergic Drugs: effects on GI

increases gastric motility and gastric secretion

dobutamine (Dobutrex)

Beta 1 selective vasoactive adrenergic drug that is similar to the naturally occurring dopamine. -increases cardiac output by increasing contractility which increases the stroke volume, ESP in patients with heart failure -only available by IV and given continuous -onset of action less than 2 minutes -duration of action: less than 10 min

Donepezil (Aricept)

-Cholinesterase inhibitor that works centrally in the brain to increase levels of acetylcholine by inhibiting acetylcholinesterase. -Used in the treatment of mild to moderate alzheimer's. -Contraindications: allergy -Adverse effects normally mild and resolve on their own. Can often be avoided by careful dose titration. Include: GI upset, drowsiness, dizziness, insomnia, muscle cramps. -Cardiovascular effects: bradycardia, syncope, hypotension w/ reflex tachycardia, or HTN. -Interacting drugs include: anticholinergics (counteract donepezil effects) and NSAIDS. -oral use

Cholinergic Blocking adverse effects:

-decreased secretions, constipation, urinary retention -CV: increased heart rate, dysrhythmias (tachycardia, palpitations) -Central nervous: excitations, restlessness, irritability, disorientation, ataxia, delirium, drowsiness, sedation, hallucination, confusion -Eye: dilated pupils (blurriness), increased intraocular pressure -GI: decreased salivation, gastric secretions and motility -GU: urinary region -Glandular: decreased sweating -respiratory: decreased bronchial secretions

autonomic nervous system

A subdivision of the peripheral nervous system. Controls involuntary activity of visceral muscles and internal organs and glands. -influences the INTERNAL organs, heart rate, digestion, respiratory rate, pupillary response, urination, sexual arousal

Captopril (Capoten)

ACE inhibitor -prevention of ventricular remodeling after MI, reduce risk of HF after MI -shortest half life- give 3-4 times a day

what are the -pril drugs

ACE inhibitors

what drug causes dry non-productive cough?

ACE inhibitors

contraindications of nitrates

Allergy Severe anemia Head trauma Pregnancy and lactation closed angle glaucoma hypotension *use of the erectile dysfunction drugs*

what do low doses of epinephrine do?

increasing the force of contraction and heart rate. used to treat acute asthma and anaphylactic shock

Tamsulosin (Flomax)

Alpha-1 blocker; relaxes smooth muscle in the bladder neck and prostate to decrease urinary outflow obstruction in men with BPH; bladder empties for effectively so they don't have to pee as often; can also be used for hypertension; side effect is floppy iris syndrome

Cholinergic Blocking Drugs* Decreases secretions

Also called anticholinergic and opposite of cholinergic, they help decrease secretions Major sites of actions of the anticholinergics are heart, respiratory tract, GI tract, and sweat/salivary glands

Losartan (Cozaar)

ARB beneficial in patients with hypertension and HF -use with caution in those with renal or hepatic dysfunction and in patients with renal artery stenosis -do not use in breastfeeding mom

what are the -sartan drugs

Angiotensin II Receptor blockers (ARBs)

bronchodilators

adrenergic -treat asthma and bronchitis by relaxing the airway or bronchodilating the airway -albuterol, terbutaline

Tamsulosin (Flomax)

adrenergic antagonist, alpha 1 blocker used in BPH to help urination

what are the five categories of the adrenergic drugs?

adrenergic neuron blockers alpha 2 receptor agonists alpha 1 receptor blockers beta receptor blockers combination alpha 1 and beta receptor blockers

what medication is used with benign prostatic hyperplasia

alpha 1 blockers- tamsulosin

Tamulosin (Flomax)

alpha blocker used to treat BPH and is exclusively used in males. -block alpha adrenergic receptors on smooth muscle within the prostate and bladder -improves urinary flow -contraindications: known drug allergy, concurrent use of erectile dysfunction medication (slidenafil) -adverse effects: headache, abnormal ejaculation, rhinitis.

nasal decongestants: androgenic or cholinergic?

androgenic

beta blockers used for antianginal effects

atenolol, metoprolol, propranolol, nadolol

bph

benign prostatic hypertrophy

Atenolol (Tenormin)

beta blocker -cardioselective -used to prevent future heart attacks in patients who have had one. -used in the treatment of hypertension and angina, and in the management of thyrotoxicosis to help block the symptoms of excessive thyroid activity -oral use

Metoprolol (Lopressor)

beta blocker -most common beta 1 blocker -increased survival rate when given to those who have experienced an MI -oral or injectable use -when given IV it is considered high alert drug; monitoring required given after MI and used for hypertension in patients unable to take oral meds -used for angina

Labetalol (Normodyne)

beta blocker -treatment of severe hypertension and hypertensive emergencies to quickly lower the blood pressure before permanent damage is done. -oral and injective use

After an MI, a high level of circulating catecholamines irritates the heart, causing an imbalance in supply and demand ratio and even leading to life threatening dysrhythmias. What class of drugs blocks the harmful effects of catecholamines thus improving survival after an MI?

beta blockers

what drugs are the -olol?

beta blockers

*Adrenergic Blocking Drugs* Cardiac::

beta blockers (ends in OL) -reduces myocardial stimulation, slows down heart rate -meds: atenolol, Labetalol, Metoprolol

alpha 1 blockers

block alpha 1 receptors= decreased bp dilate arteries and veins -also used to increased urinary flow rates -used in benign prostatic hyperplasia- tamsulosin

Beta Blockers Cause:

bradycardia *****They all end in OL*****

central nervous system includes

brain and spinal cord

beta blockers

decrease heart rate through beta 1 receptor blockade- results in decreased heart o2 demand and increased o2 delivery to the heart -causes reduced secretion of renin long term use can cause reduced peripheral vascular resistance -indicated for: angina, antihypertensive, cardiac dysrhythmias, cardioprotective effects, some used for migrants, essential tremors and stage fright

*Cholinergic Blocking drugs GU effects:

decrease urinary urgency -Tolterodine (Detrol)

anticholinergic (sympathetic) SLUDGE

decreased Salivation and sweating decreased Lacrimation decreased Urinary incontinence decreased Diarrhea decreased GI cramps decreased Emesis

Cholinergic Blocking Drugs Respiratory effects;

decreases secretions from mouth and nose

What do low doses of dopamine do?

dilate blood vessels in the brain, heart, kidneys, and mesentery, which increases blood flow to those areas

vasodilators

directly relax arteriolar or venous smooth muscle -decreases SVR, and after load

neurological cholinergic drugs

donepezil (Aricept)

what are the -lol drugs

dual action alpha 1 and beta receptor blockers

diuretics

firstling antihypertensive in the JNC 8 for treatment of hypertension -decrease plasma and extracellular fluid volumes -decreaes preload, decreased CO and total peripheral resistance -decreased workload of heart and decreases BP

adverse effects of nitrates

headaches- usually diminish in intensity and frequency with continued use reflex tachycardia postural hypotension tolerance may develop

Epinephrine (adrenaline)

is an endogenous vasoactive catecholamine. Acts directly on both beta and alpha adrenergic receptors of tissues innervated by SNS. -prototypical nonselective adrenergic agonist -administered in emergency situations and is one of the primary vasoactive drugs used in many advanced cardiac life support protocols. -at LOW doses, it stimulates mostly beta 1 adrenergic receptors, increasing the force of contraction and heart rate. used to treat acute asthma and anaphylactic shock. bronchodilatory effect. -at HIGH doses, stimulates mostly alpha adrenergic receptors causing vasoconstriction, which elevates blood pressure. -available in 1mg/ml or 0.1mg/ml

nitroglycerin

is the prototypical nitrate -large first pass effect with oral forms -used for symptomatic treatment of ischemic heart conditions -IV form used for BP control in preoperative hypertension, treatment of HF, ischemic pain, pulmonary edema associated with acute MI, and hypertensive emergencies -routes: PO, SL, metered dose aerosol that is sprayed under the tongue, IV, and topical

What do high doses of dopamine do?

it can improve cardiac contractibility and output

therapeutic objectives for antianginal drugs

minimize the frequency of attacks and decreases the duration and intensity of anginal pain -improve the patient's functional capacity with as few adverse effects as possible -prevent or delay the worst possible outcome MI

hyperkalemia is more likely to occur with the use of _____ drugs than ______ drugs

more likely to occur with ACE drugs than with ARBs drugs

Tolterodine (Detrol)

muscarinic antagonist -used to treat overactive bladder, urinary frequency, urgency, and urge incontinence caused by bladder overactivity. -dry mouth -avoid use in angle closure glaucoma or urinary retention, decreased hepatic function -oral use

dopamine (Intropin)

naturally occurring catecholamine neurotransmitter. it has potent dopaminergic as well as beta 1 and alpha adrenergic receptor activity. -used at low doses to dilate blood vessels in the brain, heart, kidneys, and mesentery, which increases blood flow to those areas - at higher infusion rates: it can improve cardiac contractibility and output -use is contraindicated in those with catecholamine secreting tumors. -available only as an IV injectable drug -onset of action 2-5min -duration of action 10 min

myocardial infarction

necrosis or death of cardiac tissue -disabling or fatal

drus for angina

nitrates or nitrites -beta blockers -calcium channel blockers

Angiotensin-converting enzyme (ACE) inhibitors

often first line of drug for hypertension and HF may be combined with a thiazide diuretic or CCB -ACE is responsible for converting angiotensin I to angiotensin II, which is a potent vasoconstrictor and causes aldosterone secretion. -when ACE is blocked, prevention of angiotensin II occurs and there is a decreased Na and H2O reabsorption= diuresis which causes a decreased preload (circulating blood volume) which results in a decreased SVR (after load), vasodilation occurs and blood pressure is decreased -used with hypertension and HF -slows the progression of left ventricular hypertrophy after MI (CARDOPROTECTIVE) -RENAL PROTECTIVE: in those with diabetes

what are the -osin drugs

peripherally acting Alpha 1 blockers

ischemia

poor blood supply to an organ

ischemic heart disease

poor blood supply to the heart muscles -atherosclerosis -coronary artery disease