Pharm Test 3: drugs affecting calcium levels and bone mineralization, Drug therapy of Gout, Pharm Exam 5: Chapter 75 - Calcium Levels & Bone Mineralization Part B, week 6 A/C Agonists & Antagonists, Drug Therapy for Rheumatoid Arthritis & gout, Advan...
Nurse Resp. for ALL Adrenergics
- monitor BP & HR - report tachycardia, palpitations, dizziness, increased BP - may give w/ food - monitor urinary output (urinary retention) - monitor blood glucose levels (hyperglycemia) - avoid OTCs
Ach
- present at all preganglionic neurons, all postganglionic neurons of parasympathetic system, all motor neurons to skeletal muscle, postganglionic to sweat glands
Lithium Cautions
-Abormal sodium loss = dehydration -Dangers in Pregnancy Cardiovascular malformation, *kidney damage*, euthyroid goiter, hypoglycemia
Factors Affecting Excretion
-Age -Concomitant disease -pH dependent ionization (urine) -Competition for active tubular transport
Dextromethorphan
-Antitussive (antagonizes NMDA glutamate receptors). -Synthetic codeine analog. Has mild opioid effect when used in excess. -Naloxone can be given for overdose. Mild abuse potential. -May cause serotonin syndrome if combined with other serotonergic agents
Enzyme Inhibition
CYP Substrate + CYP Inhibitor --> increased substrate concentration and decreased risk of toxicity
Biphosphonates
Alendronate (Fosamax) prevent and treat bone loss (dexa scan and bone density test to diagnose)
Drugs for hyperuricemia
Allopurinol, Probenecid
Alpha blockers in BPH
reduce contract of smooth muscle in prostatic capsule and bladder neck (trigone&sphincter) s/s= daytime freq, dysuria, nocturia, hesitancy, urgency, sensation of incomplete void= improve
Dyskinesias managed in (3) ways
reduce levodopa dose (PD may re-emerge) give amantadine (works in some) surgery and electrical stimulation (if above fail)
T or F: Somatic motor neurons always release ACh and effect is always excitatory, while autonomic motor neurons release either ACh or NE and they can e excitatory or inhibitory
TRUE
somatic nervous system
the division of the peripheral nervous system that controls the body's skeletal muscles
MAO-B
the enzyme that inactivates dopamine in striatum
erectile dysfunction (ED)
the inability of the male to attain or maintain an erection sufficient to perform sexual intercourse
Preparations: Carbidopa alone
Name: Lodosyn available at special request when carbidopa added to L/C combo it can ↓ levodopa induced N/V allows↓levodopa dose-promotes ↑fast response
Reversible Cholinesterase Inhibitors
Neostigmine (Prostigmin) Physostigmine Ambenonium, eddrophonium, pyridostigmine Echothiophate Drugs for Alzheimer disease
Febuxostat (Uloric)
New and expensive Alternative to Allopurinol Reduces blood levels of uric acid Used for chronic tophaceous gout
Rhabdomyolysis
dissolution of striated muscle (caused by trauma, extreme exertion, or drug toxicity; in severe cases renal failure can result)
teratogenic
disturbance of the development of a fetus or embryo
Anti-depressants - What is the main neurotransmitter involved?
Norepinephrine
transmitter released by practically all postganglionic neurons of the sympathetic nervous system
Norepinephrine
Glucocorticoids used as antiemetic
Not approved by FDA. Solumedrol and dexamethasone. Given IV.
Defective genes coding for all (3) proteins have been found in
families with inherited forms of of PD.
sympathetic
fight or flight
sloughing
formation of dead tissue that separates from living tissue
A drug that induces a loss of consciousness is a
general anesthetic
Failure to degrade alpha-synuclein appears to result from (2) causes
genetic vulnerability toxins in the environment
describe Transmitter Storage
Once transmitter is synthesized, it must be stored until the time of its release Transmitter storage takes place within vesicles - tiny packets present in the axon terminal
Dual control
Organs may receive dual innervation from parasympathetic and sympathetic causing opposing responses
Potential interventions to IMPROVE or MAINTAIN cognitive function: SOCIAL/BEHAVIORAL FACTORS
QUALITY OF EVIDENCE SHOWS SMALL PROTECTIVE EFFECT: Cognitive Training Physical Activity Non-Cognitive, Non-PhysicalLeisure Activity
The nurse is teaching a client how to recognize the symptoms of a cholinergic crisis. The nurse knows that the client understands the information when she identifies which as symptoms of this type of crisis? Select all that apply. Rapid heart rate Headache Mydriasis Nausea Muscle weakness
Rapid heart rate Headache Nausea Muscle weakness
Ballismus
Rapid involuntary jerking or clinging of proximal muscle groups
The Parasympathetic Nervous System
goes all the way across and its end point is a Muscarinic receptor, and ACh is the neurotransmitter that works on that receptor.
therapeutic agents that alter the sympathetic nervous system are used primarily for effects on the
heart, blood vessels, and lungs
bisphosphonates
help with osteoporosis pts by treating their calcium levels - "nate" alendronate risedronate ibandronate tiludronate etidronate zoledronate pamidronate
Alpha 1 adverse effects
hypertension, necrosis, bradycardia
overview of motor symptom management- therapeutic goal
ideal tx doesn't exist no cure, prevention, or reversal only provide symptomatic relief no convincing proof of delayed progression improve ability to perform ADLs
Physical measures should also be used for spasm:
immobilization cold press whirlpool baths PT
Entacapone does what?
inhibits catechol-O-methyltransferase
Parenteral Administration
injectable IV, IM, SC, intra-articular, intrathecal
epi-pen
injectable epinephrine used by pts with severe allergies, high risk for anaphylaxis injected into the thigh must carry at all times
Zolpidem (Ambien)
insomnia Ambien, Edluar, and Zolpimist are used to help you fall asleep when you first go to bed. Intermezzo, is used to help you fall back to sleep if you wake up in the middle of the night and then have trouble sleeping.
Selegiline drug interaction with levodopa
intensifies adverse effects of levo psych, dysk, OH
adrenal medulla
neuroendocrine tissue associated with the sympathetic branch
muscle relaxants
relieve muscle spasms and stiffness Possible side effects 1. Drowsiness or dizziness. 2. Possible addiction or dependence. 3. Dry mouth. 4. Urinary retention.
Dopamine agonists- Disadvantages
serious side effects: hallucinations daytime sleepiness postural hypotension USUALLY reserved for YOUNGER patients -tolerate side effects better than older pts do
Ergot Derivatives cause mild blockage of
serotonergic and alpha-adrenergic receptors = more side effects
Somatic Nervous system
single neuron, CNS origin, myelinated
*raloxifene [evista]*
structurally similar to estrogen and binds to estrogen receptors therapeutic uses: - osteoporosis - breast cancer adverse effects: - *thromboembolic events* (ex: DVT) - pulmonary embolism - stroke - fetal harm
neurochemical basis of parkinsonism
too little striatal dopamine too much acetylcholine
Mesalamine
treats ulcerative colitis
Schedule 3 controlled substances
Substances with some potential for abuse and with currently accepted medical uses. Abuse may lead to moderate or low physical dependence or high psychological dependence. Examples - Codeine, Ketamine, Anabolic Steroids, Opium or Morphine Mixtures
Which supplies more organs? Parasympathetic or sympathetic?
Sympathetic
parasympathetic effect of the bladder
urine release
sympathetic effect of the bladder
urine retention
Tizanidine promotes presynaptic inhibition by
acting as an agonist at presynaptic alpha2 receptors
Levodopa enters the brain through
active transport that carries it across BBB
drugs that tx spasticity do not tx _____
acute muscle spasm
herpes simplex Treatment
acyclovir, famciclovir, valacyclovir
atropine
anticholinergic drug that blocks muscarinic ACh receptors (dries up salvations during surgery, dilates pupils for eye exams, speeds up HR)
Pegloticase
Accelerates uric acid secretion
Haloperidol
Antipsychotic
Renal Excretion
Depends on the GFR, impaired renal function = drug dose adjustment Estimate GFR with creatinine clearance using Cockroft and Gault Formula --> creatinine is a measure of muscle breakdown and is 100% filtered by kidneys
Analgesic
(chiefly of a drug) acting to relieve pain. Tylenol!
what is highest normal BP
140/90
Beta blockers reduction of preoperative mortality
BB ↓risk for mortality associated w/ non cardiac surgery in high-risk patients. pre-treatment with bisoprolol ↓incidence of perioperative MI and death. for safe/effective Tx: dosing should begin early (days-weeks before surgery). doses should be low initially then titrated up. Tx should cont for 1 month post surgery NOTE: if BB started late (days before) and at large doses= risk of mortality actually is ↑
No drug measures for RA
Balance between rest and exercise Massage Warm baths Heat to affected extremities
Beta 1
Cardiac - 1. inc heart rate, 2. inc force of contraction, 3. inc velocity of impulse conduction through AV node Kidney 1. - release of renin-Aldosterone - vasoconstriction--BP up Used for Heart Failure, Shock, AV heart block, Cardiac arrest Adverse effects: 1. Tachycardia- from over stimulation 2. Dysrhythmias- irregular heart rhythm 3. Angina
First Generation: Nonselective BB
Carteolol (Cartrol)= beta-1, beta-2 Nadolol (Corgard)= beta-1, beta-2 Pindolol (Visken)= beta-1, beta-2 Propranolo (Inderal)l= beta-1, beta-2 Sotalol (Betapace)= beta-1, beta-2 Timolol (Blocadren)= beta-1, beta-2
Central acting alpha 2 agonists
Drugs that act within the CNS to reduce outflow if impulses along sympathetic neurons
Which of the following observations might indicate that timolol is achieving the desired effect in a patient?
The patient's intraocular pressure decreases
Pharmacodynamics
The process by which a medication works on the body.
Pharmacokinetics
The process by which drugs are absorbed, distributed within the body, metabolized, and excreted.
Cocaine/Cocaine Derivatives
Therapeutic uses: local anesthetics (Lidcocaine, etc)
idiopathic
unknown cause
cholinergic receptors are subdivided into what?
nicotinic and muscarinic
Dissociation of transmitter from receptor
(reuptake into presynaptic cell, enzymatic degradation, diffusion away from gap).
Master Molecule of Addiction
*Dopamine*
Functions of Adrenergic (sympathetic) Receptors
1. Alpha 1 2. Alpha 2 3. Beta 1 4. Beta 2 5. Dopamine
Levodopa: Drug Interactions
1. First generation antipsychotics 2. MAOIs 3. Anticholinergic 4. Pyridoxine (Vitamin B6)
autonomic nervous system (ANS)
3 principle functions - regulation of the: 1.heart 2.secretory glands, 3.smooth muscle
A nurse is monitoring the drug level of a client receiving quinidine. Which serum drug level would the nurse immediately report to the primary health care provider? 2.5 mcg/mL 4.1 mcg/mL 3.8 mcg/mL 6.2 mcg/mL
6.2 mcg/mL
Sympathetic - fight or flight HHH
3 primary functions Homeostatic Objectives 1. CV (HEART) 2. Temperature (HEAT) Regulation 3. Fight-or Flight (HECK) HEART HEAT HECK Beat the heck out of them or get the heck outta there
nystagmus
constant, involuntary movement of the eyeball
Sulfasalazine (Azulfidine)
5-aminosalicylate,, DMARD Decrease inflammation by inhibiting prostaglandin synthesis Used for IBD (Crohn's, UC), RA Can cause agranulocytosis, hemolytic and macrocytic anemia,, hepatic dusfunction, bone marrow suppression
Ephedrine
A 1 and A2, Beta 1 and 2 Receptor -Asthma Adverse Effects: -same as epi- hypertensive crisis (cerebral hemorrhage), dysrhythmias, angina, necrosis, hyperglycemia
A nurse is preparing to administer IV calcium chloride to a patient with a low serum calcium level. Which drug on the patient's medication record, administered concurrently, would require additional patient monitoring by the nurse? a.Digoxin [Lanoxin] b.Furosemide [Lasix] c.Lorazepam [Ativan] d.Pantoprazole [Protonix]
ANS: A Parenteral calcium may cause severe bradycardia in patients taking digoxin; therefore, the heart rate should be monitored closely. Concurrent administration of calcium chloride and pantoprazole, lorazepam, or furosemide is not known to lead to drug interactions.
antibiotic
A chemical secreted by a living organism that kills or reduces the reproduction rate of other organisms
addiction
A physiological or psychological dependence on a drug
medication reconciliation
A procedure to maintain an accurate and up-to-date list of medications for all patients between all phases of health care delivery.
medication reconcilliation
A procedure to maintain an accurate and up-to-date list of medications for all patients between all phases of health care delivery.
Insulin
A protein hormone secreted by the pancreas that is essential for the metabolism of carbohydrates and the regulation of glucose levels in the blood. Insulin Lispro: rapid acting Insulin Glargine: long acting
Other Muscarinic Agonists
A) Cevimeline (Evoxac): used for relief of dry mouth like in patients with Sjogren syndrome B) Pilocarpine: topical therapy of glaucoma and oral therapy for Sjogren C) Acetylcholine: used for rapid pupil constriction after cataract surgery
Pathophysiology of Rheumatoid Arthritis
A-healthy joint B-inflammation of synovial membranes C-onset of pannus formation and cartilage erosion D-Pannus formation continues and cartilage deteriorates further E-Comlete destruction of joint cavity together with fusion of bones
cholinergic receptors bind to what?
ACh
Drug interactions with Probenecid
ASA- increases uric acid crystals
Efficacy
Ability of a drug to illicit an effect also called intrinsic activity
Ethosuximide
Absence seizures thalmic T type ca++ channel blocker
Cyclophosphamide (Cytoxan)
Alkylating agent (cytotoxic antineoplastic) Kills rapidly growing cells by interrupting DNA/RNA synthesis Can cause bone marrow suppression, N/V, acute hemorrhagic cystitis, alopecia
Phenylephrine
Alpha 1 receptors -nasal congestion Adverse effects: inc. BP
Pharmacokinetic Drug-Drug Interactions
Alter ADME
PK Drug-Drug: Distribution
Altered protein binding --> co-admin of drugs that bind to same site on protein (e.g., albumin) clinical significance depends on degree of binding and Vd Increased concern with highly protein-bound drugs (when displacement occurs there will be an increased effect)
The only drug recommended for dyskinesias is
Amantadine
Acetaminophen (Tylenol)
Analgesic S/E Anemia (long term use) Liver and kidney failure Dyspnea (prolonged high doses) angioedema hives, itching
Beta Blockers: Therapeutic Uses
Angina pectoris HTN Cardiac Dysrhythmias Myocardial Infarction Reduction of Peri-operative Mortality Heart Failure Hyperthyroidism Migraine Prophylaxis Performance Anxiety Pheochromocytoma Glaucoma
Which medications are classified as neuromuscular blockers? Select all that apply. Atracurium besylate (Tracrium) Mecamylamine hydrochloride (Inversine) Dicyclomine hydrochloride (Bentyl) Succinylcholine chloride (Anectine) Ipratropium bromide (Atrovent)
Atracurium besylate (Tracrium) Succinylcholine chloride (Anectine)
Treatment for toxicology of muscarnic agonists
Atropine and supportive therapy
isoproterenol HCl
Beta agonist: B1, B2 PROTOTYPE - more specific than epinephrine - treats bronchospasms, asthma, emphysema, CHF, heart block, cardiac arrest
Adverse Effects of beta-2 blockade
Bronchoconstriction (beta-2 cause constriction) Hypoglycemia (inhibition of glycogenolysis)
epinephrine
C/I in HTN BPH (difficulty urinating) DM (hyperglycemia) Hyperthyroidism (overactive metabolism)
isoproterenol HCl
C/I in tachydysrhythmias, CAD, DM Adverse - tachycardia, angina, palpitations
According to the continuum chart, anxiety is a sign of
CNS Stimulation
Third Generation: BB w/ Vasodilating Action
Carvedilol (Coreg)= beta-1, beta-2, alpha-1 Labetalol (Trandate)= beta-1, beta-2, alpha-1 Nebivolol (Bystolic)= beta-1
Which (2) BB also block alpha receptors?
Carvedilol, Labetalol, also block alpha-adrenergic receptors in addition to beta receptors. Can cause postural hypotension.
3rd generation BBs that cause vasodilation
Carvedilol, Labetalol, Nebivolol.
Too Much Norepinephrine
Causes Anxiety
Drug-Drug Interactions
Change in pharmacologic effect of a drug when given concurrently with another drug unwanted effects --> Increased toxicity, decreased efficacy desired effects --> enhance effect, increase efficacy
The nurse is preparing discharge teaching for a client prescribed chronic antiarrhythmic medication therapy. Which signs/symptoms should be reported to the health care provider immediately? (Select all that apply.) Chest pain Nausea Dyspnea Diarrhea Heart palpations
Chest pain Dyspnea Heart palpations
Primary Receptor Types (2)
Cholinergic Receptors Adrenergic Receptors
Nicotinic M
Contraction of skeletal muscle
antitussives/expectorants
Control cough, promote elimination of mucus Ex: dextromethorphan, codeine, guaifenesin Codeine (decreases the frequency and intensity of cough)
Digoxin reversal agent
Digibind
1st choice of med for patients with mild-mod symptoms...
Dopamine agonists
COMT inhibitors
Entacapone [comtan] 200mg tabs: (initial) 200 mg daily ⇢⇡8 doses (max) 1600mg/day take w/each dose of levo/carb Tolcapone [tasmar] 100mg tabs: (initial) 100 mg TID ⇡⇢200mg TID PRN take 1st dose in am with levo/carb take next two doses 6 and 12 hrs later.
the major transmitter released by the adrenal medulla
Epinephrine
Disulfuram (Antabuse)
Ethanol Aversion Agent
Alpha- and beta- specific adrenergic agonists are primarily used to treat obstructive pulmonary conditions.
False, used to treat hypotensive states
Cytochrome P450 Enzymes
Family of heme proteins most predominant in liver but also found in the intestines, lungs, and other organs Phase I drug metabolism Most important: CYP3A*, CYP2D6, CYP2C* *Most abundant in the liver
Michaelis-Menten Kinetics
Follows linear kinetics until enzymes become saturated Enzymes responsible for metabolism/elimination become saturated resulting in non-proportional increases in drug levels *True for phenytoin and alcohol
Quinine/Quinidine
For Anti-malarial parenteral use. Anti-malarial: Suppresses parasite in the RBC (heme metabolism inhibitors/ schizonticide)
Goals of urate lowering therapy
For chronic gouty attacks Promote dissolution of urate crystals Prevent new crystal formation Prevent disease progression Reduce the frequency of acute attacks Improve quality of life
Antisecretory anticholinergics
Glycopyrrolate (Robinul, Cuvposa) mepenzolate (Cantil) methscopolamine (Pamine) propantheline Overall-reduce salivation
Gonorrhea treatment
Gonorrhea TX: IM Ceftriaxone *Cover Chlamydia with: azithromycin : 1 g orally as a single dose IM doxycycline : 100 mg orally twice daily for 7 days
Nicotene substitute
Gum, patches, nasal sprays that deliver small amounts of nicotine when trying to give up the habit
Ranitidine (Zantac)
H2 receptor antagonist. Potent inhiitor of gastric acid secretion Indications: GERD, ulcers, H. pylori, reflux, indigestion ADR: Pain, constipation, diarrhea, headache. Can cause jaundice
parasympathetic effect of the heart
HR decreases
Beta 1 hits?
Heart and lungs
toxicities of methotrexate
Hepatic fibrosis Bone marrow suppression GI ulceration Pneumoonitis- pulmonary infection Not good with pregnancies
Irreversible Cholinesterase Inhibitors
Highly toxic Used as Insecticides ONLY clinical application: Glaucoma Contains Phosphorous Lipid soluble Absorbed several routes Chemical warfare TREAT: mechanical ventilation, pralidoxime (specific antidote to poisoning by early administration), diazepam
Intra-articular Administration
Injection of drug into the joints
Antimuscarinic Toxicity
Hot as a hare (hyperthermia) Dry as a bone (dry eyes, mouth skin) Red as a beet (flushed face) Blind as a bat (mydriasis - very dilated pupils) Mad as a hatter (delirium)
Adverse effects of Allopurinol (Zyloprim)
Hypersensitivity syndrome- rash (head to toe), fever, liver or kidney Gastrointestinal effects Neurological effects
Before administering an adrenergic agonist, for what health conditions should the nurse assess in particular? Select all that apply. Hyperthyroidism Hypertension Diabetes Psoriasis Angina
Hyperthyroidism Hypertension Angina Diabetes
Volume of Distribution (Vd)
Hypothetical volume into which a drug is "dispersed" Represents a relationship between the amount of drug in the body to the plasma concentration
Methyltrexate
Immunossuppressant. Can promote short-term remission and reduce need for glucocorticoids in patients with Crohn's disease
Memantine: Therapeutic Effects
In severe AD- appears to confer modest benefits For many= can slow decline in fx In some= causes improvement of symptoms 28 wk use= ↑score on cog fx than placebo *suggests memantine slowed fx decline 24 wk mem+donepezil= ↑score> donepezil alone *suggests independent or synergistic benefits Does NOT benefit those with MILD AD
In the SNS:
In the SNS most the neurons are coming out of thorasic and lumbar areas Most the SNS are made of adrenergic fibers -> release NE-->acts on alpha and beta receptors-->acts on SNS--> bronchodilation etc. The SNS stays stimulated by catecolines (preganglionic) --> NE and EPI
An ED patient presents with dyspnea, tachycardia, and chest pain. The patient has a history of cardiomyopathy. The nursing assessment reveals hypotension with an apical pulse of 134 bpm. What would the nurse conclude might be causing the symptoms? Adequate cardiac output Inadequate cardiac output Asthma attack Hypokalemia
Inadequate cardiac output
Antidepressant MOA
Increase nor-epi and often serotonin levels in the synapse (mostly re-uptake inhibitors)
Which is a potential effect of low-dose nicotinic agonists? Relief of nausea Decreased pulse rate Increased blood pressure Symptoms of sedation
Increased blood pressure
The nurse is administering quinidine to a client who is also taking digoxin. The nurse will assess this client for which important adverse effect? Increased anticoagulant effects Decreased white blood cell count Decreased red blood cell count Increased digoxin level
Increased digoxin level
PK Drug-Drug: Elimination
Increased filtration --> consequence of tissue or protein binding displacement; increased free fraction resulting in increased amount of drug presented to kidney Interfere with tubular secretion --> prevents excretion (e.g., probenecid) Interference with tubular reabsorption --> sensitive to changes in urine pH and urine flow rate
Adverse effects of Tumor necrosis factor antagonists
Injection site reactions Serious infections Severe allergic reactions HF Hematologic disorders Cancer- leukemia, lymphoma Liver injury CNS demyelination gang disorders
sexually transmitted infections (STIs)
Infections that can be, but are not always, transmitted from one person to the next through sexual contact.
TCAs (tricyclic antidepressants)
Inhibit serotonin and NE re-uptake (Amitrptyline, Desipramine, exepin, imipramine, and Clomipramine-OCD)
Intrathecal (IT) Administration
Injection of a drug through the theca of the spinal cord and into the subarachnoid space "Into the CSF" --> usually oncology agents and antibiotics
A patient is prescribed esmolol for treatment of supraventricular tachycardia. The nurse would expect to administer this drug by which route? Intramuscular Oral Subcutaneous Intravenous
Intravenous
A client is admitted to the emergency department in ventricular fibrillation. The client is administered amiodarone hydrochloride (Cordarone). What is the major effect of this medication? It produces skeletal muscle relaxation. It slows the conduction through the AV node. It stimulates the sympathetic nervous system. It inhibits the increase of the refractory period of the cells.
It slows the conduction through the AV node.
Parkinson's Disease - Drug of choice?
Leva-dopa - it replaces dopamine but only works for five years!!! Shuttles Dopamine into the brain
Dopaminergic Drugs
Levodopa (PO) Carbidopa (PO) Pramipexole (PO) Entacapone (PO) Selegiline (PO, ODT) Amantadine (SQ)
Treatment for manic depression/bipolar disorder
Lithium - is the only drug to specifically treat bipolar disorder How does it work: - *Lithium is a monovalent cation that competes with calcium, magnesium, potassium and sodium in body tissues and at binding sites* -It alters sodium transmission in nerve and muscle cells - antimanic - both acute and recurrent attacks -takes 7-10 days to take affect -initially used in conjuction with phenothiazines -MUST KNOW *Lithium is a mood stabilizer (very weird drug)* *caution* tricyclics can cause mani relapses
Adverse effects of Febuxostat
Liver function abnormalities Nausea Arthralgia Rash Cardiac effects (in high dosages)
one example of a drug that works by altering Axonal Conduction
Local anesthetics
Inhalation Administration
Localized/topical or systemic effect Can be difficult for patient to self-administer (metered dose inhaler - use a spacer) Can be irritating
Beta blockers in Myocardial Infarction
MI= regional of myocardial necrosis by localized interruption of blood flow to heart wall. Tx w/ BB= ↓pain, infarct size, mortality, and risk of reinfarction. Effectiveness= must begin soon after MI, cont for several years.
Differences between barbiturates and benzodiazepines.
MOA: - both act at gabba receptors / chloride ion channel complex. - bind different allosteric sites. -Gabba is an inhibitory postsynaptic potentials.- Chloride flows through the channel and decreases resting membrane potential. -The neuron, therefore, is less likely to be stimulated. Benzos: major side effects and the most horrible withdrawal symptoms
Parkinson's disease cardinal symptoms
MOTOR SYMPTOMS: tremor rigidity postural instability slowed movement
Sulfasalazine
Management of RA nonbiolgic DMARDs Anti-inflammatory and immunomodulatory actions Also used for IBS Slows progression of joint deterioration Onset within one month
Hydroxychloroquine (Plaquenil)
Management of RA nonbiolgic DMARDs Early use improves long term outcomes Combined with methotrexate Take with food or milk Most serious toxicity is retinal damage- pre eye exam and then every 6 months due to adverse effect 3-6 months for therapeutic effects
Leflunomide (Arava)
Management of RA nonbiolgic DMARDs Immunosuppressant Reserved for second line use Toxic to liver; severe risk for infection
Memantine: Mechanism of Action
Memantine modulates effects of glutamate Glutamate: major excitatory transmitter in CNS NMDA receptor play critical role- learn/memory -NMDA receptor- transmembrane protein -regulate Ca+ entry into neurons (central channel) -Glutamate binds NMDA= promotes Ca+ influx Memantine displaces glutamate stops Ca+ entry -Ca+ entry= signal in learning & memory process -Excess Ca influx= impairs. possible neuron death
Alpha 2
Minimal clinical significance in PNS
1st neuron of two neuron chain
PREganglionic neuron
Amphetamines: main indications
STIMULANT: Therapeutic uses: narcolepsy, weight control, most common for ADHD
A patient, admitted to a health care facility with cardiac arrhythmia, is prescribed propranolol. Which factor should the nurse closely monitor as a part of the ongoing assessment during the therapy? Tendon reflexes Visual acuity Pulse rate Hydration
Pulse rate
Linear Pharmacokinetics
Rate of elimination is proportional to amount of drug present Dosage increases result in proportional increase in plasma drug levels
A client has been prescribed disopyramide (Norpace) to treat a tachydysrhythmia. Which factor would necessitate that the dose be reduced? Chronic diarrhea Immobility Hypertension Renal impairment
Renal impairment
A client has been prescribed disopyramide (Norpace) to treat a tachydysrhythmia. Which factor would necessitate that the dose be reduced? Renal impairment Immobility Chronic diarrhea Hypertension
Renal impairment
Which factor would necessitate a reduction in the dosage of disopyramide? Immobility Hypertension Renal impairment Chronic diarrhea
Renal impairment
Available in (3) trade names
Rytary, Sinemet, Duopa
Osmotic Laxatives
Salts draw water into the intestine causing fecal mass to soften and swell stimulating peristalsis. Low dose 6-12 hours, high dose 2-6 hours. magnesium hydroxide, magnesium citrate, polyethylene glycol, lactulose (can be used to lower blood ammonia in liver disease) * Increase fluid intake. Not good for kidney disease. Sodium phosphate exacerbates cardiac disease.
What can cause cholinergic crisis? Select all that apply. Sarin poisoning Understimulation of the parasympathetic nervous system Insecticide poisoning Overdosage of AChE inhibitors Pralidoxime chloride (2-PAM) poisoning
Sarin poisoning Insecticide poisoning Overdosage of AChE inhibitors
Pharmacology
Science that deals with the origin, nature, chemistry, effects, and uses of drugs; the characteristics or properties of a drug, especially those that make it medically effective
Nitroprusside
Short acting; increase cGMP via direct release of NO. Can cause cyanide toxicity (releases cyanide) a vasodilator that works by relaxing the muscles in your blood vessels to help them dilate (widen). This lowers blood pressure and allows blood to flow more easily through your veins and arteries. Given IV and titrated for therapeutic dose.
Nasal Decongestants
Shrink mucosal membranes and reduces fluid secretion, should not be used for more than 48 hours Afrin, Phenylephrine, pseudophedrine
***Which would be a contraindication for the use of a class II antiarrhythmic? Sinus bradycardia Hepatic dysfunction Thyroid dysfunction Diabetes
Sinus bradycardia
Pramipexole: Dangerous SE
Sleep attacks- 911 while driving Impulse control disorders- are dose related START-9 mths after. RESOLVE- after D/C compulsive gamble, shop, binge eat, hypersexual RF- young adult, fam/personal hx of ETOH abuse, and personality trait of novelty seeking (impulsivity, quick temper, low threshold for boredom)
Drug interactions with Colchicine
Statins- increased risk of muscle injury
The nurse is preparing to administer adrenergic agonists to several clients on a neurological unit. Which medication can be administered by mouth Isoproterenol Catechol-O-methyltransferase Dopamine Terbutaline
Terbutaline
GABA Neurotransmitter
The Neurotransmitter GABA is Responsible for Relaxation of Brain and Muscle. Inhibitory Neurotransmitter
A patient has recently been prescribed a drug that treats his hypertension by blocking the sympathetic receptors in his sympathetic nervous system. This action is characteristic of
an adrenergic antagonist
absence
The fact of not being present or available.
first pass effect
The initial metabolism in the liver of a drug absorbed from the gastrointestinal tract before the drug reaches systemic circulation through the bloodstream.
What is the relationship between multiple receptor types and selectivity of drug action
The more types of receptors we have to work with, the greater our chances of producing selective drug effects
Benzodiazepines
The most common group of antianxiety drugs, which includes Valium and Xanax.
What main neurotransmitter imbalance exists with anxiety?
The neurotransmitters targeted in anxiety disorders are gamma-aminobutyric acid (GABA), serotonin, dopamine, and epinephrine. Serotonin appears to be specifically important in feelings of well being, and deficiencies are highly related to anxiety and depression. Stress hormones such as cortisol also play a role.
tonic seizure
a seizure in which the muscles stiffen before the sufferer losses consciousness
Choreoathetosis
a slow involuntary writhing movement
Pharmacodynamics
The relationship between drug concentration at the site of action and the resulting effect --> "what the drug does to the body/result you see in the pt at a predefined dosage regimen" Pharmacological effect is due to the alteration of an intrinsic physiologic process and not the creation of a new process. Looks at mechanism of drug action, efficacy, and safety profile. -Receptor interaction -Signal transduction -Physiologic effect -Pt's functional status
Xanthines: main indications
Therapeutic uses: pain from headache (vasoconstriction in brain), asthma, bronchitis, *emphysema (bronchorelaxation)*, counter drowsiness.
ANILINE TYPE (ACETAMINOPHEN) (Tylenol) Non-narcotic analgesics - What are the main side effects
There is no GI irritation nor is there CNS Stimulation Aniline Derivatives is a non-narcotic analgesic agent that has the potential to cause irreversible liver damage with even a single overdose! ie Tylenol!
Tolterodine
Tolterodine Anticholinergic Drugs for Overactive bladder Nonselective muscarinic antagonist Fewer anticholinergic side effects QT interval
In nervous system communication, what happens with neurotransmitters when the action potential reaches the synaptic cleft? Select all that apply. They use the mechanism of diffusion. They are absorbed into presynaptic neuron vesicles. They help move the impulse across the cleft. They are released by presynaptic neuron vesicles. They block the mechanism of diffusion.
They help move the impulse across the cleft. They are released by presynaptic neuron vesicles. They use the mechanism of diffusion
MedWatch Program
This voluntary program encourages nurses and other health care professionals to use the MedWatch form to report when a medication, product, or medical event causes serious harm to a patient.
Methimazole (Tapazole)
Thyroid hormone antagonist. Inhibits synthesis of thyroid hormone. Used for hyperthyroidism, preoperative thyroidectomy, thyrotoxic crisis, and thyroid storm.
During the implementation phase of administering an adrenergic antagonist, for what adverse effects should you especially monitor? Select all that apply. Tinnitus Orthostatic hypotension Hypertension Syncope Double vision
Tinnitus Orthostatic hypotension syncope
What is Parkinson's Disease
Too Little Dopamine Problem: loss of dopaminergic neurons resulting in an imbalance of dopamine and acetylcholine in the basal ganglia (substancia nigra)
Nicotinic N
Transmission at all ganglia of sympathetic and parasympathetic nervous systems. Release of Epi from adrenal medulla
Drugs can act on any of these processes
Transmitter Synthesis Transmitter Storage Transmitter Release Receptor Binding Termination of Transmitter Action
Steroids in asthma
Treat flair up intermittently. May cause irritability and increased hunger. Not long term Methylprednisone, prednisone, dexamethasone
The teaching plan for a client taking amiodarone should include which instruction? Take this medication with grapefruit juice for optimal absorption. Use a reliable form of birth control while taking this medication. Drowsiness is common but will not interfere with any of your usual activities. Urinary retention is common and no need for concern.
Use a reliable form of birth control while taking this medication.
somatic nervous system
Voluntary control (skeletal muscle) Receptor is called a nicotinic M
The nurse is teaching a group of clients about effective therapies for nasal congestion. Which alpha-adrenergic agonist medications might be useful for these clients? Select all that apply. Phenylephrine hydrochloride (Sinex) Tetrahydrozoline hydrochloride (Tyzine) Midodrine hydrochloride (ProAmatine) Oxymetazoline hydrochloride (Afrin) Xylometazoline hydrochloride (Otrivin)
Xylometazoline hydrochloride (Otrivin) Oxymetazoline hydrochloride (Afrin) Phenylephrine hydrochloride (Sinex) Tetrahydrozoline hydrochloride (Tyzine)
Multiple Sclerosis (MS)
destruction of the myelin sheath on neurons in the CNS and its replacement by plaques of sclerotic (hard) tissue
tolcapone causes certain side effects with monotherapy
diarrhea, hematuria, yellow/orange urine
Give examples of ways in which neurotransmitters are removed from the synapse
diffuse away, metabolized by enzymes in the extracellular fluid, actively transported into cells, or MAO degrades norepinephrine
sympathetic effect of the pupils
dilate
Levodopa and Anticholinergics
excessive stimulation of cholinergic receptors contributes to the dyskinesias of PD blocking these receptors, anticholinergic agents can enhance responses to Levodopa
In the absence of dopamine, the excitatory influence of acetylcholine goes unopposed causing...
excessive stimulation of the neurons that release GABA
Acetylcholine is an
excitatory transmitter
Levodopa Food Interactions
high protein- ↓therapeutic response to levodopa neutral amino acids compete w/ levodopa for absorption in intestine and transport across BBB high protein can significantly ↓both amount of levodopa absorbed & transported into the brain suggests that high protein triggers an abrupt loss effect (an "off" episode) advise to spread protein consumption evenly throughout the day
Overactivity of these GABAergic neurons contributes to the
motor symptoms that characterize PD
Colchicine ADRs
n/v, diarrhea, abdominal pain, cause leukopenia, granulocytopenia, thrombocytopenia, and pancytopenia, rhabdomyolysis
Sustained-Release
often capsules filled with tiny spheres containing drug and the coating on the spheres dissolve at variable rates OR drug is imbedded in the matrix drug released steadily throughout the day usually cannot be crushed Sustained release (SR), extended release (ER, XR, XL), time release, controlled release (CR) or continuous release
autonomic nervous system
the part of the peripheral nervous system that controls the glands and the muscles of the internal organs (such as the heart). Its sympathetic division arouses; its parasympathetic division calms.
Name 2 anatomical differences between sympathetic and parasympathetic divisions
the pathways point of origin in the CNS and the location of autonomic ganglia.
seizure threshold
the point at where a seizure may be induced
describe axonal conduction
the process of conducting an action potential down the axon of the neuron
Management of Motor Fluctuations: long-term tx w/ levodopa or dopamine agonists is associated with (2) types of motor fluctuations
(1) off times- loss of symptoms relief (2) drug induced dyskinesias- involuntary movements
levodopa: wearing off can be minimized in (3) ways:
(1) shortening the dose interval (2) giving a drug that prolongs levodopa's plasma half-life (ex. entacapone) (3) giving direct acting dopamine agonist
Why is PD treated with levodopa and not with dopamine itself?
(2) reasons... dopamine cannot cross BBB dopamine has short half-life in blood (impractical to use even if it could cross BBB)
describe the 3 pathways of Termination of Transmission
(a) reuptake into the nerve terminal axon terminals contain "pumps" that transport transmitter molecules back into the neuron (b) enzymatic degradation the synapse contains large quantities of transmitter-inactivating enzymes (c) diffusion away from the gap very slow and generally of little significance
Adrenergic Antagonists cause direct
(reversible) blockade of adrenergic receptors
Type I Allergic Hypersensitivity
-Class: anaphylaxis -Mechanism: IgE mediated -Common manifestations: anaphylaxis, urticaria, angioedema -Timing: within min to hours after exposure (provided an initial antigen exposure and sensitization have occurred)
Type IV Allergic Hypersensitivity
-Class: cell mediated -Mechanism: drug-specific T lymphocytes -Common manifestations: contact dermatitis -Timing: 2-7d after exposure
Type II Allergic Hypersensitivity
-Class: cytotoxic -Mechanism: IgG or IgM mediated -Common manifestations: hemolytic anemia, thrombocytopenia, granulocytopenia -Timing: variable, typically at least 7d after exposure
clinical treatment of hypercalcemia
1) administer bolus fluid of normal saline - keeps pt from getting dehydrated 2) give pt a loop diuretic - balances out electrolytes - relationship between K and Ca - ex: *furosemide*
Agonists
A substrate (drug) which interacts with a receptor and elicits a subsequent intracellular reaction affinity + efficacy
Antagonists
A substrate (drug) which interacts with receptor (occupies it) but does not elicit an intracellular reaction. No activity. Response is determined by how much agonist is present. Affinity, but lacks efficacy
Fesoterodine
Fesoterodine Anticholinergic Drugs for Overactive bladder Nonselective muscarinic antagonist Dry mouth Constipation
Dopamine Agonists
Goal: improve ADL. not a cure. no delay of progression Apomorphine reserved for "off" episodes in PD Baseline data: assess motor symptoms: bradykinesia, akinesia, postural instability, tremor, rigidity and extent to which they interfere with life. High risk patients: caution use in elderly & psychiatric pts. pramipexole- caution in kidney dysfunction ropinirole- avoid in pregnancy compulsive dis- avoid pramipexole & ropinirole Administration concerns: PD makes self-administration of medication difficult. enlist family's help. Ongoing evaluation and interventions: evaluate for improvements during therapy med adjustments for halluc, dys, sleep attacks NV, OH- patient teaching to minimize fetal injury- stop ropinirole & switch dop-agonist impulse control dis- screen patients for RF
Selegiline does what?
Inhibits monoamine oxidase-B
Beta blockers in performance anxiety
"stage fright" s/s- diaphoresis, tachycardia, tremors by generalized discharge of the sympathetic nervous system. prevent beta-1 mediated tachycardia.
(8) alpha blockers
(1) Prazosin (2) Terazosin (3) Doxazosin (4) Tamsulosin (5) Alfuzosin (6) Silodosin (7) Phentolamine (8) Phenoxybenzamine
Adrenergic Antagonists can be divided into (2) groups:
(1) alpha-adrenergic blocking agents- drugs that produce selective blockade of alpha-adrenergic receptors (2) beta-adrenergic blocking agents- drugs that produce selective blockade of beta receptors
Lidocaine (Xylocaine) is available in a variety of dosage forms. How should a nurse administer lidocaine to a client with a ventricular arrhythmia? Topically Intravenously Intramuscularly Orally
Intravenously
Methotrexate (Rheumatrex)
It can treat cancer of the blood, bone, lung, breast, head, and neck. It can also treat rheumatoid arthritis and psoriasis.
At autopsy, these fibrils are visible as
Lewy bodies characteristic of PD pathology
A patient with cardiac arrhythmia is prescribed verapamil. Which of the following possible adverse effects should the nurse inform the patient about? Hypertension Diarrhea Peripheral edema Hyperactivity
Peripheral edema
Alpha2
location - parasympathetic nerve terminals, Referred to as "presynaptic or prejunctional" response - inhibition of transmitter release The function of these receptors is to regulate transmitter release presynaptic alpha2 receptors can help reduce transmitter release when too much transmitter has accumulated in the synaptic gap
Levodopa Acute Loss of Effect
occurs in (2) patterns: gradual loss abrupt loss
psychomotor
occurs in temporal lobe epilepsy, characterized by a temporary loss of consciousness, loss of judgement, automatic behavior, and abnormal acts
Transdermal Administration
often via patch or cream/ointment; need highly lipid soluble substance bypasses first-pass metabolism by the liver, release medications for periods of time (ranges) e.g., fentanyl, clonidine
dantrolene acts directly
on skeletal muscle
Action Potential
originates in the neuron conducting down the axon of the neuron to terminal makes everything work in our body
gingival hyperplasia
overgrowth of gums or reddened gums that bleed easily
Because this loss takes place over 5-20 yrs neuronal degeneration begins long before
overt motor symptoms appear
Cholinergic Receptors - define and give subtypes (3)
receptors that mediate responses to acetylcholine nicotinicN nicotinicM Muscarinic
Adrenergic Receptors - define and subtypes (5)
receptors that mediate responses to epinephrine (adrenaline) and norepinephrine Alpha1 Alpha2 Beta1 Beta2 Dopamine
Gout patho
recurrent inflammatory disorder characterized by hyperuricemia and episodes of severe joint pain, typically in large toe
Beta blockers in HTN
reduce peripheral vascular resistance in long-term use accounting for much of their anti-HTN effects.
Allopurinol
reduces the production of uric acid in your body. Uric acid buildup can lead to gout or kidney stones. Allopurinol is used to treat gout or kidney stones, and to decrease levels of uric acid in people who are receiving cancer treatment. ex zyloprim, aloprim Given short term for flair up, and long term to prevent Rash is side effect - stop med.
parasympathetic
rest and digest
When the parasympathetic nervous system is activated things happen:
rest and digest (house keeping) heart slows lungs constrict (airways) bladder contracts and sphincter relaxes so you can pee, can cry now increase GI motility, gastric motility/ juices increase pupils constrict (so we can see close up) errection- preparing for ejaculation.
while in the brain, Levodopa undergoes...
reuptake: into remaining dopaminergic nerve terminals that remain in the striatum after uptake: is converted to dopamine (its active form) b/c levodopa has not direct effects of its own. as dopamine: levodopa helps restore a proper balance between dopamine and acetylcholine
Dangerous reaction between selegiline and meperidine (demerol)
stupor, rigidity, agitation, hyperthermia avoid combination
Additive PD Drug-Drug
sum of the individual drug effects (1+1=2) overlapping toxicities/ADEs or increased pharmacologic effect/PD effect
Rectal Administration
suppository or enema dosage form; local or systemic effects, undergo relatively little first-pass metabolism
Sympathetic supplies visceral structures in superficial body such as:
sweat glands, arteries, and veins
variscosity
swollen regions along autonomic axons that store and release neurotransmitters
where are adrenergic receptors found?
sympathetic
Autonomic nervous system consists of:
sympathetic and parasympathetic
what controls temp regulation?
sympathetic nervous system to do that it regulates blood from to the skin
Most neuropharmacologic agents act by altering ___ why?
synaptic transmission Drugs that alter synaptic transmission can produce effects that are much more selective than those produced by drugs that alter axonal conduction (much less common)
The nurse is monitoring a client for adverse effects associated with the administration of an adrenergic antagonist. The nurse correctly teaches the client that which adverse effect is related to the first-dose phenomenon? Syncope Edema Blurred vision Urinary hesitancy
syncope
Name the effects of drugs
they can block receptors, mimic effects of neurotransmitters, or inhibit enzymes that degrade them- prolonging their effect
treatment of levodopa-induced psychosis with first generation antipsychotics is problematic.
they can ↓psychological symptoms BUT will intensify PD symptoms b/c they block receptors for dopamine in the striatum
Levothyroxine (Synthroid)
thyroid hormone Don't switch brands Take for at least 3 weeks to see if effective. Take on empty stomach and don't eat or drink for at least 30 min.
___________ refers to the state where a patient must continue to increase the dose of the drug in order to achieve the desired effect.
tolerance
describe Receptor Binding
transmitter molecules diffuse across the synaptic gap and then undergo reversible binding to receptors on the postsynaptic cell
PD: dyskinesias that characterize PD
tremor at rest rigidity postural instability bradykinesia (slowed movement) Severe PD- bradykinesia may progress to akinesia (complete absence of movement)
What class of antidepressant agents are indicated for severe depression?
tricyclics
Which type is recommended for severe depression?
tricyclics
t/f: Benzodiazepines - diazepam (valium) bind to receptor components and thereby enhance receptor activation by the natural transmitter at the site.
true
t/f: The ability of a neuron to influence the behavior of another cell depends upon the ability of that neuron to alter receptor activity on the target cell
true
t/f: dopamine itself is the only transmitter capable of activating dopamine receptors
true
t/f: there is only one neuron in the pathway from the spinal cord to the muscles innervated by somatic motor nerves
true
t/f: In some organs that receive nerves from both divisions of the autonomic nervous system, the effects of sympathetic and parasympathetic nerves are complementary, rather than opposite
true For example, in the male reproductive system, erection is regulated by parasympathetic nerves while ejaculation is controlled by sympathetic nerves
t/f:n A few structures under autonomic control receive innervation from only one division
true The principal example is blood vessels, which are innervated exclusively by sympathetic nerves
patient taking MOA inhibitor hypertensive crisis can be triggered by eating what food
tyramine certain drugs- sympathomimetics
idiosyncratic response
unpredictable and unexplained drug reaction
Functions we are aware of in the ANS
upset stomach and full bladder
Tophi
uric acid crystal deposits in joints
A client with systemic lupus erythematosus is hospitalized following total knee replacement. Eight hours after the procedure, the nurse prepares to administer bethanechol chloride (Duvoid). The nurse tells the client that the medication is being administered to treat which disorder? Urinary retention Glaucoma Dry mouth Sjogren syndrome
urinary retention
Your client, Carrie Nelson, is experiencing fluid retention a day after an operation on her hand. What is a likely outcome of administering an oral cholinergic agonist to Ms. Nelson? Blood pressure rises Pulse increases temporarily Muscle weakness increases Urination and digestion are aided
urination and digestion are aided
Alpha-2 Selective Agonists
used as antihypertensives (ex. clonidine)
norepinephrine
used in critical care units in shocky states, hypotension, cardiac arrest LOTS of vasoconstriction
Sulfinpyrazone (Anturane)
used in the treatment of chronic gout (gouty arthritis), which is caused by too much uric acid in the blood. The medicine works by removing the extra uric acid from the body. Sulfinpyrazone does not cure gout, but after you have been taking it for a few months it may help prevent gout attacks. Sulfinpyrazone will help prevent gout attacks only as long as you continue to take it.
*ibandronate [boniva]*
uses: - prevention and treatment of postmenopausal osteoporosis dosing: - once a month or once every 3 months adverse effects: - GI effects- (ex: esophagitis dyspepsia, abdominal pain) - ocular inflammation - atypical fractures - osteonecrosis of the jaw - renal damage if IV administered too rapidly
hypercalcemia
usually asymptomatic symptoms that present occur in: - kidneys - GI tract - CNS causes: - cancer - hyperparathyroidism - vitamin D intoxication - sarcoidosis - use of thiazide diuretics if elevated levels of calcium in the blood --> less calcium in the bones (not good)
Ulcer treatment
usually includes medication to decrease stomach acid production like antacids; if bacteria is cause, antibiotics may be needed; avoid smoking and drinking
Parasympathetic preganglionic axons
very long and extend all the way to target organs
Sympathetic fiber lengths:
very short preganglionic axons with long post ganglionic
Action potential causes ....
vesicles to fuse with surface of terminal and be released into synapse action potential is conducting down the axon of the neuron to terminal
Carbidopa Combination Benefit
w/o carbidopa about 98% is lost in periphery leaving 2% available to the brain when decarboxylases are inhibited by carbidopa only 90% of levodopa is lost in periphery leaving 10% for actions in the brain
SALICYTES (aspirin) Toxicities with Chronic Use
•*Hearing* (ringing in ears; hearing loss(reversable); dizziness (inhibits enzyme in the cochlea) •Possible slight decrease in GFR (glomerular filtration rate) - this is negligible compared to phenaetin or even acetaminophen toxicity - No significant liver damage - Caution if patient already has liver or kidney damage •No blood disease •No link to bladder cancer
Anti-epileptic frequent adverse effects
• Sedation - locomotor and CNS • Kidney and liver damage • Blood diseases • Each agent has it's own adverse effects
The nurse is caring for a client who developed extravasation from a dopamine drip. The nurse anticipates that the health care provider will order which medication to treat this disorder? Doxazosin mesylate (Cardura) Alfuzosin (UroXatral) Phenoxybenzamine hydrochloride (Dibenzyline) Phentolamine mesylate (Regitine)
Phentolamine mesylate (Regitine)
Beta-Adrenergic Antagonists (beta blockers)
Practically all results from Beta-1 blockade in the heart. (1) ↓HR (2) ↓force of contraction (3) ↓impulse conduction velocity thru AV node
Preperations: Dopamine Agonists- NonErgot Derivitatives [Pramipexole, Ropinirole, Rotigotine]
Pramipexole [Mirapex, Mirapex ER] IR tabs: 0.125, 0.25, 0.5, 0.75, 1, 1.5 (mg) ER tabs: 0.375, 0.75, 1.5, 2.25, 3, 4.5 (mg) Ropinirole [Requip, Requip XL] IR tabs: 0.25, 0.5, 1, 2, 3, 4, 5 (mg) ER tabs: 2, 4, 6, 8, 12 (mg) Rotigotine [Neupro] 24hr Transdermal Patch: 1, 2, 3, 4, 6, 8 (mg)
BLACK BOX WARNING selegiline
antidepressants associated with risk of suicide in patients younger than 24. selegiline, antidepressant and drug for PD, is included in this warning. carries an ↑ risk for HTN crisis in younger pts contraindicated in patients < 12
PD becomes clinically recognizable when
between 70-80% of these neurons must be lost
Casodex
bicalutamide Prostate cancer
Colestipol (Colestid)
bile acid sequestrant (older agent). Decreases fat absorpion and may decrease uptake of fat-soluble vitamins.
Colesevelam (Welchol)
bile acid sequestrants used for antilipemic meds. bile acid sequestrants reduce LDL.
Agonists
bind to receptors and cause activation
Antagonists
bind to receptors and thereby block receptor activation by other agents
phenylephrine
binds to adrenergic receptors (nasal decongestant, constricts nasal blood vessels, inhibiting secretions and reducing sinus pressure)
Competitive Antagonist
binds to same site as agonist
epoetin alfa (Epogen, Procrit)
biosynthetic form of erythropoietin
Levodopa/Carbidopa: disadvantages
carbidopa= no adverse effect on its own adverse effects of combo= carbidopa potentiating the effects of levodopa combo= abn mvmts & psych disturb can occur sooner & be ↑intense than w/ levodopa alone
Beta blockers in Angina
cardiac pain due to ischemia that occurs when O2 supplied to heart through coronary circulation not sufficient to meet cardiac O2 demand. block beta-1 receptors in heart ↓workload ↓O2 demand back into balance with O2 supply Prevents ischemia and pain.
Beta blockers in pheochromocytoma
cardiac stimulation from ↑release of catecholamines can be prevented by beta-1 blockade.
somatic motor division
carries signals to skeletal muscles with nicotinic ACh receptors
Anaphylaxis
causes hypotension, bronchoconstriction, glottis edema Treatment; epinephrine (epi-pen) IM Activated 3 types of adrengic receptors -Beta 1 -Alpha 1 -Beta 2
Topical lidocaine
causes localized vasoconstriction, producing a white ring around the wound application area. The preparation provides anesthesia in the immediate are.
Antiviral
chemical that combats a specific viral disease (e.g. herpes) (Denavir, Famivir, Relenza, Retrovir, Tamiflu, Zovirax)
Fibers that release ACh
cholinergic fibers
(2) second generation antipsychotics have been used successfully to manage levodopa-induced psychosis
clozapine quetiapine
AAN recommends use of (2) 2nd generation antipsychotics
clozapine and quetiapine clozapine can cause agranulocytosis quetiapine preferred. don't use olanzopine (2nd gen)
Ganglion
collection of cell bodies outside CNS
Spasticity is tx with
combination of drugs & PT
Selegiline should not be combined with SSRIs
combo of MAO-B inhibitor + SSRI can cause fatal serotonin syndrome withdraw SSRIs at least 5 wks before starting selegiline
Which type of neuron in the peripheral nervous system carries impulses away from the brain and spinal cord to the muscles and glands? Afferent Efferent Autonomic Sensory
efferent
Two Neuron Chain
efferent pathway to ANS effectors
diazepam & tizanidine thought to relieve spasm by:
enhancing presynaptic inhibition of motor neurons in the CNS
Diazepam promotes presynaptic inhibition by
enhancing the effects of gamma-aminobutyric acid (GABA) an inhibitory neurotransmitter
In people with PD that is not inherited
environmental toxins may explain the inability to degrade alpha-synuclein
Spasm can result from
epilepsy, hypocalcemia, acute & chronic pain syndromes, & trauma
Which endogenous substance is also known as adrenaline? Epinephrine Dopamine Norepinephrine Neurohormone
epinephrine
primary neurohormone of the adrenal medulla
epinephrine - secreted into the blood
adrenergic receptors bind to what?
epinephrine/NE
bromocriptine
ergot derivative direct-acting dop-agon activate DA receptors at striatum similar responses as pramipexole, ropinirole mono- early stage combo w/ levo- adv stage allows ↓levo dose= ↓levo induced dyskinesias adverse effects: dose dependent. 30-50% pts. nausea most common. OH and dyskinesias Corfused, nightmares, halluc, paranoid, agitated occur in 30% pts= when dose is HIGH. Rarely: retroperitoneal fibrosis, pum infiltrates, Raynaud like phenom, erythromelalgia (vasodilation in feet/hands=swell, red, pain, warm)
Zafirlukast
eukotriene (loo-koe-TRY-een) inhibitor. Leukotrienes are chemicals your body releases when you breathe in an allergen (such as pollen). These chemicals cause swelling in your lungs and tightening of the muscles around your airways, which can result in asthma symptoms. Zafirlukast is used for chronic treatment of asthma, and to prevent asthma attacks in adults and children as young as 5 years old. Take on empty stomach 1-2 hours before eating. Do not prescribe for people with liver disease.
The American Academy of Neurology (AAN) has developed
evidenced based guidelines for Tx of PD and management of individual manifestations of the disease recommendations follow the disease across the lifespan
Parasympathetic : BBBBMVP
housekeeping chores: 1. Slows heart rate (BRADYCARDIA) B 2. Increased gastric secretion (BELLY) B 3. Empties the BLADDER (B) Empties the BOWEL (B) 4. CONTRACTION of Smooth Muscle (M) 5.Focus eye for near VISION (V) 6. Pupil constriction (P) 7.Bronchial contraction 8. HR down before ejaculation
Allopurinol ADRs
hypersensitivity syndrome (rash, fever, eosinophilia and dysfunction of the liver and kidneys), initial therapy could cause acute gouty attack, Gi reactions, drowsiness, headache, metallic taste, cataracts
Propranolol is ordered for a client who has a cardiac arrhythmia. It will be important for the nurse to determine if the person has a history of: idiosyncratic reaction to cinchona derivatives. chronic heart failure secondary to a tachyarrhythmia. hypersensitivity to sulfonylureas. hypersensitivity to beta blockers.
hypersensitivity to beta blockers.
Glatirimer
immunomodulator medication currently used to treat multiple sclerosis. Reduces relapses, does not stop progress of disease.
testosterone therapy
improve sexual interest (increase libido) increase prostate cancer risk increase cholesterol levels and cause liver damage worsen BPH symptoms (not used with 5 alpha reductase inhibitor)
PD symptoms first appear
in middle age AND progress relentlessly
MAO-A
inactivate NE and Serotonin imposes risk for hypertensive crisis
A drug that increases transmitter synthesis will cause receptor activation to (increase or decrease)
increase
Drugs that promote release will (increase or decrease) receptor activation
increase
(MOA) monoamine oxidase
increase level of Dopamine in the brain
Levodopa does what?
increases dopamine synthesis
hypocalcemia
increases neuromuscular excitability clinical presentations: - *tetany* - *convulsions* - *spasm of the pharynx* ^ want to draw Ca levels if seen in a pt causes - deficiency of vitamin D - deficiency of PTH or dietary calcium - chronic renal failure - long-term use of certain medications, such as magnesium-based laxatives, and drugs used to manage osteoporosis (ex: bisphosphonates and denosumab)
Catechol-O-Methyltransferase Inhibitors (COMT) Tolcapone [tasmar] BLACK BOX WARNING
increases risk of hepatotoxicity liver injury/failure may be fatal close monitor required D/C if s/s of liver injury occur AST/ALT elevation is double upper range normal Tx limited to 3 wks in absence of beneficial resp
oral calcium salts
indications: - mild hypocalcemia - dietary supplements - colorectal adenoma adverse effects: - hypercalcemia drug interactions: - corticosteroids - tetracycline - fluoroquinolone - thyroid hormone - phenytoin - bisphosphonates (reaction depends on serum calcium levels) - loop diuretics - thiazide diuretics
Non-selective inhibitors of MAO
inhibit MAO-A and MAO-B used to treat depression pose risk for HTN crisis
Allopurinol mechanism of action
inhibit XO, an enzyme required for uric acid formation
First Generation histamine- 1 antagonists
inhibit allergic reactions of inflammation, redness, and itching caused by the release of histamine Can be used with cold symptoms. Anticholinergic property (dry mouth, urinary hesitancy) CNS depressant (sleepiness) Caution in Asthmatic patients (thickens bronchial secretions impairing breathing) Ex. diphenhydramine, promethazine, chlorpheniramine
hydantoins
inhibit sodium influx, stabilize cell membranes, reduce repetitive neuronal firing and limit seizures
A 70-year-old woman with a history of atrial fibrillation takes digoxin and verapamil to control her health problem. Verapamil achieves a therapeutic effect by: inhibiting the movement of calcium ions across the cardiac muscle cell membrane. blocking adrenergic receptors and producing antisympathetic effects. decreasing sodium and potassium conduction. weakening diastolic depolarization and the action potential duration.
inhibiting the movement of calcium ions across the cardiac muscle cell membrane.
GABA is an
inhibitory neurotransmitter
Dopamine is an
inhibitory transmitter
IM Administration
into muscle (IM) Drug needs to be in solution or particle suspension IM preparations can be immediate release or depot formulations
Meridia
intrauterine device that contains levonorgestrel. Prevent conception by producing a harmless local inflammatory response that is spermicidal. Also treats menorrhagia. Light spotting and amenorrhea are common. Risk : PID good for up to 5 years.
muscle spasm
involuntary ctx of a muscle group or muscle often painful and interferes w/ fx
Levodopa: Dyskinesias
ironically- given to alleviate movement disorders-can actually cause movement disorders about 80% develop involuntary mvmt in 1st yr some just annoying-head bobbing, tic, grimacing some disabling- ballismus, choreoathetosis some develop just before/soon after optimal dosing achieved
The nurse is caring for a client who states that he is taking dicyclomine hydrochloride (Bentyl). The nurse reviews the client 's history and determines that this medication is intended to treat which condition? Peptic ulcer disease Motion sickness Irritable bowel syndrome Asthma
irritable bowel syndrome
Aniline Derivatives
is a non-narcotic analgesic agent that has the potential to cause irreversible liver damage with even a single overdose! ie Tylenol!
IV main anesthetic
ketamine: incr. resp. and H.R., acts as stimulant, no skeletal muscle relaxation
Drugs used for motor symptoms
levodopa levodopa/carbidopa
dopaminergic agents act by several mechanisms
levodopa is converted to dopamine, which: activates dopamine receptors directly monoamine oxidase-B inhibitors (MAO-B): prevent dopamine breakdown amantadine promotes dopamine release and may also block dopamine reuptake catechol-O-methyl-transferase (COMT) inhibitors: enhance levodopa effects by block degradation
B/c of peripheral metabolism less than 2% of each dose reaches the brain if
levodopa is given alone. only small fraction of each dose reaches brain most metabolized in periphery by decarboxylase enzymes and to a lesser extent by COMT
If improving motor fx is primary objective then...
levodopa is preferred
Ulcers treatment
likely caused by H. pylori. Treat with antibiotic and pepto bismol, proton pump inhibitors (prilosec, prevacid, aciphex, nexium, protonix), H-2 blockers (zantac, pepcid, tagamet, nazatidine), antacids, and cytoprotective agens (carafate, cytotec)
nicotinicN
location - all autonomic nervous system ganglia and the adrenal medulla response - stimulation of parasympathetic and sympathetic postganglionic nerves and release of epinephrine from adrenal medulla
nicotinicM
location - neuromuscular junction response - contraction of skeletal muscle
Antineoplastics (anti-tumor)
"Stine" cytotoxic systemic chemotherapy or targeted biological therapy; designed to target specific molecular components in tumor cell biology with the hope of minimizing cytotoxicity to noncancerous cells.
Muscarinic
(target organs of ParaNS and sweat glands of SymNS) Increased glandular secretions, Contraction bronchi/sweat glands, Slowing heart rate Contraction of iris (miosis), Contraction of ciliary muscle of eye (near-vision), Dilation of blood vessels, Urinary voiding
Dopamine
*responds only to dopamine, a neurotransmitter found primarily in the CNS kidney - dilation of kidney vasculature (enhancing renal perfusion)
SALICYTES (aspirin) Non-narcotic analgesics - Acute Side Effects and Toxicities
*•G.I. irritation and decreased coagulation (bleeding) with continued use* •Gastric mucosa usually heals in 3 days •Caution Black Stools •CNS stimulation •respiratory stimulation to point of respiratory alkalosis
A client experiencing a ventricular dysrhythmia has received a bolus of lidocaine. What is the recommended rate for continuous infusion of lidocaine IV now prescribed for this client? 10 to 20 mg/min 0.25 to 0.75 mg/min 1 to 4 mg/min 6 to 8 mg/min
1 to 4 mg/min
Long Acting Beta Agonists (LABA)
1) Formoterol & Salmeterol 2) Onset 20 minutes so NOT for ACUTE attacks 3) Lasts up to 12 hours 4) *Never used alone in ASTHMA, always with inhaled corticosteroids* different with COPD. This is bc smart study showed that LABA alone for asthma can cause death.
Sources of muscarinic poisoning
1) Ingestion of certain mushrooms 2) OD on direct acting muscarinic agonists (bethanechol, pilocarpine) AND cholinesterase inhibitors (indirect acting cholinomimetics)
status epilepticus
A condition in which seizures recur every few minutes or last more than 30 minutes.
Osteoporosis
A condition in which the body's bones become weak and break easily. Treatment: Raloxifene - hormone that improves bone density Denosumab- hormone that prevents bone loss Biphosphonates: Alendronate · Ibandronate · Zoledronic acid. Prevents bone loss.
autonomic nervous system
A division of the peripheral nervous system. Controls involuntary activity of visceral muscles and internal organs and glands. Autonomic is divided into 1. Parasympathetic 2. Sympathetic
What is a Sedative?
A drug administered at a dose level to cause mild drowsiness or sedation or to reduce restlessness & anxiety. (Benzodiazapine/Xanax)
What is a general anesthetic?
A drug given at a dose to depress the CNS to a degree that causes a loss of consciousness (unarousable), as well as analgesia (cannot feel pain).
Intermittent Dose
A drug must be administered for 4-5 half-lives before steady state is reached. Peaks are the high points of fluctuation. toxic effects are most likely to be observed during peak drug concentration. Troughs are the low points of fluctuation. Lack of drug effect is most likely to occur during troughs.
Neuroleptic Malignant Syndrome (NMS)
A rare and sometimes fatal reaction to high-potency neuroleptic drugs. Symptoms include muscle rigidity, fever, and elevated white blood cell count. It is thought to result from dopamine blockage at the basal ganglia and hypothalamus. Treatment: support body through withdrawal.
After reviewing antiarrhythmic drugs, a group of nursing students demonstrate understanding of the drugs when they identify which as a class II antiarrhythmic? Select all that apply. Ibutilide Amiodarone Propranolol Verapamil Acebutolol
Acebutolol Propranolol
Epinephrine
Activates all 4 receptors Therapeutic Uses: 1. A1 delay anesthesia absorption, control superficial bleeding. 2. B1 AV block, asystole. 3. B2 asthma (others preferred). DOC for anaphylactic shock. Pharmacokinetics: Not oral (rapid destruction). Short half-lifeAdverse Effects Drug Interactions: 1. MAOI-inc effect b/c less breakdown. 2. Tricyclic antidepressants - inc effect. 3. General anesthetics - tachydysrhythmias, 4. Alpha-adrenergic blockers, 5. Beta-adrenergic blockers Administration: -watch for extravasation, -constant cardiac monitoring if IV, -not oral, can give intracardiac. -Comes in multiple concentrations - pay close attention
Receptor binding activation/inhibition
Activation - EG morphine (CNS). Epinephrine (CV), Insulin (DM) Inhibition - Naloxone (CNS). Antihistamines (allergic d/o). Propanolol (CV)
Colchicine
Acute gouty attacks PO Anti-inflammatory action only in gout (doesn't work for other inflammatory disorders) Mechanism of action largely unknown Not an analgesic, doesn't relieve pain in conditions other than gout Does not affect uric acid production or clearance
KNOW/MEMORIZE TABLE 13-2 TABLE 13-3 page 113-114 Go back over this in your voice recording!
Alpha 1: -Hit the eye-mydriasis (bigger) -Bladder contration -Constrict peripheral arterioles, -Constrict veins, -Sex organs -Ejaculation, -Contracts prostate (Sympathetic NS!) Alpa 2: Mostly in the CNS Beta 1: -heart- increased rate and force -kidney- release of renin (Parasympathetic ) Beta 2: -Lungs dilate, -Relaxes uterus, heart and skelatal muscle dilate, stimulates liver to do gluconeogenesis. arterioles (Peripheral Dopamine: Kidney (dilates)
Antiepileptic Drugs (AEDs)
Also known as anticonvulsants Goals of therapy -To control or prevent seizures while maintaining a reasonable quality of life -To minimize adverse effects and drug-induced toxicity -AED therapy is usually lifelong -Combination of drugs may be used
Pharmacodynamic Drug-Drug Interactions
Alter overall effect related to the drug's effects in the body, one drug modulates the effect of another
PK Drug-Drug: Metabolism
Alterations in hepatic blood flow Alteration in drug-metabolizing enzymes --> inducers and inhibitors of CYP450 enzymes
PD drugs: Antiviral Agent
Amantadine [generic] tablet: 100mg capsule: 100mg syrup: 10mg/mL 100mg BID (initial) ⇢⇡400mg/day (divided doses) Dose when used w/ high doses of other PD drugs 100mg/day (initial)⇢⇡200mg/day (divided doses)
Half-Life
Amount of time required for the total amount of drug in the body to decrease by one-half -important to determine time to steady state -important to determine elimination from the body
The nurse is preparing to teach a client about cholinergic antagonists. The nurse plans to explain to the client that the healthcare provider or pharmacist may also refer to this type of drug by what other name? Indirect-acting muscarinic agonists Direct-acting muscarinic agonists Muscarinic agonists Anticholinergics
Anticholinergics
Haloperidol (Haldol)
An antipsychotic drug thought to block receptor sites for dopamine, making it effective in treating the delusional thinking, hallucinations and agitation commonly associated with schizophrenia. -Preferred treatment for Tourette syndrome. -Hepatic metabolism, excreted in urine. -early extrapyramidal reactions occur frequently. Long Q-T .
Solifenacin
Anticholinergic Drugs for Overactive bladder Similar to darifenacin not as M3 selective Adverse effects: dry mouth and blurred vision QT interval
Scopolamine
Anticholinergic drug similar to atropine Therapeutic doses: sedation (versus atropine that causes excitation) Scopolamine: suppresses emesis and motion sickness (atropine does not) Principal uses: motion sickness, production of cycloplegia, mydriases, preanesthetic sedation and obstetric amnesia
Phenytoin (Dilantin)
Anticonvulsant. SEs: Nysagmus, diplopia, EOM palsies, ataxia, gingival hyperplasia. Slows down impulses of the brain that cause seizure activity.
Fluoxetine (Prozac)
Antidepressant, SSRI Treats: Depression (also bipolar, ocd, panic disorder, bulimia, pmdd). S/E: sexual dysfunction in 70% of adults. Treatment for this would involve decreasing dose, drug holiday on weekends, add a drug to treat this such as bupropion, nefazodone, mirtazapine. Weight gain and serotonin syndrome can be other side effects. Abrupt withdrawal can cause dizziness, headaches, nauea, sensory issues, tremors, anxiety and dysphoria - should be tapered down. Do not use in 3rd trimester
5FU
Antimetabolite. Anti-cancer drug used topically for skin cancer. Injection for colon and rectal, breast, gastrointestinal (anal, esphageal, pancreas and stomach), head and neck, liver, and ovarian.
Aripiprazole (Abilify)
Antipsychotic Aripiprazole is used to treat certain mental/mood disorders. It may also be used in combination with other medication to treat depression. Dizziness, Lightheadedness, Drowsiness, Nausea, Vomiting, Tiredness, Excess saliva/drooling, Blurred, vision, Weight gain
Clinical Pharmacokinetics
Application of pharmacokinetic principles to the safe and effective therapeutic management of drugs in an individual patient --> what dose to give how often, etc.
Other biological DMARDs
B-Lymphocyte- depleting agent (Rituxan) T-cell activation inhibitors (Orencia)
Schedule 1 controlled substances
Are classified as high potential for abuse. No accepted medical use. Labeled C-1. -Examples: 1. heroin 2 hallucinogens 3. LSD 4. Marijuana(except when prescribed for cancer treatment.
The nurse is preparing to administer a cholinergic antagonist to a client. When reassessing the client, which finding would the nurse consider an adverse effect of the medication? Dry mucous membranes Increased blood pressure Increased pulse rate Arrhythmia
Arrhythmia
Probenecid interactions
Aspirin and other salicylates
Muscarinic antagonists--Atropine
Atropine Best-known muscarinic antagonist Found in nature Heart: increases heart rate Exocrine Glands: decreases secretions Smooth Muscle: relaxes bronchi, decreases tone of bladder, decreases tone of GI Eyes: pupil dilation CNS: mild excitation to hallucinations and delirium
Anticholinergics
Atropine GI - Slows motility, spasm Eyes - Dilates pupils *DO NOT GIVE TO GLAUCOME PTS* Heart - Increase HR Resp - bronchodilator (Atrovent)
Dobutamine
B1 Receptor TX: Heart Failure Adverse Effects - tachycardia Drug Interactions - MAOI, tricyclic antidepressants anesthetics
dopamine
B1 selective agonist PROTOTYPE low: increased renal profusion mod: increased force of contraction high: increased BP (vasoconstriction) BUT decreased renal profusion
dobutamine
B1 selective agonist increased contractility and SV lead to an increased cardiac output
albuterol sulfate
B2 selective agonist PROTOTYPE - bronchodilation!!!
Gabba Indenpendent
Barbiturates
Selectivity
Because axonal transmission is non-specific, receptor sites must be specific
The nurse is caring for a client who is taking an adrenergic agonist. Which cardiopulmonary system effects should the nurse expect this medication to produce? Bronchospasm Decreased heart rate Decreased blood pressure Bronchodilation
bronchodilation
Gabba Dependent
Benzos Alcohol
Centrally Acting anticholinergic drug
Benztropine (PO/IM)
Albuterol
Beta 2 receptor -Asthma Adverse Effects: -tremor
Muscarine Agonists
Bethanechol
Termination of Transmitter Action
Block reuptake Inhibit degredation
Which statement would be true about the mechanism of action of class II antiarrhythmic agents? Stimulate the uptake of potassium in the tissues Block the stimulation of the adrenergic receptors Block the influx of sodium into the cells Cause depression in phase 2 of repolarization
Block the stimulation of the adrenergic receptors
When describing the action of class II antiarrhythmics, which would the nurse include? Membrane stabilization with depression of phase 0 action potential Blockage of beta receptors in the heart and kidneys Interference with calcium ion movement across the membrane Blockage of potassium channels during phase 3 action potential
Blockage of beta receptors in the heart and kidneys
A patient with type 1 diabetes is prescribed acebutolol. What would be most important to monitor? Electrocardiogram Blood glucose levels Serum electrolyte levels Liver function studies
Blood glucose levels
what toxin inhibits ACh release
Botulinum
Beta-2 Selective Agonists
bronchodilators "-erol" suffix
Digoxin (Lanoxin)
Cardiac glycoside Positive inotrope, negative chronotrope and dromotrope Used for HF, a-fib Can cause dysrhythmias, bradycardia, GI effects (EARLY), vision changes (EARLY) Hypokalemia = toxicity; hyperkalemia = decreased effects Avoid verapamil Hold if pulse < 60 Therapeutic level = 0.5-2.0ng/mL Antidote: cholestyramine or Digibind Interacts w/ many meds and bran, oats, sunflower seeds.
Alpha blockers in pheochromocytoma
Catecholamine secreting tumor derived from cells of sympathetic nervous system. Usually located in Adrenal Medulla If secretions of catecholamines (Epi, NE) is sufficiently great, persistent hypertension results HTN main cause= alpha-1 on blood vessels (also beta-1 on heart contributes) Preferred Tx: removal of tumor. Adrenergic Agonists used: (1) w/ inoperable tumors to suppress HTN. (2) preoperatively to reduce acute HTN in Sx. surgical patient at risk because manipulating tumor can cause massive catecholamine release
Too Little Norepinephrine
Causes Depression
PID treatment
Ceftriaxone 250mg IM single dose PLUS Doxycycline 100mg po bid (14days) OPTIONAL Metronidazole 500mg po bid (14 days)
Dopamine Agonists: Beneficial effects result from...
Direct activation- dopamine receptors in striatum
autonomic preganglionic neurons
cholinergic neurons
parasympathetic postganglionic neurons
cholinergic neurons
After receiving a medication, the client is experiencing dysphagia. Which intervention by the nurse is the most appropriate? Provide orange juice for the client. Ascertain fluid intake and urinary output. Raise the dose of the client's anticholinergic agent. Contact the health care provider immediately.
Contact the health care provider immediately
Phase I Metabolism
Create or unmask a more polar group required for phase II reactions Oxidative, hydrolyic, reductive reactions Enzymes involved (oxidation) --> CYP450 enzymes
Where are cholinergic receptors found?
parasympathetic
Drugs that help reduce off times
DEFINITELY EFFECTIVE Entacapone- COMT Inhibitor Rasagiline- MAO-B inhibitor PROBABLY EFFECTIVE Rotigotine- DA agonist Pramipexole- DA agonist Ropinirole- DA agonist Tolcapone- COMT Inhibitor POSSIBLY EFFECTIVE Apomorphine- DA agonist Cabergoline- DA agonist Selegiline- MAO-B Inhibitor
The nurse is caring for a client with Raynaud's syndrome who has been prescribed adrenergic antagonist therapy. Which effect of this medication will alleviate the client 's symptoms? Decreased vasospasms Increased urinary output Decreased blood pressure Decreased heart rate
Decreased vasospasms
Tolterodine
Detrol, Detrol LA Stops bladder spasms / urinary frequency or urgency S/E anticholinergic (less than Oxybutynin)
So if a pt. was given a drug to slow down their intestines and its a sympathetic agonist what type of side effects are you going to get?
Dilated pupils weak salivary flow accelerated heart rate bronchi's dilated inhibited stomach motility relaxes bladder- no peeing uterine muscle relaxes
Etanercept (Enbrel)
Disease-modifying antirheumatic drug (DMARD). Interrupts complex immune responses, preventing disease progression. Uses: slow joint degeneration and progression of rheumatoid arthritis.
Your client, Jill Aquino, presents with ophthalmic congestion. Her husband brought her to the clinic, where her health care provider prescribed naphazoline (Naphcon). During client education, what do you tell Ms. Aquino toavoid? Driving a vehicle after administration Lying down during administration Shaking the bottle before administration Removing contact lenses before administration
Driving a vehicle after administration
Cannabinoids
Dronabinol (marinol) and Nabilone (cesamet). Suppresses CINV.
Parkinson's Disease - What do the drugs do?
Drug Treatment: 1. Increases dopamine 2. Decrease acetylcholine
Factors Affecting Absorption
Drug characteristics: molecular weight, ionization, solubility, formulation --> the bigger the drugs are the harder it is for them to get through the membrane Patient end: route of administration, gastric pH, contents of GI tract
Biliary Excretion & Enterohepatic Cycling
Drugs can be excreted in the bile as parent compound or metabolite Biliary flow --> intestines In intestines drug may be hydrolyzed releasing active drug again --> absorbed --> liver & repeated -This may prolong drug action If not reabsorbed will be excreted in feces.
Movement of Drugs Across Membranes
Drugs pass through cells via: -Channels and pores --> small so only only small compounds can move this way (Na, K, etc) -Transport systems --> carriers that move drugs from one side to the other, often selective (depends on drug structure), some require energy -Direct penetration of the membrane --> must be lipid soluble (lipophilic) e.g., transdermals *NOTE: drugs can exist in charged or uncharged forms, ions are unable to travel across membranes - only neutral molecules will travel through membranes!
Adrenergic neuron blocking agents
Drugs that act within the terminals of sympathetic neurons to decrease NE release
What is a Hypnotic?
Drugs which are administered at a dose level to induce sleep or allow an individual to stay asleep
Parkinson's Drugs given through PEG-J tube
Duopa suspension and Duodopa gel [levodopa/carbidopa] given via PEG-J Tube
Olanzapine (Zyprexa)
antipsychotic (atypical), mood stabilizer, thienobenzodiazepine antagonizes dopamine and seratonin type 2 in the CNSalso has antocholinergic, antihistiminic, and anti alpha1 adernergic effects decreases manifestations of psychoses Metabolized by the liver. Peaks in 6 hours 21-54 hour half-life contraindicated in lactation S/D metabolic. can cause leukopenia and neutropenia increasing risk for infection. Somnolence.
Antagonistic control example
Effector organ: Heart sympathetic response increases heart rate parasympathetic response slows rate
Bethanechol Pharmacokinetics
Effects begin in 30-60 minutes and persist for about 1 hour The drug crosses membranes POORLY
Adrenergic agonists (sympathomimetics)
Endogenous (naturally occurring in the body) and synthetic chemicals that activate adrenergic receptors in effector cells. In doing so they mimic the action of the sympathetic nervous system, which is why they are also called "sympathomimetics". The five main categories of adrenergic receptors are: α₁, α₂, β₁, β₂, and β₃, although there are more subtypes, and agonists vary in specificity between these receptors, and may be classified respectively.
Mrs. Laura Luchow is brought to the emergency department following a barbiturate overdose. What nonselective sympathomimetic could be of therapeutic use to Mrs. Luchow? Naphazoline hydrochloride (Naphcon) Ephedrine hydrochloride (Efedron) Oxymetazoline hydrochloride (Afrin) Pseudoephedrine hydrochloride (Novafed)
Ephedrine hydrochloride (Efedron)
(2) groups of dopamine agonists
Ergot Derivative- (alkaloid found in plants) LESS selective for dopamine receptors Bromocriptine [Cycloset, Parlodel] Cabergoline [Dostinex] Non Ergot Derivative- HIGHLY selective for dopamine receptors Pramipexole [Mirapex] Ropinirole [Requip] Rotigotine [Neupro] Apomorphine [Apokyn]
(2) BBs not used for hypertension
Esmolol- short half life (15 mins) Only approved therapy: emergency IV for SVT Sotalol- inducable arrhythmias Only approved therapy: Tx of ventricular dysrhythmias and to maintain NSR in those with previous Afib/Aflutter
Alpha-Adrenergic Antagonists (alpha blockers): Therapeutic Uses
Essential HTN Reversal of toxicity Alpha-1 Agonists (Epi) BPH Pheochromocytoma Raynaud Disease
explain how neuropharmacologic drugs exert their effects
Excitation or suppression of neuronal activity By mimicking or blocking neuronal regulation, neuropharmacologic drugs can modify such diverse processes as skeletal muscle contraction, cardiac output, vascular tone, respiration, GI function, uterine motility, glandular secretion, and functions unique to the CNS, such as ideation, mood, and perception of pain
Danny Feld, a healthy young male, comes into the emergency department after being mugged near the hospital. He has sustained minor cuts and bruises, but mainly he is upset. Mr. Feld asks you why his mouth is dry, yet he is sweating. How might you, as the nurse, best reassure Mr. Feld? Explain to Mr. Feld, in simple terms, the body's natural fight-or-flight response. Tell Mr. Feld that you will request a comprehensive blood panel. Tell Mr. Feld that you will ask the health care provider to prescribe a heavy sedative. Recommend to Mr. Feld that he follow up with his health care provider.
Explain to Mr. Feld, in simple terms, the body's natural fight-or-flight response.
T or F: all sympathetic postganglionic axons release NE
FALSE; most do
The nurse is caring for a client who is receiving glycopyrrolate (Robinul) for the treatment of peptic ulcer disease. The nurse should assess the client for which symptoms that indicate the presence of an anticholinergic crisis? Select all that apply. Fever Incontinence Dysphagia Hallucinations Confusion
Fever Dysphagia Hallucinations Confusion
2nd generation antihistamines
Fexofenadine, loratadine, and cetirizine non sedating less crossing of blood brain barrier, does not suppress CNS Take daily to prevent allergic reaction.
The neurons that release acetylcholine excite the neurons that release
GABA
The neurons that release dopamine inhibit neurons that release
GABA gamma-aminobutyric acid
Adverse effects of colchicine
GI toxicity- N/V/D abd pain Myelosuppression- BM decrease Rhabdomyolysis- muscle degeneration; inflammatory response CNS effects and dizziness in the elderly Cleared by kidneys
Therapeutic agents that alter parasympathetic nervous system function are used primarily for their effects on the
GI tract, bladder, and eye
Probenecid
Generic only Increases excretion of uric acid by acting on renal tubules and inhibiting reabsorption of uric acid Acts on renal tubules to inhibit reabsorption of uric acid- prevents formation of new tophi and helps existing tophi decrease May exacerbate acute episodes of gout- add indomethacin or colchicine for relief
Oxybutynin (Ditropan)
Genitourinary Medication, Anticholinergic Stops bladder spasms S/E dry mouth
what is the goal for Urate-lowering therapy?
to promote dissolution of urate crystals, prevent new crystal formation, prevent disease progression, reduce the frequency of acute attacks and improve quality of life
Levodopa/Carbidopa (Sinemet)
Goal: Improve ADLs. Does NOT delay progression Baseline Data: assess motor symptoms: bradykinesia, akinesia, postural instability, tremor, rigidity and extent to which they interfere with life. High-Risk Patients: assess skin for changes. levo+MAO inhibitors can activate malignant melanoma. caution in pts w/ CV disease, psychiatric disorders, and those taking MAO-B inhibitors Administration concerns: easy open pill bottles. no childproof bottles. Managing acute loss of effect: "off" times can be reduce by combing levo/carb w/dopamine agonist (Pramipexole), a COMT inhibitor (entacapone) or an MAO-B inhibitor (rasagiline) Minimizing adverse effects: n/v decreased by taking med w/ food amantadine may help w/ dyskinesias monitor for dysrhythmias, psychosis, OH 1st gen antipsych- block DA sites, ↑motor deficits High protein competes w/levo-absorb/transport MAO-inbitors + levo/carb= HTN crisis Anticholinergic + levo/carb= enhance responses
sympathetic effect of the heart
HR increases
No single drug is more effective than the others so selection should be based on
tolerability, ease of use, cost
Olsalazine (Dipentum)
IBD Management - Salicylate Derivative
There are four primary classes of antidysrhythmic drugs. What class consists primarily of potassium channel blockers? III IV II I
III
Although, dopamine agonists LESS EFFECTIVE than levodopa, still has advantages....
IN CONTRAST TO LEVODOPA -not dependent on conversion to become active -not converted to potentially toxic metabolites -don't compete w/ dietary proteins (for uptake in GI or transport across BBB) CONTRASTING LEVODOPA-IN CHRONIC USE -a lower incidence of response failures -less likely to cause disabling dyskinesias
Enteral Administration
tongue --> down oral, rectal, sublingual, buccal
1st-in-class NMDA Receptor Antagonist: Memantine
INDICATED ONLY FOR MOD-SEVERE AD. unlike cholinesterase inhibitors (used for mild) unknown= >effective than cholinesterase inhibitor BUT WE DO KNOW, IT'S BETTER TOLERATED!
Memantine [Namenda, Namenda XR]
IR tab: 5, 10mg PO SOLN: 2mg/mL, 10mg/5mL Increase gradually using the following schedule: 5mg/day (5mg once)- 1 week or more 10mg/day (5mg BID)- 1 week or more 15mg/day (5mg + 10mg= AM/PM)- 1 week or more 20mg/day (10mg BID)- MAINTENANCE Admin: W/WO food SOLN: ⌀mix w/meds. use only provided device ER cap: 7, 14, 21, 28 mg Increase gradually using the following schedule: 7 mg QD x 1 week or more 14 mg QD x 1 week or more 21 mg QD x 1 week or more 21 mg QD= MAINTENANCE Mod Renal Dysfx: reduce dose D/C: patients with severe renal impairment Admin: swallowed whole or added to soft food (applesauce), contents NOT crushed/chewed
Balsalazide (Colazal)
IBD Management - Salicylate Derivative
Cyclosporine
Immunosuppressant
Allopurinol (Zyloprim)
Inhibits uric Acid formation- keeps uric acid down in cancer patients Maintenance therapy Reduce blood levels of uric acid Used for chronic tophaceous gout, hyperuricemia due to chemotherapy
Excretion
Kidney is the major site for drug excretion, cannot efficiently eliminate lipophilic drugs; can also eliminate via hepatobiliary system and lungs Most drugs excreted in urine as parent compound (UNCHANGED) or as metabolite; degree of renal excretion varies widely drug to drug 3 processes involved: -glomerular filtration -active tubular secretion -passive tubular reabsorption Total excreted = [(filtered+secreted) - reabsorbed]
Therapeutic Range
Least drug needed to be effective and least amount of drug needed to have toxic effects (NOTE: adverse effects can happen anywhere in this range) minimal effective/therapeutic/toxic relationship
Preperations: Levodopa Combinations (highly individualized doses)
Levodopa/Carbidopa (C/L) mg [Sinemet, Rytary, Duopa, Duodopa] Sinemet IR- 10/100, 25/100, 100/250 Sinemet CR- 25/100, 50/200 Rytary- 23.75/95, 36.25/145, 48.75/195 61.25/245 Duopa enteral suspen- 4.63mg/20mg per mL Duodopa intestinal gel- 5mg/20mg per mL -Initial Tx: typical dose is one tab QD or QOD. gradual↑to 8 tab QD(max) regardless of strength -Duopa/Duodopa-sometimes dose changes daily Levodopa/Carbidopa/Entacapone (C/L/E) mg [Stavelo] Stavelo- (50) 12.5/50/200, (125) 31.25/125/200 (100) 25/100/200, (150) 37.5/150/200 (75) 18.75/75/200, (200) 50/200/200 -Typical= 1 tab any strength@each dosing interval up to 8 tabs QD (max) of Stavelo 50-150 up to 6 tabs QD (max) of Stavelo 200 -Dosing intervals determined by pt response NO HIGH FAT. TAKE PILLS WHOLE.
First-Pass Metabolism
Loss of drug as it passes for the first time through an organ of elimination, the liver, during the absorption process May also be the conversion of a pro-drug to an active form (and may still "lose" drug because not all is converted to active form) Pertains to oral dosing only
What are the Anti-epileptic agents?
MOA: 2 Ways 1. Decrease movement of ions into the nerve cells (block Na) and therefore, reduce repetitive firing of neurons. 2. Alter activity of neurotransmitter (inc. GABA or dec. glutamate Phenytoin (not general depressant), Valproic Acid, carbamazepine, phenobarbital - all used as first line of therapy bc they are effective and cheaper.
Methyldopa Methyldopate
Lowers BP Activates alpha 2 Vasodilator Used in HTN in pregnancy Adverse effects: hemolytic anemia Check COombs test on starting and during treatment 6-12 months Hepatotoxic Xerostomia Sexual dysfunction Ortho hypo CNS effects
Miscellaneous Laxatives
Lubiprostone, mineral oil, glycerin suppository, polyethylene glycol- electrolyte solution, Sodium picosulfate / magnesium oxide/anhydrous citric acid
Buspirone (Buspar)
anxiolytic Buspirone is an anti-anxiety medicine that affects chemicals in the brain that may be unbalanced in people with anxiety. Buspirone is used to treat symptoms of anxiety, such as fear, tension, irritability, dizziness, pounding heartbeat, and other physical symptoms. No MAOI
Selegiline prevents development of Parkinsonism
MPTP- neurotoxin causes selective degeneration of dopaminergic neurons not caused by MPTP itself, but by toxic metabolite formation of toxic metabolite is catalyzed by MOA-B inhibition of MOA-B= prevents metabolite formation and protects against neuronal injuries. humans exposed to MPTP develop SEVERE parkonisism
Most common causes of spasticity
MS and cerebral palsy (other causes stroke, traumatic spinal cord lesions)
alzheimers RF
Major known RF- advancing age 90% pts- age of onset > 65 risk of AD double Q 10 yrs after 65 until age 85-90= risk levels off/declines other known RF- familial history female MAY be a RF possible RF: head injury, low education level, apoE4 protein production, high homocysteine levels, low folic acid levels, estrogen/progestin therapy, sedentary lifestyle, nicotine in cig smoker
Surfactant Laxatives
Meds: Docusate sodium (Colace) Docusate calcium (Surfak) temporary treatment of constipation * avoid if narrowing of intestines Give with a full glass of water or juice
(2) BBs that have high solubility
Metoprolol and Propranolol Highly lipid soluble Penetrate BBB with ease Eliminated primarily by hepatic metabolism.
What are first line agents for relieving pain of acute gouty attack?
NSAIDs
Infliximab (Remicade)
Monoclonal Antibody that binds to tumor necrosis factor (TNF) & neutralizes its activity by preventing it from binding to the cell membrane in the blood. It is an immunosuppressant & is indicated for treatment of active Crohn disease & ulcerative colitis & is generally reserved for moderate - severe cases. It is given in IV form & the vials need to be refrigerated.
Bethanechol--general
Muscarinic Agonist/Parasympathomimetic agent Selective agonist at muscarinic cholinergic receptors Therapeautic uses: Urinary retention and investigational GI uses A) Heart: Bradycardia B) Smooth Muscle: 1) Constriction of bronchi in lungs 2) increased tone and motility in GI 3) Contraction of detrusor muscle in Bladder C) Exocrine glands: increased sweating, salivation, bronchial secretions, and gastric acid D) Eye: contraction
Dicyclomine
Muscarinic Antagonists For IBS (spastic colon, mucous colitis) Functional bowel disorders (diarrhea and hypermotility)
Drugs for acute gouty arthritis
NSAIDs, glucocorticoids
Treatment of gout
NSAIDs- 1st choice, Indomethacin, Naproxen, Diclofene Glucocorticoids- prednisone, PO or IM
(2) BBs that have low solubility
Nadolol and Atenolol Low lipid solubility Penetrate BBB poorly Eliminated primarily by renal excretion.
Opioid reversal agent
Naloxone (Narcan)
Neurotransmitters of ANS
NE secreted by most sympathetic fibers & ACh released by parasympathetic
Administration: PO Parkinson's Meds
NO FOOD: Levodopa/Carbidopa= take on empty stomach Selegiline= dissolve tab on top of tongue before breakfast. wait 5 mins before eat/drink FOOD: All others= can be taken W/WO food. Food does ↓ GI upset ER tabs/Stavelo- MUST be swallowed WHOLE Levo/Carb/Enta= NO high fat foods ↓absorp (compete- absorption and transport to BBB) TIMEFRAME: Cycloset- take within 2 hrs of awakening Entacapone- take w/each dose of levo/carb Tolcapone- 1st dose w/ levo/carb QAM, next two doses 6 and 12 hrs later. Selegiline- before breakfast 5min wait before PO
Alpha-Adrenergic Antagonists (alpha-1 blockers): Adverse Responses
Orthostatic hypotension- alpha receptors on veins ↓tone in venous wall. Reflex tachycardia- baroreceptor reflex- dilation=↓BP=receptor=↑HR Nasal congestion- alpha blockade can dilate nasal mucosa vessels Inhibition of ejaculation- sexual dysfunction r/t blockade of alpha-1 Sodium retention & increased blood volume- ↓BP, ↑renal retention Na+ water, ↑blood volume
2nd neuron of two neuron chain
POSTganglionic neuron
Neurons alter receptor activity by releasing
transmitter molecules, which diffuse across the synaptic gap and bind to receptors on the postsynaptic cell
Which muscarinic agonist may be prescribed for xerostomia? Donepezil hydrochloride (Aricept) Pilocarpine hydrochloride (Salagen) Bethanecol chloride (Duvoid) Carbachol (Miostat)
Pilocarpine hydrochloride (Salagen)
Single Dose Regimen
Plasma concentration of drug rises as the drug distributes to the bloodstream, then falls as the drug is distributed to tissues, metabolized, and excreted. Drugs administered orally reach a peak plasma concentration at a later time than drugs administered IV. Oral agents must be absorbed across GI mucosa and capillary walls before entering systemic circulation.
Muscarinic Antagonists--Atropine therapeutic use
Preanesthetic medications Disorder of the eye Bradycardia Intestinal hypertonicity and hypermotility Muscarinic agonist poisoning Peptic Ulcer disease Asthma Bilary colic
Levodopa: CV effects
Postural hypotension COMMON in early Tx hypotension↓ by ↑salt and water intake alpha adrenergic agonist can help too levodopa conversion in periphery can produce excessive b1 receptor activation in the heart DYSRHYTHMIAS result, esp in pts w/ CVD
Dosing/Administration: Dopamine Agonists- NonErgot Derivatives [Pramipexole, Ropinirole, Rotigotine]
Pramipexole: IR: 0.125mg TID (initial)→↑1.5mg TID (max) ER: 0.375mg QD (initial)→↑4.5mg QD (max) -Titrate= (IR) ↑over 7 wks, (ER) ↑gradually -↓dosage for significant impairment Ropinirole: IR: 0.25 mg TID (initial)⇢⇡8mg TID (max) ER: 2mg QD (initial)⇢⇡24mg QD (max) -Titrate (PRN)= ⇡s over several months Rotigotine: -EARLY STAGE PD: {1} 2-mg patch/24hrs (initial)→↑2mg weekly OR until lowest effective dose attained OR until (max) 6mg/24hrs -ADVANCED STAGE PD: {1} 4-mg patch/24hrs (initial)→↑2mg weekly up to 8mg/24 hrs (max) -If D/C: withdrawal= same rate= ↓2mg/wk Apomorphine: Injectable: 10mg/mL, comes in 3mL cartridge Used with multi-dose injector pen 2-6mg (0.2-0.6 mL) SQ w/ each "off" episode Max: 5 doses/day Start antiemetic 3 days prior to 1st dose.
The nurse is caring for a client with myasthenia gravis. In reviewing the client 's medication list, which medications does the nurse identify as being given for treatment of this condition? Select all that apply. Donepezil hydrochloride (Aricept) Cyclosporine (Sandimmune) Pyridostigmine bromide (Mestinon) Physostigmine salicylate (Antilirium) Prednisone (Deltasone)
Prednisone (Deltasone) Pyridostigmine bromide (Mestinon) Cyclosporine (Sandimmune)
A patient is admitted to the cardiology unit of a health care facility for ventricular arrhythmia. In which condition can an anti-arrhythmic drug be safely administered? Severe congestive heart failure Premature ventricular contraction Third-degree heart block Aortic stenosis
Premature ventricular contraction
antipsychotic medications
Prescription drugs that are used to reduce psychotic symptoms; frequently used in the treatment of schizophrenia; also called neuroleptics. Block dopamine, acetylcholine, histamine, and norepinephrine receptors in the brain and periphery. Acute and chronic psychosis, schizophrenia, manic phase of bipolar disorders, Tourette's syndrome, delusional and schizoaffective disorders, dementia. Conventional (typical) or atypical. Patient education: s/s of orthostatic hypotension - move slowly when standing up. Sedation - avoid hazardous activities such as driving until sedation wears off. Impaires libido and erection / ejaculation *avoid anticholinergic drugs, barbiturates, benzos and alcohol.
Cholinesterase Inhibitors: Donepezil, Rivastigmine, Galantamine
Prevent breakdown of ACh by AChE ↑available ACh at cholinergic synapses In AD: enhanced transmission by central cholinergic neurons that have not yet been destroyed. do NOT stop disease progression BUT may slow progression by a few months
Apomorphine: antiemetic combination
Prevent n/v- treat 3 days prior w/ antiemetic Trimethobenzamide [Tigan] CANT USE: ZOFRAN OR COMPAZINE serotonin recep-antag- zofran. ↑OH. ⌀△in N/V DA recep-antag- compazine.↓effect of PD drugs
Potential interventions to delay ONSET of Alzheimer's disease: NUTRITION
QUALITY OF EVIDENCE SHOWS POSSIBLE BENEFITS: Mediterranean Diet Light-Mod Alcohol Intake Folic Acid NO BENEFITS: Ginkgo Biloba Vitamin E Homocysteine Vitamin B12 Vitamin C Omega-3 Fatty Acids Beta-Carotene
Potential interventions to delay ONSET of Alzheimer's disease: SOCIAL/BEHAVIORAL FACTORS
QUALITY OF EVIDENCE SHOWS SMALL PROTECTIVE EFFECT: Cognitive Training Physical Activity
Goals of RA
Relieve symptoms Maintain joint function Minimize systemic involvement Delay disease progression Mobility
Pharmacokinetics
Relationship between the dose and the concentration of that drug in body fluids and tissues over time "what the body does with drug" --> study of the time course of a drug -Absorption -Distribution -Metabolism/biotransformation -Excretion/elimination
Neostigmine (Prostigmin)
Reversible Cholinesterase Inhibitor (drugs that prevent degradation of acetylcholine) Used for management of Myasthenia Gravis: increases force of contraction in skeletal muscle Cannot readily cross membranes Absorbed poorly with oral administration Minimal effects on brain and fetus Poor substrate for cholinesterase Response: identical to muscarinic agonist response (the direct type)
when the sympathetic Nervous System is at work these things happen
Running from a bear fight or flight heart rate up lungs dialate- lungs open to move more oxygen stops GI system- salivation (starts digestion) don't need this right now. bladder muscle will relax and sphincter will constrict so that you won't pee, and many other unwanted things when you are ie. running from a bear. pupils dilate( get bigger) (mydriasis) ejaculation- heart rate up
albuterol sulfate
S/E - tremors, dizziness, palpitations, dysrhythmias AVOID w/ hypertension or severe cardiac disease AVOID w/ MAOIs --> hypertensive crisis
Raloxifine (Evista)
SIDE EFFECTS: - DVT, PE, and fetal harm NURSING CONSIDERATIONS: - n/a
Denosumab (Prolia, Xgerva) - monthy subQ injections
SIDE EFFECTS: - In postmenopausal women back pain, pain in extremities, musculoskeletal pain, hypercholesterolemia, bladder infections - Hypocalcemia, serious infections, dermatologic reactions, and osteonecrosis of jaw (ONJ) NURSING CONSIDERATIONS: - n/a
Conjugated Estrogen (Premarin)
SIDE EFFECTS: - Increased risk of breast cancer, cholecystitis, MI and CVA NURSING CONSIDERATIONS: - Women with intact uterus requires progestin - This drug is no longer the best treatment option
Calcitonin-Salmon Nasal Spray
SIDE EFFECTS: - Nasal dryness and irritation NURSING CONSIDERATIONS: - Should be given with supplemental calcium and vitamin D - Pulled from Canadian market in 2013 due to increased risk of malignancy
Teriparatide (Forteo) - daily subQ injections
SIDE EFFECTS: - Nausea, headache, arthralgia, back pain, leg cramps - Orthostatic hypotension and dizziness after injection NURSING CONSIDERATIONS: - Black box warning due to increased risk of osteosarcoma - Should be used with extreme caution in those with bone metastasis or history of skeletal cancer
Clozapine (Clozaril)
Second Generation (Atypical) Antipsychotic low affinity to D2 dopamine receptors treats schizophrenia and suicidal behavior. Not many EPSs. S/E weight gain, orthostatic hypotension, sedation, cholinergic, urinary retention, constipation, tachycardia.
Metoprolol (Lopressor) Info
Second generation BB Selective blockade of beta-1 At high doses- will block beta-2 as well. Preferred in asthma and DM b/c no bronchoconstriction and hypoglycemia (beta-2) ↓HR, ↓contraction force, ↓conduction velocity through AV node. (beta-1 blockade) ↓renin secretion at kidneys. does NOT block bronchial beta-2= does NOT ↑airway resistance. very lipid soluble. absorbs well after PO admin Only 40% reaches circulation after first pass. eliminated by hepatic metabolism/renal excretion Uses: Primary-HTN. Angina, HF, MI Adverse Effects: Brady, ↓CO, AV block, abrupt withdrawal causes cardiac excitation. Can cause HF even though it can treat HF. Contraindicated: Brady, AV block >1st degree. Caution: HF patients Safer than Propranolol in asthma/severe allergy and DM= Min blockade of beta-2 that cause bronchoconstriction and hypoglycemia.
Benzo & Barbiturates Therapeutic Uses
Sedative Hypnotics *Relieves anxiety *Sleep Disorders *Epilepsy (barbiturates)
Zaleplon
Sedative/Hypnotic a sedative that is used to treat insomnia. zaleplon causes relaxation to help you fall asleep and stay asleep.
Alpha blockers can be divided into (2) groups
Selective alpha-1 blockade (prazosin= block alpha-1) Nonselective alpha blockers (phentolamine= block alpha-1 and alpha-2)
MAO-B Inhibitors
Selegiline [Eldepryl, Zelapar] Capsule: (elderyl, generic) 5 mg Tablet: (generic) 5mg ODT: (Zelapar) 1.25 mg Cap/Tab: 5mg breakfast & lunch. Total= 10mg/day Dose=complete MAO-B inhibition. NO ↑dose. ODT: 1.25mg QD x 6wks⇢⇡2.5mg QD (max) PRN Dissolve on top of tongue. 5 min wait before PO. Rasagiline {Azilect] 0.5mg, 1mg tablets Monotherapy: 1mg QD or 0.5mgQD (↓hepatic Fx) W/levo: 0.5mg QD (initial) ⇢⇡1mg QD (PRN)
describe a reflex
Sensor -monitor the status of a physiologic process Information picked up by the sensor is sent to the CNS (spinal cord and brain), where it is integrated with other relevant information Effector -makes appropriate adjustments neurons connecting the sensor to the effector
The nurse is preparing to educate a client who has been prescribed an adrenergic agonist inhaler. The nurse should include which instructions in the client education? Select all that apply. Rinse the mouth with water after using the inhaler. Avoid sharing the inhaler with other family members. Monitor for rebound congestion. Sit straight up when administering the inhaler. Shake the inhaler prior to administration.
Sit straight up when administering the inhaler. Shake the inhaler prior to administration. Rinse the mouth with water after using the inhaler. Avoid sharing the inhaler with other family members.
Factors Influencing Bioavailability
Solubility of the drug --> able to cross lipid membranes and have water-solubility Drug formulation --> must "dissolve", how well? Chemical instability --> may be unstable or destroyed in GI tract (acid labile) First-pass hepatic metabolism --> drug vs. prodrug
Which division of the nervous system is responsible for voluntary control of skeletal muscles? Sympathetic nervous system Parasympathetic nervous system Somatic nervous system Autonomic nervous system
Somatic Nervous system
Peripheral Nervous System (PNS)
Somatic motor system **Controls voluntary movement Autonomic nervous system (think automatic not voluntary) *Regulates involuntary processes **Parasympathetic **Sympathetic MEMORIZE THIS PICTURE!!
Which PD drug should you avoid a high fat diet with?
Stavelo levodopa/carbidopa/entacapone
Continuous IV Infusion
Steady state (equilibrium) plasma drug concentration is reached after continuous infusion for 4-5 half-lives. Increasing the rate of infusion will not decrease the time needed to reach steady state. Increasing the rate of the infusion will, however, increase the plasma drug concentration at steady state.
Describe the steps in synaptic transmission (5)
Step 1: Transmitter Synthesis Step 2: Transmitter Storage Step 3: Transmitter Release Step 4: Receptor Binding Step 5: Termination of Transmission
Glipizide (Glucotrol)
Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites
Glyburide
Stimulates insulin release from the pancreatic beta cells; reduces glucose output from the liver; insulin sensitivity is increased at peripheral target sites
Hypoglycemics: Action
Stimulates liver to change glycogen to glucose, used for hypoglycemia (when unconscious) Glucagon.
Anti-diarrheals
Stops further occurrence of diarrhea. Notable medicines are Loperamide "Immodium", Diphenoxylate Hcl with Atropine "Lomotil", Bismuth subsalicylate "Pepto bismul" Pepto s/e: black stools and tongue
Schedule 2 controlled substances
Substances with high potential for abuse and currently accepted medical uses. Abuse may lead to severe psychic or physical dependance. Examples - Opium, Morphine, Fentanyl, Methadone, Cocaine, and Oxycodone
Schedule 5 controlled substances
Substances with very low potential for abuse and currently accepted medical uses. The substances has very limited physical or psychological dependence liability. Examples - Codeine mixtures, Ephedrine
The nurse notes that a client's current medications include both diltiazem for a dysrhythmia and nitroglycerin. The nurse should recognize the need to closely monitor the which client assessment datum? blood pressure level of consciousness oxygen saturation levels peripheral pulses
blood pressure
Toxicology of Muscarinic Antagonists
Symptoms: dry mouth, blurred vision, photophobia, hyperthermia, CNS effects, hot/dry/flushed skin Treatment: physostigmine; inhibitor of acetylcholinesterase
describe Transmitter Synthesis
Synthesis/construction of transmitter from precursor molecules
T or F: ACh binding to muscarinic can be either inhibitory or stimulatory
TRUE
Pt teaching for clonidine
Take a bedtime to reduce sedation Record BP Monitor for low BO Chew gum, sugarless candy for dry mouth Advise about CNS depression
Beta 2
Used for Asthma: -selective B2 are preferred -most by inhalation, reduces systemic effects - causes-Lung - bronchial dilation Used to delay preterm labor -relaxes uterine sm smooth muscle Adverse effects: -Hyperglycemia in diabetes -tremor
What do anticholinergic medications do? Select all that apply. Treat target SNS organ conditions Block acetylcholine from binding to receptor sites Inhibit the PNS Stimulate the PNS Aid acetylcholine in binding to receptor sites
Treat target SNS organ conditions Block acetylcholine from binding to receptor sites Inhibit the PNS
Silver sulfadiazine (Silvadene)
Treatment of burns; usually used with open method of wound care; used to avoid acid=base complication; keeps eschar soft, making debridement easier; adverse reactions: penetrates wound slowly; administer pain medication prior to dressing change
Permethrin
Treats scabies and lice
Mesalamine
Treats ulcerative colitis and mild to moderate IBD
Guanfacine
Used for HTN adhd Adverse effects: ceros Tomis, sedation, rebound HTN Take at bedtime to minimize sedation Do not take with grapefruit juice
Lubiprostone (Amitiza)
Used for IBS-C and chronic constipation Increases fluid secretion in intestine, promotes motility Can cause diarrhea, nausea (take w/ food)
Alosetron (Lotronex)
Used for IBS-D in women that has lasted > 6 months Blocks 5-HT3 receptors resulting in firm stool and decrease in urgency and frequency of defecation Can cause constipation
Alosetron (Lotronex)
Used for IBS-D in women that has lasted > 6 months Blocks 5-HT3 receptors resulting in firm stool and decrease in urgency and frequency of defecation Can cause constipation / bowel obstruction and perforation
Trospium
Trospium Anticholinergic Drugs for Overactive bladder Nonselective muscarinic antagonist Generally well tolerated Dry mouth Constipation
T or F: most of the body's regulation/adaption of internal environments involves both muscle (somatic) and smooth, cardiac or gland functioning (autonomic)
True
PD drugs benefit patient by improving
bradykinesia gait disturbance postural instability tremor and rigidity= disturbing, but less disabling
Parasympathetic fibers emerge from:
brain and sacral spinal cord
Allopurinol interactions
Warfarin
alpha-synuclein
a potentially toxic protein synthesized by dopaminergic neurons
Memantine: Pharmacokinetics
Well absorbed after PO dosing BOTH w/wo food Peak: 3-7 hrs. Met/Exc: min metab, excret unchanged in urine Half-Life is LONG: 60-80 hrs Clearance reduced in renal impaired pts. SE: Well tolerated(Min SE)- dizzy, HA, confus, constip incidence of effects same w/placebo in trials Drug Interactions: Combo: Memantine w/another NMDA antagonist (Amantadine, Ketamine)= possible (-) effects Use combination therapy w/ CAUTION
Smooth muscle
bronchi, blood vessels, urogenital system, GI tract
Serotonin Syndrome
With any drug that increases 5-HT (e.g., MAO inhibitors, SNRIs, TCAs) hyperthermia, confusion, myoclonus, cardiovascular instability, flushing, diarrhea, seizures. -Treatment: cyproheptadine (5-HT2 receptor antagonist). Can resolve on it's own by discontinuing the drug.
Atropine Adverse effects
Xerostomia-dry mouth Blurred vision and photophobia Elevation of intraocular pressure Urinary retention Constipation Anhidrosis Tachycardia Asthma
Ondesetron Class: 5HT3 receptor antagonist
Zofran Indication: Chemotherapy N/V, postoperative N/V, radiation induced N/V Oral or Parental * Prolonges QT interval (leading to torsades de pointes)
Theophylline
a bronchodilator. It works by relaxing muscles in the lungs and chest, making the lungs less sensitive to allergens and other causes of bronchospasm. Theophylline is used to treat symptoms such as wheezing or shortness of breath caused by asthma, bronchitis, emphysema, and other breathing problems Tablet form: do not crush, chew or break open. Take with full glass of water.
Crohn's disease
a chronic autoimmune disorder that can occur anywhere in the digestive tract; however, it is most often found in the ileum and in the colon
clonic seizure
a convulsive seizure
How is hyperuricemia defined?
above 7mg/dL in men or 6 in women
Continuous Infusion
administered over 24 hours
Transmitters
are made and stored in terminal in vesicles. More transmitters =more effects on cell
miosis
constricted pupils
All antipsychotic agents block the effects of
dopamine
antiseizure drugs
drugs used for epileptic seizures
Beta blockers in glaucoma
glaucoma= elevated IOP BB important drugs in Tx of glaucoma BB differ from one discussed here.
Cimetidine (a drug for PUD) can inhibit renal excretion of pramipexole, thereby
increasing its blood level
atonic seizure
loss of normal muscle tension;
Housekeeping chores
slowing functions, at rest functions
t/f: Where acetylcholine can activate all three subtypes of cholinergic receptors, not every adrenergic transmitter (epinephrine, norepinephrine, dopamine) can interact with each of the five subtypes of adrenergic receptors
true
Glycogenolysis
turn glycogen into glucose
Beta blockers in hyperthyroidism
↑thyroid hormone associated with ↑sensitivity of the heart to catecholamines (norepinephrine, epi) normal levels of sympathetic activity can generate tachy/dysrhythmias and angina. blockade of beta-1 suppresses responses.
Levodopa: mechanism of action
↓symptoms by ↑dopamine synthesis in striatum
Functions of the Parasympathetic Nervous System (rest and digest)
Slowing of heart rate Increased gastric secretion Emptying of the bladder Emptying of the bowel Focusing the eye for near vision Constricting the pupil Contracting bronchial smooth muscle
Pharmacogenetics
Study of how genetic makeup affects response to drugs (identifying genes that account for varying drug reactions in different people) Most common DNA variation are single nucleotide polymorphisms Most focused on genes encoding: -metabolic enzymes --> alter a drug's activity -defective structural proteins --> increased susceptibility to disease
buprenorphine/naloxone
Suboxone. used to treat narcotic (opiate) addiction.
Most m. receptors are in the PNS but we do have one muscarinic receptor in our ..?
Sympathetic Nervous system
T or F: all ANS (both sympathetic and parasympathetic) preganglionic axons and all parasympathetic postganglionic axons release ACh
TRUE
Non Ergot Derivatives have less side effects b/c
they are more selective highly selective to dopamine receptors
Parkinsonism may be treated with
anticholinergic drugs
Schedule 4 controlled substances
anticonvulsants, antianxiety agents: valium, phenobarb, meprobamate
fortunately, levodopa is now available only in combination with
carbidopa carbidopa and entacapone
Other TNF antagonists
Adalimumab (Humira) SQ Cerolizumab pegol (Cimizia) SQ Infliximab (Remicade) IM
Alpha-2
receptor responsible for inhibiting the release of norepinephrine (dilates blood vessels to decrease BP) Tx: hypertension
Beta-3
receptor responsible for relaxation of the bladder and lipolysis Tx: overactive bladder
Alpha-1
receptor responsible for vasoconstriction (increase BP) Tx: nasal congestion and hypotension
Neuropharmacology
study of drugs that alter processes controlled by the nervous system
describe general steps of neural communication
"Input" is received onto dendrites or cell body. (Input = excitatory or inhibitory) If the "axon hillock" is depolarized to threshold, then an "impulse" (action potential) is generated. Action Potential (electrical current) is conveyed down axon (ie "axonal conduction.") When AP reaches the axon terminus (aka synaptic bouton), it causes vesicles containing signaling molecules (neurotransmitter) to be released into synaptic gap. Signaling molecules diffuse across synaptic gap, then bind to receptors on post-synaptic cell. Neurotransmitter— Receptor binding has effect on post-synaptic cell.
ACE inhibitors
"PRIL" ex. Captopril, Enalapril, Afosiopril Antihypertensive. Blocks ACE in lungs from converting angiotensin I to angiotensin II (powerful vasoconstrictor). Decreases BP, Decreased Aldosterone secretions, Sodium and fluid loss. Check BP before giving (hypotension) *Orthostatic Hypotension
levodopa abrupt loss effect
"on-off" phenomenon occurs at any time during the dosing interval EVEN if drug levels are HIGH "off" times may last mins-hrs over course of Tx= off times likely-↑intensity/freq
Tizanidine (Zanaflex)
- Central alpha 2 agonist; a short-acting muscle relaxer. It works by blocking nerve impulses (pain sensations) that are sent to your brain. (treats MS symptoms) S/E: Liver damage, Hypotension, Dizziness, xerostomia, weakness, QT prolongation * important * > Contraindicated with ciprofloxacin and fluvoxamine due to elevated tizanidine levels
Chlorpromazine (Thorazine)
- Chlorpromazine is used to treat psychotic disorders such as schizophrenia or manic-depression, and severe behavioral problems in children ages 1 through 12. Chlorpromazine is also used to treat nausea and vomiting, anxiety before surgery, chronic hiccups, acute intermittent porphyria, and symptoms of tetanus. S/E: - This medication can cause photophobic skin reactions and damage to the retina of the eye if exposed to direct sunlight. PTs taking this should be reminded to wear protective clothing, apply sunscreen and wear sunglasses when they are outside. sedation, orthostatic hypotension, anticholinergic effects.
treatment of hypocalcemia
- IV calcium supplementation (*calcium gluconate*) once calcium levels have been restored: - calcium citrate for maintenance - vitamin D
insulin regular (Humulin R, Novolin R)
- Short-Acting Insulin - Onset: 30-60 minutes - Peak: 2-4 hours - Duration: 5-7 hours - Nursing considerations: give 30-60 minutes before meal, can mix with NPH, ONLY insulin that can be given IV!
Schizophrenia
- Too much dopamine - Anti-psychotic will decrease dopamine - Caution: extrapyramidal for locomotor affects such as the tongue rolling and lip smacking/biting
Colchicine therapeutic use
- can be used short term to treat acute gouty attack (oral, pt. can walk within hours, inflammation is completely gone in 2-3 days) - can be used long term to prevent attacks from recurring (decreases frequency and intensity of flare ups)
vitamin D
- increases calcium resorption within the bones - decrease calcium excretion by the kidney - increases calcium absorption within the intestine
calcitonin
- released from the thyroid gland when calcium levels in the blood are too high *lowers calcium levels* - inhibiting resorption of calcium within the bones - increasing calcium excretion by the kidney does not influence calcium absorption
Alpha-1 Selective Agonists
- vasoconstriction and decongestant - treat hypotension & shocky states
Individual Variation in Drug Responses
-Body weight and composition -Age --> organ immaturity/organ degeneration -Gender -End-organ function --> kidney and liver disease -Variable absorption -Adherence --> expect pt to take drugs as prescribed -Drug interactions -Genetics
Factors contributing to drug dependence
-Dependence causing drugs -Addiction ***Degree of dependence is NOT synonymous with degree of "addiction"***
Important Drug Characteristics
-Effectiveness* -Safety* -Selectivity --> don't want the drug to do more than it has to
Drug Actions at Targets
-Hormone and neurotransmitters --> e.g., histamine receptors (cemetidine), opioid receptors (morphine), beta-receptors (metoprolol) -Enzymes --> e.g., cyclooxygenase (aspirin) -Membrane transport proteins --> e.g., voltage gated ion channels (lidocaine), ion transporters (furosemide) -Other macromolecules --> e.g., membrane lipids (amphotericin B)
Factors Affecting Distribution
-Organ blood flow --> rate of distribution determined by proportion of cardiac output received by the organs (heart, liver, kidneys > skeletal muscle > skin, fat) -Protein binding --> drugs bind to plasma proteins (only UNBOUND considered active), depends on affinity of drug for the protein, > 90% considered significant; increased protein binding = decreased distribution; can have drug competition - the drug with higher protein affinity will bind -Molecular size -Lipid solubility
Treatment for erectile dysfunction
-viagra and other ED drugs -injection of vasodilating drugs into the penis -penile prosthesis or implants -vascular surgery -vacuum device therapy (few medical procedures for female sexual dysfunction)
MAOIs (monoamine oxidase inhibitors)
-antidepressants that inhibit the action of an enzyme (monoamine oxidase) that is responsible for breakdown of NE and 5-HT Ex: isocarboxizid (marplan), phenelzine (nardil), selegiline (emsam). -can have fatal side effects (hypertensive crisis) if foods rich in amino acid TYRAMINE are consumed -thus, not used unless other classes of medication have failed -Depression with ATYPICAL features respond well to MAOIs
sympathetic
-division of the autonomic nervous system for fight-or-flight response -epinephrine and norepinephrine are main neurotransmitters -excitability
Tolerance
-the state where one must increase the dose of a drug in order to achieve/maintain the drug -Metabolic or receptor-based -Always occurs during the process of physical addiction
What are the three type of main anti-depressants discussed; what are the main side affects?
1. *Tricyclics - for severe depression* Why? chiefly used in neurotic cases; inhibits reuptake of nor-epi upon release in synapse (it stays in) 2. Monoamine Oxidase Inhibitors (MOA) used only if Tricyclics failed; patient cannot be trusted not to take overdoase or with certain S/E hypertensive crisis, hypotension, constipation; anticholinergic - blurred vision, dry mouth, urinary retention 3. New agents: "Atypical" Antidepressant Agents a. Serotonin / Dopamine reuptake inhibitors (Bupropion, wellButrin) b. Tetracyclics - not tricyclic - Advantage over Tricyclic it has slightly less anticholinergic affect *Disadvantage it can cause convulsions -even grand mal with therapeutic dosage!* Side Effects: vary, however, sexual dysfunction is common with all antidepressants. All agents work; chosen depending on S/E. All claims faster onset but truth of this claim not yet established - can be compared with tricyclics.
What are the goals of anesthesia?
1. Analgesia (narcotics, Ketamine) 2. Loss of consciousness (gases, nitrous oxide) 3. Muscle relaxation (maybe curare)
Sympathetic: cardio vascular
1. Maintains blood flow to brain, 2. Redistributes blood flow during exercise 3. compensate for blood loss (vasoconstriction)
Functions of Cholinergic (Parasympathetic) Receptors
1. Nicotinic N 2. Nicotinic M 3. Muscarinic
Noraepinephrine (Levophed)
1. No Beta 2, so just like epi except no lung effects 2. Rapid inactivation Levophed - "Leave- 'em - dead"
Metronidazole (Flagyl)
1. Used to treat anaerobic infections 2. DO NOT USED ALCOHOL (antabuse effect will be nauseous) treats mild to moderate crohns diease.
Drug therapy for spasm include 2 groups:
1. analgesic antiinflammatory drusg 2. centrally acting muscle relaxants
Fight-of-flight
1. inc HR and BP, 2. shunt blood from skin and viscera to skeletal muscle 3. dilate bronchi, 4. dilate pupils- wide eyed to see better 5. mobilize energy (glucose) need energy to fight or flee
TWO MAJOR TYPES OF DEPRESSION
1. situational or reactive 2. endogenous or neurotic - some people just depressed their whole life
Sympathetic: Temperature Regulation
1.regulating blood flow to skin 2. sweat gland secretion 3. inducing piloerection- hair follicle erection
How does hyperuricemia happen?
1: excessive production of uric acid 2: impaired excretion of uric acid
Two ways that drugs work
1: short term to relieve symptoms of an acute gouty attack 2: given long term to lower blood levels of uric acid
Alpha-1 adrenergic antagonists cause orthostatic hypotension, what is first-dose effect?
1st dose may cause fainting from severe orthostatic hypotension. Take 1st dose at bedtime to minimize.
Levodopa and 1st gen Psychotics
1st gen psychotics block dopamine receptors example: chlorpromazine, haloperidol AVOID concurrent use of these meds 2nd gen can be used safely
Propranolol (Inderal) Info
1st generation BB Non-selective= beta-1 and beta-2 beta-1= ↓HR + ↓contraction force + suppress impulse conduction through AV node= ↓CO renal beta-1= suppress secretion of renin beta-2= bronchoconstriction, vasoconstriction, ↓glycogenolysis highly lipid soluble. readily cross membranes. <30%each PO dose reaches circulation= 1st pass reaches CNS. Hepatic metabolism and then excreted in urine. Uses: HTN, angina, MI, cardiac dysrhythmias Adverse Effects: Brady, AV block, HF, Rebound cardiac excitation, Bronchoconstriction, inhibition of glycogenolysis, CNS effects. Warnings/contraindications: DM: ↓glucose, but masks signs of hypoglycemia. Can exacerbate HF, AV block, Brady, asthma, bronchospasm- contraindicated in all. Caution in patients Hx of depression. Drug Interactions: CCB (verapamil/diltiazem) Effects identical to propranolol. Excessive cardiosuppresion may result.
Dopamine Agonists
1st line drugs for PD
Chlamydia
1st line: Azithromycin 1g po single dose or Doxycycline 100mg po bid x 7 days 2nd line: Erythromycin base or fluoroquinolone(levofloxacin or ofloxacin)- No sex for 7 days after initiation of treatment- Canadian guidelines state to retest after 6 months
No matter what the precise mechanism is, neuropharmacologic drugs ultimately work by influencing
receptor activity
The nurse is preparing to administer an indirect-acting cholinergic agonist to help promote chewing and swallowing for a client on a medical-surgical unit. When will the nurse plan to administer this medication? 30 minutes prior to meals 15 minutes prior to meals 60 minutes prior to meals Anytime within the medication administration window
30 minutes prior to meals
Reversible binding occurs with
receptor on postsynaptic cell
The nurse is checking a client 's blood pressure in preparation for administering an adrenergic antagonist medication. Which systolic blood pressure is unsafe for administering this class of medication? 130 mmHg 90 mmHg 150 mmHg 110 mmHg
90
Neuroleptic Malignant Syndrome (NMS)
A rare and sometimes fatal reaction to high-potency neuroleptic drugs. Symptoms include muscle rigidity "lead pipe", fever, Sweating, autonomic instability and elevated white blood cell count. It is thought to result from dopamine blockage at the basal ganglia and hypothalamus. Treatment: supportive measures, drug therapy and immediate withdrawal of antipsychotic medication.
Drug-Receptor Interactions
A receptor is anything the drug binds to to produce its effect (including enzymes and ribosomes) -could bind as is -or cause a conformational change to receptor --> this could render receptor non-functional after dissociation) D+R <--> D-R Complex ==> response Binding can be reversible or irreversible or selective or non-selective --> selective limits the types of receptors the drug binds to which limits its effects
phenylephrine
A1 selective agonist PROTOTYPE - OTC for nasal congestion - not used for shocky states - may lead to systemic hypertension & H/A
Treat of ADHD and side effects of treatment
ADHD is treated with amphetamines • Ritalin, Concerta, Focaline and Adderall Side Effects: • CNS: too much stimulation....nervousness, anxiety, sleeplessness • Cardiovascular: to much nor-epi...increase adrenergic response. Increase HR. BP, potential arrhythmias • Weight Loss, malnutrition • Kids: suppression of growth, failure to thrive, not eat • Possible bone marrow suppression
A patient with metastatic cancer has had several fractures secondary to bone metastases. The provider orders denosumab [Xgeva]. What will the nurse teach this patient? a.Denosumab may delay healing of these fractures. b.Denosumab should be given subcutaneously every 12 months. c.Denosumab will improve hypocalcemia. d.Unlike bisphosphonates, denosumab does not increase osteonecrosis of the jaw (ONJ).
ANS: A Because denosumab suppresses bone turnover, fracture healing may be delayed. Denosumab is given every 6 months. Denosumab can exacerbate hypocalcemia. Denosumab can increase the incidence of ONJ.
A patient taking risedronate IR [Actonel] for osteoporosis reports experiencing diarrhea and headaches. What will the nurse tell this patient? a.These are common side effects of this drug. b.These symptoms indicate serious toxicity. c.The patient should discuss taking risedronate DR [Atelvia] with the provider. d.The medication should be taken after a meal to reduce symptoms.
ANS: A Diarrhea and headaches are common adverse effects of risedronate IR. These symptoms do not indicate toxicity. The side effects of Atelvia are similar to those of Actonel. Taking the medication after a meal will not reduce these effects
A nurse is providing education to a patient who will begin taking alendronate [Fosamax]. Which complication should the patient be instructed to report immediately? a.Difficulty swallowing b.Dizziness c.Drowsiness d.Pallor
ANS: A Esophagitis is the most serious adverse effect of alendronate, sometimes resulting in ulceration. The nurse should instruct the patient to report difficulty swallowing immediately, because it can be a sign of esophageal injury. Dizziness is not an adverse effect of alendronate. Drowsiness is not a symptom associated with alendronate. Pallor is not a symptom associated with alendronate.
A patient with severe glucocorticoid-induced osteoporosis will start therapy with teriparatide [Forteo]. What will the nurse expect to administer? a.20 mcg once daily subQ b.20 mcg twice daily subQ c.10 mcg once daily subQ d.10 mcg twice daily subQ
ANS: A The dose of teriparatide for all indications is 20 mcg once daily subQ.
A nurse is discussing the role of vitamin D in calcium regulation with a nursing student. Which statement by the student indicates a need for further teaching? a."Adequate amounts of vitamin D occur naturally in the diet." b."Vitamin D3 is preferred over vitamin D2." c."Vitamin D can promote bone decalcification." d."Vitamin D increases the absorption of calcium and phosphorus from the intestine."
ANS: A Vitamin D does not occur naturally in the diet. Adequate amounts are gained through fortified foods, supplements, and exposure to sunlight. Vitamin D3 is preferred. If calcium intake is not sufficient, vitamin D can promote bone decalcification. Vitamin D acts to increase the absorption of calcium and phosphorus from the intestine.
Which drugs are approved for treating osteoporosis in men? (Select all that apply.) a.Alendronate [Fosamax] b.Calcitonin c.Raloxifene [Evista] d.Teriparatide [Forteo] e.Zoledronate [Reclast]
ANS: A, D, E Only five drugs have been approved to treat osteoporosis in men, including alendronate, teriparatide, and zoledronate. Calcitonin has been tried, but without proof of efficacy. Raloxifene is a SERM, used in women only.
A patient who takes teriparatide [Forteo] administers it subcutaneouslywith a prefilled pen injector. The patient asks why she must use a new pen every 28 dayswhen there are doses left in the syringe. Which is the correct response by the nurse? a."Go ahead and use the remaining drug; I know it is so expensive." b."The drug may not be stable after 28 days." c."You are probably not giving the drug accurately." d."You should be giving the drug more frequently.
ANS: B Teriparatide is supplied in 3-mL injectors. The pen should be stored in the refrigerator and discarded after 28 days, even if some drug remains in the syringe. Although the drug is expensive, it is not correct to use what is in the syringe after 28 days. Drug may be left in the syringe even with correct dosing.
A nurse provides teaching for a woman who will begin taking supplemental calcium. Which statement by the woman indicates understanding of the teaching? a."Chewable calcium tablets are not absorbed well and are not recommended." b."I should not take more than 600 mg of calcium at one time." c."I should take enough supplemental calcium to provide my total daily requirements." d."If I take calcium with green, leafy vegetables, it will increase absorption."
ANS: B To help ensure adequate absorption of calcium, no more than 600 mg should be consumed at one time. Chewable calcium tablets are recommended because of their more consistent bioavailability. The amount of supplemental calcium should be enough to compensate for what is not consumed in the diet and should not constitute the total amount needed per day. Green, leafy vegetables reduce the absorption of calcium.
A 65-year-old female patient tells a nurse that she has begun taking calcium supplements. The nurse learns that the patient consumes two servings of dairy products and takes 1200 mg in calcium supplements each day. The patient's serum calcium level is 11.1 mg/dL. What will the nurse tell this patient? a.She should increase her dietary calcium in addition to the supplements b.The amount of calcium she takes increases her risk for heart attack and stroke c.To continue taking 1200 mg of calcium supplement since she is over age 50 d.To supplement her calcium with 10,000 units of vitamin D each day
ANS: B Women older than 50 years need 1200 mg of calcium per day. Patients should take only enough supplemental calcium to make up for the difference between what the diet provides and the RDA. This patient is getting 1800 mg/day. Excess supplemental calcium can increase risks for vascular calcification, MI, stroke, and kidney stones. She does not need to increase calcium intake. Supplementing with 10,000 units of vitamin D is indicated for documented vitamin D deficiency, which is not evident in this case.
A patient who has developed postmenopausal osteoporosis will begin taking alendronate [Fosamax]. The nurse will teach this patient to take the drug: a.at bedtime to minimize adverse effects. b.for a maximum of 1 to 2 years. c.while sitting upright with plenty of water. d.with coffee or orange juice to increase absorption.
ANS: C Alendronate can cause esophagitis, and this risk can be minimized if the patient takes the drug with water while in an upright position. Taking the drug at bedtime is not indicated. The drug may be taken up to 5 years before re-evaluation is indicated. Coffee and orange juice reduce the absorption of alendronate and should be delayed for 30 minutes after taking the drug
drug tolerance
the tendency for larger doses of a drug to be required over time to achieve the same effect
A postmenopausal patient develops osteoporosis. The patient asks the nurse about medications to treat this condition. The nurse learns that the patient has a family history of breast cancer. The nurse will suggest discussing which medication with the provider? a.Estrogen estradiol b.Pamidronate [Aredia] c.Raloxifene [Evista] d.Teriparatide [Forteo]
ANS: C Raloxifene is a selective estrogen receptor modulator (SERM) that has estrogenic effects in some tissues and antiestrogenic effects in others. It can preserve bone mineral density while protecting against breast and endometrial cancers. Estrogen promotes breast cancer and would not be indicated. Pamidronate and teriparatide are not protective against breast cancer.
A patient has severe Paget's disease of the bone. The patient asks the nurse what can be done to alleviate the pain. The nurse will suggest that the patient discuss the use of which medication with the provider? a.Alendronate [Fosamax] b.Calcifediol [25-Hydroxy-D3] c.Calcitonin-salmon [Miacalcin] d.Long-acting NSAIDs
ANS: C Salmon calcitonin is the drug of choice for rapid relief of pain associated with Paget's disease. Alendronate, calcifediol, and NSAIDs are not indicated.
A 55-year-old female patient asks a nurse about calcium supplements. The nurse learns that the patient consumes two servings of dairy products each day. The patient's serum calcium level is 9.5 mg/dL. The serum vitamin D level is 18 ng/mL. The nurse will recommend adding ____ daily and ____ IU of vitamin D3 each day. a.1200 mg of calcium once; 10,000 b.1500 mg of calcium twice; 1000 c.600 mg of calcium once; 10,000 d.600 mg of calcium twice; 2000
ANS: C Women older than 50 years need 1200 mg of calcium per day. This patient is getting 600 mg/day. She should add 600 mg/day to compensate for what she does not get in her diet, because the amount of a supplement should be enough to make up the difference. Her vitamin D level is low, so she needs a vitamin D supplement. To treat deficiency, adults older than 19 years should get 10,000 IU/day. An additional intake of 1200 mg of calcium once daily is too much calcium. An additional intake of 1500 mg of calcium twice daily is too much calcium, and 1000 IU of vitamin D is not enough to treat deficiency. An additional intake of 600 mg of calcium twice daily is too much calcium, and 2000 IU of vitamin D is not sufficient to treat deficiency.
A nurse is providing teaching for a patient with osteoporosis who has just switched from alendronate [Fosamax] to zoledronate [Reclast]. Which statement by the patient indicates a need for further teaching? a."I will need to have blood tests periodically while taking this drug." b."I will only need a dose of this medication every 1 to 2 years." c."This drug is less likely to cause osteonecrosis of the jaw." d."This drug is only given intravenously."
ANS: C Zoledronate has an increased risk of osteonecrosis of the jaw, as does alendronate. The patient is correct to identify the need for periodic blood tests. Zoledronate is given only every 1 to 2 years and is given only intravenously.
A patient is taking alendronate [Fosamax] to treat Paget's disease. The patient asks the nurse why calcium supplements are necessary. The nurse will tell the patient that calcium supplements are necessary to: a.reduce the likelihood of atrial fibrillation. b.maximize bone resorption of calcium. c.minimize the risk of esophageal cancer. d.prevent hyperparathyroidism.
ANS: D Alendronate can induce hyperparathyroidism in patients with Paget's disease; calcium supplementation can prevent this effect. Giving calcium does not reduce the incidence of atrial fibrillation, maximize bone resorption of calcium, or minimize the risk of esophageal cancer.
A postmenopausal patient is at high risk for developing osteoporosis. The patient's prescriber orders raloxifene [Evista], and the nurse provides teaching about this drug. Which statement by the patient indicates understanding of the teaching? a."I may experience breast tenderness while taking this drug." b."I may experience fewer hot flashes while taking this drug." c."I should discontinue this drug several weeks before any surgery." d."I should walk as much as possible during long airline flights."
ANS: D Like estrogen, raloxifene increases the risk of deep vein thrombosis. Patients taking this drug should be cautioned to take walks on long flights or whenever they must sit for long periods. The drug does not increase breast tenderness or decrease hot flashes. There is no need to discontinue this drug before surgery
A patient reports experiencing weakness, fatigue, nausea, vomiting,constipation, and nocturia. Total serum calcium is 10.5 mg/dL. A dipstick urinalysis shows a positive result for protein. When questioned, the patient reports taking vitamin D and calcium supplements. The nurse will counsel the patient to: a.reduce the amount of vitamin D and stop taking the calcium. b.discuss taking calcitonin-salmon [Fortical] with the provider. c.stop both supplements and discuss the use of a diuretic with the provider. d.stop taking vitamin D, reduce the amount of calcium, and increase the fluid intake.
ANS: D Vitamin D toxicity can occur, and early responses include the symptoms described. Patients should be counseled to stop taking vitamin D, reduce their calcium intake, and increase their fluid intake. It is not correct to reduce the vitamin D intake and the calcium intake. Calcitonin-salmon is not indicated. A diuretic is indicated when hypercalciuria is severe.
Consequences of Metabolism
Accelerated renal drug excretion --> conversion into more polar/water soluble compounds Drug inactivation --> conversion to inactive metabolites "Increased" or "Alternate" therapeutic action --> conversion to an [more or less] active metabolite Activation of pro-drugs --> conversion to active form of drug Changes in toxicity potential --> parent compound and metabolite potential for toxicity
When educating a group of nursing students on the mechanism of the action of various anti-arrhythmic drugs, the nurse identifies which drugs as inhibiting the beta-adrenergic receptors of the heart and the kidney? Disopyramide Amiodarone Acebutolol Propafenone
Acebutolol
Second Generation: CardioSelective BB
Acebutolol (Sectral)= beta-1 Atenolol (Tenormin)= beta-1 Betaxolol (Kerlone)= beta-1 Bisoprolol (Zebeta)= beta-1 Esmolol (Brevibloc)= beta-1 Metoprolol (Lopressor)= beta-1
what is employed at most junctions of the PNS
Acetylcholine
ACh
Acetylcholine is a neurotransmitter, which is a chemical released by a nerve cell or neuron. ... Acetylcholine causes muscles to contract, activates pain responses and regulates endocrine and REM sleep functions. Deficiencies in acetylcholine can lead to myasthenia gravis, which is characterized by muscle weakness.
Sierra Solina has been taking an AChE inhibitor, but is exhibiting signs of tachycardia and muscle weakness. After a small dose of edrophonium chloride (Enlon) isadministered, Ms. Solina shows no symptomatic improvement. What action do you expect the health care provider to take next? Discontinue the AChE inhibitor Increase the dose of the AChE inhibitor Increase the dose of edrophonium chloride (Enlon) Administer atropine sulfate
Administer atropine sulfate
Intravenous Administration
Administration directly into systemic circulation, increased reliability and control of the dose of drug reaching circulation but can be very dangerous --> rapid admin = serious toxicity many but not all will have a relatively immediate effect
Which statements accurately describe the mechanisms of action of adrenergic drugs? Select all that apply. Adrenergic agonists inhibit the SNS. Sympathomimetics inhibit the SNS. Adrenergic antagonists inhibit the SNS. Adrenergic agonists stimulate the SNS. All adrenergic drugs produce a fight-or-flight response.
Adrenergic antagonists inhibit the SNS. Adrenergic agonists stimulate the SNS.
Neostigmine (Prostigmin) Adverse effects
Adverse effects: excessive muscarinic stimulation, neuromuscular blockade Treat for adverse effects: Atropine
Factors Affecting Rate of Metabolism
Age Induction or inhibition of drug-metabolizing enzymes Competition between drugs First-pass effects
Cholinergic (Parasympathetic) Receptors
Also called Parasympathetic Refers to cells that use acetylcholine (ACh) as their synaptic transmitter.
Beta-1
receptor responsible for an increased HR and force of contraction Tx: cardiac arrest, heart failure, shocky states
Parkinson's Disease Injectables
Apomorphine [Apokyn] Dopamine Agonist- Non Ergot Derivative Prepared: 10mg/mL, 3-mL for multi-dose pen Dose: 2-6 mg (0.2-0.6 mL) SQ each "off" episode Max: 5 doses/day Other: start antiemetic 3 days prior to 1st dose Ex. trimethobenzamide 300mg TID 72hrs prior Benztropine [Congentin] Centrally Acting Anticholinergic Drugs Prepared: 1mg/mL, in 2-mL vials Dose: 0.5-1mg QHS⇢⇡0.5mg Q5-6days Max: 6mg/day Other: IM injectable preferred. In PD there is NO advantage in IV admin
Ciprofloxacin (Cipro)
Antibiotic, treats crohns, used with infliximab.
Syphilis treatment (primary, secondary, early latent)
Antibiotics: large, injected dose of penicillin is most effective Benzathine penicillin G 2.4 million units IM single dose Latent: Benzathine penicillin G 7.2 million units total2.4 million units IM weekly X 3 weeks
Oxybutin
Anticholinergic Drugs for Overactive Bladder Oxybutynin (Ditropan XL, Oxytrol, Gelnique) Act at M3 muscarinic receptors
Darifenacin
Anticholinergic Drugs for Overactive bladder Greatest degree of M3 selectivity Reduced OAB symptoms while having no effect on M1 in brain and M2 in heart Dry mouth and constipation
Risperidone (Risperdal)
Antipsychotic (Atypical) rapid-acting used for schizophrenia and acute bipolar mania. Absorbed rapidly, not effected by food, peaks 1 hour after dosing. Excreted through urine. S/E: increases prolactin levels but symptoms uncommon. Metabolic effects. Sedation in large doses.
Quetiapine (Seroquel)
Antipsychotic (Atypical). Treats: Schizophrenia, major depression, bipolar Improves positive symptoms and lowers negative symptoms by blocking 5-HT2 receptors and D2 receptors. CYP3A4 - hepatic metabolism and excreted in urine and feces. S/E: metabolic effect, cataracts, long Q-T
A common therapeutic use for benzodiazepines is
the treatment of anxiety disorders
Life Cycle of Acetylcholine
As soon as Ach released from receptor, almost immediately destroyed by aceylcholinesterase
Levodopa and Pyridoxine (Vitamin B6)
B6 can ↓ amount of levodopa reaching CNS by accelerating decarboxylation of levodopa in periphery HOWEVER b/c levodopa is now always combined with carbidopa (suppresses decarboxylase activity) this potential clinical interaction is no longer a concern.
Adverse effects in neonates for beta blockade (1 & 2)
BB during pregnancy= residual effects on infant BB can remain in circulation for days. At risk for: bradycardia (beta-1 blockade) respiratory distress (beta-2 blockade) hypoglycemia (beta-2 blockade)
Beta blockers in Heart failure
BB now considered standard therapy for HF. Used to be absolute contraindication. Only (3) BBs currently shown effective for HF. (1) Bisoprolol (2) Metoprolol (3) Carvedilol
PD drugs: Centrally Acting Anticholinergic Drugs
Benztropine [congentin] tab: 0.5, 1, 2 mg injectable: 1mg/mL in 2mL vials 0.5-1 mg QHS (initial)⇢⇡0.5mg Q 5-6days Max: 6 mg/day IM preferred. No advantage to IV in PD. Trihexyphenidyl [generic] tab: 2, 5 mg Elixir: 0.4/mL 1mg QD (initial)⇢⇡2mg Q 3-5days Max: 15mg/day
Beta blockers in Cardiac dysrhythmias
Beta-adrenergic blocking agents especially useful in dysrhythmias that involve excessive electrical activity in the sinus node and atria. block beta-1 by= (1) ↓rate of sinus node discharge. (2) suppress conduction of atrial impulses through AV node. preventing the ventricles from bing driven at an excessive rate.
The nurse knows that which class of drugs prevents epinephrine and norepinephrine from occupying receptor sites on the cell membranes?
Beta-adrenergic blocking drugs
PK Drug-Drug: Absorption
Binding/chelation in the gut --> prevent absorption Altered gastric/intestinal motility Changes in bacterial flora Food effects --> food delays rate of absorption but could increase or decrease the extent of absorption, food increases acid release which can affect acid-labile drugs
SSNRIs (selective serotonin and norepinephrine reuptake inhibitors)
Block 5-HT reuptake and thereby increase 5-HT in the synapse. Examples: Desvenlafaxine (Pristiq), Duloxetine (Cymbalta), Venlafaxine (Effexor XR), LEvomilnacipran (Fetzima).
Before administering a cholinergic antagonist to a client, for what should you specifically assess? Select all that apply. Bowel and bladder habits Symptoms of cholinergic crisis History of glaucoma Skin elasticity History of malignant hyperthermia
Bowel and bladder habits Symptoms of cholinergic crisis History of glaucoma History of malignant hyperthermia
Adverse Effects of beta-1 blockade
Bradycardia (beta-1 receptors) beta-adrenergic agonist to compete for binding Reduced Cardiac Output (↓tissue perfusion) extreme caution in HF patients Precipitation of Heart Failure (↓cardiac fx) actually causes HF. notify PCP for edema, SOB. AV Heart Block (can suppress AV conduction) contraindicated w/ pre-existing AV block. Rebound Cardiac Excitation (w/abrupt cessation) long-term use. sensitize heart to catecholamines.
Dosing/Administration: Dopamine Agonists- Ergot Derivitatives [Bromocriptine & Cabergoline]
Bromocriptine [Cycloset, Parlodel] Cycloset: 0.8-mg tablet (within 2hrs of awakening) Parlodel: 5-mg tablet -Initial: 1.25mg BID slowly↑dose until desired resp or intolerable SE -Maintenance: 30mg-100mg/day Cabergoline [Dostinex, Generic in US] 0.5-mg tablet -Initial: 1 mg QD ↑using 0.5-1 mg at 1-2 week intervals -Maintenance: 2-3 mg/day
The nurse would instruct a client receiving acebutolol about which adverse effect? Improved exercise tolerance Bronchospasm Hypertension Increased libido
Bronchospasm
What are possible adverse effects of various nonselective beta-adrenergic antagonists? Select all that apply. Bronchospasms Loss of energy in skeletal muscles Risk of hyperlipidemia Increased catecholamine action Reduced intraocular pressure
Bronchospasms Loss of energy in skeletal muscles Risk of hyperlipidemia
Bethanechol Adverse effects
CV: Hypotension GI: Increased tone and motility Exacerbation of asthma Dysrhythmias in pts in hyperthyroidism
Enzyme Induction
CYP Substrate + CYP Inducer --> decreased substrate concentration and decreased substrate efficacy
Enzyme Depletion/Competition
CYP Substrate + CYP Substrate --> increased, decreased, or even substrate concentration and increased, decreased, or even efficacy or toxicity
Dronabinol (Marinol)
Cannabinoid Used for chemo N/V and as an appetite stimulant in AIDS and Cancer patients Can cause dissociation/dysphoria, hypotension, tachycardia
Four drugs approved for treating AD dementia
Cholinesterase inhibitors Donepezil Galantamine Rivastigmine NMDA recep antagonist (N-methyl-D-aspartate) Memantine
Phase II Metabolism
Conjugation reactions with endogenous substance to facilitate elimination --> forms a larger, more water soluble substance Most metabolites are inactive Acetylation, glucoronidation, sulfation
Mnemonic for Muscarinic Toxicity
DUMBELS D: Diaphoresis/Diarrhea U: Urination M: Miosis B: Bradycardia/Bronchospasm/Bronchochorrhea E: Emesis L: Lacrimation S: Salivation
Memorize the continuum Chart Stimulation Increases: Sensory Acuity Motor Activity Depression Inhibits: Sensory Acuity Motor Activity
Death Convulsions or Seizures Tremors & Hallucinations Anxiety Euphoria NORMAL - NEUTRAL Sedation (Drowsy) Hypnosis (Sleep) General Anesthesia Coma Death
The nurse is preparing to administer a beta-adrenergic antagonist to a client. The nurse anticipates that this medication will have which effects on the client? Select all that apply. Increased conduction through the AV node Increased blood pressure Decreased heart rate Decrease in angina Decreased force of myocardial contraction
Decreased heart rate Decrease in angina Decreased force of myocardial contraction
Tachyphylaxis
Decreased response to drug as a result of repeated administration; tolerance -adaptive process in response to chronic receptor occupation/saturation -depletion or marked reduction of the ant of NT responsible for creating the drug's effect (sudafed, cocaine, amphetamines) -increase in the number of receptors needing to be occupied (beta-blocker) -metabolic tolerance due to accelerated drug metabolism
Metformin
Decreases hepatic glucose production, decreases intestinal absorption of glucose and improves insulin sensitivity (increases peripheral glucose uptake and utilization)
The nurse is visiting the home of a client who is prescribed antidysrhythmic medication. The nurse will teach the client to report which possible adverse effect? Improved mentation Improved functional status Dizziness Increased energy
Dizziness
The nurse is caring for a client who is experiencing tachycardia, muscle weakness, and respiratory distress. To determine whether he is experiencing a myasthenic crisis, which medication should be administered? Mecamylamine hydrochloride (Inversine) Atracurium besylate (Tracrium) Edrophonium chloride (Enlon) Succinylcholine chloride (Anectine)
Edrophonium chloride (Enlon)
Murray Lefkowitz presents with symptoms of ptosis, diplopia, excessive muscle fatigue, and difficulty swallowing. What drug can the health care provider prescribe for Mr. Lefkowitz, in order to make a diagnosis? Prednisone (Orasone) Edrophonium chloride (Tensilon) Cyclosporine (Sandimmune) Pyridostigmine bromide (Mestinon)
Edrophonium chloride (Tensilon)
Uses of clonidine
HTN Severe pain ADHD Off label: Opioid withdrawal Smoking cessation Tourette's
Alpha blockers in reversal of alpha-1 agonist toxicity
HTN produced r/t excessive alpha-1 activation reverse vasoconstriction w/ alpha-blocking agent phentolamine= for IV infiltration. reverse constrict
The nurse is educating a client about a spinal cord injury. Which statement by the client indicates the need for further teaching regarding the effect the injury will have on the autonomic nervous system? "My breathing may be affected by the injury." "I won't be able to feed myself." "My blood pressure may be affected by the injury." "I may not have control of bladder functions."
I wont be able to feed myself
Galantamine [Razadyne, Razadyne ER]
IR tabs: 4, 8, 12 mg PO SOLN: 4mg/mL IR/SOLN: 4mg BID x 4wks⇢⇡by 4mg BID Q 4wks Maintenance: 8-12 mg BID Admin: w/ morning & evening meals ER caps: 8, 16, 24 mg 8mg QD x 4wks⇢⇡16mg QD x 4wks⇢⇡24mg QD Maintenance: 16-24 mg QD Mod Hepatic/Renal Dys: 16 mg QD (max) Severe impairment: AVOID
Methotrexate
Immunosuppressant used to treat certain types of cancer or to control severe psoriasis or rheumatoid arthritis that has not responded to other treatments. It may also be used to control juvenile rheumatoid arthritis. (aka Rheumatrex) SE: nausea, feeling tired, fever, increased risk of infection, low white blood cell counts, and breakdown of the skin inside the mouth.
Can we prevent Alzheimer's disease or delay cognitive decline?
In 2010, Preventing Alzheimer's Disease and Cognitive Decline stated that we have NO good evidence supporting association of any modifiable factor w/ reduced risk for AD. STUDIED FACTORS: diet, exercise, social interaction, economic status, nutritional supplements, medications, environmental toxins
A nurse is caring for a patient on dopamine therapy. The patient is also to be administered phenytoin under close supervision. Which of the following adverse reactions should the nurse monitor for in the patient?
Increased risk of seizures
CNS Stimulants - how do they work? What are the main types we talked about in class the main indications for use.
Increases excitability of the CNS increases levels of norepinephrine in the brain -amphetamines, xanthines, cocaine
The nurse is teaching a client how antiepileptic medications can be used to treat her seizure disorder. The nurse plans the teaching based on the knowledge that medications affect the synaptic transmission through which means? Select all that apply. Enhancing the storage of neurotransmitters Increasing or decreasing neurotransmitter synthesis Increasing or decreasing the release of neurotransmitters Stimulating or inhibiting the autonomic nervous system Preventing the breakdown of neurotransmitters
Increasing or decreasing neurotransmitter synthesis Increasing or decreasing the release of neurotransmitters Stimulating or inhibiting the autonomic nervous system Preventing the breakdown of neurotransmitters
Methotrexate
Management of RA nonbiologic DMARDs Reduce activity of T & B lymphocytes Slow progression 3-6 months
Tumor necrosis factor antagonists
Management of RA with Biological DMARDs (uses DNA within body not man made) Blocks TNF from starting the inflammatory process in the joint Decrease inflammation
Etanercept (Enbrel)
Management of RA with Biological DMARDs (uses DNA within body not man made) TNF antagonists SQ Mild to moderate RA Binds to TNF Delays progression of joint damage, suppresses signs and symptoms of joint damage
What is true about cholinergic antagonists and adrenergic agonists? Select all that apply. Many bodily effects are similar Mechanisms of action are different Results differ dramatically Both block the action of ACh Mechanisms of action are similar
Many bodily effects are similar Mechanisms of action are different
Ganglionic blocking agents
Mecamlamine
Immunomodulating drugs
Medications that therapeutically alter a patient's immune response to malignant tumor cells Drugs that modify the body's own immune response so that it can destroy various viruses and cancerous cells Second line agents in inflammatory bowel.
Dopamine
Most action in CNS: -Dilates renal blood vessels--> increase renal blood flow. -To prevent kidney failure in shock -Enhances cardiac performance -Dopamine is only available drug Table 13-4 p. 112 Heart Failure - inc cardiac contraction Acute Renal Failure - inc renal blood flow Adverse Effects - -tachycardia -dysrhythmias -angina -necrosis Drug Interactions - MAO (inc effects), TCA (inc), General anesthetics (inc), Diuretics (improve kidney effects)
Apomorphine Adverse Effects:
Most common: inject site reactions, hallucinations, yawning, drowsy, dyskinesias, rhinorrhea, N/V Rare cases: sleep attacks, CV symptoms (angina, MI, cardiac arrest, sudden death), fainting, postural hypotension, hyper sexuality, enhanced erection, priapism
Levodopa/Carbidopa
Most effective therapy for PD
Autonomic Control Baroreceptor Reflex
Most important.! Frequently opposes our attempts to modify BP with drugs Baroreceptors in carotid sinus and aortic arch - Measure and detect blood pressure Tells brain if BP is up or down Brain sends impulses to to heart/blood vessels to adjust BP Receptors cause blood vessels to constrict or relax depending on blood pressure
Autonomic Regulation of the Body
Most structures are controlled by: both sympathetic and parasympathetic nerves.
Distribution
Movement of drugs in the body drugs are distributed to body fluid, organs, and tissues (aka compartments) via the circulation; will occur until there is an equilibrium of drug concentration between the vascular space and the tissues.
Eluxadoline (Viberzi)
Mu/Kappa opioid receptor agonist and delta opioid receptor antagonist in the gut used to treat IBS prone diarrhea
Baclofen
Muscle relaxant, GABAb receptor agonist, produces hyperpolarization by increased potassium conductance also used as an antispasmodic agent. Baclofen is used to treat muscle symptoms; such as spasm, pain and stiffness; caused by multiple sclerosis, spinal cord injuries, or other spinal cord disorders. It is given intrathecally (directly into the spinal cord) or orally (by mouth).
The nurse is educating a client on the effects that adrenergic antagonists have on the body. Which statement by the client indicates an appropriate understanding of the teaching provided? "My medication will cause my eyes to be dry." "My medication will decrease my heart rate." "My medication will cause my mouth to be dry." "My medication will increase my blood pressure."
My medication will decrease my heart rate
Adverse effects of sulfasalazine
N/V/D Anorexia, abd pain Hepatitis Bone marrow suppression Not given to patients with sulfa allergied
Life Cycle of Norepinephrine (Epi)
NE transmission terminated by reuptake. Then taken back into vesicles or inactivated by MAO (monoamine oxidase) Epi is basically the same
Drugs for Neuropsychiatric Symptoms
NEUROPSYCHIATRIC SYMPTOMS: agitations, aggression, delusions, hallucinations Occur in >80% pts with AD 2 ATYPICAL ANTIPSYCH= ↓NEUROPSYCH S/S Risperidone [Risperdal] Olanzapine [Zyprexa] BUT BENEFITS ARE MODEST SLIGHTLY INCREASE MORTALITY (CV, infection) Mult Drug classes tried as Tx= BUT few effective including: antipsych, cholinesterase inhibit, mood stabilizers, antidepressant, anxiolytics, NMDA recep agonists LITTLE/NO EVIDENCE OF BENEFIT FROM: conv antipsych- (haloperidol, chlorpromazine) mood stabile (valproate, carbamazepine, lithium) antidepressants memantine
Parkinson's other symptoms
NON-MOTOR SYMPTOMS: autonomic disturbances (most common) sleep disturbances depression psychosis dementia
Memantine: Mechanism of Action
NORMAL PHYSIOLOGY: Resting post-synaptic neuron: Mg+ @NMDA receptor channel- Blocks Ca+ entry Binding- glutamate+NMDA recep= displaces Mg+ allowing Ca+ to enter glutamate disassociates from receptor. Mg+ returns to channel=blocks further Ca+ inflow *the brief period of Ca+ entry constitutes a "SIGNAL" in the learning and memory process. PATHOPHYSIOLOGY: presyn-neuron⇢slow/steady glutamate leakage keeps NMDA receptor= constantly active state allowing excessive CA+ influx which can impair memory/learning can eventually cause neuronal death. MEMANTINE EFFECT: blocks Ca+ entry⇢extracellular glutamate low allows intracellular Ca+ levels to normalize when glutamate burst released-action potential high level glutamate result⇢displaces memantine causes brief period of Ca+ entry glutamate diffuses away⇢memantine reblocks stops further Ca+ entry despite low glutamate levels in the synapses.
Drug therapy for RA
NSAIDs & glucocorticoids- pain, inflammation Disease modifying Anti-rheumatic drugs (DMARDs)
Analgesics - narcotic vs. non-narcotic
Narcotics (Opioid): •Acts on CNS •For *severe* pain •Associated with tolerance abuse, physical dependence Non-Narcotic: •Acts on periphery & CNS •for low to moderate dependence pain such as headache arthritis, peripheral pain •not generally abused and does not cause addiction
Levodopa: Adverse Effects
Nausea & vomiting Dyskinesias Cardiovascular effects Psychosis CNS Effects Other: Darken sweat and urine (harmless) may activate malignant melanoma
Cholinesterase inhibitors
Neostigmine, Physostigmine
Neupogen (filgrastim)
Neupogen is a man-made form of a protein that stimulates the growth of white blood cells in your body. White blood cells help your body fight against infection. Neupogen is used to treat neutropenia, a lack of certain white blood cells caused by cancer, bone marrow transplant, receiving chemotherapy, or by other conditions
Ganglion Stimulating agents
Nicotine
Carbidopa: mechanism of action
No effects on its own inhibits decarboxylation of levodopa in intestine & peripheral tissues=↑levodopa available to CNS does NOT prevent in conversion of levodopa to dopamine by decarboxylases in brain b/c can't cross the BBB
Administration: Transdermal (TTS) Parkinson's Med
ONLY= Rotigotine (nonergot/dopamine agonist) Apply to clean, dry, hairless, intact skin. Rotate site to ↓skin irritation/reaction Allow {2 wks} before applying TTS in same spot Ensam- marketed patch for Seleginine (MAO-B inhibitor) BUT not approved in mgmt of PD.
Blood vessels are
Only innervated by the sympathetic nerves
Calcitonin
Osteoporosis treatment: a man-made form of a hormone that occurs naturally in the thyroid gland. It increases deposition of calcium and phosphate in the bone and lowers levels in the blood, so effectively it inhibits calcium resorption by binding to a specific receptor on the osteoclasts, and inhibits their action.
if a patient is not able to pee what drug will we give them??
Parasympathetic Agonists (makes parasympathetic stuff work) i.e lower heart rate constricts bronchi stimulates intestioinsl motility etc
Degradation of alpha-synuclein requires (2) other proteins
Parkin- enzyme that catalyzes the binding of alpha-synuclein to ubiquitin Ubiquitin- when bound to ubiquitin alpha-synuclein can be degraded
The nurse is describing how medication can affect synaptic transmission. The nurse correctly states that medications are capable of what actions? Select all that apply. Preventing the breakdown or reuptake of neurotransmitters after the action potential is conveyed Binding to the postganglionic cells to stimulate or inhibit the autonomic nervous system response Increasing the storage of neurotransmitters in synaptic vesicles Increasing or decreasing the release of neurotransmitters Increasing or decreasing neurotransmitter synthesis
Preventing the breakdown or reuptake of neurotransmitters after the action potential is conveyed Binding to the postganglionic cells to stimulate or inhibit the autonomic nervous system response Increasing or decreasing the release of neurotransmitters Increasing or decreasing neurotransmitter synthesis
Alpha 1 (Sympathetic)
Primarily present in the blood vessels Vasoconstriction 1. Eyes dilate (mydriasis) 2. Blood vessels constrict- BP up 3. Male sex organs - ejaculation 4. Prostatic capsule - contraction (BHP need Alpha 1 blockers) 5. Bladder - contraction of muscles at 6. bottom of bladder (urinary retention)
Topical Administration
Produce a localized effect. Application to skin, eyes, nose, mouth, throat, rectum, vagina
Clonidine
Promoted bradycardia Vasodilation Lipid soluble Readily absorbed Single dose may last 24 hours
Amantadine does what?
Promotes dopamine release
Bioavailability (F)
Proportion of the drug that reaches the systemic circulation after oral administration "how much you really absorb" NOTE: (F) of IV formulation considered 1.0 (100%) Bioavailability = AUC oral / AUC injected x 100
PPIs
Proton-pump inhibitors - pronounced and long-lasting reduction of gastric acid production - destroyed by stomach acid (take on empty stomach) - work really well - "attack from the back" - used as a controller Ex. Omeprazole (Prilosec)
Potential interventions to IMPROVE or MAINTAIN cognitive function: MEDICATIONS
QUALITY OF EVIDENCE SHOWS NO BENEFIT: Cholinesterase Inhibitors Statins Estrogen Antihypertensives NO BENEFIT BUT POSSIBLE INCREASED RISK: Non-Steroidal Anti-Inflammatory Drugs (NSAIDS)
Potential interventions to IMPROVE or MAINTAIN cognitive function: NUTRITION
QUALITY OF EVIDENCE SHOWS NO EFFECT/NO CONSISTENT EFFECT: Vitamin E Vitamin B6 Vitamin B12 Folic Acid
Potential interventions to delay ONSET of Alzheimer's disease: MEDICATIONS
QUALITY OF EVIDENCE SHOWS POSSIBLE BENEFIT: Statins INCREASED RISK: Celecoxib, Naproxen Estrogen + Progestin NO BENEFIT: Cholinesterase Inhibitors Antihypertensives Estrogen (alone)
Your client, Mario Sabatini, has survived myocardial infarction. Mr. Sabatini has just been prescribed carvedilol (Coreg) for hypertension and left ventricular dysfunction. In reviewing Mr. Sabatini's medical history, you see that he also suffers from occasional bronchial asthma attacks. As his nurse, what should you do? Question the prescription of an alpha-adrenergic antagonist. Question the prescription of an adrenergic agonist. Question the prescription of a selective beta1-adrenergic antagonist. Question the prescription of a nonselective beta-adrenergic antagonist.
Question the prescription of a nonselective beta-adrenergic antagonist.
Nonlinear Pharmacokinetics
Rate of elimination is constant regardless of amount of drug present Dosage increases saturate binding sites and result in non-proportional increase/decrease in drug levels May also be a result of "saturated" metabolism
Alpha blockers in Raynaud's
Raynaud= PVD w/ vasospasm in toes/fingers S/S= sensations of pain and cold. alpha blockers suppress symptoms by preventing alpha-mediate vasoconstriction generally ineffective against other PVDs. only relieve symptoms in Raynaud's.
Gout
Recurrent inflammatory disorder- seen mainly in men Disease of altered purine metabolism Hyperuricemia- Uris acid level greater than 7mg/dL in men or greater than 6mg/dL in women Tophi Caused by excessive production of uric acid, impaired renal excretion of uric acid
Adverse Effects of Alpha-2 Blockade
Reflex tachycardia- response to alpha-1 block peripheral alpha-2 located presynaptically & activation inhibits NE release. If alpha-2 are blocked than release of NE ↑. b/c reflex tachy caused by block of alpha-1 is ultimately result of ↑firing of sympathetic nerves of the heart and b/c alpha-2 blockade will cause each nerve impulse to release ↑amount of NE. alpha-2 blockade will potentiate reflex tachy imitated by blockade of alpha-1 receptors drugs such as phentolamine (blocks alpha-2 and alpha-1) cause greater reflex tachycardia than do drugs that block alpha-1 receptors only.
Functions of the Sympathetic Nervous System (fight or flight)
Regulating the cardiovascular system Regulating body temperature Implementing the acute stress response homeostatic objectives
describe Transmitter Release
Release of transmitter is triggered by the arrival of an action potential at the axon terminal The action potential initiates a process in which vesicles undergo fusion with the terminal membrane, causing release of their contents into the synaptic gap
A client has a complex cardiac history that includes recurrent ventricular fibrillation. After the failure of more conservative treatments, the care team has introduced oral amiodarone. What assessments should be prioritized by the nurse who is providing care for this client? Orientation and cognition Respiratory assessment Neurological assessment Active and passive range of motion
Respiratory assessment
Adrenergic (Sympathetic) Receptors
Responds to norepinephrine or epinephrine There are subtypes receptors Alpha 1 Alpha 2 Beta 1 Beta 2 The term also pertains to the receptors acted on by norepinephrine, that is, the adrenergic receptors.
Neurotransmitter dissociates from receptor, and then has three possible fates:
Reuptake Enzymatic degradation Or, diffuse away and get absorbed into extracellular fluid, then into venous system
Alendronate (Fosamax) - PO
SIDE EFFECTS: - Uncommon, but can cause esophagitis and esophageal ulcers - Can see musculoskeletal pain, ocular inflammation, and atypical demure fractures NURSING CONSIDERATIONS: - Taken at least 30 minutes before breakfast with full glass of water
Autonomic Control Feedback Regulation (Reflex)
Self-adjustment system Sensor (detects information) + effector (make changes/adjustment) = ANS feedback loop = reflex
DEA Schedules of Controlled Substances
The Controlled Substances Act of 1970 regulates the manufacturing, distribution, and dispensing of drugs that are known to have abuse potential. The Drug Enforcement Agency (DEA) is responsible for the enforcement of these regulations. The controlled drugs are divided into five DEA schedules based on their potential for abuse and physical and psychological dependence.
what influences the body by releasing epinephrine into the bloodstream, which then produces effects much like those that occur in response to stimulation of postganglionic sympathetic nerves
The adrenal medulla
Steady State
The amount of drug administered is equal to the amount of drug eliminated within on dosing interval "drug entering = drug leaving" "plateau"/constant serum drug level Usually about 4-5 half lives to reach steady state
A nurse is the cardiac care unit is preparing to hang an intravenous dose of dofetilide (Tikosyn) for a client who has just been admitted. What is the most likely goal of this intervention? To treat sinus bradycardia accompanied by hypotension To convert the client's atrial fibrillation to normal sinus rhythm To treat the client's ventricular tachycardia To resolve the client's uncompensated heart failure
To convert the client's atrial fibrillation to normal sinus rhythm
What are the four main Transmitters used for the Peripheral Nervous System
Transmitters 1. Acetylcholine (Ach) - multiple locations 2. Norepinephrine (NE) -- sympathetic 3. Epinephrine (Epi) - adrenal medulla 4. Dopamine (Dopa) - mostly CNS, but dopamine receptors in PNS Receptors 1. Cholinergic--> (Parasympathetic)--- responds ACH 2. Adrenergic--> Sympathetic--responds to norepinephrine or epinephrine (also has subtypes)
Analgesics
Treating Pain agents that relieve pain without a loss of consciousnes Two Kinds: 1. Narcotics *(morphine sulfate, methadone, fentanyl and oxycodone)* 2. Non-Narcotics *(salicylate, acetaminophen, NSAIDS)
Laxatives
Used to ease or stimulate defecation Soften the stool Increase stool volume Hasten fecal passage through the intestine Facilitate evacuation from the rectum *Misuse comes from misconceptions of what constitutes normal bowel function
Estimating CrCL
Uses ideal body weight (IBW, kg) unless actual body weight < IBW - then use ABW -males 50 + [2.3 x (# of inches > 60in.)] -females 45 + [2.3 x (# of inches > 60in.)] CrCL = [140 - age (yrs)] x IBW (kg) / 72 x serum creatinine (SCr in mg/dL) --> (x 0.85 if female) For pt >65 yrs with SCr <1.0 mg/dL, use minimum of 1 for SCr in calculation
Terbutaline (Brethine)
Uses to relax uterine smooth muscle to inhibit uterine activity Stops preterm labor Also used for asthma attacks.
Oprelvekin (Neumega)
Uses: stimulate platelet production, thrombocytopenia related to cancer. Side effects: fluid retention, papilledema, cardiac dysrhythmia Nursing interventions: administer within 6-24 hr after chemotherapy, subcutaneous
Adverse effects of Probenecid
Usually well tolerated, but mild GI effects occasionally occur; take with food Rash
Antipsychotics (neuroleptics)
a class of psychotropic medications used for the treatment of schizophrenia and other disorders that involve psychosis. Ex. olanzapine, risperidone, haloperidol. MAOI
seizure
a disorder that results from abnormal electrical discharges from the cerebral neurons, characterized by a loss or a disturbance of consciousness and usually involuntary uncontrolled movements
If drug-induced dyskinesias are a primary concern then...
a dopamine agonists would be preferred
first generation antipsychotics
a group of medications originally developed to combat psychotic symptoms by reducing dopamine levels in the brain; also called conventional or typical antipsychotics block receptors for dopamine, acetylcholine, histamine, and norepinephrine Ex. (low potency): Chlorpromazine, Thioridazine s/e orthostatic hyposension, long Q-T syndrome, high sedation (medium potency): loxapine, perhenazine, s/e moderate sedation (high potency):fluphenazine, haloperidol, pimozide, thiothoxene, frifluoperizine s/e movement problems
antiemetic
a medication that is administered to prevent or relieve nausea and vomiting
MRSA (methicillin-resistant Staphylococcus aureus)
a mutated strain of the bacterium Staphylococcus aureus that is resistant to the antibiotic, methicillin.
Spironolactone (Aldactone)
a potassium-sparing diuretic (water pill)that prevents your body from absorbing too much salt and keeps your potassium levels from getting too low. used to treat heart failure, high blood pressure (hypertension), or hypokalemia (low potassium levels in the blood).
Hydrochlorothiazide
a thiazide diuretic (water pill) that helps prevent your body from absorbing too much salt, which can cause fluid retention. HCTZ treats fluid retention (edema) in people with congestive heart failure, cirrhosis of the liver, or kidney disorders, or edema caused by taking steroids or estrogen. This medication is also used to treat high blood pressure (hypertension). No digoxin or nsaids.
Sedatives, Hypnotics, and Anxiolytics
a.k.a. Mood Depressants. The word "Sedative = Calming, "Hypnotics = Sleep - inducing, "Anxiolytics = Decrease Anxiety.
anoxia
absence of oxygen
regulation fo calcium levels
absorbed in the small intestine excreted by the kidneys reabsorbed by the bones regulated by: - parathyroid hormone - vitamin D - calcitonin
Fiber Laxatives
absorbs water, softening feces and increasing their mass. Can be digested by colonic bacteria, whose subsequent growth increases fecal mass. ex. Bran, veggies and fruits. Meds: mehylcellulose, psyllium, polycarbophil
Metabolism
accounts for decline of plasma drug concentrations liver is the major site of metabolism, other sites include: gut, kidneys, brain, lungs, skin -primary purpose is to inactivate the agent or detoxify drugs that can harm the body -can also convert pro-drugs to an active state -metabolites are usually more water soluble to facilitate excretion
Neurotoxic fibrils form as result of
accumulation of alpha-synuclein inside the cell
After successful treatment for a myocardial infarction, a 69-year-old man has developed a ventricular arrhythmia. His care team has opted for treatment with a Class II antiarrhythmic. The nurse would understand that this client is likely to be prescribed: lidocaine. verapamil. acebutolol. amiodarone.
acebutolol
SNS - one of the two exceptions, transmitter released at postganglionic sympathetic neurons that go to sweat glands
acetylcholine
which enzyme is primarily responsible for the degradation of acetylcholine?
acetylcholinesterase
Ergot Derivatives have been associated with valvular heart disease. Why?
activation of serotonin receptors on heart valves
Probenecid actions
acts on renal tubules to inhibit reabsorption of uric acid prevents formation of new tophi and facilitates regression of existing tophi
Beta-2
receptor responsible for bronchodilation and promoting GI & uterine relaxation Tx: asthma, premature labor contractions
Levodopa and MAOIs
admin of levodopa can cause a hypertensive crisis if taking nonselective inhibitor of MAO. Levodopa ↑stores of dopamine and NE by promoting synthesis of both neurotransmitters Intraneuronal MAO serves to inactivate dopamine and NE, inhibition of MAO allows ↑stores of both to grow even larger both dopamine and NE promote vasoconstriction release in massive amounts leads to massive vasoconstriction causing BP to rise dangerously high AVOID: w/d MAOIs 2 wks before levodopa
Levocardopa pharmokinetics
administered orally undergoes rapid absorption from small intestine food delays absorption= delays gastric emptying high-protein foods ↓effects= neutral amino acids compete w/ levodopa for intestinal absorption and for transport across BBB
Bolus
administered over seconds to minutes
Short/Intermittent Infusion
administered over ~30 minutes to several hours
fibers that release norepinephrine
adrenergic fibers
sympathetic postganglionic neurons
adrenergic neurons
Adverse Drug Reactions
adverse effects = side effects 2 types: -dose dependent: arise from extension of pharmacologic properties -uncommon/unexpected (intolerance, allergic, etc.) Risk factors: dose, route of admin, polypharmacy, age, disease state, organ function, gender, genetics
Dextroamphetamine
affects chemicals in the brain and nerves that contribute to hyperactivity and impulse control. Dextroamphetamine is used to treat narcolepsy and attention deficit hyperactivity disorder (ADHD)
Lithium
affects the flow of sodium through nerve and muscle cells in the body. Sodium affects excitation or mania. Lithium is used to treat the manic episodes of bipolar disorder (manic depression). Manic symptoms include hyperactivity, rushed speech, poor judgment, reduced need for sleep, aggression, and anger. Lithium also helps to prevent or lessen the intensity of manic episodes. Check levels regularly lithium toxicity: muscle weakness, twitching, drowsiness, feeling light-headed, mood changes, blurred vision, ringing in your ears, irregular heartbeats, confusion, slurred speech, clumsiness. trouble breathing, or seizures.
Calcium Channel Blockers
agents that inhibit the entry of calcium ions into heart muscle cells, causing a slowing of the heart rate, a lessening of the demand for oxygen and nutrients, and a relaxing of the smooth muscle cells of the blood vessels to cause dilation; used to prevent or treat angina pectoris, some arrhythmias, and hypertension Ex. Nifedipine, amlodipine, Nicardipine, Diltiazam, Verapamil No grapefruit juice, Nsaids
epinephrine can activate
all alpha and beta receptors, but not dopamine receptors
A child taking methylphenidate may experience
all choices are possible possible choices: weight loss malnutrition increased heart rate and/or cardia arrhythmias suppression of growth
Cholinesterase Inhibitors: Therapeutic Effects
all cholinesterase inhibitors are approved for: mild-mod symptoms of AD donepezil- also approved for severe symptoms Con: Tx only benefits 1 in 12 pts Pros: ↑QOL/Cognitive Fx benefits in some improvements are MODEST/SHORT LASTING -are neither universal, dramatic, nor long lasting although SE common- benefit > risk in some
Adrenergic receptors are subdivided into what?
alpha and beta
norepinephrine can activate
alpha1, alpha2, and beta1 receptors, but not beta2 or dopamine receptors
dopamine can activate
alpha1, beta1, and dopamine receptors
ACh binding to nicotinic receptors are stimulatory or inhibitory?
always stimulatory
Sulconazole (Exelderm)
an antifungal medication of the imidazole class. It is available as a cream or solution to treat skin infections such as athlete's foot, ringworm, jock itch, and sun fungus
COMT converts Levodopa into
an inactive metabolite
sympathomimetic
another name for drugs that mimic the responses of the Sympathetic Nervous System, like Beta Agonists
the autonomic division is under what type of control?
antagonist (one branch is excitatory and the other branch is inhibitory)
Bicalutamide
anti-androgen. It works in the body by preventing the actions of androgens (male hormones). Bicalutamide is used together with another hormone to treat prostate cancer.
Colchicine action
anti-inflammatory agent with effects specific for gout
Ipratropium Bromide
anticholinergic drug Treat: asthma, COPD, rhinitis Inhalation or nasal spary
alzheimers symptoms
appear after 65, but may appear as young as 40 early in disease: memory loss confusion disoriented, get lost in familiar surrounds judgment becomes impaired personality may change progression of disease: self care difficult 70-90% develop behavioral problems -wander, pace, agitate, scream intensify in the evening- sundowning final stages: loses weight, appetite, speech, bladder/bowel fx unable to recognize family unable to communicate all sense of identity is lose completely dependent
Properties of Individual Cholinesterase Inhibitors: Rivastigmine [Exelon]
approved for AD and Dementia in PD IRREVERSIBLE inhibition (unlike donepezil) preparations: oral, oral soln, transdermal patch PO well absorbed-GI tract- especially w/food patch- blood levels↓/steadier⇢PO=↑tolerance patch beneficial- pts w/ difficulty swallowing 50% starting dose remains in patch after 24 hrs ESSENTIAL to remove old patch before new one to AVOID toxicity. Metab: convert inactive metabolites by AChE (not by cytochrome P450 enzymes in liver) Half-Life is short- 1.5 hrs. Elimination: urine Cause peripheral cholinergic SE N/V/D, abd pain, anorexia, weight loss Brady, faint, falls, fall related fractures ↓intensity SE w/ patch= no hepatic metabolism can intensify symptoms in patients with: PUD, Brady, SSS, urine obstruction, lung disease
Cabergoline
approved for Tx of hyperprolactinemic dis. occasional use in PD- not approved. "possibly" effective improving "off" times w/levo RARELY USED. SE: HA, dizzy, nausea, weak Adverse: development of HF & valve regurg, palm/pericardial fibrosis.
Conjugated drugs
are a class of biopharmaceutical drugs designed as a targeted therapy for treating cancer. Unlike chemotherapy, ADCs are intended to target and kill tumor cells while sparing healthy cells.
Opioids (narcotics)
are prescribed for moderate to severe pain. They are associated with respiratory depression and adverse effects of nausea, vomiting, constipation, itching, urinary retention, and altered mental processes. Sedation is an adverse effect of opioids that always precedes respiratory depression.
Beta2
arterioles - dilation bronchi - dilation uterus - relaxation liver - glycogenolysis skeletal muscle - enhanced contraction, glycogenolysis
Functions we are not aware of in the ANS
artery constrictions and peristalsis
How long should you instruct a client to wait between inhaler doses? At least 10 seconds At least 1 minute At least 30 seconds At least 2 minutes
at least two minutes
The nurse is preparing to administer a metered-dose inhaler to a client with asthma. How long should the nurse instruct the client to wait before administering a second dose
at least two minutes
Muscarinic antagonists
atropine and scopolamine
Muscarinic Antagonists for mydriasis and cycloplegia during ophthalmic procedures
atropine, homatropine, scopolamine, cyclopentolate, and tropicamide
Cariprazine (Vraylar)
atypical antipsychotic Mechanism unknown. Similar to aripiprazole.
Aripiprazole (Abilify)
atypical antipsychotic dopamine system stabilizers. Treats schizophrenia, acute bipolar mania, major depressive disorder, agitation associated with psychosis and irritability associated with autism spectrum disorder. Does not have metabolic s/e or EPSs. Food does not effect, protein bound, metabolized by liver, long elimination. S/E headache, agitation, nervousness, anxiety, insomnia, nausea, vomiting, dizziness, somnolence. High suicidality
The nurse is preparing to administer a gastrointestinal medication to a client. Which portion of the nervous system is most likely to be affected by this medication? Autonomic nervous system Somatic nervous system Efferent neurons Afferent neurons
autonomic nervous system
A female patient diagnosed with chronic atrial flutter has been prescribed verapamil in conjunction with digoxin to control ventricular rate. To enhance the therapeutic effect of the drug, the nurse will instruct the patient to: avoid grapefruit and grapefruit juice. take the medication with meals. avoid fresh fruit. take an aspirin every day.
avoid grapefruit and grapefruit juice.
There are two basic steps in the process by which neurons elicit responses from other cells:
axonal conduction synaptic transmission
Centrally acting muscle relaxants include 9 drugs:
baclofen, carisoprodol, cholorzoxazone, cyclobenzaprine, diazepam, metaxalone, methocarbamol, orphenadrine, & tizanidine All have similar properties
3 drugs tx spasticity
baclofen, diazepam, dantrolene
PD: Drug selection: Severe symptoms
begin w/ either levodopa (combined w/ carbidopa) or dopamine agonist levodopa= more effective BUT long term use= higher risk for disabling dyskinesias choice of med must be tailored to patient
PD: Drug selection: Mild symptoms
begin with MAO-B inhibitors confer mild, symptomatic benefit
SC Administration
beneath the skin (SC) Drug needs to be in solution or particle suspension There is a slower prolonged release with SC
Levodopa Teaching
benefits delayed for wks-months possible abrupt loss of therapy in off times-notify avoiding high protein meals N/V reduced by taking with food notify if N/V persists or becomes severe possible levodopa induce movement disorders (tremor, dystonic mvmt, twitching) appt→develop signs of excessive cardiac stimulation (palp, tachy, irreg heartbeat)- notify if occur hypotension w/associated dizziness may occur move slowly and lie down if dizzy/lightheaded possible levodopa-induced psychosis (visual hallucinations, vivid dreams, paranoia) →911!
Stimulant Laxatives
bisacodyl: (tablets: give at night to have BM in am , no crushing or chewing, no milk or antacids;Suppositories: BM within 15-60 min, may cause proctitis); senna: BM 6-12 hours after. May cause pink or brown urine. castor oil: acts on small intestine 2-6 hour BM. Limit to only when prep for radiology procedures. Chill and mix in juice. * easily abused, Give with a full glass of water.
Alpha blockers in Essential HTN
block alpha-1 receptors on: arterioles/veins = ↓BP Directly = vasodilation. Indirectly = ↓CO in response to vasodilation
If antipsychotic med needed avoid 1st generation because
block dopamine receptors and intensify motor symptoms
Clozapine and quetiapine cause little or no
blockade of dopamine receptors in the striatum and hence do not cause EPS
anticholinergic agents share the same mechanism:
blockade of muscarinic receptors in the striatum (unlike dopaminergic agents which have multiple mechanisms of action)
Alpha-Adrenergic Antagonists (alpha blockers)
blocks alpha-1 receptors on blood vessels (HTN) blocks alpha-1 on bladder/prostate (BPH) NOTE: blockade of alpha-1 receptors in the eyes and alpha-2 receptors= no recognized therapeutic use.
Carbidopa does what?
blocks levodopa destruction
Orlistat
blocks some of the fat that you eat, keeping it from being absorbed by your body. Used to aid in weight loss, or to help reduce the risk of regaining weight already lost. This medicine must be used together with a reduced-calorie diet and increased physical activity. Orlistat is for use only in adults that are overweight or obese. S/E bowel urgency, frequent bowel movements, oily evacuation, oily rectal leakage, steatorrhea, and flatulence with discharge
Noncompetitive Antagonist
blocks the agonist site
Differences between somatic and autonomic nervous systems
both have motor fibers, but somatic only stimulate skeletal muscle - motor fibers are usually heavily myelinated in somatic, thinly or unmyelinated in automatic - the target organs have different responses to neurotransmitters
baclofen & diazepam can be used for
both spasm and spasticity
Ergot derivatives: bromocriptine and Cabergoline
bromocriptine is approved for PD cabergoline is not. both are poorly tolerate. use is limited. activate: DA receptors mild block: serotonergic, alpa-adrenergic recep B/C POORLY SELECTIVE
ANS function: smooth muscles
bronchi, blood vessels, urogenitary, GI tract
albuterol/ipratropium
bronchodilator that relaxes muscles in the airways and increases air flow to the lungs. Albuterol inhalation is used to treat or prevent bronchospasm, or narrowing of the airways in the lungs, in people with asthma or certain types of chronic obstructive pulmonary disease (COPD). It is also used to prevent exercise-induced bronchospasm.
When describing the drugs classified as class IV antiarrhythmics, the nurse would identify these as: cardiac glycosides. beta blockers. vasodilators. calcium channel blockers.
calcium channel blockers.
parenteral calcium salts
calcium chloride calcium gluconate adverse effects: - highly *irritating* - *DO NOT give IM* - can cause IV extravasation (can destroy surrounding tissue- pt could lose limb) MONITOR PT ^ slow pump infusion drug interaction: - *digoxin*
Beta blockers in migraine prophylaxis
can reduce frequency and intensity of migraine attacks when taken prophylactically BB are effective through prophylaxis BUT cannot abort migraine once begun. Prevention mechanism for migraines= unknown.
Etoposide
cancer medicine that interferes with the growth and spread of cancer cells in the body.
Rivastigmine [Exelon]
caps: 1.5, 3, 4.5, 6 mg PO solution: 2 mg/mL Mild-Mod: 1.5mg QD⇢⇡weekly by 3mg/day 1.5 each meal to a (max) of 6mg BID PO-should be taken with morning & evening meal 24hr patch: 4.6, 9.5, 13.3 mg/24 hrs 4.6 mg patch QD⇢⇡dose PRN Severe AD: 4.6 mg (initial)↑ 13.3mg QD (max) apply (1) QD- chest, upper arm/back, lower back apply ONLY after removing the previous patch change site QD. Don't repeat for 14 days. bathing does NOT effect treatment
Levodopa/Carbidopa: advantages
combo superior to levodopa alone in 3 ways: (1) ↑levodopa fraction available for CNS actions. allows ↓levodopa dose by 75%. Example: to provide 10mg dopamine to brain we must administer 500mg levodopa (alone) but only 100mg levodopa if carbidopa is present. (2) by ↓dopamine production in periphery carbidopa ↓CV response to levodopa & N/V (3) by causing direct inhibition of decarboxylase carbidopa eliminates concern about ↓ levodopa effects by taking vitamins containing pryridoxine
symptoms management in PD
constipation- reg exercise, active, stool soft/lax OH- ↑salt/water, move slow, lie down for dizzy PLMS- levo/carb, pramipexole & ropinirole (non) insomnia- levo/carb, melatonin EDS- modafinil (non amphetamine CNS stim) depression- amitriptyline (bad side effects) dementia- donepezil and rivastigmine
parasympathetic effect of the pupils
constrict
An adult client with no known history of cardiovascular disease presents with atrial flutter. The client is prescribed propafenone PO 150 mg every 8 hours for 24 hours. What is the cardiac care nurse's priority assessment during this period? echocardiography continuous ECG monitoring every 1-hour monitoring of potassium levels blood pressure monitoring every 10 minutes
continuous ECG monitoring
Somatic Motor Neurons
control skeletal muscles and voluntary movement
Metoclopramide (Reglan)
controls post-op NV suppresses emesis and increases upper GI mobility
Autonomic Motor Neurons
controls smooth muscle, cardiac muscle, glands, and some adipose tissue
tonic-clonic
convulsive, as with a tonic-clonic seizure
Enteric-Coated
covered with a pH-dependent material that will dissolve in small intestine but not the stomach helps to protect the drug from the acid and pepsin in the stomach, also protects the stomach from irritating drugs *usually* cannot be crushed
Neuromuscular blocking agents
d-Tubocurarine, succinylcholine
Hepatotoxicity
damage to the liver. Elevated transaminase levels, jaundice (rare). Check LFT's. Avoid statins in alcohol-induced hepatitis.
Dantrium
dantrolene Treats MS skeletal muscle relaxant. S/E constipation
conversion of levodopa to dopamine catalyzed by what enzyme?
decarboxylase removes a carboxyl group from levodopa
Why is Levodopa lost?
decarboxylases in GI tract & peripheral tissues convert it to dopamine which cannot cross BBB
drugs that inhibit release will (increase or decrease) receptor activation
decrease
Drugs that interfere with transmitter storage will cause receptor activation to (increase or decrease)
decrease disruption of storage depletes vesicles of their transmitter content
Beta Blockers
decrease heart rate and dilate arteries by blocking beta receptors "olol" in the end. Ex. propanolol, atenolol, metoprolol Treat: Irregular heart rhythm (arrhythmia) Heart failure Chest pain (angina) Heart attacks Migraine Certain types of tremors May cause edema, fatigue, weight gain, depression
Additional agents (carbidopa, entacapone) in formulary
decrease the amount of decarboxylation in the periphery so that more drug can enter the CNS
Which effects are associated with various adrenergic antagonists? Select all that apply. Decreased salivation Decreased heart rate Increased lacrimation Dilated bronchioles Increased urination
decreased heart rate increased urination increased lacrimation
The nurse has just administered a muscarinic agonist to a client on a medical-surgical unit. Which physiological effect does the nurse anticipate the client may experience as a result of the medication? Decreased pulse Increased blood pressure Decreased urinary output Decreased gastrointestinal motility
decreased pulse
Imbalance of dopamine and acetylcholine results from
degeneration of the neurons in the substantia nigra that supply dopamine to the striatum
If any of these proteins (alpha-synuclein, Parkin, or ubiquitin) is defective
degradation of alpha-synuclein cannot take place
Neil McLean is an 80-year-old male client who has Parkinson's disease. His health care provider just prescribed benztropine(Cogentin), a muscarinic antagonist. Considering the possible adverse effects of this type of medication, what aspect of Mr.McLean's health history causes you concern? Difficulty with urination Excessive sweating Muscular tremors Muscular rigidity
difficulty with urination
The health care provider orders quinidine for a client who is receiving a common treatment for atrial fibrillation. The nurse would monitor this client for: digoxin toxicity. increased quinidine effect. renal dysfunction. bleeding.
digoxin toxicity.
The nurse is teaching a group of clients with asthma about the ways in which adrenergic agonists stimulate the sympathetic nervous system. Which clinical effect is evidence of this type of stimulation? Increased peristalsis Decreased heart rate Dilated pupils Decreased blood pressure
dilated pupils
mydriasis (big word big pupil)
dilated pupils
Which class IV calcium channel blocker is exclusively administered to treat acute supraventricular tachycardia? bethanechol chloride midazolam hydrochloride diltiazem chlorambucil
diltiazem
Under normal conditions, alpha-synuclein is rapidly degraded
doesn't accumulate and no harm occurs
Proper striatum function requires a balance between (2) neurotransmitters
dopamine acetylcholine
Peripheral decarboxylases converts levodopa into
dopamine (an active metabolite)
"off" times can be reduced with (3) types of drugs:
dopamine agonists COMT inhibitors MAO-B inhibitors evidence of efficacy is strongest for: entacapone (COMT inhibitor) rasagiline (an MAO-B inhibitor)
If psychosis develops
dopamine agonists amantadine anticholinergic drugs should be withdrawn
In PD there is an imbalance between
dopamine and acetylcholine in the striatum
Pramipexole does what?
dopamine receptor agonist
extrapyramidal side effects result from
dopamine receptors in the striatum being blocked by antipsychotic drugs
Of the (2) groups (dopaminergic & anticholinergic) which is most commonly used
dopaminergic agents by far the more widely employed
(2) types of drugs are used:
dopaminergic agents- directly/indirectly activate dopamine receptors anticholinergic agents- block receptors for acetylcholine
the underlying cause of motor symptoms is the loss of
dopaminergic neurons in the substantia nigra
Most side effects of Levodopa are...
dose dependent older adult especially sensitive to adverse effects
Adverse effects of clonidine
drowsiness, xerostomia, rebound hypertension Abuse potential Constipation Impotence Gynecomastia CNS effects
Allopurinol therapeutic uses
drug of choice for chronic trophaceous gout, can also be used for hyperuricemia that develops secondary to cancer chemo and to certain blood dycrasias (polycythemia vera, myeloid metaplasia, and leukemia
Transmitter Release
drugs can... Increase and decrease
Transmitter Synthesis
drugs can... Increase transmitter synthesis Decrease transmitter synthesis Cause synthesis of more effective transmitter
Transmitter Storage
drugs can... Interrupt storage --> decreased action
Receptor Binding
drugs can... Most utilized drug alteration site 1. Bind to site themselves - agonists 2. Bind to receptors to block action- antagonists 3. Bind to receptor to enhance natural action
Drugs for Cognitive Impairment
drugs may slow loss of memory and cognition and prolong independent function cannot reverse decline
second generation antipsychotics
drugs that alleviate schizophrenia with less likelihood of movement problems S/E: are associated with metabolic adverse effects (eg. weight gain, dyslipidemia, hyperglycemia, and increased risk of diabetes). As such they should be monitored for changes. Olanzapine and clozapine carry the greatest risk. Ex. apripiprazole, asenapine, brexpiprazole, cariprazine, clozapine, iloperidone, lurasidone, olanzapine (Zyprexa), Quetiapine (Seroquel), Risperidone,
vitamin D toxicity
early symptoms: - weakness - fatigue - nausea - vomiting - anorexia - abdominal cramping - constipation later symptoms: kidney function is affected - polyuria - nocturia - proteinuria neurologic: - *seizures* - confusion - ataxia *cardiac dysrhythmias* coma calcium deposition in soft tissues decalcification of bone
drug therapy for hypercalcemia
edetate disodium glucocorticoids calcitonin bisphosphonates furosemide (loop diuretic)
Synergistic PD Drug-Drug
effect is greater than the sum of individual effects (1+1=3) +/- overlap toxicities/ADEs or increased pharmacologic effect/PD effect
Antagonsitic PD Drug-Drug
effect is less than expected by using the two drugs together (1+1=1) competition for same receptor binding site, counterbalanced effects
efficacy
effectiveness
Tolcapone advantages:
extends effective time of levo by 2.9 hrs/day improves motor fx and ↓levo dose required
Drug selection and dosage are determined by
extent to which PD interferes with work, walking, dressing, eating, bathing, and other activities
movement disorders similar to those of PD can occur as side effects of antipsychotic drugs- these dyskinesias are referred to as
extrapyramidal side effects
PD: Motor symptoms result from damage to the
extrapyramidal system a complex neuronal network that helps regulate movement when EP fx disrupted- dyskinesias (disorder of movement develop)
Alpha1
eye - dilation, mydriasis (increase pupil size) blood vessels - vasoconstriction male sex organ - ejaculation prostate - contraction bladder - contraction of trigone and sphincter
Inhaled Corticosteroids (ICS)
fluticasone mometasone budesonide beclomethasone pref for persistent asthma need consistent daily use for optimal effect (NOT PRN)
approach to treatment is obvious in PD
give drugs that restore functional balance between dopamine and acetylcholine
Sublingual Administration
good absorption through capillary bed under the tongue, fast absorption, not affected by first-pass metabolism e.g., nitroglycerin
Spasticity
group of movement d/o of CNS origin heightened muscle tone spasm loss of dexterity
SNS : Pilioerection
hair follicle erection SNS- think of a dog when aroused- their hair's stand up
In which organ are the majority of beta-adrenergic receptors found?
heart
Beta1
heart - increased rate, increase force of contraction, increase AV conduction kidney - release of renin *Because renin promotes synthesis of angiotensin, a powerful vasoconstrictor, activation of renal beta1 receptors is a means by which the nervous system helps elevate blood pressure
Avoiding high-protein meals
help with reducing "off" times
Describe the baroreceptor reflex
helps regulate blood pressure
Gout
hereditary metabolic disease that is a form of acute arthritis, characterized by excessive uric acid in the blood and around the joints
Levodopa Beneficial Effects
highly effective BUT beneficial effects diminish over time. most effective drug for PD 75% pts experience 50% reduction in symptom severity at beginning of treatment. beneficial effects likely to increase over first few mths. don't expect immediate improvement. symptoms well controlled during 1st 2 years by the end of year 5= ability to fx declines to pretreatment level reflects disease progression, not tolerance
The nurse is preparing to administer a cholinergic antagonist to a client on a medical-surgical unit. Which assessment parameter is most appropriate to review before administering this medication? History of diplopia History of glaucoma Muscle strength Ability to chew
history of glaucoma
Furosemide (Lasix)
loop diuretic (water pill) that prevents your body from absorbing too much salt. This allows the salt to instead be passed in your urine. Lasix is used to treat fluid retention (edema) in people with congestive heart failure, liver disease, or a kidney disorder such as nephrotic syndrome. Also used to treat high blood pressure High doses can cause hearing loss.
Some experience early s/s of PD years before functional impairment develops
loss of smell excessive salivation clumsiness of hands worsening of handwriting bothersome tremor slower gait reduced voice volume
Statins
lower cholesterol in the blood and reduce its production in the liver by blocking the enzyme that produces it. Most effective. Reduces LDS and increases HDL. Oral, absorbed 30-90%. S/e: headache, rash, GI, muscle pain.
Beta 2 hits
lungs- dilate uterus- relax arterioles (around heart and lungs) Dialate
MOA
main enzyme responsible for breaking down catecholamines
Although there is no cure for motor symptoms, drug therapy can
maintain functional ability for years thereby substantially prolonging quality of life & life expectancy
Functions of the ANS
maintains internal conditions, has motor neurons that innervate smooth muscle, cardiac muscle and glands all throughout the body
What is the primary goal of antidysrhythmic drug therapy for a client who has been successfully cardioverted? increase in blood pressure maintenance of normal sinus rhythm (NSR) suppression of original dysrhythmia proof of increased cardiac contractility
maintenance of normal sinus rhythm (NSR)
abrupt withdrawal of tolcapone
malignant syndrome fever, muscle rigidity, altered conscious
Time of alz onset to time of death
may be 20 yrs or longer but typically is 4-8 years!
Diuretics
medications administered to increase urine secretion in order to rid the body of excess water and salt Thiazide is first line for hypertension. Loop Diuretics are common - monitor for hypokalemia
what can be looked on as the functional equivalent of a postganglionic neuron of the sympathetic nervous system
medulla of the adrenal gland
EEG (electroencephalogram)
method used to record electrical activity in the brain
Probenecid ADRs
mild GI effects (n/v, anorexia), hypersensitivity reactions, renal injury initial therapy can cause acute gouty attacks
Properties of Individual Cholinesterase Inhibitors: Donepezil
mild, mod, severe AD reversible inhibition of AChE more selective for AChE in brain than periphery Well absorbed after PO Metabolized: hepatic metabolism-P450 enzymes Eliminated: mainly in urine, partly in bile. Half-Life= prolonged= 60 hrs. Administered= ONLY once a day (half life) can cause peripheral SE- N/D (most common) Brady, faint, falls, fall related fractures Min SE: initial dose stabilized for 1-3 mths before any changes to be made
Tablets
mixture of drug + binders and fillers (powdered medication that is compacted to form a solid disc or other shapes) can differ in rates of disintegration and dissolution "delayed release"
which enzyme is primarily responsible for the degradation of catecholamines?
monoamine oxidase
Phenothiazines
more sedation, less extrapyramidal
osteoporosis
most common disorder of bone metabolism - low bone mass - increased bone fragility primary prevention: - calcium - vitamin D - lifestyle (ex: weight bearing exercise) diagnosis - measurement of bone mineral density (BMD) - dual-energy x-ray absorptiometry (DEXA)
CYP3A4
most common metabolic enzyme involved in drug interactions Inducers: phenytoin, rifampin, barbituates, carbamazepine Inhibitors: ketoconazole, itraconazole, fluconazole, erythromycin. if using these and taking drugs metabolized by this enzyme, levels will increase which may cause toxicity.
dual innervation
most viscera receive nerve fibers from both parasympathetic and sympathetic divisions the influence of sympathetic nerves opposes that of parasympathetic nerves For example, in the heart, sympathetic nerves increase heart rate, whereas parasympathetic nerves slow heart rate
Levo/Carb/Entac
now available in fixed dose combinations sold as Stalevo both carb and entac inhibit enzymatic degradation of levo= enhance therapeutic effects triple combo= more convenient= less money available ONLY in immediate release NOT= pts w/tight schedule OR if ER required
*alendronate [fosamax, fosamax plus D]*
most widely used oral bisphosphonate uses: - postmenopausal osteoporosis - male osteoporosis - glucocorticoid-induced osteoporosis adverse effects: generally safe - *esophageal ulceration* - atypical femoral fracture - esophageal cancer - musculoskeletal pain - ocular problems - osteonecrosis of the jaw - hyperparathyroidism - A-fib *pts MUST sit up for 30 mins after drug administration* - MAJOR risk for esophageal erosion - if pt cannot sit up for 30 mins then DO NOT administer - *pt should sit at at least 45 degrees*
Life Cycle of Epinephrine
much like that of norepinephrine The cycle begins with synthesis of epinephrine within chromaffin cells of the adrenal medulla These cells produce epinephrine by first making norepinephrine, which is then converted enzymatically to epinephrine. -(Because sympathetic neurons lack the enzyme needed to convert norepinephrine to epinephrine, epinephrine is not produced in sympathetic nerves.) Following synthesis, epinephrine is stored in vesicles to await release. Once released, epinephrine travels via the bloodstream to target organs throughout the body, where it can activate alpha1, alpha2, beta1, and beta2 receptors. Termination of epinephrine actions is accomplished primarily by hepatic metabolism, and not by uptake into nerves
The nurse is preparing to administer pyridostigmine bromide (Mestinon) to a client with myasthenia gravis, prior to discharge. The nurse tells the client that the medication is used to treat which symptoms associated with the disorder? Dry mouth Muscle weakness Visual disturbance Memory loss
muscle weakness
The nurse is talking to a client who has listed pseudoephedrine hydrochloride (Sudafed) as a medication taken on a daily basis. What condition is this client most likely treating with this medication? Cardiogenic shock Bronchospasms Nasal congestion High blood pressure
nasal congestion
management of PD is generally under the guidance of
neurologist who oversees pharmacologic management while other providers are over management of primary care needs and monitoring pt status.
alzheimer's patho
neuron degeneration reduced cholinergic transmission beta-amyloid and neuritic plaques neurofibrillary tangles and tau apolipoprotein E4 endoplasmic reticulum associate protein binding homocysteine
The nurse in the neurological unit is discussing the nervous system with a colleague who was recently transferred to that unit. The nurse tells the colleague that the central nervous system communicates with the parasympathetic nervous system through which cells? Acetylcholine Epinephrine Norepinephrine Neurons
neurons
Sympathetic preganglionic fibers arise from:
neurons in spinal cord T1 - L2
Neuroprotection in PD
no definitive findings for neuroprotection in PD some drugs are promising: MAO-B inhibitors: provided neuroprotective effects in animal studies dopamine agonists: demonstrated neuroprotective effects in lab studies human studies inconclusive in both levodopa= controversial. risk may outweigh benefits when given for this purpose.
What causes degeneration of dopaminergic neurons?
no one knows for sure
Pramipexole [mirapex]
non ergot dopamine receptor agonist used ALONE in early stage PD used w/ levodopa in advanced stage PD ↓motor control fluctuations allow for ↓dosage of levodopa also used for RLS
norepinephrine
non-selective agonist similar to epinephrine EXCEPT NO B2 (bronchodilation), NO Hyperglycemia
epinephrine
non-selective agonist: A1, B1, B2 PROTOTYPE - potent inotropic & vasoconstrictor - used to combat anaphylaxis
pseudoephedrine
non-selective agonist: A1, B2 - OTC cold meds - Tx rhinitis and nasal congestion
Isoproterenol
non-selective beta agonist Specific B-adrenergic (gets B1 and B2) AV block Restart heart after arrest Inc cardiac output during shock Bronchospasm during anesthesia Asthma - but now have better, more specific drugs for this Adverse Effects - I bet you can tell me... Drug Interactions - Nearly identical to epi IV, IM
Apomorphine
nonergot dop-agon approved use: acute tx of hypo mobility during "OFF" episodes in advanced PD NOT given by mouth. NOT indicated for routine mgmt. 62% improvement- pts at least 2hr off time/day benefits sustained during 4 wks of use derivative of morphine w/o opioid effects highly lipophilic BUT undergoes ext 1st pass ineffective orally, RAPID comp absorption w/SQ effects begin in 10-20 mins. persist 1 hr half-life is about 40 mins
Rotigotine
nonergot dop-agon improves DA transmission by activating post-syn DA receptors in substantia nigra approved use: early-adv stage PD, mild-mod RLS patch only. NO ORAL- b/c 1st pass= extensive TTS peak= 15-18 hrs w/ range of 4-27 hrs approx 90% of drug is protein bound half-life: 5-7 hrs after patch removal excretion: urine (70%) and feces Adverse effects: most common- CNS,neuromusc sleep dis, dizzy, HA. halluc & dysk (dose related) N/V common in beginning skin irritation at site is common hyperhidrosis (excessive perspiration) may occur
Ropinirole
nonergot dop-agon (similar to pramipexole) same receptors: highly selective D2, D3 same indications: PD, RLS early stage PD: mono therapy late stage PD: adjunctive w/ levo conversely: ropinirole- excreted by hep metab (not renal) same SE alone and w/ levodopa BUT occur less frequently in combo w/ levo than pramipexole CANNOT BE USED IN PREGNANCY- fetal harm
NSAIDs
nonsteroidal anti-inflammatory drugs S/E -Gastric ulcer/bleeding -Prolonged bleeding time (platelet interference) -Increased risk of cardiovascular events -Renal toxicity (including celecoxib)
Muscarinic
parasympathetic - rest and digest location and response: eyes - contraction, focuses for near vision, miosis heart - decreased rate lung - constriction of bronchi, promotes secretions bladder - contraction of detrusor, relaxation of trigone ad sphincter (causes voiding) GI tract - increased gastric secretions, tone, and motility (defection) sweat glands - sweating sex organs - erection blood vessels - vasodilation
irritable bowel syndrome (IBS)
periodic disturbances of bowel function, such as diarrhea and/or constipation, usually associated with abdominal pain. Intermittent diarrhea and constipation with pain. Treat and prevent symptoms: Antispasmodics, bulk forming agents, antidiarreheals and tricyclic antidepressants.
Liver function failure s/s
persistent nausea, fatigue, lethargy, anorexia, jaundice, dark urine
Buccal Administration
placed between the cheek and the gum, fast absorption, not affected by first-pass metabolism e.g., fentanyl lollipop, glucose
Initiation of the heart's electrical impulses depends predominantly on what electrolyte movement? Select all that apply. sodium and calcium ions out of a myocardial cell calcium ions into a myocardial cell potassium ions out of a myocardial cell potassium ions into a myocardial cell sodium and ions into a myocardial cell
potassium ions out of a myocardial cell sodium and ions into a myocardial cell calcium ions into a myocardial cell
Colchicine precautions and interactions
precautions: older adults, debilitated pt., cardiac, renal and GI disease Contraindicated: pt. with hepatic or renal impairment, pregnancy
Pramipexole: Adverse Effects
primarily caused by DA receptor activation most common SE when used alone: nausea, dizzy, daytime som, insomnia, constipation, weakness, hallucinations when combined w/levo 50% experience: OH, dyskinesias. Hallucination risk doubles
Tolcapone LFTs
prior Q 2 wks x 1st year Q 4 wks for next 6 months following
Levodopa: Psychosis
psychosis develops in about 20% prominent symptoms- visual hallucinations, vivid dreams/nightmares, paranoid ideation (fears of personal endangerment, sense of persecution, feelings of being followed or spied on) activation of dopamine receptors involved ↓symptoms=↓levodopa dose=BUT ↓benefits
in patients taking levodopa, clozapine and quetiapine can reduce
psychotic symptoms w/o intensifying symptoms of PD
isoproterenol HCl
pts on this beta agonist should be started on a low dose that is increased as they are able to handle it pts should also be placed on a heart monitor to look for dysrhythmias
The nurse is preparing to administer a medication that will suppress the parasympathetic nervous system. Which response does the nurse anticipate the client will experience after receiving the medication? Increased peristalsis Decreased heart rate Decreased blood pressure Pupil dilation
pupil dilation
Peripheral decarboxylases work faster in the presence of
pyridoxine
activity of decarboxylases is enhanced by
pyridoxine (vitamin B)
Selective Estrogen Receptor Modulator (SERM)
raloxifene [evista]
Levodopa: CNS Effects
range from: anxiety-depression-memory/cognitive impair insomnia and nightmares are COMMON impulse control, behavior changes associated w/ promiscuity, gambling, binge eating, ETOH abuse
Pramipexole- Pharmokinetics
rapidly absorbed. peak in 1-2 hrs. undergoes wide distribution achieves high concentration in RBCs excreted unchanged in urine
Properties of Individual Cholinesterase Inhibitors: Galantamine
reversible cholinesterase inhibitor→mild-mod AD extracted from daffodil bulbs. trials= ↑cog fx, QOL, behavior, ADL ability rapidly/completely absorbed after PO admin protein binding in plasma is low elimination is by CYP hepatic enzymes excretion is renal mod-sever liver/renal dys-delays excret+↑levels ↓dosage in these pts. AVOID if sever dysfunction Half life= about 7 hours (healthy adult) common SE: N/V/D, anorexia, weight loss (worst)donezepil > galantamin > rivastigmine(less) bronchoconstriction- avoid if asthma/copd AVOID drugs that block cholinergic receptors b/c ↓therapeutic effects
Autonomic (ANS) functions :secretory glands
salivary, gastric, sweat, bronchial
secretory glands
salivary, gastric, sweat, bronchial
Epi
secreted by adrenal medulla to act on various organs in sympathetic NS
SSRIs
selective serotonin reuptake inhibitors, used to relieve anxiety and depression by limiting reuptake of a neurotransmitter, takes about 3 weeks to work. Ex. end in [pram], [ine] citalopram [Celexa]; escitalopram [Lexapro]; fluoxetine [Prozac]; paroxetine [Paxil]
SSRIs (selective serotonin reuptake inhibitors)
selectively inhibits serotonin reuptake from synaptic gap and results in potentiation of serotonergic neurotransmissions. Examples: Luvox, Paxil, Prozac, Zoloft end in [pram], [ine] citalopram [Celexa]; escitalopram [Lexapro]; fluoxetine [Prozac]; paroxetine [Paxil] initial responses are seen approx. 1-3 weeks. Max responses can take up to 12 weeks. Take for at least 1 month before changing or increasing dose. Do NOT use with MAOIs
Selegiline (MOA-B Inhibitors)
selegiline & rasagilne= 1st line drugs BUT effects are MODEST. suggest delay dis progression by delaying neurodegeneration. neuroprotection NOT confirmed selective, irreversible inhibition of MAO-B helps preserve dopamine benefits decline dramatically in 12-24 mths
extrapyramidal symptoms
side effects of antipsychotic medications that affect a person's gait, movement, or posture Usually caused by high potency first gen. antipsychotics Also referred to as EPS Acute Dystonia: occurs within first few days of therapy. Severe spasm of the muscles of tongue, face, neck and back. Parkinsonism: bradykinesia, mask-like facies, drooling, tremor, rigidity, shuffling gait, stooped posture. Akathisia: pacing and squirming, need to move uncontrollably. develops in first 2 months of treatment. Tardive Dyskinesia: occurs with long-term therapy. Involuntary choreoathetoid movements of the tongue and face.
Parkinson's disease (PD)
slowly progressive neurodegenerative disorder that afflicts more than 1 million Americans. 2nd only to Alz as most common degenerative disease of neurons
Selegiline: selective inhibitor of MAO-B
so it is NOT used for tx of depression in little doses- does NOT pose risk of HTN crisis
Of the antiepliepleptic or anticonvulsant drugs
some are general depressants other possible answers were: some are general stimulants all are general stimulants all are general depressant
drugs that tx muscle spasm, do not tx
spasticity
Black Box Warning: Sotalol (Betapace)
starting or restarting: inpatient in facility w/ continuous ECG monitoring and cardiopulmonary resuscitation for minimum of 3 days to minimize problems associated with induced arrhythmia. Creatinine clearance should be established prior to initiating this drug. Betapace cannot be substitute for Betapace AF when treated atrial fibrillation
Colchicine interactions
statins, inhibitors of PGP and CYP3A4
Describe what is meant by "autonomic tone."
steady, day-to-day influence exerted by the autonomic nervous system on a particular organ or organ system In most organs, the parasympathetic nervous system provides the predominant tone The vascular system, which is regulated almost exclusively by the sympathetic nervous system, is the principal exception
idiosyncratic response
strange, unique, or unpredicted response to a drug
PD: neurotransmission is disrupted primarily in the brain's
striatum
Life Cycle of Acetylcholine
synthesis of ACh from two precursors: choline and acetylcoenzyme A Following synthesis, ACh is stored in vesicles and later released in response to an action potential Following release, ACh binds to receptors (nicotinicN, nicotinicM, or muscarinic) located on the postjunctional cell Upon dissociating from its receptors, ACh is destroyed almost instantaneously by acetylcholinesterase (AChE), an enzyme present in abundance on the surface of the postjunctional cell AChE degrades ACh into two inactive products: acetate and choline. Uptake of choline into the cholinergic nerve terminal completes the life cycle of ACh
Life Cycle of Norepinephrine
synthesis of norepinephrine from a series of precursors. The final step of synthesis takes place within vesicles, where norepinephrine is then stored before release. Following release, norepinephrine binds to adrenergic receptors. Norepinephrine can interact with postsynaptic alpha1 and beta1 receptors (but not with beta2 receptors) and with presynaptic alpha2 receptors. Transmission is terminated by reuptake of norepinephrine back into the nerve terminal. (Note that the termination process for norepinephrine differs from that for ACh, whose effects are terminated by enzymatic degradation rather than reuptake) Following reuptake, norepinephrine can undergo one of two fates: -uptake into vesicles for reuse -inactivation by monoamine oxidase (MAO), an enzyme found in the nerve terminal
Donepezil [Aricept]
tablet: 5, 10, 23 mg Mild-Mod: 5mg QD⇢⇡10mg QD after 4-6 wks Severe AD: 10mg QD⇢⇡23mg QD after 3 mths should be taken at bedtime taken W/WO food Aricept 23 mg MUST be swallowed WHOLE
Selegiline pharmacokinetics
tabs/cap rapid GI absorption, travels to brain, quickly penetrates BBB irreversible inhibition of MAO-B follows hepatic metabolism followed by renal excretion amp/methamphetamine produced= harmful CNS excitation persists until more MOA-B is synthesized because inhibition by selegiline was irreversible. bioavailability higher in ODT= doses can be lower absorbed through oral mucosa but same pharm.
Nitroglycerin (Nitrostat)
take up to 3 tabs during single episode place under tongue store in original container discard on expiration date May be taken on a schedule. Take prior to exercise / sexual activity
baclofen & diazepam work in
the CNS
FDA approval
the FDA can prevent marketing of any drug it judges to be incompletely tested or dangerous. -only drugs considered to be safe by the FDA are approved for marketing.
efficacy
the ability to produce a desired or intended result effectiveness
Half-life of a medication
the amount of time it takes for half of the drug to be eliminated. Liver and kidney disease, aging, absence of food, and slowed metabolic rate prolong half-life because of their effects on metabolism and excretion.
dependence
the condition that results when the brain develops a chemical need for a drug and cannot function normally without it
withdrawal
the discomfort and distress that follow discontinuing the use of an addictive drug
An adult client with a long-standing dysrhythmia has been taking oral propranolol for the last several months, resulting in acceptable symptom control. What is a priority teaching point for the nurse to communicate to this client? the need to limit intake of high-potassium foods the importance of not stopping the medication abruptly the need to measure the radial pulse for 1 minute prior to each dose of propranolol the need to avoid taking over-the-counter antacids
the importance of not stopping the medication abruptly
Movement in PD is normal when
the inhibitory influence of dopamine and the excitatory influence of acetylcholine are in balance
peripherally acting drugs that affect somatic motor system function have only one site of action:
the neuromuscular junction
Muscarinic receptors are in ?
the parasympathetic nervous system there is one in the sympathetic nervous system that acts on sweat glands but also responds to ACh
describe synaptic transmission
the process by which information is carried across the gap between the neuron and the postsynaptic cell requires the release of neurotransmitter molecules from the axon terminal followed by binding of these molecules to receptors on the postsynaptic cell
Potency
the size of the dose needed to elicit a given response
Define neuropharmacology
the study of drugs that alter processes controlled by the nervous system
most of our body is regulated by both parasympathetic and sympathetic
we call this a reflex. the baroreceptors are in our carotid artery and in our aortic arch
levodopa gradual loss
wearing off develops near end of the dosing interval indicates that drug levels have declined to sub therapeutic level
Tolcapone pharmokinetics
well absorbed after oral dosing peaks: 2 hrs highly bound-plasma proteins in blood > 99.9% undergoes ext hep metab followed by renal exc half life is 2-3 hrs.
Pharmacokinetics
what the body does to the drug
Pharmacodynamics
what the drug does to the body
what is divergence?
when a few presynaptic neurons branch to affect a larger number of postsynaptic neurons
terminal
where the neurotransmitter is released into the synapse to make an action on the next cell neurotransmitter will either freely disassociate from the receptor or an enzyme can make them disconnect
Avoid sympathomimetics/tyramine while on seglegiline
while taking medication and for 2 wks after stopping medication
Anti-Parkinsonian Agents
• *Leva-dopa - replaces dopamine for only works for five years!!* • Carbidopa (decarboxylase inhibitor = Sinemet) - if on exam if between Leva and Carb - chose carb bc you need less • Bromocriptine - stimulates postsynaptic dopamine receptors • Selegiline - decreases MAO-B, which leads to a decrease in the degradation of dopamine • Anticholinergic drugs: blocks ACH receptors and helps restore "false" balance • Artane, Gognetic Kemadrin • COMT inhibitor - entacapone • Amantadine
Benzodiazapines & Barbiturate Cautions
• Additive with other sedative-hypnotics • Drug abuse and habituation • Symptoms can last up to 6 weeks or longer
CNS depressants - how do they work?
• An agent which decreases the excitability of the tissue in the CNS. • Produces sedation hypnosis, general anesthesia, coma, death. • All drugs in this category can be used as sedatives, hypnotics or general anesthetics...it is dose dependent • The higher the dose the greater the depression.
Anti-epileptic Goal of Treatment
• Control seizures without significant CNS impairment (this is difficult bc they all hyperpolarize)
Benzodiazapines & Barbiturate Side Effects
• Drowsiness • Impaired performance or decreased perception and judgement • Hangover effect • Hyperalgesia (barbiturates only) - abnormally heightened sensitivity to pain. • Overdose - respiratory depression (barbiturates, but can be true of any depressants in combination)
Anti-anxiety agents - What are they? Major side effects?
• Prescribed more frequently than any other CNS class •Designed for short term use Drugs: •Sedative Hypnotics Common: Valium Caution: Insomnia may accompany anxiety or depression - insomnia may be treated with sedative hypnotic, however, if insomnia is accompanying depression, a sedative-hypnotic should *not* be used. •Beta Blockers - not approved by the FDA to help individuals through temporary stress, will alleviate "pounding" heart and may also lessen muscular "tremor" or shaking hands. Advantage: no sedation and no addiction potential •Buspirone (BuSpar) - a new chemical entity - not related to benzos - not a controlled substance - no euphoria or additive CNS depression - in contrast, nervousness may be a problem - not as effective as benzos - may take 1-2 weeks for effect - ok for short term use; long term safety needs to be established
ANILINE TYPE (ACETAMINOPHEN) (Tylenol)
•*extremely hard on the liver and many OD on this might be #1 or close to #1 for liver failure •*after acetaminophen OD, prompt treatment is necessary! Within 10 Hours!! With acetylcysteine (mucomyst) can prevent hepatic damage and death in many patients! •*Kidney or liver damage - irreversible liver damage with even one overdose* •Blood diseases - anemia •Possible link to bladder cancer
Psychotrophic Agents
•Antidepressants •Anti-anxiety agents •Antipsychotic agents •Drugs to treat manic depression episodes
ANILINE TYPE (ACETAMINOPHEN) (Tylenol) Non-narcotic analgesics - Therapeutic Effects/What are they and what are the indications
•Relief of pain such as headache, dysmenorrhea •Antipyretic - decreases fever *It is not an antiinflammatory nor is it an anticoagulant!*
SALICYTES (aspirin) Non-narcotic analgesics - Therapeutic Effects; What are they and what are the indications
•Relief of pain such as headache, dysmenorrhea, arthritis •Antpyretic - decreases fever *•Antiinflammatory* such as Rheumatoid arthritis and Rheumatic fever and decreases the scarring of heart valve *•Anticoagulant effect* - for veneous coronary thrombosis and after mycardial infarction to prevent stroke
Cholinesterase Inhibitors: Adverse Effects
↑ACh in periphery= typical cholinergic SE N/V, Dyspepsia, Diarrhea, Dizziness, Headache Bronchoconstriction (caution-asthma/COPD) UNCOMMON: serious CV effects- brady, faint, falls/fracture, PM CV-SE= withdrawal especially if NO cog benefit DRUG INTERACTIONS: drugs-block cholinergic rec↓therapeutic effects anticholinergics, 1st gen antihistamine, tricyclic antidepressant, conventional antipsychotics DOSAGE/DURATION OF TREATMENT: carefully titrate dose. cont as long as needed ↑dose= ↑benefits= ↑SE initial dose= low w/gradual ↑to tolerable level Tx cont indefinitely or until benefit is lost or SE become intolerable
