Pharm Exam I
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- hemicholinium
- inhibiting Na dep. choline transporter
- vesamicol
- inhibits storage of acetylcholine in synaptic vesicles through vesicle associated transporter
- botulinum toxin
- blocks the reslease of acetyl choline
- reserpine
- inhibits storage of catecholamines in vesicles carried out by VMAT
- cocaine and tricyclic antidepressants
- inhibits reuptake of catecholamines by NET
- norepinephrine
- binds alpha2 receptor
- epinephrine
-
direct-acting, non-selective agonist--activates a1,a2,b1,b2
released from adrenal medulla
Effects: ionotropic force of contraction and chronotropic (rate of contraction), may cause vasodilation in skeletal muscle
Therapy: relief of hypersensitivity, prolong anesthetic effect by vasoconstriction, used to restore cardiac rhythms in patients with cardiac arrest, topical hemostatic agent
- isoproternol
-
direct acting selective agonist B1,B2
Effect: chronotropic, ionotropic effects, increase in CO w/ decrease in diastolic and mean BP, slight increase in systolic BP
Toxic: palpitations, tachycardia, flushing, cardiac ischemia, arrhythmias
therapy: increase HR in bradycardia or heart block - Dobutamine (Dobutrex)
-
catecholamine, nonselective btwn a and b receptors but selective for B1> B2
Effects: increase CO thru B1 and positive ionotropic and chronotropic effect
racemic mixture: + isomer b1 and a1 receptor antagonist (-) isomer-a1 agonist
t1/2: 2 min
Therapy: treat cardiac decompensation after cardiac surgery or CHF
Toxic: patients with atrial fibrillation, can cause increased ventricular rate, development of ventricular ectopic activity - phenylephrine
-
non-catecholamine, poor selective a agonist
longer duration of action (not targeted by COMT)
Therapy: mdriatic, decongestant, raise BP
Toxic: hypertension - ephedrine
-
non catecholamine, plant alkaloid, ma huang
a mixture of 4 enantiomers, one enantiomer pseudoephedrine is a decongestant
non-xlective mixed agonists (a and b)
Actions: enhances release of nerephinephrine and raises BP
Therapy: decongestant, bronchodilator, treat urinary incontinence
toxic: urinary retention in pts with prostrate problems
- dopamine
-
catecholamines act as agonist at D1 receptor in renal, mesenteric, and coronary beds, increase cAMP, vasodilation
Therapy: CHF, esp pts with low or normal peripheral resistance, cardiogenic septic shock
Toxic: nausea, vomiting, tachycardia, arrhythmias, hypertension, vasoconstriction, extravasation of dopamine cn cause necrosis, gangrene - amphetamine
-
acts as a CNS stimulant, elevates mood/alertness, depresses appetite
peripherally acts as an indirect adrenergic agonist by releasing catecholamines - clonidine
-
a2 selective direct agonist in CNS
decreases sympathetic outflow from CNS
Therapy: hypertension, decreases CNS input to blood vessels - tyramine
-
indirect sympathomimetic, causes release of NE from adrenergic nerves
found in fermented foods, a normal metabolite of tyrosine
interacts with MAO with aged/fermented foods - phentolamine
-
a1 and a2 antagonist
effects:
decrease in peripheral resistance (a1)
baroreceptor mediated tachycarida
increase release of NE (block a2)
limited absorption after oral use
t1/2: 5-7hrs
Toxic: tachycardia, nasal congestion, headache
Therapeutic use: treatment of pheochromocytoma and Male ED - prazosin
-
antagonist selective for a1
effects: relaxes arterial and venous vascular smooth muscle, like in prostrate a1 receptor
high first pass metabolism, extensively metabolized in humans
t1/2: 3 hrs
Toxic: lacks reflex tachycardia
Therapeautic: treat hypertension, treat benign prostatic hypertrophy
- Tamsulosin (FLOMAX)
-
competitive a1 antagonist, t1/2= 9-15 hrs
greater effect in inhibiting prostrate smooth muscle contraction since it involves a1
therapy: treat benign prostatic hypertrophy - phenoxybenzamine
-
nonselective, irreversible alpha antagonist
binds alpha receptor for 14-48hrs or more
effects: blocks reuptake of NE, reduces BP when sympathetic tone is high, CO may increase due to reflex effects, inhibits uptake of catecholamines into neuronal, non-neuronal tissues
absorbed after oral admin
Toxic: orthostatic hypotension, tachycardia, nasal stuffines, inhibit ejaculation, CNS: fatigue, sedation, and nausea
Treatment of pheochromocytoma - propranolol
-
non-selective reversible B-antagonist, pure competitive antagonist
high first pass metabolism, large Vd
Therapy: hypertension, angina, supraventricular/ventricular arrythmias, premature ventricular contraction, MI, pheochromocytoma, prophylaxis of migraine
Toxic: bradycardia, negative ionotropic effect, decrease CO, bronchoconstriction, excercise intolerance, fatigue, sleep disturbances
Contraindications: diabetes milletus - pindolol
-
reversible, pure competitive non-selective Beta antagonist
partial agonist
ISA-agonist in absence of agonist activity, works as an antagonist in the presence of agonist
Therapy: hypertension, angina - Metoprolol (Lopressor)
-
pure B1 selective compretitive reversible antagonist
no ISA and no membrane stabilizing activity
Therapy: stable angina, CHF
Contraindications: acute MI, higher order heart block
- Atenolol (Tenormin)
-
pure competitive B1 selective antagonist (reversible)
no ISA or membrane stabilizing activity
Therapy: hypertension - Labetalol
-
non-selective competitive B antagonist, pure competitive selective a1 antagonist
ISA at B receptor
Therapeutic: hypertension
Toxic: rare hepatic failure - Carvedilol (COREG)
-
pure competitive antagonist B1, B2, and a1
antioxidant
anti-proliferative effects, blocks remodeling heart failure, membrane stabilizing effects, lacks ISA, vasodilation
Therapy: CHF - carbachol
- cholinomimetic that acts on muscarinic and nicotinic receptors, not metabolized by AchE
- acetylcholine
- acts on both muscarinic and nicotinic receptors, poor lipid solubility, short action (5-30s)
- Nicotine
-
acts on nicotine receptor like pilocarpine, acts 1-6hrs, high lipid solubility
therapy-smoking deterrent - methacholine
-
direct acting cholinomimetic, acts on muscarinic receptors, resistant to AchE, quaternary amine (lipid insoluble)
used in bronchial challenge test, can have adverse effects of bradycardia and hypotension - atropine
-
direct anticholinergic, nonselective for M1-M5, widely distributed including CNS, oral, parenteral, and opthalmic
Therapy: bradycardia, acute treatment, AV-block, acute - Ipratropium
-
Anticholinergic , direct antagonist
quaternary amine (less absorbed), inhaled aerosol
Treatment: asthma, COPD - tropicamide
-
direct acting Anticholinergics (muscarinic)
opthalmic
therapy: produce mydriasis and cycloplegia - scopalamine
-
direct acting, Ach inhibitors, muscarinic
oral, parenteral, opthalmic, transdermal
Treatment: motion sickness - oxybutynin
-
direct antagonists, anticholinergics muscarinic
oral and transdermal
treatment: reduce urgency, spasm, incontinence - pancuronium
-
nicontinic Ach receptor blocker
use: muscle relaxer used during surgery - succinylcholine
-
nicotinic Ach receptor blocker--depolarizing
muscle relaxer and paralysis - edrophonium
-
Indirect agonist-AchE inhibitor
quaternary amine, short acting (min), parenteral admin
used in Myasthenia gravis as a diagnostic - neostigmine
-
AChE inhibitor-indirect agonist
acts in minutes-hours, oral and parenteral, long term treatment of myasthenia gravis - pyridostigmine
-
indirect agonist-AchE inhibitor, reversible carbamate ester
oral and parenteral, acts for hours
treatment: myasthenia gravis , prophylaxis for organophosphate poisining - physostigmine
-
indirect agonist AChE inhbitor, carbamate ester
acts min-hrs, parenteral,
treatment: anticholinergic poisoning - malathion, parathion
-
irreversible indirect agonists, AChE inhibitors
toxins, lipid soluble, organophosphates - hexamethonium
-
indirect antagonist, ganglionic nicotinic blocker
old treatment for hypertension, side effects of combined symp and parasymp blockade - mecamylamine
-
indierect antagonist nicotinic ganglionic blocker
old treatment for hypertension side effects of combined symp and parasymph activity - trimethaphan
-
indirect antagonist of nicotinic ganglion
blocks both sympathetic and parasymp activity
prev used for hypertension - pralidoxime
-
cholinesterase regenerator, not a receptor antagonists
used to treat organophosphate poisoning - diazepan
-
benzodiazepine, vallium
anti-seizure, sedative - Haldol
- knocks patient out, creates orthostatic hypotension
- ompeprazole
- proton pump inhibitor
- itraconazole
- anti-fungal, inhibits cytochrome p450 so it can interfere with other drugs actions
- propofol
- anesthetic agent, hydrophilic
- chloroquine
- malaria drug, very lipid soluble