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

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