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Exam 1 drugs
adrenergics, muscarinics, heart disease drugs
79
Pharmacology
Professional
02/05/2012

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Term
B nonselective blocker specifically formulated for glaucoma tx, topical
Definition
timolol
Term
ultra fast-acting "B blocker" with partial agonist activity at B receptors
Definition
pindolol
Term
nonselective 3rd generation B blocker, unique w/ antioxidant activity and 1st shown to reduce morbidity/mortality in CHF pts
Definition
carvedilol
Term
mixed antagonist, 3rd generation, has activity at A1 to contribute to vasodilation
Definition
labetalol
Term
B1 selective antagonist, shows cardioselectivity, has higher bioavailability and hepatic clearance
Definition
metropolol
Term
irreversible, nonspecific A antagonist
Definition
phenoxybenzamine
Term
selective A1 antagonists, competitive
Definition
prazosin
terazosin
Term
A1 specific antagonist, targets urinary flow
Definition
tamsulosin
Term
ultra-short acting B blocker, given by iv to limit catecholamine-mediated cardiac stimulation in surgery, susceptible to enzymatic hydrolysis in the blood
Definition
esmolol
Term
B1 selective antagonist, shows cardioselectivity, 2nd generation, has lower bioavailability and renal clearance
Definition
atenolol
Term
nonselective A blocker, competitive, useful in treating pheochromocytoma
Definition
phentolamine
Term
competitive B antagonist, depresses membrane excitability, has adverse effects (cardiac depression, bronchoconstriction, hypoglycemia in susceptible pts, and CNS effects)
Definition
propanolol
Term
selective B2 agonist, short-acting, used for rescue therapy/bronchodilation in asthmatics
Definition
albuterol
Term
selective B2 agonist, used for long-term asthma therapy
Definition
salmeterol
Term
stimulation of D1 receptors in kidney, also has direct A/B agonist properties and indirect sympathomimetic activity, tx for shock
Definition
dopamine iv infusion
Term
non-selective A/B agonist, tx for anaphylaxis
Definition
epinephrine
Term
non-selective B agonist, more potent at active site than epinephrine
Definition
isoproterenol
Term
A2 agonist, acts in CNS to decrease SNS heart and BV activity, known for causing hypertensive crisis following rapid withdrawal
Definition
clonidine
Term
A1 agonist, constricts smooth muscle, treats nasal congestion/ophthalmic hyperemia/shock
Definition
phenylephrine
Term
direct and indirect agonist at A, causes vasoconstriction and relieves swelling in nasal mucosa
Definition
pseudoephedrine
Term
direct B agonist, indirect agonist for both, has more sustained action due to MAO/CoMT resistance, shows risk of potentiation when combined with MAOI
Definition
ephedrine
Term
fermented by bacteria in cheese and aged wine, broken down by MAO, has strong indirect sympathomimetic effect if it reaches nerve terminals, causes "wine and cheese syndrome"
Definition
tyramine
Term
amphetamine-like CNS stimulant, tx for ADHD
Definition
methylphenidate
Term
CNS-active indirect sympathomimetic agent, potent stimulator, can suppress appetite, has sympathetic adverse effects
Definition
amphetamine
Term
stimulates A/B1, has lower potency than EPI
Definition
norepinephrine
Term
selective A2 agonist at presynaptic terminals, inhibits adrenergic output, decreases NE, tx for hypertension during pregnancy, has rare hepatic side effects
Definition
methyldopa
Term
drug of abuse, chemical composition close to pseudoephedrine, acts as indirect sympathomimetic (A) activity
Definition
methamphetamine
Term
blocks NET, enhances NE signaling, decreases uptake for recycling, produces euphoria and dangerous cardiac effects, used as vasoconstrictor for nasal surgeries
Definition
cocaine
Term
selective inhibitor of NET, also acts at A2, enhances NE levels in synapse, used for ADD tx
Definition
atomoxetine
Term
blocks MAO, increases concentration of catecholamines, used to treat depression
Definition
iproniazid
Term
COMT inhibitor, adjunct therapy of Parkinson's
Definition
entacapone
Term
acts as fake substrate, blocks tyrosine hydroxylase, depletes NE, blocks sympathetic transmission
Definition
metyrosine
Term
blocks VMAT, decreases NE, used for hypertension, rarely used due to severe depression
Definition
reserpine
Term
blocks NET, displace NE from vesicle, depletes NE after gradual release, almost never used for hypertension
Definition
guanethedine
Term
used to make diagnosis of Horner's syndrome from pre- or postganglionic causes...if postganglionic source pupil will constrict
Definition
hydroxyamphetamine
Term
cholinesterase inhibitor, carbamate, serves as substrate, medium-acting (30min-6h) enters CNS, treats myasthenia gravis
Definition
physostigmine
Term
cholinesterase inhibitor, medium-acting, does not enter CNS
Definition
neostigmine
Term
reversible cholinesterase inhibitor, noncovalent, very short acting (2-10min), treats Alzheimer's
Definition
donepezil
Term
reversible noncovalent cholinesterase inhibitor, does not enter CNS
Definition
edrophonium
Term
irreversible cholinesterase inhibitor, organophosphate, for topical use only
Definition
echothiophate
Term
organophosphate cholinergic inhibitors, used as insecticides, cause muscle weakness/resp failure/asphyxiation/bradycardia/death
Definition
parathion, malathion
Term
nerve gases, cause resp failure/death
Definition
sarin, VX
Term
treats peripheral effects of organophosphate poisoning, pulls off irreversible substrates, reverses NMJ effects/bradycardia/secretions
Definition
2-PAM
Term
treats CNS effects of organophosphate poisoning, reverses decreased resp drive/convulsions/muscarinic R hyperactivity; is anticholinergic at muscarinic receptors, formerly used in COPD/asthma tx, problem is selectivity
Definition
atropine
Term
muscarinic agonist, found in nature, enters CNS, causes bradycardia/N/V/secretions/visual disturbances/hypertension, may present in the ED as "a bad batch of 'shrooms"
Definition
muscarine
Term
used in S. America as cure for poisoning, "that which causes slobbering," now used as glaucoma/xerostomia tx, notorious for not staying where it is put topically
Definition
pilocarpine
Term
synthetic Ach analog, causes GI stimulation and treats urinary retention
Definition
bethanecol
Term
synthetic Ach analog, used in asthma evaluation, causes hyperreactive airways in asthmatics, NEVER ADMINISTER IV OR IM!!!, contraindications: asthma/peptic ulcer/coronary insufficiency
Definition
methacholine
Term
activator of nicotinic Rs in periphery and CNS, can cause CNS stimulation/vomiting/ADH release/tachycardia/hypertension/increased parasymp response then blocks/NMJ block
Definition
nicotine
Term
"Sux the life out of you," produces depolarizing blockade at nicotinic cholinergic R, used for muscle paralysis during surgery, side effects: muscle soreness/hyperkalemia
Definition
succinylcholine
Term
A4B2 partial nicotinic Ach R agonist that binds in CNS and releases dopamine from reward center in brain, blocks nicotine binding, half-life=24hr, excreted unchanged in urine, has adverse effects like nausea/weird dreams/constipation/vomiting
Definition
varenicline
Term
anticholinergic that is highly lipophilic, enters CNS more readily than atropine, transdermal administration useful in tx of motion sickness
Definition
scopolamine
Term
antimuscarinic with similar activity to atropine, has quaternary nitrogen in molecular structure, used in tx of asthma/COPD due to poor absorption and therefore fewer systemic side effects
Definition
ipratropium
Term
antimuscarinic lacking R selectivity, used to treat overactive bladder, causes typical anticholinergic effects but w/ less severity
Definition
tolterodine
Term
ganglionic blocker, action is to block nicotinic acetylcholine R channel, paralyzes entire autonomic nervous system, tx for HTN (obsolete), dissecting AoA, hemorrhage during surgery, and autonomic hyperreflexia
Definition
hexamethonium
Term
competitive antagonist at the nicotinic Rs at the NMJ, contains quaternary nitrogen, used in paralysis during surgery, adverse effect is arterial pressure fall
Definition
d-tubocurarine
Term
class IA antiarrhythmics, dissociate intermediately from resting state of fast Na channel, channel block modestly enhanced at faster heart rates, increase AP duration, prolong refractory period by blocking K channels for phase 3
Definition
quinidine, procainamide
Term
act at phase 0 of depolarization by blocking fast Na channels, slow conduction and create favorable conditions for a block, suppress abnormal automaticities, terminate reentrant arrhythmias and protect ventricles in supraventricular tachyarrhythmias
Definition
Class I antiarrhythmic drugs in general
Term
class IB antiarrhythmic, IV only for antiarrhythmic tx, no ANS effects, dissociates very quickly from rested state of Na channel, causes greater blockade when HR is high by creating beat-to-beat accumulation of Na blocked channels, decreases both effective refractory period and AP duration, rapid hepatic clearance, DO NOT GIVE WITH EPINEPHRINE
Definition
lidocaine
Term
class IA, for oral use only, acts as muscarinic and A adrenergic receptor blocker, interacts w/ digoxin to double plasma levels of digoxin, adverse effects: hypotension/GI effects/decreased contractility/syncope
Definition
quinidine
Term
muscarinic R blocker in ANS, oral or IV use, metabolized 3-4hr hepatic and renal, metabolite has Class III (K+ channel blocking) properties, adverse effects: N/V/lupus-like autoimmune syndrome/torsades de pointes
Definition
procainamide
Term
B adrenergic R antagonists, decrease rate of phase 4 depolarization in automatic cells--decreased HR and ectopic automaticity, enhance AV block, lower contractility and O2 demand, ex: propanolol, esmolol
Definition
Class II drugs
Term
prolong AP duration/refractory period/repolarization, blocks phase 3 K channels, specific to atrial, ventricular, and Purkinje fibers
Definition
Class III drugs
Term
class IC, block fast Na channels, decreases slope of phase 0, shows marked effects at normal HRs, greatly slows conduction w/ little effect on refraction or AP duration, oral only, also blocks K channel in repolarization (longer AP in ventricles)
Definition
flecainide
Term
oral and IV use, class III, prolongs duration by blocking K channels, also decreases slope of phase 4 depolarization/AV conduction through Ca channel block/Vmax of fast response Na channels, highly lipophilic, long-term use can cause potentially fatal pulmonary fibrosis at high doses
Definition
amiodarone
Term
Ca channel blockers, blockade of L-type myocardial and SM channels, have major effects on slow response APs (sinus and AV nodes, damaged/depolarized cardiomyocytes), decrease slope of phase 4 depolarization AND slow HR, decrease rate/amplitude in phase 0 causing slow AV conduction, more effective at faster HRs
Definition
Class IV drugs
Term
oral or IV use, hepatic metabolism, half-life 4 hrs, decreases cardiac contractility, decreases arterial pressure (beware of baroreflex tachycardia), tx for supraventricular arrhythmias, Ca channel blocker, significant effect on coronary vasodilation, decreases node rates/HR/contractility
Definition
diltiazem
Term
miscellaneous drug, ultra-fast-acting drug given by IV bolus, acts through G-protein coupled receptors, vagomimetic, slows AV conduction/inhibits DADs, used for conversion of paroxysmal supraventricular tachycardia to sinus rhythm
Definition
adenosine
Term
cardiac glycoside, blocker of Na/K/ATPase, used to treat A-fib and heart failure, slows conduction and increases refractory period, depolarizes baroreceptor nerve endings resulting in their sensitization, increases parasympathetic activity, problems: DADs, complete heart block, ventricular arrhythmia
Definition
digoxin
Term
ACE inhibitor, first of its kind, hepatic and renal metabolism, half-life 2 hrs, PO, can cause: hypotension/chronic cough/angioedema/fetal pathologies in 2nd and 3rd trimester/hyperkalemia
Definition
captopril
Term
ACE inhibitor pro-drug that must be de-esterified to active form, renal excretion, half-life 11hrs, fewer GI effects than counterpart
Definition
elanapril
Term
ACE inhibitor active as parent compound
Definition
lisinopril
Term
inhibit conversion of angiotensin I to II, increase bradykinin (vasodilator) by inhibiting kininase II, cause vasodilation/decreased aldosterone/decreased sympathetic activity/reduced interstitial fibrosis and myocardial remodeling/anti-apoptotic, mandatory tx of heart failure
Definition
ACE inhibitors
Term
AT1 receptor blockers, block apoptosis and hypertrophic growth, address issues where ACEs stop, do not produce cough and are just as effective
Definition
ARBs
Term
acts as an exogenous NO donor, allows for relaxation of smooth muscle and decreases arterial wall tension, can be administered in 5 different ways, rapid onset
Definition
NTG
Term
acts as an exogenous NO donor, given sublingually and orally, half-life=hours, subject to first-pass effect
Definition
isosorbide dinitrate
Term
Ca channel blocker, has moderate activity in peripheral/coronary vasodilation, decreases HR/ SA node firing/ AV node firing/ contractility
Definition
verapamil
Term
Ca channel blocker, has significant vasodilation properties in arterial and coronary sites, INCREASES HR, has no effect on contractility or node firing
Definition
nifepidine
Term
phosphodiesterase 5 inhibitor, increases cGMP in smooth muscle cells, increases vasodilation, has low oral bioavailability, metabolized by CYP3A4, ABSOLUTELY CONTRAINDICATED W/ NITRATES, adverse effects: fatal reduction in arterial P/ flushing/ dyspepsia/ transient abnormal vision
Definition
sildenafil
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