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Sympatholytics

sypatholytic drugs

QuestionAnswer
alpha antagonist nonspecific phenoxybenzamine phentolamine
alpha one selective antagonist Prazosin Terazosin Doxazosin Alfuzosin Tamsulosin
alpha 2 selective antagonist Yohimbine
Beta antagonist nonspecific Propranolol Penbutolol Pindolol Carteolol Nadolol Sotalol Timolol
Beta 1 selective antagonist butoxamine
mixed alpha and beta activity Carvedilol labetalol
Tyrosine hydroxylase inhibitor Metyrosine
phenoxybenzamine MOA, kinetics, clinical use, toxicity MOA: ire inhib of aR, preve up of NE, block H1, AcHR, and sero receptors. Mainly blocking vasocon by a1R on vasc kine: long dur, 14-48 hrs, oral adm w/ grad increas dose use: pheochromocytoma tox: postural hypotension, reflex tachycard sedation nas n
phentolamine revers a antagonist NE release via a2 presynap R block, inhibits ser, agonist at mus, H1 and H2 histamine R kine: oral availability use: pheochromocytoma, and injected in penis to treat male ED tox:"dirty drug" effects many R sys, similar tox as phe
Prazosin Terazosin Doxazosin Alfuzosin MOA and tox antagonist to alpha-adrenergic receptors= prevents vasculature constriction (hypotension), Miosis (outflow of aqueous humor), relaxes SM in urinary tract tox:orthostatic hypotension, first dose syncope, palpitations, blurred vision, priapism, GI upset
Prazosin Terazosin Doxazosin uses hypertension, Raynaud's phenomenon, BPH-urinary obstruction
Alfuzosin kinetics and use t 1/2 5 hours use: BPH-urinary obstruction
Tamsulosin a (one A) antag, a1A R are promin in prostate and less important in vasc SM contrac (does not effect BP) high bioavail, long T1/2- 9-15 hr BPH-urinary obstruction 1st dose syncope, abnormal ejaculation, headache, dizziness, sleep problems, GI-diarrhe
Yohimbine alpha 2 receptor antagonist (= more norepinephrine release from sympathetic terminals) impotence (disputed) increased catechol tone via blockade of presynaptic a2 (inhibitory receptors) leading to non attenuated NE release
Propranolol MOA prototype nonspecific beta receptor blocker, slow heart rate and reduce contractile force, inhibit rennin release from kidney, reduce aqueous humor secretion, bronchoconstriction, inhibit hepatic glycogenolysis, anesthetic properties
propranolol kinetics oral absorption, extensive first pass metabolism, variable bioavailability half life 3-6 hours
propranolol clinical uses: hypertension, glaucoma, ischemic heart disease, post-MI prophylaxis, stage fright, tremor, migraines, portal hypertension,
propranolol toxicity bronchocons (avoid asthma or COPD), bradycardia, (-)ive inotropy (avoid with CHF), hypoten, arrhythmias, sedation and depres, reduce recover from hypogly (problem with diabetics), withdraw occur (taper dose), impotence, (-)ive GI effects, alter lip pan
Penbutolol MOA and kinetics (ISA) Partial agonist, similar effects to propranolol, except incomplete blockade of lungs and heart function and no anesthetic action high lipid solubility (CNS effects), good bioavailability, t1/2 5 hr
Pindolol MOA (ISA) Partial agonist, similar effects to propranolol, except incomplete blockade of lungs and heart functionsimilar to penbutolol, moderate lipid solubility
Penbutolol Pindolol use and tox: used for hypertension and angina when less bradycardia or bronchodilation is important similar to propranolol, except less bradycardia and bronchodilation and perhaps more CNS effects
Carteolol MOA (ISA) similar to penbutolol low lipid solubility, otherwise similar to penbutolol topical drops for glaucoma, similar topical beta blockers (timolol, betaxolol, levobunolol, metipranolol)
Carteolol Nadolol toxicity similar to penbutolol except less CNS effects
Nadolol Sotalol Timolol MOA similar to propranolol without anesthetic action tox: similar to propranolol
Nadolol long duration, 14-24 hours, low lipid solubility portal hypertension (w. Isosorbide mononitrate)
Sotalol as above but w/ t1/2 12 hrs. Supraventricular arrhythmias
Timolol moderate solubility, t1/2 4-5 hours topical glaucoma treatment
butoxamine blockade of beta two receptors does nothing but produce bronchoconstriction no clinical value bronchoconstriction
Metyrosine inhibits the rate limiting enzyme (tyrosine hydroxylase) necessory for all catecholamine synthesis pheochromocytoma extrapyramidal symptoms (loss of dopamine), orthostatic hypotension (loss of sympathetic control of vessels), crystalluria
Acebutolol (ISA) more selective at beta 1 with partial agonist activity, anesthetic effects low lipid solubility, otherwise similar to penbutolol hypertension, angina,
Created by: 925love
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