adrenergic agonists and antagonists

25 terms by lindsayjoproud 

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phenylephrine

alpha 1 selective agonist
causes vasoconstriction and mydriasis
uses: nasal decongestant, eye surgery

oxymetazoline

non-selective alpha agonist
causes vasoconstriction and mydriasis
uses: nasal decongestant, eye surgery

clonidine

alpha 2 selective agonist
inhibits medullary CV center to lower BP
IV: 1st dose idiosyncratic (extrajunctional receptors), remaining doses decrease NE release (presynaptic receptors)
Oral: accumulates in brain, inhibits CV center
WITHDRAWAL: major concern, headache, etc. REBOUND HYPERTENSION

methyldopa

alpha 2 selective prodrug
converted > methyl-dopamine > methyl-NE
inhibits medullay CV center

dobutamine

beta 1 selective agonist, DA analog
causes increased contractility > increase CO
not much effect on HR
uses: cardiogenic shock, congestive heart failure

metaproterenol

non-specific beta agonist
uses: asthma, bronchospasm

albuterol, pirbuterol, terbutamine

beta 2 specific agonist
short duration
uses: asthma, bronchospasm, also given IV to stop labor

salmeterol, formoterol

beta 2 selective agonists
long duration of action
uses: asthma (in conjunction with steroids)

ephedrine

mimics epinephrine effect, less potent
uses: asthma and myasthenia gravis

pseudoephedrine

mimics epinephrine effect, less potent
uses: nasal decongestant

phentolamine

non-selective alpha antagonist
alpha 1 block: vasodilation of veins and arteries > orthostatic hypotension and decreased BP
alpha 2 block: prevents negative feedback to increase NE release
uses: short-term treatment of HTN in patients with pheochromocytoma

phenoxybenzamine

predominant alpha 1 blocker, some alpha 2 antagonism
IRREVERSIBLE
drop in arterial pressure > reflex increase in CO and HR
increased NE release
increased cutaneous and splanchnic flow
uses: Raynaud's, pheochromocytoma

prazosin (doxazosin, alfuzosin, tamsulosin)

selective alpha 1 blocker
inhibits contraction of smooth muscle > vasodilation
less intense response than non-selectives, no increased NE release
uses: essential hypertension, CHF, UTI associated with BPH
side effects: 1st dose postural hypotension and syncope

indoram

selective alpha 1 blocker
uses: hypertension, Raynaud's

yohimbine

selective alpha 2 blocker
causes vasodilation
uses: erectile dysfunction, Raynaud's

propandolol

non-selective beta antagonist
beta 1 block > decreased contractility and HR > decreased CO
decreased slope of pacemaker potential > prevent reentrant arrhythmias
uses: angina, arrhythmias, hypertension
side effects: bradycardia, bronchospasm, AV block, hypoglycemia

pindolol

beta 1 antagonist + beta 2 partial agonist
antihypertensive
less likely to cause bronchoconstriction and hypoglycemia, because of beta 2 partial agonism

metoprolol

selective beta 1 blocker
decreases CO, antihypertensive, antiarrhythmic
less bronchoconstriction
less hypoglycemia
crosses BBB > depression, fatigue, loss of libido

atenolol

selective beta 1 blocker
less bronchoconstrictoin
less hypoglycemia
does not enter CNS

esmolol

selective beta 1 blocker
very short half-life
rapid onset and cessation of beta blockade
used in URGENT setting when immediate onset is needed

labetalol

beta 1 antagonist + beta 2 partial agonist + alpha 1 antagonist
alpha 1 block > vasodilation
beta 1 block > decreased HR, decreased renin > decreased BP
beta 2 partial agonism > less bronchoconstriction and hypoglycemia
uses: chronic hypertension, hypertensive crisis (IV)

carvedilol

beta 1 antagonist + beta 2 partial agonist + alpha 1 antagonist + antioxidant and antiproliferative properties
uses: congestive heart failure, myocardial infarction, chronic heart failure

nebivolol

beta 1 antagonist + vasodilatory effects
lowers BP without decreasing left ventricular function
reduces peripheral resistance
vasodilation mediated by NO

metyrosine

inhibits tyrosine hydroxylase > no catecholamine production
uses: pheochromocytoma

quanethidine

rarely used antihypertensive
decreases activity of postganglionic sympathetic neurons
inhibits synaptic vesicle fusion

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