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51 Cards in this Set
- Front
- Back
Isoproterenol
|
isuprel
non-selective Beta-AR agonist extremely potent Beta-AR potent vasodilator positive chronotropy |
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Adverse reactions: isoproterenol
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tachycardia, BP, arrhythmias
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Phenylephrine
(neosynephrine) |
alpha-1 AR agonist
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Phenylephrine
|
relatively pure alpha-AR agonist
potent constrictor similar but less potent than NE not inactivated by COMT (increase the bioavailability) nasal decongestion, mydriatic (dilation of pupil), hypertensive |
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Clonidine
|
catapress
alpha-2 AR agonist |
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Clonidine
|
alpha-2 agonist
orally prolonged hypotensive response (CNS) IV, acute hypertensive response followed by hypotension |
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Clinical uses for Clonidine
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hypertension, menopausal flushing, and migraines
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Adverse effects of Clonidine
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remember, Clonidine is an alpha-2 agonist
dry mouth, sedation, and contact dermatitis |
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Dobutamine
|
Dobutrex
Beta-1 AR agonist |
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Dobutamine
Dobutrex |
Beta-1 AR agonist
acts directly on B1-AR in the heart force > rate cardiogenic shock |
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Dobutamine
Dobutrex (non-heart related things) |
dilates renal and mesenteric vessels
IV infusion for (+) inotropic effect in cardiac decompensation |
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Dobutamine
Adverse reactions |
tachycardia, hypertension, hypotension, ectopic activity
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Albuterol
|
Ventolin
Beta-2 AR agonist |
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Albuterol
(Ventolin) |
bronchodilator: oral, inhalation, and IV
adverse reactions: tachycardia, tremor, tolerance |
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Ephedrine
|
indirect acting agonist
alkaloid from plant increases NE release, direct agonism prolonged action duration, potent CNS stimulant nasal decongestant, treatment hypotension |
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adverse reactions of Ephedrine
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hypertension, insomnia, tachyphylaxis
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Amphetamine
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indirect acting agonist
release of biogenic amines from storage has no hydroxyl groups and is therefore hydrophobic...can easily get into the CNS |
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Amphetamine activites
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potent CNS stimulant
prolonged action duration treatment of obesity, narcolepsy, attention deficit disorder |
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Adverse reactions of amphetamine
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restlessness, tremor, irritability, insomnia, dependency, and tolerance
|
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Tyramine
|
indirect acting agonist
release of biogenic amines from storage (like NE and epi) byproduct of tyrosine metabolism high concentration in fermented blood metabolized by liver MAO caution MAO inhibitors, severe hypertension |
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Cocaine
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indirect acting agonist
inhibition of NE and dopamine reuptake local anesthetic effect also potent CNS stimulant shorter lasting, but more intense, than amphetamine hypertension, AMI, arrhythmias, seizures |
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activation of alpha-1 AR causes...
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contraction and constriction
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activation of alpha-2 AR causes...
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inhibition of NE release
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activation of Beta-1 AR causes...
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increase in heart rate and contractility
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activation of beta-2 AR causes...
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relaxation of smooth muscle airways and uterus
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sympatholytic
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blocks sympathetic activity
|
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3 mechanisms to block sympathetic activity
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1. decrease sympathetic outflow from brain
2. suppress nerve terminal NE (inhibit synthesis, deplete granules, and suppress release of NE) 3. block postsynaptic receptors (best way) |
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bretylium and guanethidine
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inhibits the release of NE from the nerve terminal
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alpha-AR blockers
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vasodilation, decreases BP
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Phentolamine
(Regitine) |
Regitine
a nonselective alpha-AR blocker reversible rarely used |
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Phenoxybenzamine
(Dibenzyline) |
Dibenzyline
alpha-AR blocker irreversible use in peripheral vasospasm |
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adverse reactions to alpha-AR blockers
|
hypotension, tachycardia
|
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alpha-1 selective blockers
|
vasodilation and reduction in arterial pressure
no reflex tachycardia useful for hypertension and BPH no decrease cardiac function |
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alpha-2 selective blockers
|
are not clinically useful
|
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Prazosin
|
Minipress
antihypertensive used alone or in combination alpha-1 AR selective blockers |
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Adverse reactions of prazosin (minipress)
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"first dose" effect
postural hypotension |
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Beta-1 AR blockade reactions
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CV effects:
reduce HR, delay AV conduction, decrease rate of depolarization, decrease force of contraction, decrease O2 consumption, decrease BP, inhibit renin release, and peripheral edema |
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Beta-2 AR blockade reactions
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vasoconstriction in arterioles, increased airways resistance, decreased glycogenolysis and gluconeogenesis, and inhibition of insulin release
(MUST be careful in diabetic and asthmatic patients...for diabetics, you can really cause severe hypoglycemia) |
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Propranolol
|
Inderal
beta-AR non selective blocker |
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Propranolol
Inderal |
beta-AR non selective blocker
degree of antagonism is dependent on the prevailing sympathetic tone exhibits equal affinity for beta 1 and beta 2 highly lipophilic, readily enters CNS membrane stabilizing effect observed at higher concentrations |
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Uses of propranolol (Inderal)
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used in treatment of hypertension and IHD
IV for life-threatening arrhythmias IV and oral formulations |
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Serious reactions of Propranolol (Inderal)
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severe bradycardia, CCF, bronchoconstriction, hypoglycemia, and aggravated PVD
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Timolol
|
Blocadren
beta-AR non selective blocker |
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Timolol (Blocadren)
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no intrinsic sympathomimetic activity
no membrane stabilizing low lipophilicity used to treat open angle glaucoma adverse reactions: bronchoconstriction |
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Pindolol
|
Visken
has intrinsic sympathomimetic activity partial agonist activity low degree of membrane stabilization adverse reaction: bronchoconstriction, bradycardia |
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the partial agonist activity of Pindolol is important because...
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1. maintains some degree of beta-1 AR activation while blunting the cardiac response to increased SANS
2. produces smaller reductions in resting HR 3. useful in patients dependent on sympathetic drive because of poor cardiac reserve 4. preferred in patients subject to bradycardia |
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Sotalol
|
Betapace
beta-AR non-selective blocker prolongs cardiac action potential blocks K+ channels used for atrial and ventricular tachyarrhythmias |
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Metoprolol
|
Lopressor
Beta-1 AR selective blocker no ISA hepatic biotransformation (can give to patients with renal insufficiency) used for hypertension, ischemic HD adverse reactions: bronchoconstriction and bradycardia |
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Atenolol
|
Tenormin
Beta-1 selective blocker hypertension renal excretion (use with patients who have liver problems) ischemic heart disease adverse reaction: bronchoconstriction, bradycardia |
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Labetolol
|
Normodyne, trandate
Beta-non selective blocker and alpha-1 AR blocking Beta-1 = beta 2 > alpha 1 > alpha 2 hypertension and pheochromocytoma adverse reactions: hypotension, tachycardia |
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Carvedilol
|
Coreg
beta-AR non selective blocker and alpha-AR blocking Beta-1 = Beta-2 > alpha1 > alpha2 antioxidant effects improves survival with heart failure |