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Pharm Autonomic NS

Adrenergic Antagonists

QuestionAnswer
NONSELECTIVE ALPHA ANTAGONISTS phentolamine[Regitine], phenoxybenzamine [Dibenzyline]
approximate equal affinities for postsynaptic alpha 1, presynaptic alpha 2
as a result of the blockade of the postsynaptic alpha 1 lowered BP
as a result of the blockade of presynaptic alpha 2 reflex cardiac stimulation b/c the negative feedback inhibition of neurotransmitter release is being blocked
not used for tx of HTN, but used in tx of pheochromocytoma to prophylax against hypertensive crisis as a result of release of norepi from the tumor
SELECTIVE ALPHA 1 ANTAGONISTS doxazosin [Cardura], prazosin [Minipress], terazosin [Flomax], alfuzosin [Uroxatral], silodosin [Rapaflo]
reversibly block the effects of catecholamines at the postsynaptic aplha 1 receptors in vascular smooth muscle and in the smooth muscle of the bladder neck and prostate
can be used to treat HTN and BPH doxazosin [Cardura], prazosin [Minipress], terzosin [Hytrin]
used to tx BPH only tamsulosin [Flomax], alfuzosin [Uroxatral], silodosin [Rafapflo]
pharmacodynamics: reversible block postsynaptic alpha 1 resulting in decreased arterial and venous vasoconstriction, decrease in peripheral vascular resistance
both supoine and standing BP are lowered with most pronounced affect on diastolic BP
alpha 1 receptors are densely located in the bladder neck and prostate galnd therefore these drugs are able to reduce bladder outflow obstruction without afffecting bladder contractility
all the azosin drugs are contraindicated in the presence of volume depletion and CHF because of peripheral vasodilaton
risk for a 'first dose' reaction within 30-90 minutes of orthostatic hypotension, esp with terazosin
alpha 1 adrenergic blockade nasal congestion, blurred vision, dry mouth, constipation, impotence, and urinary frequency
clinical use: hypertension drug of choice for treating HTN in older men with BPH
All drugs in this class also raise HDL levels and reduce total cholesterol and triglycerides
Doxazosin and terazosin also lower LDL
also enhance insulin sensitivity, cause regression of LVH and improve the activity of the fibrinolytic system making them useful for pts with DM and HF
usually must be used in combination therapy because of troublesome adverse rxns in almost all patients.
also used off label to facilitate the passage of kidney stones Hytrin, Flomax, and Cardura
Cardura may be used as monotherapy because it is the least likely in class to produce postural hypotension and fluid retention
leading cause of nonadherence is ejaculatoion inhibition and impotence (Uroxatral has less problem with this)
Created by: heatherbrown2020
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