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Pharm Autonomic NS
Adrenergic Antagonists
| Question | Answer |
|---|---|
| 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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