Absorption Metabolism Excretion

Prazosin is readily absorbed after oral administration, peak serum levels occur approximately 2 hours after a single oral dose, and the antihypertensive effect of pra-zosin persists for up to 10 hours. Its half-life in plasma ranges from 2.5 to 4 hours, and elimination from plasma appears to follow first-order kinetics. The drug is extensively (perhaps as high as 97%) bound to plasma proteins; this observation partially explains the lack of correlation between plasma drug levels and persistence of antihypertensive effect.

Hepatic O-dealkylation and glucuronide formation appear to be major pathways of biotransformation. Only about 10% of orally administered prazosin is excreted in the urine. Plasma levels of prazosin are increased in patients with renal failure; the nature of this interaction is unknown.

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