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Pharmacokinetics: Absorption: Rapid; food decreases the rate but the extent of absorption; administration with food minimizes risks of orthostatic hypotension.
Metabolism: First-pass metabolism, extensively metabolized primarily by aromatic ring oxidation and glucuronidation (2% excreted unchanged); 3 active metabolites (4-hydroxyphenyl metabolite is 13 times more potent than parent drug); plasma concentrations in the elderly and those with cirrhotic liver disease are 50% and 4-7 times higher, respectively.
Bioavailability: 25-35%.
Half-Life: 7-10 hrs.
Elimination: Primarily via bile into feces.
