Review of the Pharmacokinetics of Fosinopril in Special Populations

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Fosinopril, the first of a new class of angiotensin-converting enzyme (ACE) inhibitors, the phosphinic acids, is a prodrug that is rapidly and completely hydrolysed to its pharmacologically active form, fosinoprilat. In contrast to other long-acting ACE inhibitors such as enalapril and lisinopril, which are eliminated exclusively by the kidney, fosinoprilat is eliminated by both the hepatobiliary and renal routes. Compensatory excretion of the active metabolite by the unimpaired route occurs in patients with impaired renal or hepatic function. Accumulation of active ACE inhibitor is significantly less in renally compromised patients receiving fosinopril 10 mg/day than in those receiving enalapril 2.5mg or lisinopril 5 mg/day. There is no significant difference between young and elderly volunteers in the pharmacokinetics of fosinoprilat. These data suggest that modification of the fosinopril dosage on the basis of advanced age or impaired renal or hepatic function is not necessary.