Pharmacokinetics and depressor effect of delapril in patients with essential hypertension.
The pharmacokinetics and depressor effect of a nonsulfhydryl angiotensin-converting enzyme inhibitor, delapril, was assessed by administering a single dose of 30 mg to nine patients with mild to moderate essential hypertension. Orally administered delapril is a prodrug and must be deesterified to its active metabolites, delapril diacid and 5-hydroxy delapril diacid. The pharmacokinetic parameters for delapril, delapril diacid, and 5-hydroxy delapril diacid were, respectively: t 1/2 0.30, 1.21, and 1.40 hours; Cmax 489, 635, and 229 ng/ml; AUC 572, 1859, and 948 ng X hr/ml. Delapril produced significant decreases in systolic blood pressure and angiotensin-converting enzyme activity 24 hours after dosing. There were no significant changes in the endogeneous creatinine clearance after the drug. Thus delapril may represent a useful antihypertensive agent for control of blood pressure in patients with essential hypertension.
D000328:Adult; D000959:Antihypertensive Agents; D001794:Blood Pressure / Q000187:drug effects; D003864:Depression, Chemical; D005260:Female; D006207:Half-Life; D006801:Humans; D006973:Hypertension / Q000378:metabolism*; D007189:Indans / Q000378:metabolism* / Q000494:pharmacology; D007192:Indenes / Q000378:metabolism*; D007700:Kinetics; D008297:Male; D008875:Middle Aged; D011674:Pulse / Q000187:drug effects; D012084:Renin-Angiotensin System / Q000187:drug effects
D000959:Antihypertensive Agents; D007189:Indans; D007192:Indenes; C047759:delapril