Pharmacokinetics and depressor effect of delapril in patients with essential hypertension.

Abstract

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.

• Authors: H Shionoiri, G Yasuda, A Ikeda, T Ohta, E Miyajima, Y Kaneko
• Journal: Clinical pharmacology and therapeutics (Clin Pharmacol Ther) Vol. 41 Issue 1 Pg. 74-9 (Jan 1987) ISSN: 0009-9236 [Print] United States
• PMID: 3802709 (Publication Type: Journal Article)

Chemical References

• Antihypertensive Agents
• Indans
• Indenes
• delapril

Topics

• Adult
• Antihypertensive Agents
• Blood Pressure (drug effects)
• Depression, Chemical
• Female
• Half-Life
• Humans
• Hypertension (metabolism)
• Indans (metabolism, pharmacology)
• Indenes (metabolism)
• Kinetics
• Male
• Middle Aged
• Pulse (drug effects)
• Renin-Angiotensin System (drug effects)