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Pharmacokinetics and pharmacodynamics of benazepril hydrochloride in patients with major proteinuria.

Schweizer, C and Kaiser, Guenther and Dieterle, W and Mann, Jacinta (1993) Pharmacokinetics and pharmacodynamics of benazepril hydrochloride in patients with major proteinuria. European journal of clinical pharmacology, 44 (5). pp. 463-466. ISSN 0031-6970

Abstract

We have investigated whether the pharmacokinetics and pharmacodynamics of the ACE inhibitor benazepril hydrochloride are altered with proteinuria by studying 8 patients with major proteinuria of different causes who were given a single dose of 10 mg p.o. The maximum plasma concentration of benazepril was found between 0.5 and 2 h after dosing (median 1 h). Its elimination was almost complete within 6 h. Peak plasma levels of benazeprilat, the active metabolite of benazepril, were observed between 1 and 6 h (median 2.5 h). The elimination of benazeprilat from plasma was biphasic, with mean initial and terminal half-lives of 3.0 and 17.3 h, respectively. On average, the pharmacokinetic parameters of benazepril and benazeprilat in the patients did not differ from those in a historical control group of healthy volunteers, but intersubject variability in the AUC and half-lives of benazeprilat was greater in the patients. Plasma ACE was completely inhibited from 1.5 to 6 h after dosing, and at 48 h the mean inhibition was still 42%. Plasma renin showed substantial intersubject variation. Mean supine blood pressure (systolic/diastolic) was reduced from baseline by a maximum of 18/13 mm Hg at 6 h. Proteinuria was diminished after benazepril in 7 patients. In conclusion, the results of this study suggest that proteinuria in the nephrotic range does not require a change in benazepril dosage.

Item Type: Article
Date Deposited: 31 Jan 2012 00:45
Last Modified: 01 Feb 2013 00:45
URI: https://oak.novartis.com/id/eprint/6614

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