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The influence of food on the pharmacokinetics and ACE inhibition of cilazapril.
Author(s) -
Massarella JW,
DeFeo TM,
Brown AN,
Lin A,
Wills RJ
Publication year - 1989
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1989.tb03483.x
Subject(s) - cilazapril , pharmacokinetics , bioavailability , crossover study , chemistry , metabolite , active metabolite , pharmacology , cmax , angiotensin converting enzyme , urine , ramipril , oral administration , endocrinology , ace inhibitor , medicine , biochemistry , blood pressure , placebo , alternative medicine , pathology
1. The influence of food on the pharmacokinetics and angiotensin‐ converting enzyme (ACE) inhibitory effects of oral 5 mg doses of cilazapril was investigated in a two‐way crossover study in 16 volunteers. 2. Plasma and urine concentrations of cilazaprilat, the active diacid metabolite of cilazapril, and plasma ACE activity were determined by a radio‐enzymatic method. 3. Cmax decreased by 30% (P less than 0.05) with a delay in (t)max of 1 h (P less than 0.05) and area under curve (AUC) was decreased by 14% (P less than 0.05). The elimination rate was unaltered. 4. Onset of ACE inhibition was delayed by approximately 30 min but degree and duration were unaffected. 5. The effect of food on the bioavailability of cilazapril at this dose would not be expected to be clinically significant.