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The pharmacokinetics and dose proportionality of cilazapril.
Author(s) -
Massarella J,
DeFeo T,
Lin A,
Limjuco R,
Brown A
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.tb03482.x
Subject(s) - cilazapril , pharmacokinetics , pharmacology , active metabolite , crossover study , angiotensin converting enzyme , chemistry , ace inhibitor , metabolite , medicine , blood pressure , placebo , alternative medicine , pathology
1. The pharmacokinetics and dose proportionality of cilazapril, an orally active angiotensin‐converting enzyme (ACE) inhibitor, were investigated in a four‐way randomized crossover study in 24 volunteers, over the 0.5 to 5 mg dose range intended for therapeutic use. 2. Plasma concentrations of cilazapril and of the active metabolite cilazaprilat together with plasma ACE activity were determined by radio‐enzymatic assay. 3. Plasma concentrations of both cilazapril and cilazaprilat increased in proportion to dose over the range studied. All doses produced substantial inhibition of ACE. Higher doses were associated with earlier onset and longer duration of maximal effect.