Abstract
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.
Keywords: cilazapril, pharmacokinetics, volunteers, ACE inhibition
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- Fasanella d'Amore T., Bussien J. P., Nussberger J., Waeber B., Turini G. A., Brunner H. R., Kler L., Francis R. J. Effects of single doses of the converting enzyme inhibitor cilazapril in normal volunteers. J Cardiovasc Pharmacol. 1987 Jan;9(1):26–31. [PubMed] [Google Scholar]
- Francis R. J., Brown A. N., Kler L., Fasanella d'Amore T., Nussberger J., Waeber B., Brunner H. R. Pharmacokinetics of the converting enzyme inhibitor cilazapril in normal volunteers and the relationship to enzyme inhibition: development of a mathematical model. J Cardiovasc Pharmacol. 1987 Jan;9(1):32–38. [PubMed] [Google Scholar]
- Hefti F., Fischli W., Gerold M. Cilazapril prevents hypertension in spontaneously hypertensive rats. J Cardiovasc Pharmacol. 1986 May-Jun;8(3):641–648. doi: 10.1097/00005344-198605000-00030. [DOI] [PubMed] [Google Scholar]
- Todd P. A., Heel R. C. Enalapril. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension and congestive heart failure. Drugs. 1986 Mar;31(3):198–248. doi: 10.2165/00003495-198631030-00002. [DOI] [PubMed] [Google Scholar]