Repeated administration of the converting enzyme inhibitor cilazapril to normal volunteers

Détails

ID Serval
serval:BIB_A662A689DBEC
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
Repeated administration of the converting enzyme inhibitor cilazapril to normal volunteers
Périodique
Journal of Cardiovascular Pharmacology
Auteur⸱e⸱s
Nussberger  J., Fasanella d'Amore  T., Porchet  M., Waeber  B., Brunner  D. B., Brunner  H. R., Kler  L., Brown  A. N., Francis  R. J.
ISSN
0160-2446 (Print)
Statut éditorial
Publié
Date de publication
01/1987
Volume
9
Numéro
1
Pages
39-44
Notes
Clinical Trial
Controlled Clinical Trial
Journal Article
Research Support, Non-U.S. Gov't --- Old month value: Jan
Résumé
Cilazapril 1.25 and 5.0 mg p.o. q.d. was administered in double-blind fashion to two groups of six normal volunteers on 8 consecutive days. Blood pressure, heart rate, and plasma converting enzyme activity were measured each day prior to drug administration and up to 72 h after the last dose. Plasma renin activity, blood angiotensin I, plasma angiotensin II, and aldosterone as well as plasma cilazaprilat levels were determined on the first and the last day of active treatment at times 0, 4, and 24 h. The drug was very well tolerated by all volunteers. At 4 h postdrug, plasma converting enzyme activity was reduced in dose-dependent fashion on the first and the eighth day; plasma cilazaprilat levels were also clearly dose dependent. Nevertheless, 24 h postdrug cilazaprilat levels were similar on the first and last day of drug administration, and plasma converting enzyme activity was also stable throughout the 8 days. The various components of the renin-angiotensin system responded in the usual fashion. These results provide strong evidence that cilazapril is a very potent and highly effective converting enzyme inhibitor. Doses well below 5 mg/day will probably suffice for therapeutic efficacy. These data also confirm the hypothesis formulated in the preceding article, i.e., that there is no accumulation of the drug with repeated administration despite its long pharmacological half-life (t1/2).
Mots-clé
Adult Aldosterone/blood Angiotensin I/blood Angiotensin II/blood *Angiotensin-Converting Enzyme Inhibitors Blood Pressure/drug effects Cilazapril Double-Blind Method Drug Administration Schedule Heart Rate/drug effects Humans Kinetics Male Pyridazines/*administration & dosage/pharmacology Renin/blood
Pubmed
Web of science
Création de la notice
05/03/2008 16:40
Dernière modification de la notice
20/08/2019 15:11
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