A potent converting enzyme inhibitor CGS 13928C: drug profile in normal volunteers

The converting enzyme inhibitor CGS 13928C was evaluated in 15 healthy male volunteers. First the efficacy of a single oral dose of 0.5, 1, 2 or 5 mg in antagonizing the pressor response to exogenous angiotensin I was tested with continuous monitoring of the blood pressure and heart rate by an intra...

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Bibliographic Details
Published in:European journal of clinical pharmacology 1984-01, Vol.26 (4), p.419-424
Main Authors: SCHALLER, M. D, BRUNNER, D. B, NUSSBERGER, J, TURINI, G. A, SEN, S. B, CHEN, D, WAEBER, B, BRUNNER, H. R
Format: Article
Language:English
Subjects:
Adult
Angiotensin I - pharmacology
Angiotensin-Converting Enzyme Inhibitors
Biological and medical sciences
Blood Pressure - drug effects
Cardiovascular system
Dose-Response Relationship, Drug
Drug Evaluation
Heart Rate - drug effects
Humans
Indoles - pharmacology
Male
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Pressoreceptors - drug effects
Renin-Angiotensin System - drug effects
Time Factors
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Summary:The converting enzyme inhibitor CGS 13928C was evaluated in 15 healthy male volunteers. First the efficacy of a single oral dose of 0.5, 1, 2 or 5 mg in antagonizing the pressor response to exogenous angiotensin I was tested with continuous monitoring of the blood pressure and heart rate by an intraarterial catheter. CGS 13928C 1, 2 and 5 mg consistently reduced the response to angiotensin within 2 to 3 h and for a period exceeding the 4 h of monitoring. The 2 mg dose was hardly more effective than 1 mg and 5 mg did not further enhance the blockade. Subsequently, plasma renin and converting enzyme activity, angiotensin I, angiotensin II and aldosterone were measured serially before and up to 72 h following oral administration of either 1 mg (n = 7) or 2 mg (n = 8) CGS 13928C. As expected, plasma renin activity and angiotensin I rose, while plasma converting enzyme activity, angiotensin II and aldosterone fell following both doses of the drug. No side-effects occurred. In normal volunteers CGS 13928C is an effective and extremely potent, orally active converting enzyme inhibitor.
ISSN:0031-6970
1432-1041
DOI:10.1007/BF00542134