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European Journal of Clinical Pharmacology

, Volume 26, Issue 4, pp 419–424 | Cite as

A potent converting enzyme inhibitor CGS 13928C. Drug profile in normal volunteers

  • M. D. Schaller
  • D. B. Brunner
  • J. Nussberger
  • G. A. Turini
  • S. B. Sen
  • D. Chen
  • B. Waeber
  • H. R. Brunner
Originals

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.

Key words

converting enzyme inhibitor blood pressure decrease exogenous angiotensin plasma angiotensin I and II plasma renin aldosterone healthy male volunteers CGS 13928C 

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Copyright information

© Springer-Verlag 1984

Authors and Affiliations

  • M. D. Schaller
    • 1
  • D. B. Brunner
    • 1
  • J. Nussberger
    • 1
  • G. A. Turini
    • 1
  • S. B. Sen
    • 2
    • 1
  • D. Chen
    • 2
    • 1
  • B. Waeber
    • 1
  • H. R. Brunner
    • 1
  1. 1.Division of Nephrology and HypertensionCentre Hospitalier UniversitaireLausanneSwitzerland
  2. 2.Ciba-Geigy CorporationSummitUSA

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