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Effect on blood pressure and the renin-angiotensin system of repeated doses of the converting enzyme inhibitor CGS 14824A

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Summary

A new, orally active angiotensin converting enzyme (ACE) inhibitor, CGS 14824A, was evaluated in 12 healthy male volunteers. Two groups each of 6 volunteers were given 5 or 10 mg once daily p.o. for 8 days. Four hours after the first and the last morning doses, plasma angiotensin II, aldosterone and plasma converting enzyme activity had fallen, while blood angiotensin I and plasma renin activity had risen. Throughout the study, more than 90% inhibition of ACE was found immediately before giving either the 5 or 10 mg dose and 50% blockade was still present 72 h following the last dose. Based on the determination of ACE, there was no evidence of drug accumulation. No significant change in blood pressure or heart rate was observed during the course of the study. CGS 14824A was an effective, orally active, long-lasting and well tolerated converting enzyme inhibitor.

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References

  1. Ferguson RK, Vlasses PH, Rotmensch HH (1984) Clinical applications of angiotensin-converting enzyme inhibitors. Am J Med 77: 690–698

    Google Scholar 

  2. Cohn JN, Levine TB (1982) Angiotensin-converting enzyme inhibition in congestive heart failure: the concept. Am J Cardiol 49: 1480–1483

    Google Scholar 

  3. Ferguson RK, Turini GA, Brunner HR, Gavras H, McKinstry DN (1977) A specific orally active inhibitor of angiotensin-converting enzyme in man. Lancet 1: 775–778

    Google Scholar 

  4. Biollaz J, Burnier M, Turini GA, Brunner DB, Porchet M, Gomez HJ, Jones KH, Ferber F, Abrams WB, Gavras H, Brunner HR (1981) Three new long-acting converting-enzyme inhibitors: Relationships between plasma converting-enzyme activity and response to angiotensin I. Clin Pharmacol Ther 29: 665–670

    Google Scholar 

  5. Brunner HR, Nussberger J, Waeber B (1985) The present molecules of converting enzyme inhibitors. J Cardiovasc Pharmacol 7 [Suppl 1]: 2–11

    Google Scholar 

  6. Schaller MD, Nussberger J, Waeber B, Bussien JP, Turini GA, Brunner H, Brunner HR (1985) Haemodynamic and pharmacological effects of the converting enzyme inhibitor CGS 14824A in normal volunteers. Eur J Clin Pharmacol 28: 267–272

    Google Scholar 

  7. Nussberger J, Fasanella d'Amore T, Porchet M, Waeber B, Brunner DB, Brunner HR, Kler L, Brown AN, Francis RJ (1986) Repeated administration of the converting enzyme inhibitor cilazapril to normal volunteers. J Cardiovasc Pharmacol (in press)

  8. Chen DS, Brunner HR, Waeber B (1984) In-vitro response of plasma angiotensin converting enzyme to precursors and active forms of converting enzyme inhibitors. Curr Ther Res 35: 253–262

    Google Scholar 

  9. Nussberger J, Waeber B, Brunner HR, Vetter W (1984) Highly sensitive microassay for aldosterone in unextracted plasma: Comparison with two other methods. J Lab Clin Med 104: 789–796

    Google Scholar 

  10. Nussberger J, Brunner DB, Waeber B, Brunner HR (1984) Measurement of low angiotensin concentrations after ethanol and Dowex extraction procedures. J Lab Clin Med 103: 304–312

    Google Scholar 

  11. Francis RJ, Brown AN, Kler L, Fasanella d'Amore T, Nussberger J, Waeber B, Brunner HR (1986) Pharmacokinetics of the converting enzyme inhibitor cilazapril in normal volunteers and the relationship to enzyme inhibition: Development of a mathematical model. J Cardiovasc Pharmacol (in press)

  12. Bussien JP, Fasanella d'Amore T, Perret L, Porchet M, Nussberger J, Waeber B, Brunner HR (1986) Single and repeated administration of the converting enzyme inhibitor perindopril to normal volunteers. Clin Pharmacol Ther 39: 554–558

    Google Scholar 

  13. MacGregor GA, Markandu ND, Morton JJ (1983) Angiotensin converting enzyme inhibitor reveals an important role for the renin system in the control of normal and high blood pressure in man. Clin Exp Hypertens A5: 1367–1380

    Google Scholar 

  14. Hodsman GP, Zabludowski JR, Zoccali C, Fraser R, Morton JJ, Murray GD, Robertson JIS (1984) Enalapril (MK 421) and its lysine analogue (MK 521): A comparison of acute and chronic effects on blood pressure, renin-angiotensin system and sodium excretion in normal man. Br J Clin Pharmacol 17: 233–241

    Google Scholar 

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Waeber, G., Fasanella d'Amore, T., Nussberger, J. et al. Effect on blood pressure and the renin-angiotensin system of repeated doses of the converting enzyme inhibitor CGS 14824A. Eur J Clin Pharmacol 31, 643–646 (1987). https://doi.org/10.1007/BF00541289

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  • DOI: https://doi.org/10.1007/BF00541289

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