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. 1989;27(Suppl 2):217S–223S. doi: 10.1111/j.1365-2125.1989.tb03485.x

The assessment of ACE activity in man following angiotensin I challenges

A comparison of cilazapril, captopril and enalapril

J Essig, G G Belz, A Wellstein
PMCID: PMC1379751  PMID: 2548551

Abstract

1 The aim of the studies was to develop a new methodology to estimate the pharmacodynamic properties and potency of angiotensin converting enzyme (ACE) inhibitors in man.

2 Angiotensin I dose-response curves were derived by continuous infusion of angiotensin I in increasing dose steps; steady state was reached within 3 min.

3 Interaction between angiotensin I (agonist) and ACE inhibitors (antagonist) was characterized according to Schild-plot methodology by measuring agonist dose-response curves using diastolic blood pressure in the absence and the presence of varying doses of the antagonist.

4 Cilazapril shifted the angiotensin I dose-response curves to the right. A twofold shift (apparent Ki-dose) was observed with approximately 0.6 mg cilazapril.

5 The effect of angiotensin I on diastolic blood pressure was determined before and up to 36 h after administration of 25 mg captopril, 10 mg enalapril, 4 mg cilazapril and a placebo orally. The pharmacodynamic half-life of captopril was about 2 h, whereas the effect of enalapril and cilazapril was about 4 h.

6 Angiotensin I dose-response curves are useful methods of investigating the pharmacodynamic properties of ACE-inhibitors in man.

Keywords: kinetics, pharmacodynamic properties, angiotensin I, ACE inhibitors

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

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