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Pharmacokinetics of angiotensin converting enzyme inhibitors.
Author(s) -
Burnier M,
Waeber B,
Nussberger J,
Brunner HR
Publication year - 1989
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1989.tb03588.x
Subject(s) - renin–angiotensin system , angiotensin converting enzyme , pharmacokinetics , angiotensin ii , pharmacology , chemistry , plasma renin activity , enzyme inhibitor , ace inhibitor , enzyme , blood pressure , endocrinology , medicine , biochemistry
1. The pharmacokinetics of most ACE inhibitors have been evaluated indirectly by the measurements of plasma ACE activity and circulating levels of angiotensin I and II. 2. Although plasma ACE activity is very useful to study the degree and the time‐course of ACE inhibition, one has to be aware that very different results can be obtained depending on the substrate employed in the assay. It is therefore impossible to compare the results of different inhibitors unless an identical methodology is used. 3. A clear dissociation between plasma angiotensin II levels and the antihypertensive effects of ACE inhibitors has been reported. This observation is in part linked to problems with the measurement of angiotensin II. New methods of determination of plasma angiotensin II have now allowed demonstration of the complete disappearance of plasma angiotensin II following acute ACE inhibition. During chronic treatment, however, angiotensin II generation is effectively blocked only during part of the day, but blood pressure remains controlled permanently. 4. Among the different pharmacokinetic characteristics of ACE inhibitors presently available, the route of excretion and to a lesser degree the half‐life appear to be the most clinically relevant. However, the importance of the ability of ACE inhibitors to inhibit tissue renin‐angiotensin systems remains to be defined.