Pharmacokinetics of Angiotensin Converting Enzyme Inhibitors in Plasma and Tissue Using Radioinhibitor Binding and Displacement Assays

Abstract

Angiotensin converting enzyme (ACE) inhibitors now have an important place in the treatment of hypertension and congestive cardiac failure1-3. After the introduction of the first angiotensin converting enzyme inhibitor Captopril there has been a profusion of new second and third generation ACE inhibitors4 which is analogous to the multiplicity of beta-blockers. These compounds all act by binding to and inhibiting the active site of the enzyme. However, whether inhibition of plasma ACE is the only determinant of the hypotensive effect of these agents or whether inhibition of tissue ACE is also essential has yet to be determined5. ACE occurs in a great variety of tissues, including the endothelium of blood vessels, the brain, kidney, reproductive organs, gastrointestinal tract, adrenal and lung. It is possible that different ACE inhibitors may have variable bioavailability in different tissues or may have differential effects on individual tissue ACE.KeywordsAngiotensin Converting EnzymeAngiotensin Converting Enzyme InhibitorHypotensive EffectRenin Angiotensin SystemDisplacement AssayThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.