Captopril

Captopril (D-3-mercapto-2-methylpropranoyl-L-proline [SQ 14,225, Capoten]) is the first orally active inhibitor of angiotensin-converting enzyme, the enzyme responsible for conversion of inactive angiotensin I to the potent pressor peptide angiotensin II. It is a potent, relatively specific competitive inhibitor of angiotensin-converting enzyme (kininase II), as well as an effective antihypertensive agent. Prior experience with the nonapeptide inhibitor of angiotensin-converting enzyme, teprotide (SQ 20,881), demonstrated that this parenterally administered agent was effective in the treatment of most patients with hypertension. 1 , 2 The search for an orally effective inhibitor led to the development of captopril (Fig. 1), 3 which has since undergone intensive clinical investigation . . .