Antihypertensives renin-angiotensin system agents

Introduction - The search for new antihypertensives and for a better understanding of existing ones remains quite intense with emphasis this past year on 3-blockers (see Chapter 9) and on agents that affect the renin-angiotensin system. Diuretics were reviewed last year and are not included in this chapter. Structures of drugs mentioned in this review are shown or may be found in recent volumes of Annual Reports in Medicinal Chemistry. 

In hypertension, timolol may be used either alone or in combination with most other antihypertensive agents. The combination with angiotensin-converting enzyme inhibitors is probably less nseful becanse both agents exert part of their effect by diminishing the activity of the renin-angiotensin system. Combination with verapamil should be avoided because of the effect on AV nodal conduction. 

Renin-Angiotensin System Development of Antihypertensive Agents.264... 

RENIN-ANGIOTENSIN SYSTEM DEVELOPMENT OF ANTIHYPERTENSIVE AGENTS... 

Aliskiren blocks the renin-angiotensin-aldosterone system at its point of a activation, which results in reduced plasma renin activity and BP. It provides BP reductions comparable to an ACE inhibitor, ARB, or CCB. It also has additive antihypertensive effects when used in combination with thiazides, ACE inhibitors, ARBs, or CCBs. It is approved for monotherapy or in combination with other agents. 

Captopril is designated chemically as l-[(2S)-3-mercapto-2-methylpropionyl]-L-proline (14) (Fig. 8). It is used as an antihypertensive agent through suppression of the renin-angiotensin-aldosterone system [36,37], Captopril and other compounds such as enalapril and lisinopril prevent the conversion of angiotensin I to angiotensin II by inhibition of ACE. 

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