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肾素-血管紧张素醛固酮系统(RAAS)在高血压、充血性心力衰竭及慢性肾功能衰竭的重要性早已为人们所认识。利用血管紧张素转化酶抑制剂(ACEI)或血管紧张素受体拮抗剂(ARB)对这些疾病能够有益地干预。肾素抑制剂可以在高水平起始位点上阻滞RAAS系统,可提供新的治疗高血压的药物疗法。阿利吉仑(aliskiren)是一种可口服、非蛋白、低分子量的肾素抑制剂,迄今是进展到临床试验Ⅲ期的肾素抑制剂。本文综述阿利吉仑的药理学特性及在临床中的应用进展。
The importance of the renin-angiotensin aldosterone system (RAAS) in hypertension, congestive heart failure and chronic renal failure has long been recognized. Use of angiotensin-converting enzyme inhibitors (ACEIs) or angiotensin receptor blockers (ARBs) can beneficially interfere with these diseases. Renin inhibitors block the RAAS system at high levels of initiation sites and offer new drug therapies for the treatment of hypertension. Aliskiren is an orally available, non-protein, low molecular weight renin inhibitor that has so far served as a renin inhibitor that progresses to phase III of clinical trials. This article reviews the pharmacological properties of aliskiren and its clinical application.