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血管紧张素Ⅱ1型受体拮抗剂在高血压治疗中的应用:厄贝沙坦带来了哪些启示?

AT1-receptor antagonism in hypertension: what has been learned with irbesartan?

作者信息

Waeber Bernard, Burnier Michel

机构信息

University Hospital, Division of Pathophysiology, Lausanne, Switzerland.

出版信息

Expert Rev Cardiovasc Ther. 2003 May;1(1):23-33. doi: 10.1586/14779072.1.1.23.

Abstract

Irbesartan is a long-acting angiotensin II antagonist acting specifically at the level of the Type 1-receptor subtype (AT1-receptor). This compound lowers blood pressure dose-dependently in hypertensive patients and has a placebo-like tolerability. The antihypertensive efficacy of irbesartan is greatly enhanced by the coadministration of a diuretic, and fixed-dose combinations of irbesartan and hydrochlorothiazide are now available. Irbesartan-based treatment appears especially effective for high-risk patients, such as those with diabetes, renal disease and cardiac hypertrophy. In patients with Type 2 diabetes, irbesartan delays the development of nephropathy as well as the progression of renal failure. Irbesartan may have antiatherosclerotic properties beyond those expected from blood pressure lowering per se: this AT1-blocker decreases the vascular oxidative stress and prevents the procoagulant as well as the pro-inflammatory effects of angiotensin II. Irbesartan given alone or in combination with a diuretic therefore represents a rational approach to treat hypertensive patients.

摘要

厄贝沙坦是一种长效血管紧张素II拮抗剂,特异性作用于1型受体亚型(AT1受体)水平。该化合物在高血压患者中可剂量依赖性地降低血压,且具有类似安慰剂的耐受性。联合使用利尿剂可大大增强厄贝沙坦的降压疗效,目前已有厄贝沙坦与氢氯噻嗪的固定剂量复方制剂。基于厄贝沙坦的治疗对高危患者似乎特别有效,如糖尿病、肾病和心脏肥大患者。在2型糖尿病患者中,厄贝沙坦可延缓肾病的发展以及肾衰竭的进展。厄贝沙坦可能具有除本身降压作用之外的抗动脉粥样硬化特性:这种AT1阻滞剂可降低血管氧化应激,并预防血管紧张素II的促凝和促炎作用。因此,单独使用厄贝沙坦或与利尿剂联合使用是治疗高血压患者的合理方法。

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