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替米沙坦:一种针对不同人群的新型血管紧张素II受体阻滞剂?

Telmisartan: a different angiotensin II receptor blocker protecting a different population?

作者信息

Burnier M

机构信息

Division of Nephrology and Hypertension Consultation, Centre Hospitalier Universitaire Vaudois, Lausanne, Switzerland.

出版信息

J Int Med Res. 2009 Nov-Dec;37(6):1662-79. doi: 10.1177/147323000903700602.

DOI:10.1177/147323000903700602
PMID:20146864
Abstract

The ONgoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial (ONTARGET()) showed that the angiotensin II receptor blocker (ARB) telmisartan was as protective as the reference-standard ramipril in a broad cross-section of patients at increased cardiovascular risk, but was better tolerated. Telmisartan has a unique profile among ARBs, with a high affinity for the angiotensin II type 1 receptor, a long duration of receptor binding, a high lipophilicity and a long plasma half life. This leads to sustained and powerful blood pressure lowering when compared with the first marketed ARBs, such as losartan and valsartan. Some pharmacological properties of telmisartan clearly distinguish it from other members of the ARB class and may contribute to the clinical effects seen with telmisartan. A class effect for ARBs cannot be assumed. To date, telmisartan is the only ARB that has been shown to reduce cardiovascular risk in at-risk cardiovascular patients.

摘要

替米沙坦单药及与雷米普利联合应用的全球终点试验(ONTARGET)表明,在心血管风险增加的广泛患者群体中,血管紧张素II受体阻滞剂(ARB)替米沙坦与参考标准药物雷米普利具有同样的保护作用,但耐受性更好。替米沙坦在ARB类药物中具有独特的特性,对血管紧张素II 1型受体具有高亲和力、受体结合持续时间长、高亲脂性以及长血浆半衰期。与首个上市的ARB类药物如氯沙坦和缬沙坦相比,这导致其能持续强效降低血压。替米沙坦的一些药理特性使其明显区别于ARB类的其他成员,可能促成了替米沙坦所观察到的临床效果。不能假定ARB类有类效应。迄今为止,替米沙坦是唯一已被证明可降低心血管高危患者心血管风险的ARB。

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