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替米沙坦的多效性作用在临床上是否相关?

Are the pleiotropic effects of telmisartan clinically relevant?

作者信息

Rizos C V, Elisaf M S, Liberopoulos E N

机构信息

Department of Internal Medicine, School of Medicine, University of Ioannina, Ioannina, Greece.

出版信息

Curr Pharm Des. 2009;15(24):2815-32. doi: 10.2174/138161209788923859.

Abstract

Hypertension is one of the major risk factors for cardiovascular disease. Angiotensin receptor blockers (ARBs) are a class of antihypertensive drugs with established efficacy and favorable safety profile. Telmisartan, a member of the ARB family, holds some additional traits which differentiate it from the rest ARBs. A pivotal role in these characteristics plays its ability to partially activate the peroxisome proliferator activated receptor-gamma, which in turn controls a number of metabolism-related genes. Indeed, telmisartan has shown a number of pleiotropic effects in experimental and clinical studies. These include the amelioration of insulin resistance, improvement of lipid profile and favorable fat redistribution. Moreover, telmisartan has been associated with beneficial effects on vascular function, cardiac remodeling and renal function. However, do all these pleiotropic effects translate into clinical benefit? Recent studies have tried to answer this question with promising but not definitive results.

摘要

高血压是心血管疾病的主要危险因素之一。血管紧张素受体阻滞剂(ARBs)是一类具有确切疗效和良好安全性的抗高血压药物。替米沙坦是ARB家族的一员,具有一些使其有别于其他ARB的额外特性。在这些特性中起关键作用的是其部分激活过氧化物酶体增殖物激活受体γ的能力,这反过来又控制许多与代谢相关的基因。事实上,替米沙坦在实验和临床研究中已显示出多种多效性作用。这些作用包括改善胰岛素抵抗、改善血脂谱以及有利的脂肪重新分布。此外,替米沙坦还与对血管功能、心脏重塑和肾功能的有益作用相关。然而,所有这些多效性作用都能转化为临床益处吗?最近的研究试图回答这个问题,结果虽有希望但并不确定。

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