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噻唑烷二酮类药物在糖尿病管理中的当前作用。

The current role of thiazolidinediones in diabetes management.

机构信息

Department of Internal Medicine, Medical School, University of Ioannina, 45110, Ioannina, Greece.

出版信息

Arch Toxicol. 2016 Aug;90(8):1861-81. doi: 10.1007/s00204-016-1737-4. Epub 2016 May 10.

Abstract

Among the epidemics of modern time, type 2 diabetes mellitus (T2DM) is one of the main contributors to overall morbidity as well as mortality. A number of different treatment options are available for the management of diabetes. Among them thiazolidinediones (TZDs) is an interesting drug class since it does not target the result of T2DM, i.e., hyperglycemia but rather some of the core mechanisms of the disease. Indeed, glitazones increase insulin sensitivity by activating the peroxisome proliferator-activated receptor γ, which plays an important role in regulating various metabolic parameters. Although TZDs have an established efficacy in T2DM treatment, their usage during the past years was questioned following the emergence of some alarming data regarding their safety and especially the cardiovascular safety of rosiglitazone. As a result, there is often some skepticism about the current role of TZDs in T2DM management. This mainly affects rosiglitazone even leading to its withdrawal from several markets in contrast to pioglitazone, which has shown a beneficial cardiovascular profile. A comprehensive assessment of the benefit-to-risk ratio of TZDs is required in order to better understand the place of these drugs in T2DM management.

摘要

在现代传染病中,2 型糖尿病(T2DM)是导致总发病率和死亡率的主要原因之一。有许多不同的治疗选择可用于糖尿病的管理。其中,噻唑烷二酮类(TZDs)是一种很有趣的药物类别,因为它不是针对 T2DM 的结果,即高血糖,而是针对疾病的一些核心机制。事实上,格列酮通过激活过氧化物酶体增殖物激活受体 γ 来增加胰岛素敏感性,该受体在调节各种代谢参数方面发挥着重要作用。尽管 TZDs 在 T2DM 治疗中具有既定的疗效,但由于出现了一些关于其安全性,特别是罗格列酮的心血管安全性的令人担忧的数据,近年来它们的使用受到了质疑。因此,人们对 TZDs 在 T2DM 管理中的当前作用常常持怀疑态度。这主要影响到罗格列酮,甚至导致其在一些市场上被撤出,而吡格列酮则显示出了有益的心血管特征。为了更好地了解这些药物在 T2DM 管理中的地位,需要对 TZDs 的获益-风险比进行全面评估。

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