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二甲双胍再评价。

A reappraisal on metformin.

机构信息

Department of Pharmaceutical Toxicology, Hacettepe University, Ankara, Turkey.

Department of Medical Biochemistry, Hacettepe University, Ankara, Turkey.

出版信息

Regul Toxicol Pharmacol. 2018 Feb;92:324-332. doi: 10.1016/j.yrtph.2017.12.023. Epub 2017 Dec 30.

Abstract

This review investigates the different biological effect of Metformin (MET) in different conditions. MET is an oral antidiabetic drug used for the treatment of type 2 diabetes mellitus (T2DM) particularly in overweight people. The main mechanism of action of the MET is inhibition of hepatic glucose production and reduction of insulin resistance. In addition to its antidiabetic effects, MET is also found to be related with the risk for development of several human solid cancers types such as colorectal, breast and pancreas cancer in the diabetic patients. Nowadays according to some researches, MET is believed to decrease or prevent aging and mortality. Moreover, clinical and experimental evidence has shown that MET has beneficial effects in patient with obesity, polycystic ovarian syndrome and Alzheimer's disease. Recent studies have shown that activation of adenosine monophosphate-activated protein kinase (AMPK) by MET can explain its beneficial metabolic effects. In this manuscript, a reevaluation of mechanisms as well as pharmacokinetic properties, genetic variants of transporters, drug-drug interactions, side effects and potential clinical benefits of MET have been reviewed.

摘要

这篇综述探讨了二甲双胍(MET)在不同情况下的不同生物学效应。MET 是一种口服降糖药,用于治疗 2 型糖尿病(T2DM),特别是超重人群。MET 的主要作用机制是抑制肝葡萄糖生成和降低胰岛素抵抗。除了降糖作用外,研究还发现 MET 与糖尿病患者发生多种人类实体癌(如结直肠癌、乳腺癌和胰腺癌)的风险有关。如今,根据一些研究,MET 被认为可以降低或预防衰老和死亡。此外,临床和实验证据表明,MET 对肥胖症、多囊卵巢综合征和阿尔茨海默病患者有有益的作用。最近的研究表明,MET 通过激活单磷酸腺苷激活的蛋白激酶(AMPK)来解释其有益的代谢作用。在本文中,重新评估了 MET 的机制以及药代动力学特性、转运体的遗传变异、药物相互作用、副作用和潜在的临床获益。

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