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二甲双胍——最新进展

Metformin--an update.

作者信息

Bailey C J

机构信息

Department of Pharmaceutical Sciences, Aston University, Birmingham, England.

出版信息

Gen Pharmacol. 1993 Nov;24(6):1299-309. doi: 10.1016/0306-3623(93)90411-p.

Abstract

Metformin (dimethylbiguanide) is an antihyperglycaemic drug used to treat non-insulin dependent diabetes mellitus. It acts in the presence of insulin to increase glucose utilization and reduce glucose production, thereby countering insulin resistance. The effects of metformin include increased glucose uptake, oxidation and glycogenesis by muscle, increased glucose metabolism to lactate by the intestine, reduced hepatic gluconeogenesis and possibly a reduced rate of intestinal glucose absorption. Metformin appears to facilitate steps in the postreceptor pathways of insulin action, and may exert effects that are independent of insulin. In muscle, metformin increases translocation into the plasma membrane of certain isoforms of the glucose transporter. The effects of metformin are generally moderate, and do not cause clinical hypoglycaemia or increased weight gain. Metformin has an antihypertriglyceridaemic effect and exerts various potentially useful effects on haemostasis. A risk of lactic acidosis is negligible provided that the contraindications, particularly renal incompetence are respected.

摘要

二甲双胍(二甲基双胍)是一种用于治疗非胰岛素依赖型糖尿病的抗高血糖药物。它在胰岛素存在的情况下发挥作用,增加葡萄糖利用并减少葡萄糖生成,从而对抗胰岛素抵抗。二甲双胍的作用包括肌肉对葡萄糖摄取、氧化和糖原生成增加,肠道将葡萄糖代谢为乳酸增加,肝糖异生减少以及可能肠道葡萄糖吸收速率降低。二甲双胍似乎促进胰岛素作用的受体后途径中的步骤,并且可能发挥独立于胰岛素的作用。在肌肉中,二甲双胍增加某些葡萄糖转运蛋白异构体向质膜的转位。二甲双胍的作用通常较为温和,不会引起临床低血糖或体重增加。二甲双胍具有抗高甘油三酯血症作用,并对止血有各种潜在的有益作用。只要遵守禁忌症,特别是肾功能不全,乳酸酸中毒的风险可以忽略不计。

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