Goodarzi Mark O, Bryer-Ash Michael
Department of Medicine and the Gonda (Goldschmied) Diabetes Center, David Geffen School of Medicine, University of California, Los Angeles, CA 90095, USA.
Diabetes Obes Metab. 2005 Nov;7(6):654-65. doi: 10.1111/j.1463-1326.2004.00448.x.
The usefulness of metformin as an oral antidiabetic agent is widely accepted. However, several other classes of oral antidiabetic agents have been recently introduced, raising the need to evaluate the role of metformin as initial therapy and in combination with these newer drugs for treatment of type 2 diabetes mellitus (DM).
Synthesis of information was preceded by a comprehensive review of the English language literature using Medline. We also reviewed bibliographies of relevant articles. The studies most pertinent to the mechanism of action, efficacy, toxicity and administration of metformin were selected for citation in this review.
Metformin acts by increasing tissue sensitivity to insulin, principally in the liver. Beneficial properties of metformin include weight reduction, favourable effects on the lipid profile and the fibrinolytic pathway, and improvement of ovarian function in some insulin-resistant women. It does not cause hyperinsulinaemia or hypoglycaemia. Metformin is effective as monotherapy and, in combination with both insulin secretagogues and thiazolidinediones (TZDs), may obviate the need for insulin treatment. Several fixed-dose combination pills containing metformin and other agents are available. A protocol for the initiation of therapy with contemporary oral agents for type 2 DM is presented, with emphasis on the continuing central role of metformin.
Metformin remains a safe and effective agent for the therapy of patients with type 2 DM. It is useful as monotherapy or in combination regimens with the newer insulin secretagogues, TZDs or insulin. It is still in most circumstances the agent of choice for initial therapy of the typical obese patient with type 2 DM and mild to moderate hyperglycaemia.
二甲双胍作为口服抗糖尿病药物的效用已被广泛认可。然而，最近又引入了其他几类口服抗糖尿病药物，这就需要评估二甲双胍作为初始治疗药物以及与这些新药联合用于治疗2型糖尿病（DM）的作用。
在综合信息之前，我们使用医学在线数据库（Medline）对英文文献进行了全面综述。我们还查阅了相关文章的参考文献目录。本综述选择了与二甲双胍作用机制、疗效、毒性及给药方式最相关的研究进行引用。
二甲双胍主要通过增加肝脏等组织对胰岛素的敏感性发挥作用。二甲双胍的有益特性包括减轻体重、对血脂谱和纤溶途径有有利影响，以及在一些胰岛素抵抗女性中改善卵巢功能。它不会引起高胰岛素血症或低血糖症。二甲双胍作为单一疗法有效，并且与胰岛素促分泌剂和噻唑烷二酮类（TZDs）联合使用时，可能无需胰岛素治疗。有几种含二甲双胍和其他药物的固定剂量复方片剂可供使用。本文提出了一种使用当代口服药物治疗2型糖尿病的起始治疗方案，重点强调了二甲双胍持续的核心作用。
二甲双胍仍然是治疗2型糖尿病患者的一种安全有效的药物。它作为单一疗法或与新型胰岛素促分泌剂、TZDs或胰岛素联合使用均有效。在大多数情况下，它仍然是治疗典型肥胖的2型糖尿病和轻度至中度高血糖患者初始治疗的首选药物。
