Seufert Jochen, Lübben Georg, Dietrich Karin, Bates Peter C
Medizinische Poliklinik, University of Würzburg, Wuerzburg, Germany.
Clin Ther. 2004 Jun;26(6):805-18. doi: 10.1016/s0149-2918(04)90125-7.
Type 2 diabetes mellitus is a condition characterized by impaired insulin secretion and resistance to insulin-mediated glucose uptake and utilization. A number of oral antidiabetic medication are available for its treatment, including metformin and the thiazolidinediones (TZDs). The TZDs have been shown to improve insulin resistance, and it has been suggested that metformin has similar effects. Although both types of agents improve glycemic control, their mechanisms of action and effects on metabolic processes differ.
The goal of this review was to compare the effects of TZDs and metformin on metabolic control in patients with type 2 diabetes.
A search of MEDLINE to March 2004 using the terms metformin and biguanides, and thiazolidinediones and glitazones was conducted to identify preclinical and clinical studies focusing on the mechanisms of action and comparative effects of TZDs and metformin. Also searched were published abstracts from recent major diabetes and endocrinology conferences.
In the studies reviewed, both TZDs and metformin demonstrated the ability to improve glycemic control, although long-term monotherapy with TZDs appeared to be more effective than metformin. There continues to be debate about whether metformin is more effective than TZDs in terms of inhibition of hepatic glucose production. However, various studies have found TZDs to be more effective in promoting an increase in whole-body insulin sensitivity. With respect to lipid metabolism, patients who received TZDs had a greater reduction in concentrations of both plasma triglycerides and free fatty acids. Metformin was more effective in promoting weight loss in patients with type 2 diabetes, although TZDs may decrease visceral fat levels. Treatment with either metformin or TZDs was associated with a reduction in the risk of cardiovascular disease, although the mechanisms by which they accomplished this seem to differ.
The evidence suggests that the predominant effect of metformin is inhibition of hepatic glucose production, whereas the primary effects of TZDs is reduction of insulin resistance and promotion of peripheral glucose uptake. TZDs appear to have more positive effects on other metabolic processes and to be associated with greater improvements in cardiovascular risk factors compared with metformin.
2型糖尿病是一种以胰岛素分泌受损以及对胰岛素介导的葡萄糖摄取和利用产生抵抗为特征的疾病。有多种口服抗糖尿病药物可用于其治疗，包括二甲双胍和噻唑烷二酮类（TZDs）。已证明TZDs可改善胰岛素抵抗，并且有人提出二甲双胍也有类似作用。尽管这两类药物都能改善血糖控制，但其作用机制以及对代谢过程的影响有所不同。
本综述的目的是比较TZDs和二甲双胍对2型糖尿病患者代谢控制的影响。
检索了截至2004年3月的MEDLINE数据库，使用“二甲双胍和双胍类”以及“噻唑烷二酮类和格列酮类”等检索词，以识别专注于TZDs和二甲双胍作用机制及比较效果的临床前和临床研究。还检索了近期主要糖尿病和内分泌学会议发表的摘要。
在所综述的研究中，TZDs和二甲双胍都显示出有改善血糖控制的能力，尽管长期使用TZDs单药治疗似乎比二甲双胍更有效。关于二甲双胍在抑制肝糖生成方面是否比TZDs更有效，仍存在争议。然而，各种研究发现TZDs在促进全身胰岛素敏感性增加方面更有效。在脂质代谢方面，接受TZDs治疗的患者血浆甘油三酯和游离脂肪酸浓度降低得更多。二甲双胍在促进2型糖尿病患者体重减轻方面更有效，尽管TZDs可能会降低内脏脂肪水平。使用二甲双胍或TZDs治疗均与心血管疾病风险降低相关，尽管它们实现这一目标的机制似乎有所不同。
证据表明，二甲双胍的主要作用是抑制肝糖生成，而TZDs的主要作用是降低胰岛素抵抗并促进外周葡萄糖摄取。与二甲双胍相比，TZDs似乎对其他代谢过程有更积极的影响，并且与心血管危险因素的更大改善相关。
