Safety and efficacy of sitagliptin-metformin in fixed combination for the treatment of type 2 diabetes mellitus.
Safety and efficacy of sitagliptin-metformin in fixed combination for the treatment of type 2 diabetes mellitus.
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DOI：
10.4137/cmed.s7314
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发表时间：
2013-09-01
期刊：
影响因子：
--
通讯作者：
Gough SC
中科院分区：
文献类型：
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作者：
Ballav C;Gough SC
双胍类药物二甲双胍被认为是 2 型糖尿病的一线治疗药物。西他列汀是一种二肽基肽酶 4 (DPP-4) 抑制剂，通过肠降血糖途径发挥作用，并具有葡萄糖依赖性作用模式。这些药物的互补降血糖特性使固定剂量联合治疗具有诱人的前景。最近临床试验的证据表明，该组合对疗效具有有益影响，糖化血红蛋白 (HbA1c)、空腹和餐后血糖水平的显着改善证明了这一点。与任一药物的单一疗法相比，固定剂量组合可能具有更高的患者耐受性，因为低血糖发生率低、体重中性且副作用发生率较低。然而，高昂的获取成本和缺乏长期安全数据是其广泛使用的潜在障碍。本综述概述了二甲双胍-西格列汀组合近期试验的药理学和临床结果，以及该组合如何适应 2 型糖尿病治疗方案。
The biguanide, metformin, is considered first-line treatment for type 2 diabetes. Sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor acts through the incretin pathway and has a glucose dependent mode of action. The complementary hypoglycemic properties of these drugs make fixed dose combination treatment an attractive prospect. Evidence from recent clinical trials suggests a beneficial effect of the combination on efficacy, demonstrated by significant improvement of hemoglobin A1c (HbA1c), fasting and postprandial glucose levels. The fixed dose combination is likely to have greater patient tolerability compared with monotherapy with either agent because of low rates of hypoglycemia, weight neutrality, and lower rates of side effects. High acquisition cost and paucity of long-term safety data are, however, potential barriers to their wider use. An overview of the pharmacology and clinical outcomes from recent trials of the metformin-sitagliptin combination and how the combination could fit into the type 2 diabetes treatment algorithm is presented in this review.