University of Liège, CHU Sart Tilman, Division of Diabetes, Nutrition and Metabolic Disorders and Division of Clinical Pharmacology, Department of Medicine, Liège, Belgium .
Expert Opin Drug Metab Toxicol. 2010 Oct;6(10):1265-76. doi: 10.1517/17425255.2010.513699.
Type 2 diabetes is an increasingly prevalent disease resulting from various complex combinations of defects in insulin secretion and insulin action. Adequate blood glucose control is necessary to minimize complications. DPP IV inhibitors (sitagliptin, vildagliptin, saxagliptin) offer new options for combined pharmacological therapy.
An extensive literature search was performed to analyze the potential pharmacokinetic (PK) and pharmacodynamic (PD) interactions between metformin (first-line drug for the management of type 2 diabetes) and sitagliptin (first commercialized DPP IV inhibitor). Metformin and sitagliptin may be administered together, either separately or in fixed-dose combination.
Updated information about PK/PD data on metformin alone, sitagliptin alone and sitagliptin plus metformin. Metformin and sitagliptin are not prone to PK drug-drug interactions. Their co-administration, either separately or in a fixed-dose combination, improves blood glucose control more potently than either compound separately, without hypoglycemia and without increasing metformin-related gastrointestinal side effects.
The combination sitagliptin plus metformin may be used as a first- or second-line therapy in the management of type 2 diabetes.
2 型糖尿病是一种日益流行的疾病，是由于胰岛素分泌和胰岛素作用的各种复杂缺陷的组合。需要充分的血糖控制，以尽量减少并发症。DPP IV 抑制剂（西他列汀，维格列汀，沙格列汀）为联合药物治疗提供了新的选择。
进行了广泛的文献检索，以分析二甲双胍（治疗 2 型糖尿病的一线药物）和西他列汀（首个上市的 DPP IV 抑制剂）之间潜在的药代动力学（PK）和药效学（PD）相互作用。二甲双胍和西他列汀可以联合使用，单独使用或固定剂量联合使用。
关于单独使用二甲双胍、西他列汀和西他列汀加二甲双胍的 PK/PD 数据的最新信息。二甲双胍和西他列汀不易发生 PK 药物相互作用。它们的联合应用，无论是单独使用还是固定剂量联合使用，都能比单独使用任何一种药物更有效地控制血糖，而不会出现低血糖，也不会增加与二甲双胍相关的胃肠道副作用。
西他列汀加二甲双胍的联合治疗可作为 2 型糖尿病治疗的一线或二线治疗。
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