Department of Diabetes and Endocrinology, Heart of England NHS Foundation Trust, Birmingham, UK.
Postgrad Med. 2009 Nov;121(6):70-100. doi: 10.3810/pgm.2009.11.2079.
Type 2 diabetes is a very common worldwide disorder, with major consequences for patients, society, and health care services. Good glycemic control is an important aspect of diabetes management because it has a significant impact on diabetes-related microvascular and possibly macrovascular complications. Based on our understanding of the pathogenesis of diabetes, multiple pharmacological interventions have been developed in the past 60 years. Although effective, none have had a lasting effect on glycemic control because of the progressive nature of type 2 diabetes requiring combination therapies and insulin treatment. In addition, several pharmacologic interventions have undesirable side effects, including hypoglycemia and weight gain. Drugs targeting the incretin pathway are the latest addition to the available antidiabetes agents. Incretin-based therapy is either delivered orally (dipeptidyl peptidase-4 [DPP-4]) inhibitors or injected subcutaneously (glucagon-like peptide-1 [GLP-1] mimetics and analogues). Dipeptidyl peptidase-4 inhibitors are effective either as a single or combination therapy in lowering glycated hemoglobin, fasting and postprandial glucose levels, with a low incidence of hypoglycemia and no weight gain. There are 3 DPP-4 inhibitors currently available (sitagliptin, saxagliptin, and vildagliptin), with more expected to be available in the future. In this article, we review the scientific background for incretin-based therapy and the available evidence regarding the role and efficacy of DPP-4 inhibitors in the treatment of patients with type 2 diabetes.
2 型糖尿病是一种非常普遍的全球性疾病，对患者、社会和医疗保健服务都有重大影响。良好的血糖控制是糖尿病管理的一个重要方面，因为它对糖尿病相关的微血管和可能的大血管并发症有重大影响。基于我们对糖尿病发病机制的理解，在过去的 60 年中已经开发了多种药理学干预措施。尽管这些干预措施有效，但由于 2 型糖尿病的进展性质需要联合治疗和胰岛素治疗，它们都没有对血糖控制产生持久的影响。此外，一些药物干预措施有不良的副作用，包括低血糖和体重增加。针对肠促胰岛素途径的药物是现有抗糖尿病药物的最新补充。肠促胰岛素治疗可以口服（二肽基肽酶-4 [DPP-4] 抑制剂）或皮下注射（胰高血糖素样肽-1 [GLP-1] 类似物和类似物）。DPP-4 抑制剂无论是单独使用还是联合治疗，都能有效降低糖化血红蛋白、空腹和餐后血糖水平，低血糖发生率低，体重无增加。目前有 3 种 DPP-4 抑制剂（西他列汀、沙格列汀和维格列汀），预计未来还会有更多的药物。本文综述了基于肠促胰岛素的治疗的科学背景以及 DPP-4 抑制剂在治疗 2 型糖尿病患者中的作用和疗效的现有证据。
