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口服和静脉输注葡萄糖后,胰高血糖素样肽1(GLP-1)和葡萄糖依赖性促胰岛素分泌多肽(GIP)开始分泌,从而促进胰岛素分泌。这个过程被称为肠促胰岛素分泌效应(incretin effect)。肠促胰岛素分泌效应受损(GIP和GLP-1分泌减少)是导致2型糖尿病发病的一个重要原因。补充外源性GLP-1,很快会被二肽基肽酶Ⅳ(DPP-Ⅳ)降解,临床价值不大。目前上市的DPP-Ⅳ口服制剂被证明可以提高内源性GLP-1水平,提高葡萄糖耐量,持久改善A1C,改善β细胞功能。DPP-Ⅳ一般不会引起体重增加,且患者耐受性较好。美国和墨西哥(2006年)及欧洲(2007年)已经批准一种DPP-Ⅳ抑制剂口服制剂西他列汀每日1次用于治疗2型糖尿病。其他DPP-Ⅳ抑制剂的研发正处于Ⅲ期临床阶段。
After oral and intravenous glucose administration, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) begin to be secreted, thereby promoting insulin secretion. This process is called the incretin effect. Impaired secretion of incretin secretion (decreased GIP and GLP-1 secretion) is a leading cause of type 2 diabetes. Exogenous GLP-1 supplementation will soon be dipeptidyl peptidase Ⅳ (DPP-Ⅳ) degradation, clinical value is not. Currently available DPP-IV oral preparations have been shown to increase endogenous GLP-1 levels, increase glucose tolerance, improve A1C permanently and improve beta-cell function. DPP-IV generally does not cause weight gain, and patient tolerance is better. The United States and Mexico (2006) and Europe (2007) have approved sitagliptin, an oral DPP-IV inhibitor, once daily to treat type 2 diabetes. Development of other DPP-IV inhibitors is in phase III clinical stage.