Reuter H, Erdmann E
Klinik III für Innere Medizin, Universität zu Köln, Köln.
Dtsch Med Wochenschr. 2007 Mar 16;132(11):571-4. doi: 10.1055/s-2007-970380.
The incretin hormone glucagon-like peptide 1 (GLP-1) is being synthesized from L-cells in the gut and enhances glucose-induced insulin secretion. Metabolic control of type 2 diabetic patients can be markedly improved by additional administration of GLP-1, however, this peptide is almost immediately degraded and therefore has little clinical value. The synthetic GLP-1 agonist exenatide underlies a different metabolism and has recently been approved by the U.S. Food and Drug Administration for the adjunctive treatment of patients with type 2 diabetes who are suboptimally controlled with metformin and/or sulfonylurea. First controlled clinical trials provided evidence that glycaemic control under exenatide administered twice daily in a dose of 5-10 microg was not inferior to conventional insulin therapy. Novel aspects in the treatment of type 2 diabetes by GLP-1 receptor stimulation further include its influence on the insulin secretory pattern, insulin/glucagon ratio, body weight and possibly even pancreatic beta cell mass. However, a general application of exenatide in the treatment of type 2 diabetes will also largely depend on the therapy behavior of patients, a possible immunogenicity and the rate of adverse events. Furthermore, a possible indication for exenatide as first-line therapy of type 2 diabetes and the prognostic relevance of this novel therapeutic approach have yet to be defined.
肠促胰岛素激素胰高血糖素样肽-1(GLP-1)由肠道的L细胞合成,可增强葡萄糖诱导的胰岛素分泌。额外给予GLP-1可显著改善2型糖尿病患者的代谢控制,然而,这种肽几乎会立即降解,因此临床价值不大。合成的GLP-1激动剂艾塞那肽具有不同的代谢方式,最近已被美国食品药品监督管理局批准用于辅助治疗二甲双胍和/或磺脲类药物控制不佳的2型糖尿病患者。首批对照临床试验提供的证据表明,每日两次给予5-10微克剂量的艾塞那肽时,血糖控制效果不劣于传统胰岛素治疗。通过刺激GLP-1受体治疗2型糖尿病的新特点还包括其对胰岛素分泌模式、胰岛素/胰高血糖素比值、体重甚至可能对胰腺β细胞量的影响。然而,艾塞那肽在2型糖尿病治疗中的广泛应用在很大程度上还将取决于患者的治疗行为、可能的免疫原性以及不良事件发生率。此外,艾塞那肽作为2型糖尿病一线治疗的可能适应证以及这种新型治疗方法的预后相关性尚未明确。