研究人员在5月《糖尿病护理》杂志(Diabetes Care 2005;28:1083-1091)上报告,对二甲双胍、磺酰脲联合治疗控制不足的2型糖尿病人,加用exenatide改善了血糖控制。 如资深研究人员美国圣地亚哥Amylin制药公司的巴隆(Alain D. Baron)告诉路透社记者的,“exenatide现已被批准以Byetta的商品名上市,是肠降血糖素模拟剂中的第一种药,对病情严重度不一和一、二种常用降血糖药治疗没能充分控制的2型糖尿病人已证明它能改善血糖控制”。他和同事指出,许多调节葡萄糖的肽类都表明有希望用于治疗2型糖尿病。 为研究exenatide的作用,他们进行了一项有733名病人的双盲、安慰剂对照研究。研究组每天注射两次5或10mg的exenatide。所有病人继续原有的二甲双胍治疗,并被随机分为或最大有效剂量或最低推荐量的磺酰脲。30周时,10mg exenatide组的血红蛋白为1.0%,5mg组为0.8%。另外,两个exenatide组都有显著体重减轻。 轻或中度恶心是最常见的副作用,10mg组轻中度低血糖的发病率为28%,5mg组为19%,安慰剂组13%。接受最低推荐剂量碘酰脲的病人似乎低血糖的发病率较低。 巴隆总结,此药“通过一套独特的作用方式起作用,其最重要的特征是恢复1期胰岛素分泌,因此可能是2型糖尿病重要的辅助治疗工具――此病现在越来越流行,而且难于控制”。 目前正在进行exenatide治疗2型糖尿病的试验。临床试验结果表明exenatide能够将血糖水平降低到正常水平范围内。这种对血糖的控制有可能是因为该药与肠促胰岛素GLP-1激素相似的原因。当血糖水平升高时,GLP-1激素能够刺激机体诱导胰岛素产生反应。在动物试验中,GLP-1给药维持并且形成新的β细胞,2型糖尿病患者的胰腺中没有胰岛素诱导细胞。
Exenatide (Byetta) is the first of a new type of treatment called 'incretin mimetics' designed to lower blood glucose in patients with type 2 diabetes. Exenatide mimics the effect of a hormone called GLP-1 and was originally discovered in the saliva of the Gila monster shown in the picture but is now synthesised chemically in a laboratory. Exenatide has to be given twice a day by subcutaneous (under the skin) injection using a pen device shown on the right. This is very much like giving insulin injections but exenatide works in a different way to insulin. Exenatide is licensed for treatment of type 2 diabetes in combination with metformin, and/or sulphonylureas in patients who have not achieved adequate glycaemic control on tolerable doses of these oral treatments. Exenatide has an advantage over in that it helps patients to lose weight whereas insulin usually causes weight gain, which is undesirable in patients who are already overweight. |