A clinical review of GLP-1 receptor agonists: efficacy and safety in diabetes and beyond.
A clinical review of GLP-1 receptor agonists: efficacy and safety in diabetes and beyond.
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DOI：
10.7573/dic.212283
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发表时间：
2015-01-01
期刊：
影响因子：
--
通讯作者：
Isaacs, Diana
中科院分区：
文献类型：
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作者：
Prasad-Reddy, Lalita;Isaacs, Diana
2型糖尿病的患病率正在以惊人的速度增长。许多用于治疗2型糖尿病的药物都有低血糖和体重增加的不良影响。高血糖素样多肽-1(GLP-1)受体激动剂代表了治疗糖尿病的一种独特方法，其益处延伸到血糖控制之外，包括对体重、血压、胆固醇水平和β细胞功能的积极影响。它们模仿胰岛素激素GLP-1的作用，GLP-1是肠道对食物摄入的反应。它们的作用包括增加胰岛素分泌，减少胰高血糖素的释放，增加饱腹感，减缓胃排空。目前，美国已批准的GLP-1受体激动剂有四种：埃塞那肽、利拉鲁肽、阿尔比鲁肽和度卢肽。第五种药物lixisenatide在欧洲上市。每种药物都有重要的药效学、药动学和临床差异。GLP-1治疗最常见的不良反应包括恶心、呕吐和注射部位反应。其他警告和预防措施包括胰腺炎和甲状腺细胞癌。GLP-1受体激动剂是一种创新和有效的改善血糖控制的选择，还有其他潜在的好处，如保留β细胞功能、减肥和提高胰岛素敏感性。每周一次的配方也可能提高患者的依从性。总体而言，这些药物都是治疗2型糖尿病患者的有效药物，这些患者要么没有得到二甲双胍的控制，要么对二甲双胍不耐受。
The prevalence of type 2 diabetes is increasing at an astounding rate. Many of the agents used to treat type 2 diabetes have undesirable adverse effects of hypoglycemia and weight gain. Glucagon-like peptide-1 (GLP-1) receptor agonists represent a unique approach to the treatment of diabetes, with benefits extending outside glucose control, including positive effects on weight, blood pressure, cholesterol levels, and beta-cell function. They mimic the effects of the incretin hormone GLP-1, which is released from the intestine in response to food intake. Their effects include increasing insulin secretion, decreasing glucagon release, increasing satiety, and slowing gastric emptying. There are currently four approved GLP-1 receptor agonists in the United States: exenatide, liraglutide, albiglutide, and dulaglutide. A fifth agent, lixisenatide, is available in Europe. There are important pharmacodynamic, pharmacokinetic, and clinical differences of each agent. The most common adverse effects seen with GLP-1 therapy include nausea, vomiting, and injection-site reactions. Other warnings and precautions include pancreatitis and thyroid cell carcinomas. GLP-1 receptor agonists are an innovative and effective option to improve blood glucose control, with other potential benefits of preserving beta-cell function, weight loss, and increasing insulin sensitivity. Once-weekly formulations may also improve patient adherence. Overall, these are effective agents for patients with type 2 diabetes, who are either uncontrolled on metformin or intolerant to metformin.