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Clin Drug Investig. 2019 Aug;39(8):805-819. doi: 10.1007/s40261-019-00826-0.
Glucagon-like peptide-1 receptor analogues/agonists (GLP-1RAs) are well established as effective adjuncts to lifestyle modification in the treatment of type 2 diabetes (T2D) as monotherapy or in combination with oral glucose-lowering drugs ± insulin. The six subcutaneous GLP-1RA formulations (i.e. twice-daily exenatide, once-daily liraglutide and lixisenatide, and once-weekly dulaglutide, exenatide and semaglutide) currently available in the EU and USA have many similarities, but also some unique features and properties. By stimulating GLP-1 receptors, GLP-1RAs increase insulin secretion and suppress glucagon release in a glucose-dependent manner, thereby improving clinical and patient-reported outcomes related to glycaemic control and weight. They also have been shown to reduce, or at least not increase, the risk of major cardiovascular outcomes. GLP-1RAs are generally well tolerated, with gastrointestinal and injection-site reactions being the most troublesome drug-related adverse events, and are associated with a very low intrinsic risk of hypoglycaemia. Treatment with GLP-1RAs should be customized to meet the clinical needs and personal preferences of the individual.
胰高血糖素样肽-1 受体激动剂/类似物 (GLP-1RAs) 已被广泛确立为治疗 2 型糖尿病 (T2D) 的有效辅助手段，可单独使用或与口服降糖药物联合使用，还可与胰岛素联合使用。目前在欧盟和美国可用的六种皮下 GLP-1RA 制剂（即每日两次的艾塞那肽、每日一次的利拉鲁肽和利西那肽，以及每周一次的度拉糖肽、艾塞那肽和司美格鲁肽）具有许多相似之处，但也具有一些独特的特征和特性。GLP-1RAs 通过刺激 GLP-1 受体，以葡萄糖依赖性方式增加胰岛素分泌并抑制胰高血糖素释放，从而改善与血糖控制和体重相关的临床和患者报告的结果。它们还被证明可以降低（或至少不增加）主要心血管结局的风险。GLP-1RAs 通常具有良好的耐受性，胃肠道和注射部位反应是最麻烦的药物相关不良事件，并且与低血糖的内在风险非常低相关。GLP-1RA 的治疗应根据个体的临床需求和个人偏好进行定制。
