Department of Endocrinology and Diabetes, University Hospital, Nantes, France.
Diabetes Obes Metab. 2011 Feb;13(2):99-117. doi: 10.1111/j.1463-1326.2010.01317.x.
Management guidelines recommend metformin as the first-line therapy for most patients with type 2 diabetes uncontrolled by diet and exercise. Efficacy with metformin therapy is usually of limited duration, which necessitates the early introduction of one or two additional oral agents or the initiation of injections, glucagon-like peptide-1 (GLP-1) agonists or insulin. Although safe and effective, metformin monotherapy has been associated with gastrointestinal side effects (≈20% of treated patients in randomized studies) and is contraindicated in patients with renal insufficiency or severe liver disease. Patients treated with a sulphonylurea are at increased risk for hypoglycaemia and moderate weight gain, whereas those receiving a thiazolidinedione are subject to an increased risk of weight gain, oedema, heart failure or fracture. Weight gain and hypoglycaemia are associated with insulin use. Thus, there is an unmet need for a safe and efficacious add-on agent after initial-therapy failure. Evidence suggests that incretin-based agents, such as GLP-1 receptor agonists and dipeptidyl peptidase-4 inhibitors, can successfully achieve glycaemic targets and potentially provide cardiovascular and β-cell-function benefits. This review will examine current approaches for treating type 2 diabetes and discuss the place of incretin therapies, mainly GLP-1 agonists, in the type 2 diabetes treatment spectrum.
管理指南建议二甲双胍作为大多数未经饮食和运动控制的 2 型糖尿病患者的一线治疗药物。二甲双胍治疗的疗效通常是有限的，这需要早期引入一种或两种额外的口服药物或开始注射、胰高血糖素样肽-1 (GLP-1) 激动剂或胰岛素。尽管安全有效，但二甲双胍单药治疗与胃肠道副作用有关（随机研究中约 20%的治疗患者），并且在肾功能不全或严重肝病患者中禁忌使用。接受磺脲类药物治疗的患者发生低血糖和中度体重增加的风险增加，而接受噻唑烷二酮类药物治疗的患者体重增加、水肿、心力衰竭或骨折的风险增加。体重增加和低血糖与胰岛素的使用有关。因此，在初始治疗失败后，需要一种安全有效的附加药物。有证据表明，基于肠促胰岛素的药物，如 GLP-1 受体激动剂和二肽基肽酶-4 抑制剂，可以成功地达到血糖目标，并可能提供心血管和β细胞功能益处。这篇综述将检查治疗 2 型糖尿病的当前方法，并讨论肠促胰岛素治疗，主要是 GLP-1 激动剂，在 2 型糖尿病治疗谱中的地位。
