Department of Diabetes and Endocrinology, Cedar Centre at the Royal Surrey County Hospital, Guildford, UK.
Int J Clin Pract. 2010 Sep;64(10):1402-14. doi: 10.1111/j.1742-1241.2010.02465.x.
Established therapies for type-2 diabetes effectively reduce blood glucose, but are often associated with adverse effects that pose risks to patient's health or diminish adherence to treatment. Weight gain, hypoglycaemia and gastrointestinal symptoms are commonly reported and some agents may not be safe for use in patients with renal impairment or elevated cardiovascular risk. New treatments based on the action of the endogenous human hormone glucagon-like peptide-1 (GLP-1), including exenatide and liraglutide, are available. These therapies provide a novel pharmacological approach to glycaemic control via multiple mechanisms of action, and accordingly exhibit different safety and tolerability profiles than conventional treatments. GLP-1 receptor agonists stimulate insulin release only in the presence of elevated blood glucose and are therefore associated with a fairly low risk of hypoglycaemia. Gastrointestinal symptoms are common but transient, and there appears to be little potential for interaction with other drugs. GLP-1 receptor agonists are associated with weight loss rather than weight gain. As protein-based therapies, these agents have the potential to induce antibody formation, but the impact on efficacy and safety is minor. GLP-1 receptor agonists thus offer a new and potentially useful option for clinicians concerned about some of the common adverse effects of type-2 diabetes therapies.
用于 2 型糖尿病的既定疗法能有效降低血糖，但往往与不良反应相关，这些不良反应对患者的健康构成风险或降低患者对治疗的依从性。体重增加、低血糖和胃肠道症状较为常见，某些药物在肾功能受损或心血管风险升高的患者中可能不安全。新型疗法基于内源性人类激素胰高血糖素样肽-1（GLP-1）的作用，包括艾塞那肽和利拉鲁肽。这些疗法通过多种作用机制提供了一种新颖的血糖控制药理学方法，因此与传统治疗相比，具有不同的安全性和耐受性特征。GLP-1 受体激动剂仅在血糖升高时才刺激胰岛素释放，因此与低血糖的风险相当低相关。胃肠道症状常见但短暂，与其他药物相互作用的可能性似乎很小。GLP-1 受体激动剂与体重减轻而非体重增加相关。作为基于蛋白质的疗法，这些药物有引发抗体形成的潜力，但对疗效和安全性的影响较小。因此，GLP-1 受体激动剂为关注 2 型糖尿病治疗常见不良反应的临床医生提供了一种新的、有潜在用途的选择。
