Ridge T, Moretto T, MacConell L, Pencek R, Han J, Schulteis C, Porter L
American Health Network, Indianapolis, IN, USA.
Diabetes Obes Metab. 2012 Dec;14(12):1097-103. doi: 10.1111/j.1463-1326.2012.01639.x. Epub 2012 Jul 19.
Exenatide is a glucagon-like peptide-1 receptor agonist shown to improve glycaemic control in patients with type 2 diabetes (T2DM). Intermittent exenatide exposure is achieved with the twice-daily formulation (ExBID), while the once-weekly formulation (ExQW) provides continuous exenatide exposure. This integrated, retrospective analysis compared safety and tolerability of ExQW vs. ExBID in patients with T2DM.
Data were pooled from two open-label, randomized, comparator-controlled, trials directly comparing ExQW (N = 277) to ExBID (N = 268). Between-group differences in adverse event (AE) and hypoglycaemia incidences were calculated. Incidence over time and duration of selected AEs (nausea, vomiting, and injection-site-related AEs) were also summarized.
The most common AEs were nausea, diarrhoea, injection-site pruritus, and vomiting. Nausea and vomiting occurred less frequently with ExQW vs. ExBID, peaking at initiation (ExQW) or at initiation and dose escalation (ExBID), and decreasing over time. Few patients discontinued because of gastrointestinal-related AEs. Injection-site AEs were more common with ExQW but decreased over time in both groups. No major hypoglycaemia occurred; minor hypoglycaemia occurred with low incidence in patients not using concomitant sulphonylurea, with no difference between ExQW and ExBID. Serious AEs and discontinuations because of AEs were reported with similar frequency in both groups.
Both exenatide formulations were generally safe and well-tolerated, with ExQW associated with less nausea and vomiting but more injection-site AEs. Continuous vs. intermittent exposure did not impact the overall tolerability profile of exenatide, with no evidence of prolonged duration or worsened intensities of AEs with continuous exposure.
艾塞那肽是一种胰高血糖素样肽-1受体激动剂，已被证明可改善2型糖尿病（T2DM）患者的血糖控制。每日两次给药方案（ExBID）可实现间歇性艾塞那肽暴露，而每周一次给药方案（ExQW）可实现持续的艾塞那肽暴露。这项综合回顾性分析比较了ExQW与ExBID在T2DM患者中的安全性和耐受性。
数据来自两项开放标签、随机、对照试验，直接将ExQW（N = 277）与ExBID（N = 268）进行比较。计算不良事件（AE）和低血糖发生率的组间差异。还总结了选定AE（恶心、呕吐和注射部位相关AE）的发生率随时间的变化及持续时间。
最常见的AE是恶心、腹泻、注射部位瘙痒和呕吐。与ExBID相比，ExQW的恶心和呕吐发生率较低，在开始时（ExQW）或开始及剂量增加时（ExBID）达到峰值，并随时间下降。很少有患者因胃肠道相关AE停药。注射部位AE在ExQW中更常见，但两组均随时间下降。未发生严重低血糖；在未使用磺脲类药物的患者中，轻度低血糖发生率较低，ExQW和ExBID之间无差异。两组报告的严重AE和因AE停药的频率相似。
两种艾塞那肽制剂总体上安全且耐受性良好，ExQW与较少的恶心和呕吐相关，但注射部位AE较多。持续暴露与间歇性暴露对艾塞那肽的总体耐受性无影响，没有证据表明持续暴露会使AE持续时间延长或强度恶化。
