Caremel Romain, Loutochin Oleg, Corcos Jacques
Department of Urology, Jewish General Hospital, McGill University, 3755 cote sainte catherine E-936, Montreal, QC, H3T 1E2, Canada.
Int Urogynecol J. 2014 Feb;25(2):165-70. doi: 10.1007/s00192-013-2161-4. Epub 2013 Aug 7.
Mirabegron is a novel β3-adrenoceptor agonist recently approved by Japanese, American, and European authorities for overactive bladder (OAB) therapy. Here we review existing knowledge on this new class of medication, analyze existing literature on the topic, and make recommendations regarding its administration and necessary future studies.
We reviewed the current literature and analyzed mirabegron efficacy, safety, and suitability for treating OAB symptoms. We performed a systematic search of Medline/PubMed, and Embase. Studies exploring mechanisms involved in the effects of mirabegron were included. Searches were limited to the English language.
Two phase II and two large-scale phase III multinational randomized controlled trials have supported mirabegron efficacy and tolerability with up to 12 weeks of therapy in OAB patients. The reported frequency and severity of treatment-emergent and serious adverse events were similar to antimuscarinics but with more than threefold lower incidence of dry mouth than with tolterodine. However, effects on the cardiovascular system, cognitive functions, pharmacokinetic interactions with other drugs, and long-term adverse events have not yet been fully investigated.
Anticholinergic drugs should remain the first-line pharmacologic treatment for OAB until head-to-head comparative study eventually shows that mirabegron has equivalent or superior efficacy. However, it seems logical to use mirabegron as second-line treatment of OAB in patients who are poor responders or intolerant to anticholinergics.
米拉贝隆是一种新型β3肾上腺素能受体激动剂，最近已获日本、美国和欧洲当局批准用于治疗膀胱过度活动症（OAB）。在此，我们回顾关于这类新型药物的现有知识，分析该主题的现有文献，并就其给药方法及未来必要的研究提出建议。
我们回顾了当前文献，分析了米拉贝隆治疗OAB症状的疗效、安全性及适用性。我们对医学文献数据库/医学期刊数据库（Medline/PubMed）和荷兰医学文摘数据库（Embase）进行了系统检索。纳入了探索米拉贝隆作用机制的研究。检索限于英文文献。
两项II期和两项大规模III期多国随机对照试验均支持米拉贝隆在治疗OAB患者长达12周时的疗效和耐受性。所报告的治疗中出现的不良事件及严重不良事件的频率和严重程度与抗胆碱能药物相似，但口干发生率比托特罗定低三倍多。然而，其对心血管系统、认知功能、与其他药物的药代动力学相互作用以及长期不良事件尚未得到充分研究。
在头对头比较研究最终表明米拉贝隆具有同等或更高疗效之前，抗胆碱能药物仍应作为OAB的一线药物治疗。然而，对于对抗胆碱能药物反应不佳或不耐受的OAB患者，将米拉贝隆用作二线治疗似乎是合理的。
