Bhide Alka A, Digesu G Alessandro, Fernando Ruwan, Khullar Vik
Department of Urogynaecology, St. Mary's Hospital, Cambridge Wing, Praed Street, W1 1NY London, UK.
Int Urogynecol J. 2012 Oct;23(10):1345-8. doi: 10.1007/s00192-012-1724-0. Epub 2012 Mar 13.
The lack of an alternative to antimuscarinics has led to the search for new drug targets for overactive bladder (OAB) symptoms. The presence of β-3 adrenoreceptors in the bladder has been confirmed, and they are known to have a role in bladder relaxation. Targeting these receptors improves bladder compliance on filling and increases bladder capacity. MEDLINE literature search on efficacy and safety of mirabegron was performed. The US Food and Drug Administration Web site, clinicaltrials.gov, and controlled-trials.com online trial registries were searched for English-language articles containing the term "mirabegron". Finally, abstracts from recent International scientific meetings were searched for randomised controlled trials (RCTs). Studies show that mirabegron reduces the number of micturitions and incontinence episodes in a 24-h period compared with placebo. Dry mouth and gastrointestinal disturbances are the most common side effects, but these have been rated as mild to moderate. A small rise in mean heart rate and blood pressure has been shown. Further investigations are ongoing and results are awaited. Although mirabegron is metabolised by CYP2D6, it is also thought to inhibit the activity of this enzyme. Therefore, potential drug interactions with other CYP2D6 substrates need to be further studied. Mirabegron is a promising alternative to antimuscarinics. Further information on its long-term use in terms of efficacy, safety, and tolerability is awaited.
由于缺乏抗毒蕈碱药物的替代药物,人们开始寻找治疗膀胱过度活动症(OAB)症状的新药物靶点。膀胱中β-3肾上腺素能受体的存在已得到证实,并且已知它们在膀胱舒张中起作用。作用于这些受体可改善膀胱充盈时的顺应性并增加膀胱容量。对米拉贝隆的疗效和安全性进行了医学文献检索。在美国食品药品监督管理局网站、clinicaltrials.gov和controlled-trials.com在线试验注册库中搜索了包含“米拉贝隆”一词的英文文章。最后,在最近国际科学会议的摘要中搜索了随机对照试验(RCT)。研究表明,与安慰剂相比,米拉贝隆可减少24小时内的排尿次数和尿失禁发作次数。口干和胃肠道不适是最常见的副作用,但这些副作用被评为轻度至中度。已显示平均心率和血压有小幅上升。进一步的研究正在进行中,结果有待观察。虽然米拉贝隆由CYP2D6代谢,但它也被认为会抑制这种酶的活性。因此,与其他CYP2D6底物的潜在药物相互作用需要进一步研究。米拉贝隆是抗毒蕈碱药物的一种有前景的替代品。期待关于其长期使用的疗效、安全性和耐受性的更多信息。