Gomelsky A, Dmochowski Roger R
Louisiana State University Health Sciences Center, Shreveport, Louisiana, USA.
Drugs Today (Barc). 2010 Feb;46(2):81-90. doi: 10.1358/dot.2010.46.2.1437712.
Overactive bladder (OAB) is a common condition that causes a profound impact on an individual's overall health and quality of life. Muscarinic antagonists are the mainstay of oral pharmacotherapy for OAB. The most-recently introduced muscarinic antagonist, fesoterodine fumarate, is unique in that the parent compound has no antimuscarinic efficacy due to its rapid and complete hydrolysis after oral administration. The active metabolite, 5-hydroxymethyl tolterodine, is responsible for all of the antimuscarinic effects. In two phase III studies, fesoterodine has been shown to significantly reduce mean urgency and urge urinary incontinence (UUI) episodes over placebo. As many as 60% of patients actively treated with fesoterodine reported no urge urinary incontinence episodes on a 3-day voiding diary, a significant improvement over placebo. Finally, several quality of life indices were significantly improved over placebo. There was a dose-related increase in antimuscarinic adverse events, such as dry mouth and constipation; however, few patients discontinued fesoterodine due to side effects.
膀胱过度活动症(OAB)是一种常见病症,对个人的整体健康和生活质量产生深远影响。毒蕈碱拮抗剂是OAB口服药物治疗的主要手段。最近推出的毒蕈碱拮抗剂富马酸非索罗定独具特色,其母体化合物在口服后会迅速且完全水解,因此没有抗毒蕈碱功效。活性代谢物5-羟甲基托特罗定产生所有抗毒蕈碱作用。在两项III期研究中,与安慰剂相比,非索罗定已显示出能显著减少平均尿急和急迫性尿失禁(UUI)发作次数。在一份为期3天的排尿日记中,多达60%接受非索罗定积极治疗的患者报告无急迫性尿失禁发作,与安慰剂相比有显著改善。最后,与安慰剂相比,几个生活质量指标也有显著改善。抗毒蕈碱不良事件如口干和便秘呈剂量相关增加;然而,很少有患者因副作用而停用非索罗定。