School of Pharmacy, Wingate University, Wingate, NC 28174, USA.
Ann Pharmacother. 2009 Dec;43(12):1992-2000. doi: 10.1345/aph.1M308. Epub 2009 Nov 17.
To review pharmacologic, pharmacokinetic, efficacy, and safety data for fesoterodine and determine its role in the treatment of overactive bladder.
A MEDLINE search (1966-July 2009) was conducted using the key words fesoterodine, tolterodine, muscarinic receptor antagonist, anticholinergic, overactive bladder, urge incontinence, efficacy, safety, adverse effect, pharmacology, pharmacokinetic, and receptor binding.
All articles written in English that were identified from the data sources were evaluated, prioritizing randomized, controlled trials with human data. The references of published articles that we identified were examined for any additional studies appropriate for the review.
Fesoterodine, a competitive muscarinic receptor antagonist, is converted to its active metabolite, 5-hydroxymethyltolterodine, by nonspecific esterases, bypassing the cytochrome P450 system. Two randomized controlled Phase 3 trials examined the safety and efficacy of fesoterodine in the treatment of overactive bladder. Fesoterodine was found to produce significant improvements in the treatment of overactive bladder symptoms compared with placebo. Post hoc analysis of these trials demonstrated significant improvements in health-related quality of life in patients with overactive bladder. Only one study included tolterodine, and direct comparisons between fesoterodine and tolterodine were not conducted. The most common treatment-emergent adverse effects associated with fesoterodine included dry mouth, constipation, urinary tract infection, and headache.
Fesoterodine appears to be effective and generally safe for the treatment of overactive bladder. The efficacy and safety of fesoterodine in overactive bladder treatment seem to be at least similar to that of tolterodine. Although additional comparative trials are needed, based on available data, it does not appear that fesoterodine provides a substantial advantage over extended-release tolterodine in either efficacy or safety.
综述索利那新的药理学、药代动力学、疗效和安全性数据，确定其在治疗膀胱过度活动症中的作用。
使用关键词“索利那新、托特罗定、毒蕈碱受体拮抗剂、抗胆碱能药、膀胱过度活动症、急迫性尿失禁、疗效、安全性、不良反应、药理学、药代动力学、受体结合”，对 1966 年 7 月至 2009 年 7 月的 MEDLINE 进行了检索。
评估从资料来源中识别的所有英文文章，优先选择具有人类数据的随机、对照试验。检查已发表文章的参考文献，以确定是否有其他适合综述的研究。
索利那新是一种竞争性毒蕈碱受体拮抗剂，通过非特异性酯酶转化为其活性代谢物 5-羟甲基托特罗定，绕过细胞色素 P450 系统。两项随机对照 3 期试验研究了索利那新治疗膀胱过度活动症的安全性和疗效。与安慰剂相比，索利那新治疗膀胱过度活动症症状有显著改善。这些试验的事后分析显示，膀胱过度活动症患者的健康相关生活质量有显著改善。只有一项研究包括托特罗定，未进行索利那新与托特罗定的直接比较。与索利那新相关的最常见治疗中出现的不良反应包括口干、便秘、尿路感染和头痛。
索利那新似乎对治疗膀胱过度活动症有效且通常安全。索利那新治疗膀胱过度活动症的疗效和安全性似乎至少与托特罗定相似。尽管需要更多的比较试验，但根据现有数据，在疗效或安全性方面，索利那新似乎并没有明显优于控释托特罗定。
