Département d'Urologie, Transplantation Rénale et Andrologie, CHU Rangueil, TSA50032, 31059 Toulouse, France.
Service d'Urologie, CHU de Rennes, Rennes, France.
Eur J Pharmacol. 2018 Aug 15;833:155-157. doi: 10.1016/j.ejphar.2018.05.036. Epub 2018 May 24.
Fesoterodine (as one of three drugs: dutasteride, finasteride and fesoterodine) was classified B (beneficial) by LUTS-FORTA 2014, indicating that it is a medicinal product with proven or obvious efficacy in the elderly, with limited side effects and/or safety concerns. A systematic literature review was undertaken in January 2018 using the PubMed and Google Scholar databases with the following individual and combined keywords: "fesoterodine", "pharmacology", "overactive bladder" and "antimuscarinics". The aim of the review was to determine which of fesoterodine's pharmacological properties explains its clinical benefits in general patient populations with OAB and the elderly in particular. The articles in the results were then selected by publication language (English and French only), methodology (off-topic studies, reported cases and literature reviews were excluded), relevance to the subject matter and publication date prior to 31 January 2018. A total of 205 articles was initially obtained, with 115 read and 45 selected. It appears that the association of four pharmacological properties specific to fesoterodine can explain that this drug has a good balance between efficacy and tolerability. These properties are namely the drug's high and nearly equal affinity for both the M2 and M3 muscarinic receptors, poor penetration of the blood-brain barrier, lack of hepatic first-pass activation -fesoterodine being rapidly and extensively converted to its active metabolite, 5-hydroxymethyl tolterodine, by ubiquitous esterases-, and its extended-release formulation. Fesoterodine's pharmacological profile is optimal for the treatment of overactive bladder. It is now recognized as one of the leading first-line treatment for this indication.
非索罗定（三种药物之一：度他雄胺、非那雄胺和非索罗定）在 2014 年 LUTS-FORTA 中被归类为 B 类（有益），这表明它是一种在老年人中具有已证明或明显疗效的药物，副作用有限且/或安全性担忧。2018 年 1 月，我们使用 PubMed 和 Google Scholar 数据库进行了系统的文献综述，使用了以下单独和组合的关键词：“非索罗定”、“药理学”、“膀胱过度活动症”和“抗毒蕈碱药”。该综述的目的是确定非索罗定的药理学特性中哪些可以解释其在一般 OAB 患者人群和老年人中的临床益处。然后根据出版语言（仅英语和法语）、方法学（排除非相关研究、报告病例和文献综述）、与主题的相关性以及在 2018 年 1 月 31 日之前的出版日期对结果中的文章进行选择。最初获得了 205 篇文章，其中 115 篇被阅读，45 篇被选择。似乎与非索罗定的四个特定药理学特性相关联可以解释该药物在疗效和耐受性之间具有良好的平衡。这些特性包括该药物对 M2 和 M3 毒蕈碱受体的高亲和力和几乎相等的亲和力、较差的血脑屏障穿透性、缺乏肝首过激活-非索罗定迅速且广泛地转化为其活性代谢物 5-羟甲基托特罗定，由无处不在的酯酶-，以及其缓释制剂。非索罗定的药理学特征最适合治疗膀胱过度活动症。它现在被认为是该适应症的一线治疗方法之一。
