Role of fesoterodine in the treatment of overactive bladder.

Kylie J Mansfield
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引用次数: 5

Abstract

Muscarinic receptors have long been the target receptors for treatment of patients with overactive bladder (OAB). These patients experience symptoms of urgency, urinary frequency and nocturia, with or without urge incontinence (the involuntary leakage of urine associated with urge). Fesoterodine, a pro-drug, structurally and functionally related to tolterodine, is the newest agent developed for the treatment of OAB. Fesoterodine is broken down to the active metabolite, 5-hydroxy-methyl-tolterodine (5-HMT) by non-specific esterases. This metabolism results in the complete breakdown of the parent compound and is responsible for dose related improvements in clinical efficacy and health related quality of life. Like other antimuscarinic agents including tolterodine, fesoterodine is associated with improvements in clinical variables related both to bladder filling (decreasing micturition frequency and increasing mean voided volume) and urgency (urgency and urge incontinence episodes). Improvements in health related quality of life following treatment with fesoterodine is indicated by improvements in 7 of the 9 variables measured by the King's Health Questionnaire. Also like other antimuscarinic agents, fesoterodine use is associated with adverse events including dry mouth. However the incidence of dry mouth is reduced with fesoterodine, compared to oxybutynin, due to the improved bladder selectivity of 5-HMT.

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非索特罗定治疗膀胱过动症的作用。
毒蕈碱受体一直是治疗膀胱过动症(OAB)的靶受体。这些患者出现急症、尿频和夜尿症症状,伴有或不伴有急迫性尿失禁(与急迫性尿失禁相关的不自主尿漏)。非索特罗定是最新开发的治疗OAB的药物,在结构和功能上与托特罗定相似。非特异性酯酶将非索罗定分解为活性代谢物5-羟基甲基托特罗定(5-HMT)。这种代谢导致母体化合物的完全分解,并负责临床疗效和健康相关生活质量的剂量相关改善。与包括托特罗定在内的其他抗毒蕈碱药物一样,非索特罗定与膀胱充血(减少排尿频率和增加平均排尿量)和尿急(急迫性和急迫性失禁发作)相关的临床变量的改善有关。国王健康问卷测量的9个变量中有7个变量的改善表明,使用非索特罗定治疗后与健康相关的生活质量有所改善。与其他抗蛇毒胺药物一样,使用非索罗定也会引起包括口干在内的不良事件。然而,与奥昔布宁相比,由于5-HMT的膀胱选择性提高,非索特罗定减少了口干的发生率。
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