Louisiana State University Health Sciences Center - Shreveport, 1501 Kings Highway, Shreveport, LA 71130, USA.
Expert Opin Pharmacother. 2012 Jun;13(9):1337-43. doi: 10.1517/14656566.2012.688953.
Overactive bladder (OAB) is a common condition that has a profound impact on an individual's overall health and quality of life. Muscarinic receptor antagonists are the mainstay of oral pharmacotherapy for OAB. While all of the medications in this class are significantly more effective than placebo, they are also associated with more adverse events that may limit their overall use. Transdermal application of oxybutynin has been shown to avoid first-pass metabolism and, thus, may be associated with fewer antimuscarinic side effects.
This paper reviews the pharmacology of transdermal oxybutynin gel and summarizes the available data regarding this product in the treatment of OAB. It also discusses the role of this product in the OAB treatment armamentarium.
Oxybutynin transdermal gel has been shown to have significant advantages over placebo, in terms of urgency incontinence episodes, urinary frequency and voided volume in a Phase III study. Application site effects were higher in the gel group, but the incidence of antimuscarinic side effects were lower than those seen with oral preparations. The lower incidence of skin side effects, as compared with the transdermal patch, may confer a theoretical advantage toward the gel product. While promising, unanswered questions remain regarding persistence with treatment after this mode of therapy, and head-to-head comparisons with other antimuscarinics are absent.
膀胱过度活动症(OAB)是一种常见病症,对个体的整体健康和生活质量有深远影响。毒蕈碱受体拮抗剂是治疗 OAB 的口服药物治疗的主要方法。虽然该类药物均明显优于安慰剂,但它们也会引起更多的不良反应,从而可能限制其总体应用。经皮应用奥昔布宁可避免首过代谢,因此可能与较少的抗毒蕈碱副作用相关。
本文综述了经皮奥昔布宁凝胶的药理学,并总结了该产品在治疗 OAB 方面的现有数据。还讨论了该产品在 OAB 治疗手段中的作用。
在一项 III 期研究中,奥昔布宁经皮凝胶在急迫性尿失禁发作、尿频率和排尿量方面,与安慰剂相比具有显著优势。在凝胶组中,应用部位的不良反应更高,但抗毒蕈碱副作用的发生率低于口服制剂。与经皮贴剂相比,皮肤不良反应发生率较低,可能使凝胶产品具有理论优势。虽然前景广阔,但这种治疗方式的治疗持续时间仍存在未解决的问题,并且缺乏与其他抗毒蕈碱药物的头对头比较。