Tufts University School of Medicine, St. Elizabeth's Medical Center, Boston, MA 02135, USA.
Expert Opin Pharmacother. 2009 Dec;10(18):3103-11. doi: 10.1517/14656560903451682.
Oxybutynin, a cholinergic-muscarinic receptor antagonist, is established as a safe and effective pharmacological treatment for patients with overactive bladder syndrome (OAB). Oxybutynin is available in multiple immediate- and extended-release oral and two transdermal formulations. Oxybutynin chloride topical gel (OTG) (Gelnique), Watson Pharmaceuticals, Corona, CA, USA) was approved in January 2009 by the US FDA. OTG was designed to provide consistent plasma oxybutynin levels with daily application, favorably altering the circulating N-desethyloxybutynin metabolite:oxybutynin ratio, and to utilize a biocompatible delivery system, thus minimizing both the anticholinergic adverse effects of oral formulations and the application-site skin reactions associated with other available forms of transdermal delivery.
OBJECTIVE/METHODS: This review summarizes the pharmacological properties and the clinical efficacy and safety profile of OTG based on the published literature and unpublished data provided by the manufacturer upon request.
RESULTS/CONCLUSION: OTG represents an efficacious, safe, and convenient alternative to other oxybutynin formulations and other oral anticholinergic medications for the treatment of OAB. Future studies and broad clinical experience should confirm the promising early experience observed with this formulation.
奥昔布宁是一种胆碱能毒蕈碱受体拮抗剂，已被确立为治疗膀胱过度活动症（OAB）患者的安全有效药物。奥昔布宁有多种速释和缓释口服制剂以及两种透皮制剂。奥昔布宁盐酸盐局部凝胶（OTG）（Gelnique），美国 Watson 制药公司，美国加利福尼亚州 Corona）于 2009 年 1 月获得美国 FDA 批准。OTG 的设计目的是通过每日应用提供稳定的血浆奥昔布宁水平，有利地改变循环中 N-去乙基奥昔布宁代谢物：奥昔布宁的比值，并利用生物相容性的给药系统，从而最大限度地减少口服制剂的抗胆碱能不良反应和其他可用透皮给药形式相关的应用部位皮肤反应。
目的/方法：这篇综述根据已发表的文献和制造商应要求提供的未发表数据，总结了 OTG 的药理学特性以及临床疗效和安全性概况。
结果/结论：OTG 是一种有效、安全且方便的替代其他奥昔布宁制剂和其他口服抗胆碱能药物的选择，可用于治疗 OAB。未来的研究和广泛的临床经验应该证实这种制剂早期观察到的有希望的结果。
