盐酸奥昔布宁的重新定位:合成、作用方式、代谢和配方的最新进展

Jean Jacques Vanden Eynde
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引用次数: 0

摘要

几十年来,盐酸奥昔布宁一直被用来改善尿失禁和尿频的膀胱控制。本文综述了该消旋药物的合成方法,并详细介绍了合成(S)- oxybutin的关键中间体(S)-2-环己基-2-羟基-2-苯基乙酸的制备方法。简要介绍作用方式和代谢,以解释与其使用有关的主要不利影响,并证明在各种商业配方中观察到的演变。在多汗症、潮热和阻塞性睡眠呼吸暂停的临床试验中,重新定位的机会被讨论。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Repositioning Oxybutynin Hydrochloride: State of the Art in Synthesis, Mode of Action, Metabolism, and Formulations
For decades, oxybutynin hydrochloride has been prescribed to improve bladder control in cases of incontinence and excessive urination frequency. This review summarizes synthetic methods enabling the preparation of the racemic drug and, in a detailed manner, preparation of (S)-2-cyclohexyl-2-hydroxy-2-phenylacetic acid, a key intermediate in the synthesis of (S)-oxybutynin. The mode of action and metabolism are briefly addressed in order to explain the main adverse effects associated with its use and to justify the evolution observed in the diverse commercial formulations. Repositioning opportunities are discussed in terms of clinical trials for the management of hyperhidrosis, hot flashes, and obstructive sleep apnea.
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