Antimuscarinics for the treatment of overactive bladder: current options and emerging therapies.
Antimuscarinics for the treatment of overactive bladder: current options and emerging therapies.
复制标题
用于治疗膀胱过度活动症的抗毒蕈碱药：当前选择和新兴疗法。
DOI：
--
复制
发表时间：
2004
影响因子：
--
通讯作者：
J. Jasper
中科院分区：
文献类型：
--
作者：
S. Hegde;M. Mammen;J. Jasper
二十多年来，抗毒蕈碱药物一直是治疗膀胱过度活动症（OAB）的主要药物。理想的抗毒蕈碱药物是可以使膀胱功能正常化而不干扰其他器官的副交感神经调节的药物。目前，托特罗定（托特罗定-ER）和奥昔布宁（奥昔布宁-ER和奥昔布宁-TDS）的缓释制剂作为OAB药物治疗的基石。尽管这些产品相对于较旧的药物有显著的改进，特别是在给药方案的便利性方面，但其耐受性问题和适度的疗效使其不太理想。我们对毒蕈碱受体药理学的理解的进展提高了我们通过选择性靶向五种毒蕈碱亚型中的一种或多种来扩大治疗指数和增加抗毒蕈碱药物疗效的能力的乐观态度。具有不同受体选择性特征（非选择性、M3选择性、M2选择性、M2保留和M5保留）的一组结构多样的分子正在开发用于OAB。在准确判断这些药物的治疗价值之前，必须等待这些药物的临床试验结果。
Antimuscarinic drugs have been the mainstay in the treatment of overactive bladder (OAB) for over two decades. An ideal antimuscarinic medicine is one that can normalize bladder function without interfering with parasympathetic regulation of other organs. Currently, extended-release formulations of tolterodine (tolterodine-ER) and oxybutynin (oxybutynin-ER and oxybutynin-TDS) serve as the cornerstone in the pharmacotherapy of OAB. Although these products represent a significant improvement over older agents, especially with respect to convenience of dosing schedule, their tolerability concerns and modest efficacy make them less than ideal therapies. Advances in our understanding of muscarinic receptor pharmacology have raised optimism in our ability to widen the therapeutic index and increase the efficacy of antimuscarinics by selectively targeting one or more of the five muscarinic subtypes. A structurally diverse group of molecules, having varying receptor-selectivity profiles (non-selective, M3 selective, M2 selective, M2 sparing and M5 sparing), are in development for OAB. Results of clinical trials with these drugs must be awaited before their therapeutic value can be accurately judged.