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Maximizing anticholinergic therapy for overactive bladder: has the ceiling been reached?

机译:最大化膀胱过度活动症的抗胆碱能疗法:是否达到上限?

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Urinary incontinence affects an estimated 20-33% of adults the USA and 55% of the country's elderly [1], having a more substantial impact on the physical and mental dimension of quality of life than other common chronic diseases. Muscarinic receptor antagonists, including oxybutynin, tolterodine, trospium chloride, darifenacin, and solifenacin, are front-line therapies for overactive bladder (OAB), with an efficacy of 65-75% in reducing major symptoms. Strategies to increase the therapeutic index have included behavioural therapy, flexible dosing, and dose escalation, as well as newer formulations that reduce anticholinergic side-effects. Among approved OAB agents, the oxybutynin transdermal-delivery system has been associated with a lower incidence of dry mouth than immediate- and extended-release formulations of traditional agents. With a low propensity for drug interactions and dry mouth, it is a likely candidate for older patients taking multiple medications. The transdermal patch bypasses systemicand first-pass metabolism, avoiding higher plasma concentrations of the active metabolite (N-desethyloxybutynin) thought to be associated with dry mouth symptoms. Anticholinergics have a significant role to play in the management of OAB; newer drugs targeted toward muscarinic receptors, and novel delivery systems, continue to increase the therapeutic index for this condition.
机译:尿失禁影响了美国约20-33%的成年人和该国老年人的55%[1],比其他常见的慢性疾病对生活质量的身心影响更大。毒蕈碱受体拮抗剂,包括奥昔布宁,托特罗定,氯化钾,达利福星和索非那新,是膀胱过度活动症(OAB)的一线治疗方法,其缓解主要症状的功效为65-75%。提高治疗指数的策略包括行为疗法,灵活剂量和剂量递增,以及减少抗胆碱能副作用的新型制剂。在批准的OAB药物中,奥昔布宁透皮递送系统的口干发生率低于传统药物的立即和延长释放制剂。由于药物相互作用和口干的可能性低,因此它可能是服用多种药物的老年患者的候选药物。透皮贴剂可绕过系统性和首过代谢,从而避免了血浆中较高浓度的活性代谢产物(N-去乙基羟丁宁)被认为与口干症状有关。抗胆碱药在OAB的管理中起着重要作用。针对毒蕈碱受体的新型药物和新颖的递送系统,继续增加了针对这种情况的治疗指数。

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