Antimuscarinic agents are now widely used as the pharmacological therapy for overactive bladder (OAB) because neuronal (parasympathetic nerve) and non-neuronal acetylcholine play a significant role for the bladder function. In this review, we will highlight basic and clinical aspects of eight antimuscarinic agents (oxybutynin, propiverine, tolterodine, solifenacin, darifenacin, trospium, imidafenacin, and fesoterodine) clinically used to treat urinary dysfunction in patients with OAB. The basic pharmacological characteristics of these eight antimuscarinic agents include muscarinic receptor subtype selectivity, functional bladder selectivity, and muscarinic receptor binding in the bladder and other tissues. The measurement of drug-receptor binding after oral administration of these agents allows for clearer understanding of bladder selectivity by the integration of pharmacodynamics and pharmacokinetics under in vivo conditions. Their central nervous system (CNS) penetration potentials are also discussed in terms of the feasibility of impairments in memory and cognitive function in elderly patients with OAB. The clinical aspects of efficacy focus on improvements in the daytime urinary frequency, nocturia, bladder capacity, the frequency of urgency, severity of urgency, number of incontinence episodes, OAB symptom score, and quality of life (QOL) score by antimuscarinic agents in patients with OAB. The safety of and adverse events caused by treatments with antimuscarinic agents such as dry mouth, constipation, blurred vision, erythema, fatigue, increased sweating, urinary retention, and CNS adverse events are discussed. A dose-dependent relationship was observed with adverse events, because the risk ratio generally increased with elevations in the drug dose of antimuscarinic agents. Side effect profiles may be additive to or contraindicated by other medications.

抗毒蕈碱剂现在被广泛用作膀胱过动症（OAB）的药物治疗，因为神经元（副交感神经）和非神经元乙酰胆碱对膀胱功能起着重要作用。在这篇综述中，我们将重点介绍临床上用于治疗OAB患者尿功能障碍的八种抗毒蕈碱剂（奥昔布宁，普罗维林，托特罗定，索非那新，达利福星，托泊铵，伊达非那辛和非索罗定）的基本和临床方面。这八种抗毒蕈碱剂的基本药理特征包括毒蕈碱受体亚型选择性，功能性膀胱选择性以及在膀胱和其他组织中的毒蕈碱受体结合。口服这些药物后对药物受体结合的测量可以通过在体内条件下整合药效学和药代动力学来更清楚地了解膀胱的选择性。还从老年OAB患者记忆和认知功能受损的可行性方面讨论了它们的中枢神经系统（CNS）渗透潜力。疗效的临床方面集中在通过抗毒蕈碱药物改善患者的白天尿频，夜尿症，膀胱容量，尿频，尿急程度，失禁发作次数，OAB症状评分和生活质量（QOL）评分与OAB。由抗毒蕈碱药物治疗引起的安全性和不良事件，例如口干，便秘，视力模糊，红斑，疲劳，讨论了多汗，尿retention留和中枢神经系统不良事件的增加。观察到与不良事件的剂量依赖性关系，因为风险率通常随着抗毒蕈碱剂药物剂量的增加而增加。副作用可能是其他药物的补充或禁忌。