Truzzi José C, Sartori Marair G F, Kemp Vitorio L
Urology Medical Affairs Department, Federal University of Sao Paulo, 775, Dr. Diogo de Faria Street, Cj 84, Sao Paulo, 04037-002, Brazil.
Gynecology and Obstetrics Department, Federal University of Sao Paulo, Sao Paulo, Brazil.
Adv Ther. 2025 Jul 3. doi: 10.1007/s12325-025-03275-8.
Trospium chloride (TCL) is a quaternary amine derived from atropine, classified as an oral anticholinergic, the class of drugs most commonly used in the treatment of overactive bladder syndrome (OAB) and detrusor overactivity (DO). It is a large and hydrophilic molecule, with a low water-oil partition coefficient, which hinders the passage through lipid membranes and has demonstrated poor penetration into the central nervous system (CNS), generally without deleterious effects on the cognitive functions of healthy patients or those already with dementia. This molecule is excreted practically unchanged in the urine, and the metabolized part undergoes spontaneous hydrolysis. Thus, it is subject to very few drug interactions in the metabolic process, favoring its application to polypharmacy user populations. Numerous randomized, placebo-controlled trials and post-marketing studies of TCL have demonstrated efficacy and safety, including long-term follow-up. Adverse events associated with the use of TCL are typical of those presented by antimuscarinic therapy, most commonly, dry mouth, with an incidence similar to that of other representatives of this class of drugs. So far, in general, TCL presents a favorable profile for the treatment of patients with OAB and DO. The study reviews literature specifically on TCL. While most available data stems from early studies conducted during its launch, the current investigation was prompted by renewed focus on the cognitive side effects of antimuscarinics. These effects are not limited to elderly patients but may also affect long-term users of this medication class. TCL emerges as a potentially safer option compared to many other antimuscarinics.
氯化托品铵（TCL）是一种源自阿托品的季铵类化合物，属于口服抗胆碱能药物，这类药物是治疗膀胱过度活动症（OAB）和逼尿肌过度活动（DO）最常用的药物类别。它是一种大分子亲水性分子，水油分配系数低，这阻碍了其通过脂质膜，并且已证明其对中枢神经系统（CNS）的渗透较差，通常对健康患者或已患有痴呆症的患者的认知功能没有有害影响。该分子在尿液中几乎原样排泄，代谢部分会发生自发水解。因此，它在代谢过程中很少发生药物相互作用，有利于其应用于联合用药的人群。TCL的大量随机、安慰剂对照试验和上市后研究已证明其有效性和安全性，包括长期随访。与使用TCL相关的不良事件是抗毒蕈碱治疗常见的不良事件，最常见的是口干，其发生率与该类药物的其他代表药物相似。到目前为止，总体而言，TCL在治疗OAB和DO患者方面表现出良好的概况。该研究专门回顾了关于TCL的文献。虽然大多数现有数据来自其上市初期进行的早期研究，但目前的调查是由于对抗毒蕈碱药物认知副作用的重新关注而引发的。这些影响不仅限于老年患者，也可能影响这类药物的长期使用者。与许多其他抗毒蕈碱药物相比，TCL似乎是一种潜在更安全的选择。
