Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM'S NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, India.
Curr Drug Metab. 2020;21(2):79-88. doi: 10.2174/1389200221666200425211139.
Overactive bladder syndrome is a broadly occurring urological disorder with a distressing impact on the quality of life. The commonly used antimuscarinic drugs show poor patient compliance because of unsatisfactory potency, tolerability and high occurrence of adverse effects such as dry mouth, blurred vision, constipation, dizziness etc. Mirabegron is the first approved β3-adrenoreceptor agonist, used as mono or in combination therapies for overactive bladder syndrome.
The present review provides an insight into the mechanism, pharmacokinetics, toxicokinetics, clinical trials and the development of various conventional and modified-release dosage forms of mirabegron for the treatment of overactive bladder syndrome.
The clinical trials of phase II and phase III of mirabegron demonstrated symptomatic relief from the overactive bladder without disturbing the micturition cycle. To date, mirabegron showed promising results for safety, tolerability and efficacy in patients with overactive bladder syndrome. The modified-release tablet dosage form of mirabegron appear to be a proficient and suitable replacement for antimuscarinics and revealed the tremendous potential to overcome the adverse effects of conventional antimuscarinic drugs like Oxybutyline chloride ER, Detrol LA, VESIcare, etc. Conclusion: Mirabegron shows a distinct mode of action, i.e., targeting β3-adrenoreceptors and improving bladder storage without altering void contractions. The limited side effects, high safety, efficacy and tolerability of mirabegron present an adequate substitute to antimuscarinics. However, long-term analysis and clinical studies are prerequisites for assessing the safety, tolerability and efficacy profile of mirabegron.
膀胱过度活动症是一种广泛存在的泌尿系统疾病，对生活质量有很大的影响。常用的抗毒蕈碱药物由于疗效不佳、耐受性差以及口干、视力模糊、便秘、头晕等不良反应发生率高，导致患者依从性差。米拉贝隆是第一个被批准的β3-肾上腺素能受体激动剂，可作为单一药物或联合治疗用于治疗膀胱过度活动症。
本综述深入探讨了米拉贝隆治疗膀胱过度活动症的作用机制、药代动力学、毒代动力学、临床试验以及各种普通和缓释制剂的开发。
米拉贝隆的 II 期和 III 期临床试验表明，米拉贝隆可缓解膀胱过度活动症状，而不影响排尿周期。迄今为止，米拉贝隆在治疗膀胱过度活动症患者的安全性、耐受性和疗效方面表现出了良好的效果。米拉贝隆的缓释片剂型似乎是一种有效的、合适的抗毒蕈碱药物替代品，显示出克服传统抗毒蕈碱药物（如奥昔布宁 ER、盐酸达特罗定 LA、盐酸维司地尔等）不良反应的巨大潜力。结论：米拉贝隆具有独特的作用机制，即靶向β3-肾上腺素能受体，改善膀胱储尿功能，而不改变排尿收缩。米拉贝隆的副作用有限、安全性高、疗效好、耐受性好，为抗毒蕈碱药物提供了一个充分的替代品。然而，长期分析和临床研究是评估米拉贝隆安全性、耐受性和疗效的前提。
