Berger Amnon A, Winnick Ariel, Izygon Jonathan, Jacob Binil M, Kaye Jessica S, Kaye Rachel J, Neuchat Elisa E, Kaye Adam M, Alpaugh Edward S, Cornett Elyse M, Han Andrew H, Kaye Alan D
Anesthesiology, Critical Care, and Pain Medicine, Beth Israel Deaconess Medical Center.
Soroka University Medical Center and Faculty of Health Sciences; School of Optometry, University of California.
Health Psychol Res. 2022 Jun 28;10(3):36074. doi: 10.52965/001c.36074. eCollection 2022.
Parkinson's Disease (PD) is a common neurodegenerative disorder and the leading cause of disability. It causes significant morbidity and disability through a plethora of symptoms, including movement disorders, sleep disturbances, and cognitive and psychiatric symptoms. The traditional pathogenesis theory of PD involves the loss of dopaminergic neurons in the substantia nigra (SN). Classically, treatment is pursued with an assortment of medications that are directed at overcoming this deficiency with levodopa being central to most treatment plans. Patients taking levodopa tend to experience "off episodes" with decreasing medication levels, causing large fluctuations in their symptoms. These off episodes are disturbing and a source of morbidity for these patients. Opicapone is a novel, peripherally acting Catechol-O-methyl transferase (COMT) inhibitor that is used as adjunctive therapy to carbidopa/levodopa for treatment and prevention of "off episodes." It has been approved for use as an adjunct to levodopa since 2016 in Europe and has recently (April 2020) gained FDA approval for use in the USA. By inhibiting COMT, opicapone slows levodopa metabolism and increases its availability. Several clinical studies demonstrated significant improvement in treatment efficacy and reduction in duration of "off episodes." The main side effect demonstrated was dyskinesia, mostly with the 100mg dose, which is higher than the approved, effective dose of 50mg. Post-marketing surveillance and analysis are required to further elucidate its safety profile and contribute to patient selection. This paper reviews the seminal and latest evidence in the treatment of PD "off episodes" with the novel drug Opicapone, including efficacy, safety, and clinical indications.
帕金森病(PD)是一种常见的神经退行性疾病,也是导致残疾的主要原因。它通过大量症状导致显著的发病和残疾,这些症状包括运动障碍、睡眠障碍以及认知和精神症状。PD的传统发病机制理论涉及黑质(SN)中多巴胺能神经元的丧失。传统上,治疗采用多种药物,旨在通过左旋多巴来克服这种缺乏,左旋多巴是大多数治疗方案的核心。服用左旋多巴的患者往往会随着药物水平的降低而经历“关期”,导致症状大幅波动。这些关期令人困扰,是这些患者发病的一个原因。奥匹卡朋是一种新型的外周作用儿茶酚-O-甲基转移酶(COMT)抑制剂,用作卡比多巴/左旋多巴的辅助治疗,用于治疗和预防“关期”。自2016年以来,它在欧洲已被批准作为左旋多巴的辅助药物使用,最近(2020年4月)获得了美国食品药品监督管理局(FDA)在美国使用的批准。通过抑制COMT,奥匹卡朋减缓左旋多巴的代谢并增加其可用性。多项临床研究表明,治疗效果有显著改善,“关期”持续时间缩短。所显示的主要副作用是运动障碍,大多出现在100mg剂量时,该剂量高于批准的有效剂量50mg。需要进行上市后监测和分析,以进一步阐明其安全性概况,并有助于患者选择。本文综述了使用新型药物奥匹卡朋治疗PD“关期”的重要和最新证据,包括疗效、安全性和临床适应症。