Jost Wolfgang H
Parkinson-Klinik Ortenau, Wolfach, 77709, Germany.
Neuropsychiatr Dis Treat. 2022 Aug 6;18:1603-1618. doi: 10.2147/NDT.S279362. eCollection 2022.
COMT (catechol--methyltransferase) inhibitors are key therapeutic agents in the management of motor fluctuations (MF) in patients with Parkinson's disease (PD). As levodopa/DDCI add-on therapy, their main benefit lies in increasing ON-time and reducing OFF-time for PD patients in the middle stages of the disease. Two of the three available COMT inhibitors, tolcapone and entacapone, have been approved for over two decades. Opicapone, a third-generation COMT inhibitor approved in 2016, was designed with the aim of overcoming specific challenges of the earlier generation compounds, specifically hepatotoxicity and short effect duration. This review aims at highlighting the specific properties and characteristics of opicapone, namely combining efficacy with good tolerability as demonstrated in the registration studies and since then confirmed under real-world conditions. Opicapone has been shown to be effective in patients with early, as well as late motor fluctuations. Whilst patients in the earlier Hoehn and Yahr stages benefit more than patients in later stages, the incidence of dyskinesia in patients with recent onset MF is around half that of patients with more established fluctuations. With the added advantage of a once-daily administration, this particular COMT inhibitor provides a simple, yet effective therapy for patients with Parkinson's disease and MF.
儿茶酚-O-甲基转移酶（COMT）抑制剂是帕金森病（PD）患者运动波动（MF）管理中的关键治疗药物。作为左旋多巴/多巴脱羧酶抑制剂的附加疗法，它们的主要益处在于增加疾病中期PD患者的“开”期时间并减少“关”期时间。三种可用的COMT抑制剂中的两种，托卡朋和恩他卡朋，已获批超过二十年。奥匹卡朋是2016年获批的第三代COMT抑制剂，其设计目的是克服早期化合物的特定挑战，特别是肝毒性和作用持续时间短的问题。本综述旨在突出奥匹卡朋的具体特性，即在注册研究中所证明的并在现实世界条件下得到证实的疗效与良好耐受性相结合的特性。奥匹卡朋已被证明对早期和晚期运动波动患者均有效。虽然处于早期霍恩和雅尔分期的患者比晚期患者获益更多，但近期发生运动波动的患者中异动症的发生率约为波动更明显患者的一半。由于具有每日一次给药的额外优势，这种特定的COMT抑制剂为帕金森病和运动波动患者提供了一种简单而有效的治疗方法。
