Feldman Matthew, Margolesky Jason
Department of Neurology, University of Miami Miller School of Medicine, Miami, Florida, USA.
Int J Neurosci. 2023 May;133(5):532-543. doi: 10.1080/00207454.2021.1929217. Epub 2021 Jun 1.
Levodopa formulations are the workhorses of the labor against motor symptoms management in Parkinson's disease (PD). Progression of PD on levodopa inevitably leads to motor fluctuations. It is important to understand the safety and efficacy of opicapone, the most recent addition to the clinician's armamentarium against these fluctuations. We review the development of COMT inhibitors in the treatment of PD as well as the efficacy and safety data reported in the currently published literature of opicapone in PD. The "currently published literature" is defined as all published, PubMed indexed trials including the word "opicapone." Finally, we compare opicapone to the competitor pharmaceuticals on the market to treat symptom fluctuations in PD and share our opinion of opicapone's place in clinical practice. From the reported results of phase 3 and 4 trials of opicapone in PD, it is a safe and efficacious option to combat motor fluctuations for our PD patients taking levodopa. A reduction of "off" time by up to 1 h per day can be expected, increasing "on" time with fewer dyskinesias. Opicapone is not generally hepatotoxic, and the most reported side-effects-dyskinesia, dry mouth, dizziness, diarrhea, and constipation-were seen in only 1.4% of the OPTIPARK (a large phase 4 clinical trial) study population. One should consider utilizing opicapone, perhaps in combination with other augmenting medications with different mechanisms of action, to help treat motor and non-motor fluctuations in PD.
左旋多巴制剂是对抗帕金森病（PD）运动症状的主要药物。使用左旋多巴治疗PD的过程中，病情进展不可避免地会导致运动波动。了解奥匹卡朋的安全性和有效性非常重要，它是临床医生对抗这些波动的最新药物。我们回顾了COMT抑制剂在PD治疗中的发展，以及目前已发表的关于奥匹卡朋治疗PD的文献中所报道的有效性和安全性数据。“目前已发表的文献”定义为所有已发表的、被PubMed索引且包含“奥匹卡朋”一词的试验。最后，我们将奥匹卡朋与市场上用于治疗PD症状波动的其他竞争药物进行比较，并分享我们对奥匹卡朋在临床实践中地位的看法。从奥匹卡朋治疗PD的3期和4期试验报告结果来看，对于服用左旋多巴的PD患者而言，它是对抗运动波动的一种安全有效的选择。预计每天可减少“关”期时间达1小时，增加“开”期时间，且异动症较少。奥匹卡朋一般无肝毒性，在OPTIPARK（一项大型4期临床试验）研究人群中，最常报告的副作用——异动症、口干、头晕、腹泻和便秘——仅在1.4%的患者中出现。临床医生应考虑使用奥匹卡朋，或许可与其他具有不同作用机制的增效药物联合使用，以帮助治疗PD的运动和非运动波动。
