帕金森病新药Opicapone的研究进展  

Research progress of new drug Opicapone for Parkinson′s disease

作　　者：陈信捷 罗恩丽[2] 陈雅芳 雒晓东[2] 郑春叶[2] CHEN Xinjie;LUO Enli;CHEN Yafang;LUO Xiaodong;ZHENG Chunye(The Second Clinical Medical School,Guangzhou University of Chinese Medicine,Guangdong Province,Guangzhou 510405,China;Department of Neurology,Fangcun Hospital,Guangdong Provincial Hospital of Traditional Chinese Medicine,Guangdong Province,Guangzhou 510370,China)

机构地区：[1]广州中医药大学第二临床医学院,广东广州510405 [2]广东省中医院芳村分院神经内科,广东广州510370

出　　处：《中国医药导报》2019年第20期29-33,共5页China Medical Herald

基　　金：国家自然科学基金面上项目(81873358、81373712)

摘　　要：帕金森病(PD)是发病率仅次于阿尔茨海默病的第二大神经系统退行性病变。当前治疗PD的主要途径仍然是左旋多巴治疗,然而长期服用左旋多巴会导致一系列副作用,如运动障碍、疗效减退、“开-关”现象和剂末效应等。儿茶酚-O-甲基转移酶(COMT)抑制剂能抑制周围左旋多巴的代谢,增加左旋多巴的传输量,从而用于左旋多巴附加疗法,用来增强左旋多巴疗效。作为一种新的三代COMT抑制剂,Opicapone能用于左旋多巴附加疗法中,用来改善波动效应和剂末现象。Opicapone在体内具有长时间的持续活性,当前建议剂量是每天睡前口服50mg。Opicapone诱导的COMT抑制剂的半衰期较前两代Opicapone抑制剂更长,且能显著升高左旋多巴全身性暴露,具有更有效、更安全、更持久的特性。Parkinson′s disease (PD) is the second most common neurodegenerative disease after Alzheimer′s disease.At present,the main way to treat PD is still Levodopa therapy.However,long-term use of Levodopa can lead to a series of side effects,such as dyskinesia,decreased efficacy,"on-off" phenomena,end of dose phenomena,and soon.The catechol-O-methyltransferase (COMT) inhibitor can inhibit the metabolism of surrounding Levodopa and increase the transmission amount of Levodopa,so it is used in Levodopa additional therapy to enhance the efficacy of Levodopa.As a new third-generation COMT inhibitor,Opicapone can be used in Levodopa addition therapy to improve the motor fluctuations and end of dose phenomena.Opicapone has sustained activity in vivo for a long time.The current recommended dose is 50 mg per day taken orally before bedtime.The half-life of opicapone-induced COMT inhibitors is longer than that of the previous two generations of Opicapone inhibitors,and can significantly increase Levodopa systemic exposure,with more effective,safer and more lasting properties.

关 键 词：帕金森病 Opicapone 左旋多巴 儿茶酚氧位甲基转移酶抑制剂 

分 类 号：R742.5[医药卫生—神经病学与精神病学]