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目的研究儿茶酚－氧位－甲基转移酶抑制剂（ＣＯＭＴＩ）托卡朋对帕金森病（ＰＤ）患者在复方左旋多巴治疗过程中出现的运动功能波动，如开－关现象、剂末现象、疗效减退、左旋多巴用量减少情况，并观察不良反应。方法对６９例ＰＤ患者采用多中心自身对照开放方法进行临床观察。应用复方左旋多巴剂量稳定６周后，对符合入选条件者给予托卡朋５０～１００ｍｇ每天３次，１疗程为６周，总的临床观察时间为１２周。结果托卡朋治疗前改良Ｗｅｂｓｔｅｒ评分为（１４．６４±４．４３）分，治疗后为（９．７１±４．０３）分，平均分数减少了３３．２％（Ｐ＜０．０１）。６９例中，显效１０例（１４．５％），进步４３例（６２．３％），稍有进步１５例（２１．７％），无效１例（１．５％）；总有效率为９８．５％。有开－关现象的２２例中，从患者日记统计，托卡朋治疗后“开”期从（６．２３±２．８０）小时延长至（９．００±３．３５）小时（Ｐ＜０．０１）。６９例中，有８例左旋多巴剂量在治疗后较治疗前减少３４．６％。６９例患者中３４例出现不同类型的轻度不良反应，随治疗进行可自行缓解。结论托卡朋是治疗使用复方左旋多巴时出现的运动功能波动，如开－关现象、剂末现象和疗效减退者的有效药?
OBJECTIVE: To investigate the motor function fluctuations during the treatment of compound levodopa in patients with Parkinson’s disease (PD), such as the on-off phenomenon, and the effects of COMTI toxapram The end phenomenon, curative effect decreased, levodopa dose reduction, and observed adverse reactions. Methods A total of 69 patients with PD were treated with a multi-center self-control open method. Application of compound levodopa dosage stable 6 weeks, eligible for inclusion were given tokapene 50 ~ 100mg three times a day, a course of 6 weeks, the total clinical observation time was 12 weeks. Results The modified Webster score was (14.64 ± 4.43) before treatment and (9.71 ± 4.03) after treatment, with a mean reduction of 33.2% (P <0.01) . Of the 69 cases, 10 (14.5%) were markedly effective, 43 (62.3%) were advanced, 15 (21.7%) were slightly improved and 1 (1.5%) were ineffective. The total effective rate 98.5%. In the 22 patients with on-off status, from the patient’s diary statistics, the “on” phase after tokapene treatment prolonged from (6.23 ± 2.80) hours to (9.00 ± 3.35) hours (P < 0.01). Of the 69 patients, 8 received levodopa dose reduction of 34.6% after treatment. In 69 patients, 34 patients showed different types of mild adverse reactions, with the treatment can be self-remission. Conclusion Tokapen is an effective drug for the treatment of fluctuations in motor function when used with compound levodopa, such as the on-off phenomenon, end-point symptoms, and hypogonadism.