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首页> 外文期刊>Journal of neural transmission >Pharmacokinetic behaviour of levodopa and 3-O-methyldopa after repeat administration of levodopa/carbidopa with and without entacapone in patients with Parkinson's disease.
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Pharmacokinetic behaviour of levodopa and 3-O-methyldopa after repeat administration of levodopa/carbidopa with and without entacapone in patients with Parkinson's disease.

机译：在帕金森氏病患者中，反复使用左旋多巴/卡比多巴联合和不联合entacapone后，左旋多巴和3-O-甲基多巴的药代动力学行为。

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摘要

Addition of the catechol-O-methyltransferase (COMT) inhibitor entacapone (EN) prolongs plasma metabolism of levodopa (LD). Objectives were to determine the clinical response after EN addition and the plasma degradation of LD and 3-O-methyldopa [3-OMD]. Not optimum treated hospitalised patients with Parkinson's disease received the same LD dosage on the first day only with carbidopa (CD) and on the second day with CD and EN (t.i.d.) within a standardised setting. We scored motor symptoms and measured LD- and 3-OMD levels on both days at fixed moments. Motor impairment significant better improved probably due to significant higher maximum concentrations [C(max)] and computed area under the curve values of LD levels during the LD/CD/EN condition. Time to C(max) of LD was significantly delayed after the first two LD/CD/EN intakes. An impact of EN on 3-OMD levels appeared. A possibly augmented LD absorption and a prolonged LD metabolism after EN supplementation may contribute to a more continuous LD delivery to the brain.
机译：儿茶酚-O-甲基转移酶（COMT）抑制剂entacapone（EN）的添加延长了左旋多巴（LD）的血浆代谢。目的是确定添加EN后的临床反应以及LD和3-O-甲基多巴[3-OMD]的血浆降解。未经过最佳治疗的帕金森氏病住院患者在第一天仅在标准环境中使用卡比多巴（CD）接受了相同的LD剂量，第二天接受CD和EN（t.i.d.）我们在固定的两天对运动症状评分并测量了LD-和3-OMD水平。在LD / CD / EN条件下，最大的最高浓度[C（max）]和LD水平曲线值下的计算面积明显较高，可以明显改善运动障碍。前两个LD / CD / EN摄入后，达到LD C（max）的时间明显延迟。出现了EN对3-OMD水平的影响。补充EN后，可能会增加LD的吸收并延长LD的代谢，可能有助于LD向大脑的递送更加连续。

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