COMT inhibition
COMT inhibition
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COMT抑制
DOI：
10.1212/wnl.50.5_suppl_5.s3
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发表时间：
1998
期刊：
影响因子：
9.9
通讯作者：
C. Adler
中科院分区：
文献类型：
--
作者：
M. Kurth;C. Adler
在帕金森病的初始阶段，左旋多巴加脱羧酶抑制剂（卡比多巴或苄丝肼）治疗可充分控制症状。然而，随着疾病的进展，对治疗的临床反应经常开始波动，变得越来越与左旋多巴的血浆浓度波动相关-“磨损”现象。许多策略都试图增加左旋多巴及其活性代谢物的可用性，从而减少这些反应的波动，并取得了不同程度的成功。本文综述了新的儿茶酚O-甲基转移酶（COMT）抑制剂托卡朋和恩他卡朋作为左旋多巴治疗药物的作用。这些药物通过延长左旋多巴的半衰期有效且安全地增加可进入大脑的左旋多巴量，从而使血浆中的水平更稳定并延长“作用”时间。
During the initial stages of Parkinson's disease, treatment with levodopa plus a decarboxylase inhibitor (carbidopa or benserazide) provides adequate control of symptoms. However, as the disease progresses, the clinical response to treatment often begins to fluctuate, becoming increasingly correlated with fluctuations in plasma concentrations of levodopa-the"wearing-off" phenomenon. Many strategies have attempted, with various degrees of success, to increase the availability of levodopa and its active metabolites, thus reducing these fluctuations in response. This review focuses on the role of the new catechol O-methyltransferase (COMT) inhibitors tolcapone and entacapone as adjuncts to levodopa therapy. These agents act effectively and safely to increase the amount of levodopa that is available to enter the brain by extending the half-life of levodopa, resulting in more stable levels in the plasma and prolonging "on" time.