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左旋多巴的药代动力学与药效学

Pharmacokinetics and pharmacodynamics of levodopa.

作者信息

Nutt John G

机构信息

Department of Neurology, Oregon Health & Science University, Parkinson Disease Research, Education and Clinical Center, Portland VA, Oregon, USA.

出版信息

Mov Disord. 2008;23 Suppl 3:S580-4. doi: 10.1002/mds.22037.

Abstract

The pharmacokinetics and pharmacodynamics of levodopa are dominated by two features: the short plasma half-life of the drug and the portion of the antiparkinsonian response that parallels the plasma levodopa levels, the so-called short-duration response. These features are the basis of motor fluctuations that complicate long-term therapy with levodopa. Motor fluctuations will predictably improve with measures that prolong the elevations of plasma levodopa or prolong the efficacy of dopamine synthesized from exogenous levodopa. Because dyskinesia is closely linked to the short-duration response and conceivably part of the short-duration response, it is less clear that dyskinesia will be improved by therapeutic strategies that reduce motor fluctuations.

摘要

左旋多巴的药代动力学和药效学主要由两个特点决定

药物的血浆半衰期短,以及抗帕金森病反应中与血浆左旋多巴水平平行的部分,即所谓的短期反应。这些特点是左旋多巴长期治疗中出现运动波动的基础。通过延长血浆左旋多巴升高时间或延长外源性左旋多巴合成多巴胺的疗效的措施,运动波动有望得到改善。由于异动症与短期反应密切相关,并且可以想象是短期反应的一部分,因此通过减少运动波动的治疗策略是否能改善异动症尚不清楚。

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