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多巴胺激动剂、受体选择性与帕金森病中的异动症诱导

Dopamine agonists, receptor selectivity and dyskinesia induction in Parkinson's disease.

作者信息

Jenner Peter

机构信息

Neurodegenerative Diseases Research Centre, Guy's, King's, and St Thomas' School of Biomedical Sciences, King's College, London, UK.

出版信息

Curr Opin Neurol. 2003 Dec;16 Suppl 1:S3-7. doi: 10.1097/00019052-200312001-00002.

Abstract

Levodopa and the dopamine agonists are effective symptomatic treatments for Parkinson's disease, and all patients receive at least one of these agents during their illness. Long-term use of levodopa is commonly associated with motor complications such as dyskinesia, and both the dosing frequency and total daily dose of levodopa determine the rate of onset and severity. Dopamine agonists have gained popularity as first-line monotherapy in Parkinson's disease, as they effectively reverse motor deficits and reduce the risk of motor complications. Long-acting dopamine agonists providing continuous, rather than pulsatile, dopaminergic stimulation appear able to avoid dyskinesia induction. Current treatments act predominantly on D2 receptors, but drugs acting on both the D1 and D2 receptor families may produce an additive motor response, although this remains to be proven in patients with Parkinson's disease. Most currently used dopamine agonists are selective for D2-like receptors, with only pergolide and apomorphine potentially interacting with D1 receptor populations.

摘要

左旋多巴和多巴胺激动剂是治疗帕金森病有效的对症治疗药物,所有患者在患病期间至少会使用其中一种药物。长期使用左旋多巴通常会出现诸如运动障碍等运动并发症,左旋多巴的给药频率和每日总剂量决定了其起效速度和严重程度。多巴胺激动剂作为帕金森病的一线单药治疗已越来越普遍,因为它们能有效逆转运动功能缺损并降低运动并发症的风险。提供持续而非脉冲式多巴胺能刺激的长效多巴胺激动剂似乎能够避免诱发运动障碍。目前的治疗主要作用于D2受体,但作用于D1和D2受体家族的药物可能会产生叠加的运动反应,尽管这一点在帕金森病患者中仍有待证实。目前大多数使用的多巴胺激动剂对D2样受体具有选择性,只有培高利特和阿扑吗啡可能与D1受体群体相互作用。

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