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多巴胺受体激动剂治疗早期或晚期帕金森病。

Dopamine receptor agonists for the treatment of early or advanced Parkinson's disease.

机构信息

Department of Clinical Pharmacology and Neurosciences, Hospital and University of Toulouse and INSERM CIC9023 and UMR 825, Toulouse, France.

出版信息

CNS Drugs. 2010 Nov;24(11):941-68. doi: 10.2165/11537810-000000000-00000.

Abstract

Dopamine receptor agonists are indicated for the symptomatic treatment of early, moderate or advanced Parkinson's disease as well as for the reduction of levodopa-related motor complications. Ergolinic dopamine agonists, such as bromocriptine or pergolide, were initially developed and marketed, and then non-ergolinic dopamine agonists, such as pramipexole and ropinirole, were introduced, reducing the risk of drug-induced fibrotic reactions. Once-daily, controlled-release oral and transdermal formulations have been developed aiming at providing more stable 24-hour plasma drug concentrations and more convenient administration. A disease-modifying effect of dopamine agonists has not been demonstrated clinically. As with any other drug, dopamine agonists can also cause adverse drug reactions, which can be related or unrelated to dopaminergic hyperactivation. Dopaminergic reactions include nausea, hallucinations, confusion and orthostatic hypotension, among others, which were readily identified in pre-marketing clinical trials. During post-marketing surveillance, important adverse reactions were identified, such as daytime somnolence, impulse-control disorders and heart valve fibrosis. Other issues, including the efficacy of dopamine agonists for the treatment of non-motor symptoms, remain under evaluation.

摘要

多巴胺受体激动剂适用于早期、中期或晚期帕金森病的症状治疗,以及减少与左旋多巴相关的运动并发症。最初开发和销售的是麦角类多巴胺激动剂,如溴隐亭或培高利特,随后推出了非麦角类多巴胺激动剂,如普拉克索和罗匹尼罗,从而降低了药物引起的纤维性反应的风险。为了提供更稳定的 24 小时血浆药物浓度和更方便的给药,已经开发了每日一次的控释口服和透皮制剂。多巴胺受体激动剂并没有显示出临床的疾病修饰作用。与任何其他药物一样,多巴胺受体激动剂也会引起不良反应,这些不良反应可能与多巴胺能过度激活有关,也可能无关。多巴胺能反应包括恶心、幻觉、意识混乱和体位性低血压等,这些反应在上市前的临床试验中很容易被识别。在上市后监测期间,发现了一些重要的不良反应,如白天嗜睡、冲动控制障碍和心脏瓣膜纤维化。其他问题,包括多巴胺受体激动剂治疗非运动症状的疗效,仍在评估中。

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