Departments of Clinical Pharmacology and Neurosciences, University Hospital and University of Toulouse, France and INSERM CIC-9023 and UMR-825, Toulouse, France; Department of Clinical Pharmacology, Faculty of Medicine, 37 Allées Jules Guesde, 31000, Toulouse, France.
Expert Rev Neurother. 2011 Jul;11(7):925-35. doi: 10.1586/ern.11.75.
Pramipexole is a nonergolinic dopamine agonist, with high affinity for the D2 subfamily of dopamine receptors. Pramipexole is efficacious for the symptomatic treatment of early Parkinson's Disease (PD) and its early use, before that of levodopa can delay the emergence of levodopa-related motor complication. Dosage should be increased gradually from a starting dose of 0.375 mg/day up to a maximum of 4.5 mg/day in equally divided doses taken three times per day with pramipexole immediate-release or equivalent daily dosages once-daily with pramipexole extended-release. Pramipexole can also improve depressive symptoms and possibly health-related quality of life in PD. Nonetheless, its use is not devoid of tolerability problems. While peripheral adverse drug reactions, such as nausea, vomiting or orthostatic hypotension, can be effectively treated and usually pose few problems to most patients, neuropsychiatric events can seriously limit the use of pramipexole in some cases. Indeed, excessive daytime somnolence, impulse-control disorders, hallucinations or delusions can severely affect patients, causing important personal or social handicap. Patients should be informed about the risk of such neuropsychiatric complications and their presence should be actively detected at each consultation. More effort will have to be put into further studying the risk-benefit ratio of pramipexole and other dopamine agonists in the treatment of early PD.
普拉克索是一种非麦角类多巴胺激动剂，对多巴胺 D2 亚家族受体具有高亲和力。普拉克索对早期帕金森病（PD）的症状治疗有效，其早期使用可以延迟左旋多巴相关运动并发症的出现。剂量应从起始剂量 0.375mg/天逐渐增加，每日 3 次，分剂量服用，普拉克索速释或等效每日剂量每日 1 次服用普拉克索缓释。普拉克索还可以改善 PD 患者的抑郁症状并可能改善其健康相关生活质量。然而，其使用并非没有耐受性问题。虽然外周不良反应，如恶心、呕吐或体位性低血压，可以有效治疗，通常对大多数患者没有什么问题，但神经精神事件在某些情况下可能严重限制普拉克索的使用。事实上，白天过度嗜睡、冲动控制障碍、幻觉或妄想会严重影响患者，导致严重的个人或社会障碍。应告知患者存在此类神经精神并发症的风险，并在每次就诊时积极检测。需要进一步努力研究普拉克索和其他多巴胺激动剂在早期 PD 治疗中的风险-效益比。
