Department of Neurology, Innsbruck Medical University, Anichstraße 35, A-6020 Innsbruck, Austria.
Expert Rev Neurother. 2011 Sep;11(9):1229-34. doi: 10.1586/ern.11.122.
Pramipexole extended release (ER) is a new once-daily formulation of pramipexole, a nonergot dopamine agonist, which is available in five dosage strengths: 0.26 (0.375) mg, 0.52 (0.75) mg, 1.05 (1.5) mg, 2.1 (3) mg and 3.15 (4.5) mg (all doses are expressed in terms of pramipexole base and the corresponding dose strengths of pramipexole salt are given in brackets). Pramipexole ER is currently approved as monotherapy in early Parkinson's disease (PD), as well as an adjunct therapy to levodopa in advanced PD. Compared with the immediate release (IR) formulation, the ER formulation offers several advantages, including the potential for improved compliance owing to its simple once-daily dosing regimen and steadier plasma levels over 24 h. Double-blind, randomized, placebo and active comparator controlled trials in early, as well as advanced PD, established the superiority of both pramipexole ER and IR over placebo. The overnight switch from pramipexole IR three times a day to ER once-daily in early PD has been shown to be successful in more than 80% of patients. Pramipexole ER is well tolerated, with a similar adverse event profile to pramipexole IR. The aim of this article is to provide a short review of the most relevant pharmacological and clinical data on pramipexole ER.
普拉克索延长释放(ER)是一种新的每日一次的普拉克索配方,是一种非麦角多巴胺激动剂,有五种剂量强度:0.26(0.375)mg、0.52(0.75)mg、1.05(1.5)mg、2.1(3)mg 和 3.15(4.5)mg(所有剂量均以普拉克索碱表示,相应的普拉克索盐剂量强度用括号表示)。普拉克索 ER 目前被批准用于早期帕金森病(PD)的单药治疗,以及晚期 PD 中与左旋多巴的辅助治疗。与即时释放(IR)制剂相比,ER 制剂具有几个优势,包括由于其简单的每日一次给药方案和 24 小时内更稳定的血浆水平,潜在的改善依从性。在早期和晚期 PD 中进行的双盲、随机、安慰剂和活性对照试验证实了普拉克索 ER 和 IR 优于安慰剂。在早期 PD 中,将普拉克索 IR 每日三次转换为 ER 每日一次的夜间转换,在超过 80%的患者中取得了成功。普拉克索 ER 耐受性良好,与普拉克索 IR 的不良反应谱相似。本文的目的是提供普拉克索 ER 的最相关药理学和临床数据的简要回顾。