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长效和缓释多巴胺受体激动剂:罗匹尼罗缓释研究综述。

Long half-life and prolonged-release dopamine receptor agonists: a review of ropinirole prolonged-release studies.

机构信息

Department of Oncology and Neurosciences, University G. d'Annunzio, Chieti-Pescara, Italy.

出版信息

Parkinsonism Relat Disord. 2009 Dec;15 Suppl 4:S85-92. doi: 10.1016/S1353-8020(09)70842-9.

Abstract

Our review summarizes the five main studies conducted to evaluate the efficacy and pharmacokinetics of ropinirole prolonged release (PR) in Parkinson's disease (PD). The PR formulation was developed with Geomatrix coating technology in order to obtain constant pharmacokinetics throughout 24 hours. The areas under the curve were not significantly different from those observed with similar doses of ropinirole immediate-release (IR) formulation, administered 3 times a day, but concentration fluctuations were less for ropinirole PR (2-fold vs 5-fold). The efficacy study of the PR versus IR formulations showed non-inferiority of the PR formulation, similar tolerability and feasibility of overnight switches, and indicated that the optimal doses of ropinirole in patients with de novo PD is in the range of 8-12 mg/day. The efficacy study in PD patients with motor fluctuations treated with L-dopa showed that adding ropinirole PR significantly reduced "off" time and increased "on" time in comparison with placebo. The study with ropinirole as an add-on to L-dopa showed a reduced incidence of dyskinesias.

摘要

我们的综述总结了五项主要研究,旨在评估罗匹尼罗控释(PR)治疗帕金森病(PD)的疗效和药代动力学。PR 制剂采用 Geomatrix 包衣技术,以实现 24 小时内的稳定药代动力学。曲线下面积与每天 3 次给予类似剂量的罗匹尼罗速释(IR)制剂观察到的结果无显著差异,但 PR 制剂的浓度波动更小(2 倍 vs 5 倍)。PR 与 IR 制剂的疗效研究表明 PR 制剂具有非劣效性,相似的耐受性和夜间转换的可行性,并表明新诊断为 PD 的患者中罗匹尼罗的最佳剂量范围为 8-12mg/天。在接受左旋多巴治疗的伴有运动波动的 PD 患者中进行的疗效研究表明,与安慰剂相比,添加 PR 制剂显著减少了“关”期并增加了“开”期时间。与左旋多巴联合应用罗匹尼罗的研究显示,异动症的发生率降低。

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