Boehringer Ingelheim Pharma GmbH & Co. KG, Pharmaceutical Development, 88397 Biberach, Germany.
Parkinsons Dis. 2010 Dec 19;2010:612619. doi: 10.4061/2010/612619.
Pramipexole, the most commonly prescribed dopamine agonist worldwide, meanwhile serves as a reference substance for evaluation of new drugs. Based on numerous clinical data and vast experiences, efficacy and safety profiles of this non-ergoline dopamine agonist are well characterized. Since October 2009, an extended-release formulation of pramipexole has been available for symptomatic treatment of Parkinson's disease. Pramipexole administration can be cut down from three times to once a day due to the newly developed extended-release formulation. This is considerable progress in regard to minimizing pill burden and enhancing compliance. Moreover, the 24 h continuous drug release of the once-daily extended-release formulation results in fewer fluctuations in plasma concentrations over time compared to immediate-release pramipexole, given three times daily. The present study summarizes pharmacokinetics and all essential pharmacological and clinical characteristics of the extended-release formulation. In addition, it provides all study data, available so far, with regard to transition and de-novo administration of extended-release formulation for patients with Parkinson's disease. It further compares efficacy and safety data of immediate-release pramipexole with the extended-release formulation of pramipexole.
普拉克索是世界范围内最常用的多巴胺激动剂，同时也是评估新药的参考物质。基于大量的临床数据和丰富的经验，这种非麦角类多巴胺激动剂的疗效和安全性特征得到了很好的描述。自 2009 年 10 月以来，一种普拉克索的缓释制剂已被用于治疗帕金森病的症状。由于新开发的缓释制剂，普拉克索的给药次数可以从每天三次减少到一次。这在减少药物负担和提高依从性方面取得了重大进展。此外，与每天三次给予的即时释放普拉克索相比，每天一次的缓释制剂可实现 24 小时持续药物释放，从而使血浆浓度随时间的波动减少。本研究总结了缓释制剂的药代动力学和所有重要的药理学和临床特征。此外，它还提供了迄今为止所有关于帕金森病患者转换和新开始使用缓释制剂的研究数据。它还比较了即刻释放普拉克索和普拉克索缓释制剂的疗效和安全性数据。
