Antonini Angelo, Bernardi Laura, Calandrella Daniela, Mancini Francesca, Plebani Mauro
Department for Parkinson's disease, IRCCS San Camillo, Venice, Italy.
Funct Neurol. 2010 Jan-Mar;25(1):21-5.
Rotigotine (Neupro) is a non-ergolinic dopamine agonist available as a transdermal patch that can be applied once daily. To date, it is approved as monotherapy for the treatment of early Parkinson's disease (PD), and as adjunctive therapy to levodopa in the treatment of PD, including the advanced stage of the disease, when the efficacy of levodopa is reduced or becomes inconsistent and there are fluctuations in the therapeutic effect (end-dose, 'ON-OFF' phenomenon). The potential advantages of the rotigotine patch include immediacy of effect onset as intestinal absorption is not needed, constant drug delivery, and ease of use. This review provides an overview of several aspects of the use of the rotigotine transdermal patch, including the important issue of the management of sleep disorders in advanced PD patients, as well as the chemistry, preclinical and clinical pharmacology, efficacy, safety and tolerability of the drug. Furthermore, the rationale for the treatment of PD with the rotigotine transdermal patch is discussed, focusing in particular on the related sleep disorders.
罗替戈汀(Neupro)是一种非麦角林类多巴胺激动剂,有透皮贴剂剂型,每日只需给药一次。迄今为止,它已被批准用于早期帕金森病(PD)的单药治疗,以及在PD治疗中作为左旋多巴的辅助治疗,包括疾病晚期,此时左旋多巴疗效降低或变得不稳定,且治疗效果出现波动(终末剂量、“开-关”现象)。罗替戈汀贴剂的潜在优势包括起效迅速(无需肠道吸收)、药物持续释放以及使用方便。本综述概述了罗替戈汀透皮贴剂使用的几个方面,包括晚期PD患者睡眠障碍管理这一重要问题,以及该药物的化学性质、临床前和临床药理学、疗效、安全性和耐受性。此外,还讨论了使用罗替戈汀透皮贴剂治疗PD的理论依据,尤其关注相关的睡眠障碍。