Department of Neurology, University of Szeged , H-6725 Szeged, Semmelweis u. 6 , Hungary.
Expert Opin Investig Drugs. 2014 May;23(5):729-42. doi: 10.1517/13543784.2014.897694. Epub 2014 Mar 21.
Parkinson's disease (PD) is a neurodegenerative disorder characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta. Non-dopaminergic neurotransmitter systems are also involved in its pathomechanism. The aim of the treatment is to improve the dopamine-deficient state and to alleviate the motor and the non-motor symptoms. Safinamide is an α-aminoamide derivative with a combined, dopaminergic and non-dopaminergic mode of action. Phase III clinical trials with safinamide, as add-on therapy to a dopamine agonist (DAA) and to levodopa (LD) in early and advanced stage PD, respectively, demonstrated an improvement of the motor symptoms.
The review discusses the pharmacokinetic and pharmacodynamic properties of safinamide and provides an overview of the clinical trials conducted with safinamide in PD. A literature search was made in PubMed for safinamide, safinamide pharmacokinetics, PD treatment and monoamine oxidase-B inhibitors, and in PubMed and on the ClinicalTrials.gov site for clinical trials with safinamide in PD.
The place of safinamide in the therapy of PD is yet to be determined. However, the authors believe that safinamide is a valuable drug in the treatment of PD treatment with favorable pharmacokinetic and side-effect profiles. Data so far suggest that it can be used beneficially as add-on therapy both to DAAs in early PD and to LD in the later stages of the disease.
帕金森病(PD)是一种神经退行性疾病,其特征是黑质致密部多巴胺能神经元丧失。非多巴胺能神经递质系统也参与其发病机制。治疗的目的是改善多巴胺缺乏状态,缓解运动和非运动症状。沙芬酰胺是一种α-氨基酰胺衍生物,具有联合的多巴胺能和非多巴胺能作用模式。沙芬酰胺的 III 期临床试验,作为添加疗法,分别用于早期和晚期 PD 的多巴胺激动剂(DAA)和左旋多巴(LD),结果显示运动症状得到改善。
本文综述了沙芬酰胺的药代动力学和药效学特性,并概述了沙芬酰胺在 PD 中的临床试验。在 PubMed 中对沙芬酰胺、沙芬酰胺药代动力学、PD 治疗和单胺氧化酶-B 抑制剂进行了文献检索,并在 PubMed 和 ClinicalTrials.gov 网站上对 PD 中的沙芬酰胺临床试验进行了检索。
沙芬酰胺在 PD 治疗中的地位尚未确定。然而,作者认为沙芬酰胺是一种有价值的药物,具有良好的药代动力学和副作用特征,可用于治疗 PD。迄今为止的数据表明,它可以作为添加疗法,对早期 PD 的 DAA 和疾病后期的 LD 均有益。