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甲磺酸沙芬酰胺治疗中晚期帕金森病的药代动力学药物评价。

Pharmacokinetic drug evaluation of safinamide mesylate for the treatment of mid-to-late stage Parkinson's disease.

机构信息

a Department of Neurology , St. Joseph Hospital Berlin-Weißensee , Berlin , Germany.

出版信息

Expert Opin Drug Metab Toxicol. 2017 Jun;13(6):693-699. doi: 10.1080/17425255.2017.1329418.

DOI:10.1080/17425255.2017.1329418
PMID:28537214
Abstract

Patients with Parkinson's disease suffer from a heterogeneous expression of neurotransmitter deficits. They cause an individual variable expression of motor and non-motor symptoms. Thus, drugs with various mechanisms of actions are suitable to counteract these disease related neurotransmitter alterations. Areas covered: This invited review suggests safinamide as an ideal compound for therapy of Parkinson's disease, as its pharmacological profile includes reversible monoamine oxidase B inhibition, blockage of voltage-dependent sodium channels, modulation of calcium channels and abnormal glutamate release. Safinamide may provide benefits effects on non-motor symptoms in addition to the demonstrated amelioration of motor impairment in levodopa treated patients with Parkinson's disease. Safinamide was well tolerated and safe when administered in dose of 50 or 100 mg daily in pivotal trials. Expert opinion: Clinical handling, safety and tolerability of Safinamide are better than of dopamine agonists or levodopa. Safinamide supplements the existing armamentarium of drugs for Parkinson's disease. Safinamide will help to reduce dosing of levodopa but also of dopamine agonists during long term treatment in patients with Parkinson's disease.

摘要

帕金森病患者表现出神经递质缺失的异质性。这些缺失导致运动和非运动症状的个体差异表达。因此,具有不同作用机制的药物适合对抗这些与疾病相关的神经递质改变。 涵盖领域:这篇特邀综述认为,氨磺必利是治疗帕金森病的理想化合物,因为其药理学特性包括可逆性单胺氧化酶 B 抑制、阻断电压依赖性钠通道、钙通道调节和异常谷氨酸释放。氨磺必利除了对接受左旋多巴治疗的帕金森病患者的运动障碍有改善作用外,可能对非运动症状也有疗效。氨磺必利在关键性试验中每天以 50 或 100mg 的剂量给药,具有良好的耐受性和安全性。 专家意见:氨磺必利在临床处理、安全性和耐受性方面优于多巴胺激动剂或左旋多巴。氨磺必利为帕金森病的现有药物治疗手段提供了补充。氨磺必利将有助于减少帕金森病患者长期治疗中左旋多巴和多巴胺激动剂的剂量。

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