Adjuvant therapies for Parkinson's disease: critical evaluation of safinamide.
Adjuvant therapies for Parkinson's disease: critical evaluation of safinamide.
复制标题
DOI：
10.2147/dddt.s77749
复制
发表时间：
2016
期刊：
影响因子：
--
通讯作者：
Torti M
中科院分区：
文献类型：
--
作者：
Stocchi F;Torti M
Safinamide（SAF）是一种治疗帕金森病（PD）的新药。它是一种苄氨基衍生物，具有多种作用机制和抗帕金森病、抗惊厥和神经保护特性。SAF抑制单胺氧化酶B和多巴胺再摄取以及谷氨酸释放，阻断电压依赖性钠通道，并调节钙通道。虽然抗帕金森病作用部分归因于单胺氧化酶B的抑制，在50 mg剂量下完全抑制，但在100 mg剂量下观察到的增强获益可能是由于非多巴胺能机制。SAF将是早期和晚期PD患者的重要选择。在早期PD患者中，在多巴胺受体激动剂基础上添加SAF可能是改善运动功能、延长多巴胺受体激动剂使用时间和/或延迟左旋多巴引入的有效治疗策略。在晚期帕金森病患者中，SAF已被证明按时显著增加，没有或无麻烦的运动障碍。进行的所有研究都证明了其在早期和晚期PD患者中的短期和长期生活质量结局方面的疗效。SAF已在长期（24个月）、双盲、安慰剂对照研究中进行了研究，显示出非常好的安全性特征。SAF尚未在原发PD患者中进行研究，其对运动障碍的潜在积极作用值得进一步专门研究。
Safinamide (SAF) is a new drug developed for the treatment of Parkinson’s disease (PD). It is a benzylamino derivative with multiple mechanisms of action and antiparkinsonian, anticonvulsant, and neuroprotective properties. SAF inhibits monoamine oxidase B and dopamine reuptake and glutamate release, blocks voltage-dependent sodium channels, and modulates calcium channels. Although the antiparkinsonian effect can be ascribed in part to the inhibition of the monoamine oxidase B, which is complete at 50 mg, the enhanced benefit seen at the 100 mg dose is probably due to nondopaminergic mechanisms. SAF will represent an important option for patients with both early and advanced PD. In early PD patients, the addition of SAF to dopamine agonists may be an effective treatment strategy to improve motor function, prolong the use of dopamine agonists, and/or delay the introduction of levodopa. In advanced parkinsonian patients, SAF has been demonstrated to significantly increase on time with no, or nontroublesome dyskinesias. All studies performed have demonstrated its efficacy in benefiting both short-term and long-term quality-of-life outcomes in both early and advanced PD patients. SAF has been investigated in long-term (24 months), double-blind, placebo-controlled studies, where it showed a very good safety profile. SAF has not been studied in de novo PD patients, and its potential positive effect on dyskinesia deserves further dedicated studies.