Life and Health Sciences Research Institute (ICVS), School of Medicine, University of Minho, Braga, Portugal; ICVS/3Bs - PT Government Associate Laboratory, Braga/Guimarães, Portugal.
Life and Health Sciences Research Institute (ICVS), School of Medicine, University of Minho, Braga, Portugal; ICVS/3Bs - PT Government Associate Laboratory, Braga/Guimarães, Portugal; Neurology Department, Hospital da Senhora da Oliveira, EPE, Guimarães, Portugal.
Drug Discov Today. 2018 Mar;23(3):736-744. doi: 10.1016/j.drudis.2018.01.033. Epub 2018 Jan 12.
The loss of dopaminergic neurons (DAn) and reduced dopamine (DA) production underlies the reasoning behind the gold standard treatment for Parkinson's disease (PD) using levodopa (L-DOPA). Recently licensed by the European Medicine Agency (EMA) and US Food and Drug Administration (FDA), safinamide [a monoamine oxidase B (MOA-B) inhibitor] is an alternative to L-DOPA; as we discuss here, it enhances dopaminergic transmission with decreased secondary effects compared with L-DOPA. In addition, nondopaminergic actions (neuroprotective effects) have been reported, with safinamide inhibiting glutamate release and sodium/calcium channels, reducing the excitotoxic input to dopaminergic neuronal death. Effects of safinamide have been correlated with the amelioration of non-motor symptoms (NMS), although these remain under discussion. Overall, safinamide can be considered to have potential antidyskinetic and neuroprotective effects and future trials and/or studies should be performed to provide further evidence for its potential as an anti-PD drug.
多巴胺能神经元（DAn）的丧失和多巴胺（DA）产生减少是左旋多巴（L-DOPA）作为治疗帕金森病（PD）的金标准背后的推理依据。 safinamide [一种单胺氧化酶 B（MOA-B）抑制剂] 最近获得了欧洲药品管理局（EMA）和美国食品和药物管理局（FDA）的许可，是 L-DOPA 的替代品；正如我们在这里讨论的那样，与 L-DOPA 相比，它增强了多巴胺能传递，而次级副作用却降低了。此外，还报道了非多巴胺能作用（神经保护作用），safinamide 抑制谷氨酸释放和钠/钙通道，减少对多巴胺能神经元死亡的兴奋性毒性输入。 safinamide 的作用与改善非运动症状（NMS）相关，尽管这些仍在讨论中。总体而言，safinamide 可以被认为具有潜在的抗运动障碍和神经保护作用，未来的试验和/或研究应该进行，以提供更多证据证明其作为抗 PD 药物的潜力。
