摘要
目的评价抗帕金森病(Parkinson's disease,PD)新药沙芬酰胺的作用机制、药动学行为、临床试验及安全性等,为临床用药提供参考。方法查阅相关文献30篇。结果与结论沙芬酰胺是一种α-氨基酰胺衍生物,既可抑制多巴胺的再摄取,又可高效、选择性和可逆性地抑制单胺氧化酶-B的活性。此外,沙芬酰胺还是谷氨酸释放抑制剂,具有钠离子通道阻滞作用和钙离子通道调节作用。临床用于突发性帕金森成年患者的辅助治疗,在中期至晚期波动患者中,单独或与其他帕金森药物联合使用可以稳定左旋多巴的剂量。其应用前景良好。
Objective To evaluate the mechanism, pharmacokinetic behavior, clinical trials and safety of safinamide to provide reference for the treatment of Parkinson' s disease (PD) in clinic. Methods Thirty related literatures were reviewed. Results and Conclusion Safinamide is an alpha-aminoamide derivative, which can inhibit the uptake of dopamine. It is a very potent, highly selective and reversible monoamine oxidase-B (MAO-B)inhibitor. Furthermore, safinamide can also act as a glutamate release inhibitor, a sodium channel antagonist and calcium channel regulator. Safinamide has been used as an add-on therapy for the treatment of adult patients with a sudden onset of PD. Safinamide can attenuate the dose fluctuant of levodopa for mid-to late-stage PD patients, when levodopa is used alone or combined with other drugs for PD treatment. Safinamide has good application prospects for PD treatment.
出处
《沈阳药科大学学报》
CAS
CSCD
北大核心
2016年第9期754-758,共5页
Journal of Shenyang Pharmaceutical University
基金
国家科技部"十二五"重大新药创制专项(2013ZXD9402103)