Department of Neurology, Weill Medical College of Cornell University New York, USA.
Neuropsychiatr Dis Treat. 2008 Feb;4(1):23-32.
Rasagiline (N-propargyl-1 (R)-aminoindan) is a novel propargylamine, irreversible, selective monoamine oxidase inhibitor for treatment of Parkinson's disease (PD), a progressive condition associated with degeneration of dopaminergic neurons in the substantia nigra. Rasagiline inhibits striatal dopamine metabolism, thereby providing relief from motor symptoms of PD. It may be dosed once daily and, unlike selegiline, it is metabolized to non-amphetamine compounds. In a large clinical trial, rasagiline has proved effective, safe, and well tolerated in early PD as monotherapy. In two phase III clinical trials in advanced PD with motor fluctuations, rasagiline as an adjunct to levodopa significantly decreases "off" time. In animal models of PD, data supports a neuroprotective effect of rasagiline, and its active metabolite aminoindan. Analysis of delayed-start clinical trial suggests the potential for disease modification, and further trials are examining this effect.
雷沙吉兰(N-丙炔基-1(R)-氨基茚满)是一种新型的丙炔胺,是非麦角类、不可逆、选择性单胺氧化酶抑制剂,用于治疗帕金森病(PD),这是一种与黑质多巴胺能神经元变性相关的进行性疾病。雷沙吉兰抑制纹状体多巴胺代谢,从而缓解 PD 的运动症状。它可以每天服用一次,与司来吉兰不同,它代谢为非安非他命化合物。在一项大型临床试验中,雷沙吉兰在早期 PD 的单药治疗中已被证明是有效、安全且耐受良好的。在两项伴有运动波动的晚期 PD 的 III 期临床试验中,雷沙吉兰作为左旋多巴的辅助治疗可显著减少“关期”。在 PD 的动物模型中,数据支持雷沙吉兰及其活性代谢物氨基茚满具有神经保护作用。延迟启动临床试验的分析提示其具有疾病修饰作用,进一步的试验正在研究这种作用。