rasagiline的综合复习,第二代单胺氧化酶抑制剂,用于治疗帕金森病。

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斯沃普DM,陈JJ Dashtipour K

rasagiline的综合复习,第二代单胺氧化酶抑制剂,用于治疗帕金森病。

其他。2007年9月,29 (9):1825 - 49。

PubMed ID

18035186 (在PubMed

]

文摘

背景:单胺氧化酶抑制剂(毛)和对毛泽东的选择性和特异性B型(缺氧)延长的作用持续时间内生和体内多巴胺。Rasagiline [N-propargyl-l (R) -aminoindan)是第二代propargylamine药效基因选择性和不可逆抑制大脑缺氧,是专门设计用于治疗帕金森病(PD)。摘要目的:本研究的目的是审查药理学,耐受性,rasagiline治疗PD的临床疗效。方法:MEDLINE(1966 - 2007年4月),Cochrane系统评价数据库,国际制药摘要(1970 - 2007年4月)寻找原始研究和评论文章发表在英语。搜索词单胺氧化酶,神经保护,帕金森病,propargylamine rasagiline,司立吉林。文章的参考书目也咨询了,因为被rasagiline制造商提供的信息。结果:63临床和实验室研究的数据进行了分析。基于这些研究结果,我们得出的结论是,rasagiline阿宝QD、治疗剂量范围的0.5到1破布/ d,完全是有效和耐受性良好,选择性,特别是抑制缺氧。药物,rasagiline被发现比司立吉林< = 10倍或更有效的和没有代谢安非他命衍生品。Rasagiline是有效的单一治疗在早期PD,推进PD患者的辅助治疗和运动波动。 As monotherapy, rasagiline provided modest yet clinically meaningful benefit. A randomized, double-blind, placebo-controlled study found that, after 26 weeks of treatment, the adjusted effect size for total Unified Parkinson's Disease Rating Scale score was -4.20 (95% CI, -5.66 to -2.73) for rasagiline 1 mg/d versus placebo (P < 0.001). Preliminary long-term data from an open-label study suggest a sustained therapeutic advantage when rasagiline is initiated early (before the need for dopaminergic agents) rather than later. In patients with more advanced disease who received treatment with dopaminergic agents, rasagiline and entacapone were associated with reductions of "off" time significantly greater than placebo (-1.18 and -1.2 vs 0.4 hour; both, P < or = 0.001). Rasagiline was well tolerated in younger (aged <;70 years) and older (aged > or =70 years) patients with early or advanced PD. Pharmacologically, rasagiline has the potential to augment the vasopressor effects of diet-derived tyramine (ie, the "cheese reaction"). However, clinical challenge studies of tyramine have found this unlikely to occur even with ingestion of supraphysiologic amounts of tyramine. In experimental models, rasagiline has been found to have neuroprotective properties that may be independent of MAO-B inhibition. CONCLUSIONS: Based on this review, rasagiline has been found to be well tolerated and effective in the treatment of early PD and as adjunctive treatment in motor fluctuations. Whether rasagiline is associated with clinically significant neuroprotection (ie, disease modification) in PD is the subject of ongoing clinical trials.

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药物

Rasagiline

药物靶点

药物	目标	类	生物	药理作用	行动
Rasagiline	胺氧化酶(flavin-containing) B	蛋白质	人类	是的	抑制剂	细节

药物酶

药物	酶	类	生物	药理作用	行动
Rasagiline	细胞色素P450 1 a2	蛋白质	人类	未知的	底物	细节