Leflunomide:回顾它的使用在活跃的风湿性关节炎。

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普拉卡什,贾维斯B

Leflunomide:回顾它的使用在活跃的风湿性关节炎。

药。1999年12月,58 (6):1137 - 64。

PubMed ID

10651393 (在PubMed

]

文摘

A77 1726年leflunomide的活性代谢物,是一种免疫调制剂在激活淋巴细胞抑制细胞增殖活跃的风湿性关节炎患者。因为A77 1726半衰期很长(约2周),治疗口腔leflunomide启动负荷剂量为100毫克每日一次,3天,持续20毫克每日一次。结果的大型随机、双盲、多中心试验的24个月的时间显示,leflunomide显著优于安慰剂,至少柳氮磺胺吡啶一样有效的改善主要结果的措施,如温柔的接头数量、关节肿胀数和医生和病人的全球评估,在成年患者积极的风湿性关节炎。而改善所有主要结果措施与leflunomide类似与甲氨蝶呤或明显低于12个月后,两个代理的功效相似后24个月。leflunomide出现早期的治疗效果比柳氮磺胺吡啶(4周)或甲氨蝶呤,从基线值和减少功能障碍与leflunomide明显大于与柳氮磺胺吡啶、甲氨蝶呤在端点或安慰剂。Leflunomide和柳氮磺胺吡啶或甲氨蝶呤至少有效延缓疾病的放射学进展率。最常见的不良事件报告的病人接受leflunomide随机双盲、安慰剂对照试验是腹泻(27%)、呼吸道感染(21%)、呕吐(13%)、头痛(13%)、皮疹(12%),增加血清肝转氨酶(10%)、消化不良(10%)和脱发(9%)。Leflunomide耐受性良好,柳氮磺胺吡啶或甲氨蝶呤在临床试验中。监测血清肝酶水平建议病人接受leflunomide等等。毒品不建议女性患者或可能怀孕。 Drug treatment should be discontinued, and hastened drug elimination procedure should be considered, in male patients wishing to father a child. 16 potential cases of pancytopenia and 9 cases of serious skin reactions have been associated with the use of leflunomide in 76,000 patients to date. CONCLUSIONS: Leflunomide is a disease-modifying antirheumatic drug which reduces the signs and symptoms of inflammatory arthritis and delays the radiological progression of disease in adult patients with active rheumatoid arthritis. The drug appears to be as effective and as well tolerated as sulfasalazine or methotrexate, and represents a suitable alternative to these agents in adult patients with active rheumatoid arthritis. Benefits with leflunomide are evident within 4 weeks and efficacy is maintained for durations of up to 24 months.

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药物靶点

药物	目标	类	生物	药理作用	行动
Leflunomide	Dihydroorotate脱氢酶(醌),线粒体	蛋白质	人类	是的	抑制剂	细节