Leflunomide,一种新型的免疫调制剂用于治疗风湿性关节炎的活跃。

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Leflunomide,一种新型的免疫调制剂用于治疗风湿性关节炎的活跃。

其他。1999年11月,21(11):1837 - 52个;讨论1821年。

PubMed ID
10890256 (在PubMed
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文摘

类风湿性关节炎(RA)是一种慢性疾病影响了0.8%的人口。非甾体类抗炎药减轻风湿性关节炎的疼痛和炎症,改善流动性但不要减缓关节损伤的进展。疾病修饰治疗风湿病的药物(DMARDs)限制潜在的不可逆转的关节损伤,可能影响疾病进展。综述了最近批准DMARD leflunomide, isoxazole-based免疫调制剂。不像其他的DMARDs, leflunomide逮捕激活淋巴细胞的生长通过抑制酶dihydroorotate脱氢酶,尿苷一磷酸生产的一个关键环节。Leflunomide迅速代谢活跃的主要代谢物A77 1726年,负责药物的药理活性。Leflunomide产生抑制活动在RA动物模型。已经证明了其临床疗效对照试验。在两个跨国52周的研究和两个24周的研究中,所有leflunomide-treated患者接受一个初始负荷剂量100毫克的3天,随后20毫克/天。对风湿性关节炎的症状和体征的影响进行评估使用美国风湿病学院(ACR) 20响应者指数,温柔和关节肿胀数和分数,病人和医生的全球评估,和疼痛强度指数。 Erosions and joint-space narrowing were assessed by radiography. Compared with placebo, leflunomide significantly improved the signs and symptoms of RA (41%-64% improvement) by ACR 20 responder criteria (P < 0.001). Leflunomide, methotrexate, and sulfasalazine were equally effective in terms of symptom outcomes. In terms of retarding the progression of disease, leflunomide was significantly superior to placebo, with no consistent difference from methotrexate or sulfasalazine. In a trial using a combination of leflunomide and methotrexate therapy, 53% of patients were responders by ACR 20 criteria. Adverse effects in RA patients receiving leflunomide included diarrhea, elevated liver enzymes, alopecia, and rash. Additional adverse events occurring with a frequency >5% included allergic reaction, asthenia, abdominal pain, back pain, and hypertension, among others. Thus leflunomide may be used in selected RA patients (ie, those starting RA therapy for the first time or failing earlier DMARD therapy). However, the product labeling requires monthly monitoring of liver enzymes until stable concentrations are reached. Other labeled warnings include a risk of immunosuppression and an increased risk of fetal death or teratogenic effects in pregnant women. Methotrexate, which is also hepatotoxic, is usually the initial DMARD recommended for use in patients with aggressive RA.

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药物
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