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金诺芬的作用机制、药理学、临床疗效及副作用。一种用于治疗类风湿性关节炎的口服有机金化合物。

Mechanism of action, pharmacology, clinical efficacy and side effects of auranofin. An orally administered organic gold compound for the treatment of rheumatoid arthritis.

作者信息

Furst D E

出版信息

Pharmacotherapy. 1983 Sep-Oct;3(5):284-98. doi: 10.1002/j.1875-9114.1983.tb03277.x.

Abstract

The mechanism of action of auranofin, an oral organic gold compound used in the treatment of rheumatoid arthritis, is probably similar to the previously available parenteral gold compounds. Auranofin affects polymorphonuclear cells and monocytes at lower concentrations than gold sodium thiomalate and generally affects humoral and cell-mediated immunity in the same direction as the latter drug. The pharmacokinetics of auranofin are different from the intramuscular gold compounds. Auranofin is 20-25% orally absorbed and has less total body retention, greater fecal excretion, and less urinary excretion than gold sodium thiomalate. This may be due in part to its differing chemistry, including its lipophilicity and monomeric structure (at least in vitro). While many clinical studies are not yet complete, auranofin (6 mg/day) is clearly more effective than placebo for treating rheumatoid arthritis. Its efficacy relative to gold sodium thiomalate is not clear. Auranofin may be slightly less effective than gold sodium thiomalate, but because it is generally less toxic than intramuscular gold compounds, its therapeutic index may be more favorable.

摘要

金诺芬是一种用于治疗类风湿性关节炎的口服有机金化合物,其作用机制可能与先前可用的肠胃外金化合物相似。与硫代苹果酸金钠相比,金诺芬在较低浓度下就能影响多形核细胞和单核细胞,并且通常与后一种药物一样,对体液免疫和细胞介导免疫产生相同方向的影响。金诺芬的药代动力学与肌肉注射用金化合物不同。金诺芬的口服吸收率为20%至25%,与硫代苹果酸金钠相比,其全身潴留较少,粪便排泄较多,尿液排泄较少。这可能部分归因于其不同的化学性质,包括其亲脂性和单体结构(至少在体外)。虽然许多临床研究尚未完成,但金诺芬(6毫克/天)在治疗类风湿性关节炎方面明显比安慰剂更有效。其相对于硫代苹果酸金钠的疗效尚不清楚。金诺芬的疗效可能略低于硫代苹果酸金钠,但由于它通常比肌肉注射用金化合物毒性更小,其治疗指数可能更有利。

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