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  • Title: Review of auranofin, an oral chrysotherapeutic agent.
    Author: Delafuente JC, Osborn TG.
    Journal: Clin Pharm; 1984; 3(2):121-7. PubMed ID: 6426843.
    Abstract:
    The chemistry, pharmacology, pharmacokinetics, clinical use and efficacy, adverse effects, and dosage of auranofin, an oral chrysotherapeutic agent used in treatment of rheumatoid arthritis, are reviewed. Auranofin is lipid-soluble and is monomeric in solution. It has a modulatory effect on both the humoral and cellular immune systems. Auranofin may be a condition-dependent immunoregulating agent rather than an immunosuppressive agent. It inhibits (1) monocyte-mediated antibody-dependent cellular toxicity, (2) release of enzymes from polymorphonuclear leukocytes that may contribute to the pathogenesis of rheumatoid arthritis, and (3) neutrophil activity. In patients with rheumatoid arthritis, 15-33% of an oral dose of auranofin 6 mg is absorbed. Peak plasma gold concentrations are achieved in one to two hours. Gold is highly protein bound. Elimination occurs through the feces and urine; 73-100% of auranofin gold is excreted. Plasma half-life is three weeks. Patients receiving auranofin 3 mg twice daily for rheumatoid arthritis reported improvement after five weeks of therapy; improvement has also been reported with lower doses. Diarrhea, rashes, and pruritus were the most common adverse effects. Auranofin is safe and effective for short- and long-term treatment of patients with rheumatoid arthritis. Its relative safety and potency compared with injectable gold salts and other drugs need further study.
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