title: Review of auranofin, an oral chrysotherapeutic agent.
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.
mesh_terms: D000917:Antibody Formation / Q000187:drug effects; D001172:Arthritis, Rheumatoid / Q000188:drug therapy*; D001310:Auranofin; D006051:Aurothioglucose / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D055598:Chemical Phenomena; D002621:Chemistry; D006046:Gold / Q000031:analogs & derivatives*; D006801:Humans; D007111:Immunity, Cellular / Q000187:drug effects; D007408:Intestinal Absorption; D007700:Kinetics; D010353:Patient Education as Topic; D014018:Tissue Distribution
chemical_list: D006051:Aurothioglucose; D001310:Auranofin; D006046:Gold