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.