Gold Preparations

Information about Gold Preparations

Gold salts, including auranofin and gold sodium thiomalate, have been used for the therapy of rheumatoid arthritis for many decades, but have recently been replaced by more modern disease-modifying antirheumatic drugs.

Liver toxicity of Gold Preparations

Parenteral gold therapy (chrysotherapy) can cause acute, clinically apparent hepatitis that is usually cholestatic and self-limited in nature, but can be severe and even fatal. In contrast, oral gold preparations (such as auranofin) are associated with a low rate of serum enzyme elevations during, treatment but have not been convincingly linked to clinically apparent liver injury.

Mechanism of action of Gold Preparations

Gold given as a conjugate with thioglucose, thiosulphate or thiomalate salt has disease modifying activity in rheumatoid arthritis and can induce remission in up to 50% of patients. The mechanism of action is not well defined, but gold has clear antiinflammatory activity and lowers serum immunoglobulin levels. The use of gold as an antiinflammatory agent arose out of observations by Robert Koch who reported that gold salts had in vitro activity against mycobacterium tuberculosis. Trials of gold therapy in tuberculosis were unsuccessful, but clinically apparent antiinflammatory activity was found during treatment of patients with discoid lupus erythematosus, which at that time was believed to be due to tuberculosis.

History of Gold Preparations

Chrysotherapy was introduced in the treatment of rheumatoid arthritis in the 1930s and it became a common approach to management of severe rheumatoid arthritis until the 1960s, when it was gradually replaced by more modern forms of disease modifying antirheumatic drugs (DMARDs) such as methotrexate, leflunomide, d-penicillamine, hydroxychloroquine, sulfasalazine, enteracept and imfliximab. Previous formulations of gold salts included a parenteral form as gold sodium thiomalate which was available as 50 mg/mL under brand names including Aurolate and Myochrysine (now no longer generally available in the United States).

Dosage and administration for Gold Preparations

The recommended dose was 10 mg intramuscularly once weekly, gradually increasing to a maintenance dose of 25 to 50 mg weekly or every other week. An oral form of gold, audafolin (aw ran' o fin), continues to be available as capsules of 3 mg under the brand name of Ridaura, the recommended dose of which is 3 to 9 mg daily. Therapy with gold salts is often limited by toxicity, some of which is cumulative. The effect may take weeks to months to occur, but therapy should be discontinued after an accumulative dose of 1 gram if beneficial results are not achieved. Common side effects include abdominal discomfort, nausea, pruritus, skin rash, urticaria and proteinuria. Fatal instances of hypersensitivity reactions, renal dysfunction and bone marrow suppression have been reported.

antirheumatic agents

• gold preparations
  • auranofin, gold salts, gold sodium thiomalate

• interleukin receptor antagonists
  • anakinra, canakinumab, rilonacept, sarilumab, tocilizumab

• major immunosuppressive agents (also used in transplant medicine)
  • cyclosporine, mycophenylate, sirolimus, tacrolimus

• monoclonal antibodies
  • adalimumab, canakinumab, certolizumab, golimumab, infliximab, rituximab, sarilumab, tocilizumab, ustekinumab

• thiopurines
  • azathioprine, mercaptopurine, thioguanine

• tumor necrosis factor antagonists
  • adalimumab, certolizumab, etanercept, golimumab, infliximab

• tyrosine (janus) kinase inhibitors
  • baricitinib, tofacitinib

• miscellaneous
  • abatacept, flavocoxid, hydroxychloroquine, leflunomide, methotrexate, penicillamine

• Dailymed label info on Gold Preparations
• FDA Gold Preparations