Injectable Gold Compounds: An Overview

Abstract

Injectable gold compounds have enjoyed widespread, but occasionally controversial, use in rheumatoid arthritis since the 1920s. This overview examines the data from controlled trials and longer-term observational studies. We conclude that gold is equivalent to other widely used second-line agents in terms of efficacy. Toxicity profiles are similar, apart from methotrexate. It is most efficacious and toxic in the first 2 yr of treatment. There appears to be a dose-response relationship for both efficacy and toxicity. Gold is one of the few agents that decreases the rate of progression of erosions (RR 0.38, 95% CI 0.23-064). Gold compounds, therefore, have a definite place in the rheumatologist's armamentarium, but further research is required to determine optimal monitoring regimes as well as the role of maintenance therapy and combination therapy.

Chrysotherapy: a synoptic review

“…After injection of sodium gold thiomalate, gold was rapidly absorbed with maximal levels in plasma at 2 h postinjection [8]. In general, gold concentrations in blood and blood components were unsatisfactory in predicting impending toxicity or in evaluating appropriate regimens for continued courses of therapy [3].…”

“…In general, gold concentrations in blood and blood components were unsatisfactory in predicting impending toxicity or in evaluating appropriate regimens for continued courses of therapy [3]. In chrysotherapy, about 70 % of the administered gold was retained in the body and may be detectable in patients for up to 23 years posttreatment, suggesting a capture by proteins before storage in the intracellular compartments from which turnover may be slow [8,49]. Gold was usually excreted in the feces and urine [84].…”

“…Sodium gold 4-amino-2-yes mercaptobenzoic acid Auranofin 3-triethylphosphinegold + -n o 2,3,4,6-tetra-O-acetyl-1-thio-B-D-glucopyranoside; 2,3,4,6-tetra-O-acetyl-1-thio-B-Dpyranosato-S-(triethylphosphine) -Au + ever, a small number of disease-modifying antirheumatic drugs have demonstrated ability to slow or arrest the progress of the disease [35]. Injectable gold compounds have been used to treat RA since 1929 [8,43]. In general, gold was equivalent to other widely-used second line agents in terms of efficacy and were most effective -and toxic -in the first two years of treatment, with a dose-response relation for both efficacy and toxicity [8].…”

“…Injectable gold compounds have been used to treat RA since 1929 [8,43]. In general, gold was equivalent to other widely-used second line agents in terms of efficacy and were most effective -and toxic -in the first two years of treatment, with a dose-response relation for both efficacy and toxicity [8]. Complex Au + drugs, especially gold thiomalate, gold thioglucose, and gold thiosulfate were used frequently in the treatment of RA to produce durable remissions of this chronically progressive disease [3,9].…”

“…Adverse side effects of chrysotherapy in 30 to 45 % of treated patients resulted in discontinuation [14, 39, 47 -51]. Adverse side effects included skin rashes; protein in the urine; inflammation of the mouth; reduction in the number of circulating leukocytes; decreased number of blood platelets; aplastic anemia due to organ damage; lung abnormalities; adverse immune reactions, such as stomatitis, eosinophilia, lymphadenopathy, hypergamma globulinemia; severe hypotension, angina, myocardial infarction, nephrotoxicity and nephrotic syndrome; hepatitis; colitis; and chrysiasis (pigmentation) of the cornea, lens, and skin [3,8,14,44,50,52,53,57]. The most common side effect of chrysotherapy was skin toxicity, accounting for up to 60 % of all adverse reactions, especially lichenoid eruptions and non-specific dermatitis [3,47,54,55].…”