The concentrations of gold in whole blood, serum, urine and blood cells of patients with rheumatoid arthritis were measured during 6 months of oral treatment either with Auranofin or placebo. Any adverse effects attributable to the treatments were also recorded. Although the time course of gold during Auranofin therapy was similar to that of injected gold, the blood and serum gold concentrations were significantly lower than those measured in patients receiving injected gold. Between 45 and 58% of Auranofin gold in the blood was associated with blood cells. In comparison, following injections of gold thiomalate, only about 4% of the gold was present in the blood cells. During the 6-month period, 2 patients receiving Auranofin withdrew because of diarrhoea and another because of rash. 1 placebo patient withdrew because of headaches. No laboratory evidence of haematological, renal or hepatic abnormality was encountered. It is suggested that the markedly lower concentrations of gold in the body sustained during treatment with Auranofin may be the critical factor towards a greater tolerance of the drug in the treatment of rheumatoid arthritis.
The tissue and subcellular pharmacokinetics of gold following single and repeated oral doses of triethylphosphine gold (auranofin) has been studied in rats. After a single dose, the tissue and subcellular gold levels were 5-10 times lower than those reached with injectable gold compounds. In the liver tissues, gold concentrations peaked within 24 h followed by a biphasic clearance, with an initial rapid phase (t1/2 32 h) and a slow terminal phase (t 1/2 11 days). Renal gold concentrations continued to increase for 3 to 5 days and then decreased exponentially with a first order t 1/2 of about 7 days. Intracellularly, between 60-80% of hepatic and 50-70% of renal gold was present in the cytosol. In rats given repeated doses of auranofin, the hepatic and renal gold concentrations were 3-5 times higher than those measured after a single dose. The proportion of cellular gold present in the cytosol was markedly lower, with 43% in the liver and 30% in kidney tissues. In both the liver and kidney, gold concentrations were dose-dependent, whereas in the gastrointestinal tissues the increases as a function of dose were minimal.
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