Auranofin/aurothioglucose

The exact mechanism of action of the gold compounds (for example, gold sodium thiomalate, aurothioglucose, and auranofin) in the suppression or prevention of... 

GOLD COMPOUNDS. Aurothioglucose and gold sodium thiomalate are given intramuscularly, preferably in the upper outer quadrant of the gluteus muscle. The nurse gives auranofin orally. 

Augite, Mossbauer spectrum of, 6 474 Au(PRj) fragment, addition to homonuclear gold cluster compounds, 39 329-332 Auranofin, 36 21 cytotoxicity, 36 22, 34 Auro-bis(thiosulfate), 36 18-19 Aurosomes, gold in, 36 21-22 Aurothioglucose, 36 18-19 Aurothiomalate, 36 18-21... 

Gold compounds were first proved to be effective in a large double-blind trial in 1960. Because of their toxicity, they are used infrequently today. Their intramuscular formulations (aurothiomalate and aurothioglucose) contain 50% elemental gold. The oral formulation (auranofin) contains 29% elemental gold. 

FIGURE 16-21 Gold Antiarthritic Drugs, (a) Sodium aurothioraalate. (b) Aurothioglucose. (c) Auranofin. 

Gold drugs, such as aurothioglucose, gold sodium thiomalate, and auranofin, have long been used in the treatment of rheumatoid arthritis. The most common adverse effects associated with gold therapy appeared in skin and mucous membranes (about 15% of all patients) and kidneys (about 5-10%), mostly as proteinuria. 

Aurothioglucose (2, Table 1) was identified by TLC on a plate impregnated with silicic acid and a fluorescent compound, according to the Rf value and fluorescence quenching120. Various studies were published for the speciation of auranofin (i)266-267 and sodium aurothiomalate (3)268 in urine, blood and plasma. Using an ICP-MS detector it was possible to detect five gold-containing metabolites of 12 .270. 

Tissue damage present in RA is attributed in part to action of lytic lysosomal enzymes released by phagocytic cells in inflammed tissue. Auranofin inhibits the release of lysosomal enzymes from phagocytizing leukocytes at micromolar concentrations (1-10 uM) (44> 45). It did not produce leukocyte cytotoxicity nor inhibition of cell free lysosomal enzyme activity at these effective concentrations. Sodium aurothiomalate, aurothioglucose and odium aurothiosulfate did not exhibit this potent activity. 

It may be prepared by the condensation of the tetraacetate ester of aurothioglucose with triethylphosphine to yield the co-ordination complex, auranofin. 

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