Complexes chrysotherapy

Table 6.1 Medicinally important chrysotherapy complexes. Adapted from Shaw [17].

The earliest use of gold complexes in medicine primarily involved gold thiolates, which being yellow or even gold-colored in solution, led to their designation as chrysotherapy (chrysos is Greek for gold). 

This type of in vitro study is relevant because it mimics likely physiological conditions. Red cells contain 1-2 mM GSH so the formation of glutathione complexes would be a likely consequence when auranofin metabolites enter red cells [112, 113]. Compared with typical in vivo gold concentrations of 10-15 pM observed in patients, the Ki values for the four gold complexes are less than anticipated. This indicates that chrysotherapy can greatly depress GSH-Pxase activity in vivo so the normal cellular redox balance would be displaced, favoring the accumulation of H2O2 and possibly GSH [3, 79, 114]. 

The complexes which have been used in chrysotherapy (the treatment of rheumatoid arthritis by gold drugs) are given in Table 9. Of these, (11), (12) and (18) are the most important. Complexes (11) and (12) were for many years dominant, but they must be administered parenterally, and the new drug (18) is unique in that it is therapeutically beneficial when administered orally.9-14 240... 

The complexes sodium aurothiomalate and sodium aurothioglucose provide effective therapy for rheumatoid arthritis but can produce unpleasant and toxic reactions because of the relatively large doses used (up to 250jumol (50 mg) per week). The resultant high concentrations of Au in plasma of patients receiving chrysotherapy may be measured easily by solvent extraction and FAAS. The main advantages of ETA—AAS are the direct analysis and the sensitivity to measure the various Au containing species in body fluids. 

All the gold compounds used in therapy today (chrysotherapy) are Au(I) compounds (45-47) (10-14). Gold has an intriguing chemistry dominated hy relativistic effects (48) and it is interesting to consider the reasons why Au(III) complexes are not used as anticancer agents like those of Pt(II) are used. 

The pathogenesis of immune complex type glomerular lesions associated with chrysotherapy remains... 

Gold compounds have been used in medicine for centuries, an application known as chrysotherapy. Since 1940, however, complexes of gold have been used most successfully to treat arthritic disorders in humans and other animals. Au(I) compounds are currently the only class of pharmaceuticals known to halt the progression of rheumatoid arthritis. 

Therapeutic results with copper alone were found by Hangarter to be comparable with those of chrysotherapy, although copper treatment was associated with considerably fewer side effects [246]. One ampoule of Permalon contained 20 ml of an aqueous solution containing 2.0 g (12.5 mM) of sodium salicylate and 2.5 mg (39 mM, 2.5 mg of Cu) of copper, added as the chloride. It is likely that this solution contained copper complex(es) of the added salicylate. 

In chrysotherapy, following earlier uses of potable gold and of colloidal gold, the intact complex compounds (with trade names) used in the form of aque-... 

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