Chrysotherapy - the treatment of rheumatoid arthritis (RA) patients with monovalent gold drugs possessing anti-inflammatory and other properties - has been used with some success for more than 70 years; however, the metabolites generated from gold drugs have not been identified positively and the mechanisms of action are not known with certainty. This account selectively reviews recent available literature on the history of gold in medicine, with emphasis on RA; the role of Au(+) and Au(+) metabolites (Au(CN)(2)(-), Au(+3), Au(o)) and other mechanisms in chrysotherapy; current treatment regimes for RA using gold drugs; chrysotherapy case histories based on 2166 RA patients; and adverse effects of chrysotherapy, mainly various forms of dermatitis. More research seems needed on the role of gold metabolites in the treatment of RA, the use of more sensitive and uniform indicators of treatment success, improved routes of drug administration for maximum efficacy, and the development of gold drugs with minimal side effects.