IS LOCAL BIOTRANSFORMATION THE KEY TO UNDERSTANDING THE PHARMACOLOGICAL ACTIVITY OF SALICYLATES AND GOLD DRUGS

It is suggested that some drugs may be converted by inflammatory cells to yield active species. The transformation may be non-enzymatic, alt hough being driven by the enzymatic production of highly reactive spec ies which are normal products of activated leukocytes, such as singlet oxygen, hydrogen peroxide, hypochlorite, hydroxyl radical and nitric oxide. Drugs which may be transformed in this fashion are the anti-rhe umatic gold complexes which may be converted either to aurocyanide or to Au(III) complexes by myeloperoxidase in polymorphonuclear leukocyte s. Salicylate may also be activated by its oxidation to dihydroxybenzo ates although evidence for its transformation is weaker than for the g old complexes.