A reduction in the serum urate concentration in hyperuricemic subjects can be achieved by increasing the renal excretion of uric acid, by inhibiting its synthesis, or by a combination of both modalities. The three most commonly used hypouricemic drugs are probenecid, sulfinpyrazone and allopurinol. Each drug has been considered in detail with regard to its mechanism of action, metabolism, diverse metabolic effects, side effects and interaction with other drugs. In addition, guidelines for the use of these drugs in hyperuricemic subjects are proposed.