Hypouricemia is defined as a serum uric acid concentration of ≤ 2.0 mg/dL or 119 μmol/L. Hypouricemia may occur secondarily to a number of underlying conditions, including severe hepatocellular disease, neoplasia, defective renal tubular reabsorption of uric acid, inherited metabolic defect in purine metabolism, and drugs. Medications are an important cause of hypouricemia. They can cause hypouricemia by a variety of mechanisms. Drug-induced hypouricemia mostly occurs as overtreatment of hyperuricemia by urate-lowering therapies including xanthine oxidase inhibitors, uricosuric agents and uricases. Drugs not used in the treatment of gout may also lead to a decrease of uric acid levels. In this literature review, medications leading to hypouricemia are summarized with regard to their mechanism of action and clinical significance.