The antimicrobial combination of trimethoprim and sulfamethoxazole is active in vitro against various gram-positive and gram-negative bacteria. Clinically, it is useful for prophylaxis and treatment of selected infections of the genitourinary, respiratory, and gastrointestinal tracts. Trimethoprim-sulfamethoxazole by itself or in combination with other antimicrobial agents is indicated for most Nocardia asteroides infections and is the antimicrobial agent of choice for Pneumocystis carinii pneumonia. The drug is relatively nontoxic in patients who do not have the acquired immunodeficiency syndrome (AIDS) and is available in both oral and intravenous forms. The native compounds and the metabolites of trimethoprim and sulfamethoxazole are excreted primarily in the urine. When the creatinine clearance is less than 30 ml/min, the dosage of trimethoprim-sulfamethoxazole should be adjusted.