Isoniazid, rifampin, and ethambutol are the three major drugs used in the modern treatment of patients with tuberculosis. Data on these drugs in children have been derived primarily from their clinical use in pediatrics and extrapolation from experiences in adults. A number of questions remain concerning the clinical pharmacology and appropriate use of these drugs in children. Additional pediatric pharmacokinetic studies are necessary to confirm the current dosage recommendation and use of these agents in the pediatric patient.