The contemporary treatment of the child infected with human immunodeficiency virus (HIV) unavoidably requires combination therapy with antiretroviral agents and may include additional drugs for the prevention and treatment of opportunistic infections or other disease states. The current guidelines for the treatment of the HIV-infected child recommend that the same principles of treatment for adults should apply to children. However, the pharmacokinetic and pharmacodynamic characteristics of many agents and regimens used in adults have not been defined adequately in children, and large-scale clinical trials to establish safety and show efficacy have not been completed. Therefore, the clinician will be required to use agents with incomplete knowledge about their pharmacologic properties. The purpose of this article is to provide an overview of the pediatric pharmacologic principles, a review of the pharmacologic characteristics of selected antiretroviral agents in children, and a prospectus on the design of drug dosing regimens in children.