Advances in antiretroviral therapy for human immunodeficiency virus (HIV)-infected pregnant women have improved maternal health and successfully reduced perinatal transmission from 25% to less than 5%. Maternal treatment is individualized and based on physical and laboratory evaluations. Three categories of drugs are currently approved for use in HIV disease including: (11 nucleoside and nucleotide reverse transcriptase inhibitors; (2) non-nucleoside reverse transcriptase inhibitors; and (3) protease inhibitors. Treatment decisions during pregnancy are complex and require consideration of the physiologic changes of pregnancy, drug interactions, possible maternal and fetal side effects, and psychosocial issues that influence adherence to the chosen therapy.