Reproductive-age women constitute an increasing percentage of individuals infected with human immunodeficiency virus. As clinical management issues particular to pregnancy become increasingly common, they are also becoming increasingly complex. With the approval of new antiretroviral agents, monotherapy with zidovudine, although still standard for prevention of mother-to-child transmission of human immunodeficiency virus, has become inadequate therapy for treatment of the mother. Clinicians must now consider alternative therapeutic strategies in spite of a dearth of experience in the setting of pregnancy. To facilitate optimal drug treatment of human immunodeficiency virus-infected pregnant women while maintaining a focus on prevention of transmission, we reviewed Medline, Reprotox, personal files, and pharmaceutical industry information about the antiretroviral agents currently approved. After summarizing potential beneficial and detrimental effects in both the pregnant and nonpregnant individual, we suggest clinical strategies and discuss the ethical and legal principles that should guide therapeutic decisions in pregnancy.