Women have emerged as the fastest growing human immunodeficiency virus (HIV) infected population worldwide, mainly because of the increasing occurrence of heterosexual transmission. Most infected women are of reproductive age and one of the greatest concerns for both women and their physicians is that more than 1,600 infants become infected with HIV each day. Almost all infections are a result of mother-to-child transmission of HIV. With the advent of combination antiretroviral therapies, transmission rates lower than 2% have been achieved in clinical studies. Antiretroviral compounds differ from most other new pharmaceutical agents in that they have become widely prescribed in pregnancy in the absence of proof of safety. We reviewed antiretroviral agents used in pregnant women infected with human immunodeficiency virus, mother-to-child transmission, and their consequences for infants.