Introduction: Antiretroviral (ARV) drug use during pregnancy significantly reduces mother-to-child HIV transmission, delays disease progression in the women and reduces the risk of HIV transmission to HIV-serodiscordant partners. Pregnant women are susceptible to the same adverse reactions to ARVs as nonpregnant adults as well as to specific pregnancy-related reactions. In addition, we should consider adverse pregnancy outcomes and adverse reactions in children exposed to ARVs during intrauterine life. However, studies designed to assess the safety of ARV in pregnant women are rare, usually with few participants and short follow-up periods. Areas covered: In this review, we discuss studies reporting adverse reactions to ARV drugs, including maternal toxicity, adverse pregnancy outcomes and the consequences of exposure to ARV in infants. We included results of observational studies, both prospective and retrospective, as well as randomized clinical trials, systematic reviews and meta-analyses. Expert opinion: The benefits of ARV use during pregnancy outweigh the risks of adverse reactions identified to date. More studies are needed to assess the adverse effects in the medium- and long term in children exposed to ARVs during pregnancy, as well as pregnant women using lifelong antiretroviral therapy and more recently available drugs.