Continued spread of HIV infection among women has led to the use of antiretrovirals in pregnant women and their newborns. Regional strategies to prevent mother-to-child transmission are evolving. Altered drug disposition during pregnancy may require altered dosing or 'boosted' therapies to avoid treatment failure. Maturing drug elimination pathways in newborns must also be considered for effective therapy. Potential teratogenic effects and increased sensitivity to antiretroviral toxicities might be encountered in this population. Use of highly active antiretroviral therapy (HAART) to suppress viral replication combined with formula feeding can reduce the rate of mother-to-child HIV transmission to less than 2%. In resource-limited settings, less intensive regimens including zidovudine, lamivudine and nevirapine still substantially reduce mother-to-child transmission. Although difficult to perform, clinical trials to determine the safety, pharmacokinetics and optimal dosing of antiretroviral in pregnant women and their newborns are urgently needed.