The article based on numerous literature data provides a comprehensive analysis of the problem of the gestational drug safety during antiretroviral therapy (ARVT) in HIV-infected pregnant women. It is emphasized that the ARVT goal during pregnancy is, on the one hand, in preventing HIV vertical transmission from mother to child, and on the other, ensuring the pregnant woman optimal treatment with the drug minimal undesirable effects on the mother’s and the unborn child’s bodies. Pregnancy in HIV-infected women, despite modern approaches to managing it, is significantly different from pregnancy in HIV-uninfected women. The HIV persistence in a woman’s body has a significant impact on both the pregnancy and childbirth course and the child’s health. As concerns the clinical pharmacology, the issues of optimal use of modern antiretroviral drugs in HIV-infected pregnant women are considered following the principle of maximum adherence to gestational safety. The information provided is of great practical importance for practitioners.