Antiretroviral therapy is the recognized treatment for human immunodeficiency virus (HIV) infection involving several antiviral agents. Even though highly active antiretroviral therapy has been proven to be very effective
in suppressing HIV replication, the antiretroviral drugs, belonging to different pharmacological classes, present quite
complex pharmacokinetic properties such as extensive drug metabolism and transport by membrane-associated drug
carriers. Moreover, due to uncomplications or complications in HIV-infected populations, an antiretroviral-based multiple-drug coadministration therapy strategy is usually applied for treatment effect, thus raising the possibility of drugdrug interactions between antiretroviral drugs and common drugs such as opioids, stains, and hormonal contraceptives.
Herein, thirteen classical antiretroviral drugs approved by US Food and Drug Administration were summarized. Besides, relative drug metabolism enzymes and transporters known to interact with those antiretroviral drugs were detailed and described. Furthermore, one after the summarized antiretroviral drugs, the drug-drug interactions between
two antiretroviral drugs or antiretroviral drug - conventional medical drugs of the past decade were discussed and
summarized. This review is intended to deepen the pharmacological understanding of antiretroviral drugs and promote
more secure clinical applications for antiretroviral drugs to treat HIV.