In the realm of antimicrobials, antiretrovirals stand out as a specialized class designed to combat the unique challenges posed by retroviruses, with a primary focus on the human immunodeficiency virus (HIV). These drugs serve as key players in antiretroviral therapy (ART), contributing to the suppression of viral replication and the mitigation of HIV-associated immunodeficiency. Antiretrovirals are categorized into different classes based on their mechanism of action, including nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), integrase strand transfer inhibitors (INSTIs), and entry/fusion inhibitors. The combination of these classes in treatment regimens helps enhance efficacy and reduce the likelihood of drug resistance. Despite the remarkable advancements facilitated by antiretrovirals, challenges persist, such as the need for lifelong adherence to the medication, potential side effects, and the emergence of drug-resistant strains. Ongoing research and development aim to address these issues and pave the way for more effective and accessible antiretroviral therapies, bringing us closer to the goal of ending the global HIV/AIDS pandemic.