PTCE: The Basics of Medications - Antiretroviral Agents

Antiretroviral agents, listed below, are used for the treatment of the human immunodeficiency virus (HIV) and are categorized based on their reaction with HIV replication. Nucleoside (NRTIs)/nucleotide (NtRTI) reverse transcriptase inhibitors stop HIV DNA synthesis by attaching to the HIV DNA chain. Side effects of NRTIs and NtRTIs may include anemia, hepatotoxicity, lactic acidosis, lipodystrophy (fat redistribution), and skin rash. Non-nucleoside reverse transcriptase inhibitors (NNRTIs) inhibit the conversion of HIV RNA to HIV DNA. These agents may have adverse effects, including hepatotoxicity, lipodystrophy, and skin rash. Protease inhibitors (PIs) exert their action by interfering with protease, an enzyme that breaks the HIV virus into small segments. Side effects of protease inhibitors include hepatotoxicity, hyperglycemia, hyperlipidemia, lipodystrophy, osteonecrosis (bone death), and skin rash. A C-C motif chemoreceptor 5 (CCR5) inhibitor interferes with the HIV virus’s ability to bind to the outer surface of a cell. This class of drug may cause hepatotoxicity.

Integrase inhibitors block the HIV enzyme integrase; the virus uses the enzyme to help transfer its genetic material into the DNA of infected cells.

Fusion inhibitors prevent HIV from entering a cell by interfering with the virus’s ability to fuse with the cell membrane. A novel class, HIV-1 attachment inhibitors, prevent the initial interaction between the virus and host cell, thereby preventing HIV from infecting those cells and multiplying.

Table: Antiretroviral Agents