Antiretroviral Therapy

To reduce the risk of disease progression and to prevent the transmission of the virus to others, antiretroviral therapy (ART) is recommended for all patients with HIV infection. The Food and Drug Administration has approved more than 25 antiretroviral drugs in 6 mechanistic classes (Table 4).25,26 Recommended regimens are those with durable virologic efficacy, favorable tolerability and toxicity profiles, and ease of use (including some newer combinations).

Table 4. Drugs for Antiretroviral Therapy (ART).25,26
Class Drugs Mechanisms of Action
CCR5 antagonists maravoric Blocks CCR5, one of two major co-receptors, used by HIV-1 to attach to host cells
Fusion inhibitors enfuvirtide An anti-HIV peptide structurally similar to a segment of the HIV protein (gp41) - blocks membrane fusion
Nucleoside reverse transcriptase inhibitors (NRTIs) abacavir
didanosine
emtricitabine
lamivudine
stavudine
zidovudine
tenofovir (the only nucleotide RTI)
Mimic deoxyribonucleoside triphosphate, the natural substrate for reverse transcriptase – they become incorporated into the growing DNA chain, terminate elongation and decrease or prevent HIV replication
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) efavirenz
etravirine
nevirapine
Bind near the catalytic site of reverse transcriptase and inhibit a crucial step in the transcription of the RNA genome into a double-stranded retroviral DNA
Protease inhibitors (PIs) atazanavir
darunavir
fosamprenavir
indinavir
lopinavir
nelfinavir
ritonavir
saquinavir
tipranavir
Prevent cleavage of viral proteins during assembly and maturation – a process essential for the newly formed virus to become infectious
Integrase strand transfer (InST) inhibitors raltegravir Blocks HIV-1 integrase – prevents viral DNA from integrating with host cell DNA