Skip to main content
. 2016 Sep 16;1(2):109–121. doi: 10.1016/j.bioactmat.2016.09.004

Table 1.

Antiretroviral medications.

Medication Target Type Usage Toxicity
Enfuvirtide gp41 Fusion inhibitor Binds & blocks conformational change in gp41 Significant
Maraviroc gp120 Entry inhibitor Blocks binding of gp120 to CCR5 hepatotoxic
Abacavir RT NRTI Inhibit DNA-dependent synthesis +
Didanosine RT NRTI Inhibit DNA-dependent synthesis ++++
Emtricitabine RT NRTI inhibit DNA-dependent synthesis +
Lamivudine RT NRTI Inhibit DNA-dependent synthesis +
Stavudine RT NRTI Inhibit DNA-dependent synthesis ++++
Tenofovir RT NRTI Inhibit DNA-dependent synthesis +
Zidovudine RT NRTI Inhibit DNA-dependent synthesis ++
Zalcitabine RT NRTI inhibit DNA-dependent synthesis ++++
Raltegravir Enzyme active site Integrase inhibitor Inhibit DNA strand transfer activity Adverse effects
Elvitegravir Enzyme active site Integrase inhibitor Inhibit DNA strand transfer activity Adverse effects
Dolutegravir Enzyme active site Integrase inhibitor Inhibit DNA strand transfer activity Adverse effects
Efavirenz RT NRTI & NtRTI Induce conformational change of RT Toxic effects to CNS
Saquinavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Ritonavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Darunavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Indinavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Tipranavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Fosamprenair Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Nelfinavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Atazanavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Lopinavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity
Amprenavir Aspartyl protease Protease inhibitor Viral protease inhibitor GI toxicity

++++ Strongest association with mitochondrial toxicity, +weakest association with mitochondrial toxicity; Enfuvirtide has common adverse events which include pain, erythema, pruritus, and induration. Central nervous system (CNS) toxicity involves abnormal mood, delusions, and insomnia; Gastrointestinal toxicity (GI) includes abdominal pain, nausea, emesis, diarrhea; Adverse effects: nausea, dizziness, headache, insomnia, and fatigue [271], [272].