Table 1.
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].