Left part is for HIV, right part is for other virus.

ClassExample(s)Mechanism of action
NRTITenofovir, emtricitabine, lamivudine, abacavir, zidovudineInhibits HIV DNA synthesis from RNA template by terminating DNA chain elongation
NRTI: Competitive nucleoside/nucleotide RT inhibitor
NNRTI (-vir-)Efavirenz, nevirapineNNRTI: Allosteric RT inhibitor
PI (-navir)Atazanavir, darunavir, indinavir, ritonavirInhibits HIV polyprotein cleavage
Integrase inhibitor (-gravir)Dolutegravir, raltegravirInhibits HIV DNA integration into host genome
Fusion inhibitorEnfuvirtideInhibits HIV fusion with target cell membrane by binding to HIV gp41
CCR5 antagonistMaravirocInhibits HIV entry by blocking the HIV gp120 allosteric interaction with CCR5 (tropism testing required)

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs)

  • Medications in class
    • Abacavir (ABC)
    • Didanosine (ddI)
    • Emtricitabine (FTC)
    • Lamivudine (3TC)
    • Stavudine (d4T)
    • Tenofovir (nucleotide analog, also called nucleotide reverse-transcriptase inhibitor; NtRTI)
      • Tenofovir disoproxil (TDF)
      • Tenofovir alafenamide (TAF)
    • Zidovudine (ZDV, formerly AZT)
  • Mechanism of action
    • Competitive inhibitors of HIV reverse transcriptase.They are nucleoside/tide analogs that lack a 3’-OH group, causing chain termination upon incorporation into viral DNA.
    • Require intracellular phosphorylation to become active.
      • thus, NRTI efficacy is reliant on kinase availability and activity, which varies depending on cell functionality and activation state.
  • Adverse effects
    • Abacavir hypersensitivity reaction
      • Potentially life-threatening systemic reaction consisting of fever, rash, constitutional symptoms, vomiting, diarrhea, and, occasionally, respiratory distress
      • Avoid abacavir in HLA-B*5701-positive patients.
    • Pancreatitis: didanosine, stavudine
    • HIV-associated lipodystrophy (Cushing syndrome-like appearance): abnormal distribution of fat
      • Can caused by NRTI or PI
      • Loss of subcutaneous fatty tissue (lipoatrophy) in the face, extremities, and buttocks
      • Probable accumulation of fat in liver, muscles, abdomen, breasts, neck (double chin), and upper back (enlarged dorsocervical fat pad)
      • Metabolic changes: impaired glucose tolerance, hyperlipoproteinemia (elevated triglycerides, elevated total cholesterol, lowered HDL)

Mnemonic

Zidovudine get rid of hemoglobin anemia

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

  • Mechanism of action
    • Allosteric (non-competitive) inhibitors of HIV reverse transcriptase. Bind to a different site than NRTIs.
    • NNRTIs do not require intracellular phosphorylation for activation because they are direct inhibitors.

(The dog is trying to poop in the den)

Protease inhibitors


  • Mechanism of action: inhibition of viral HIV-1 protease (encoded by pol gene) → inability to cleave viral polyproteins into functional units → generation of impaired viral proteins → production of immature (noninfectious) virions

Mnemonic

Navir (never) tease a protease.

Integrase inhibitors

Mnemonic

Integrase -tegravir

Fusion inhibitors

Mnemonic

  • Enfuvirtide inhibits fusion.
  • Mazda Maraviroc

ART regimens

  • 2 NRTIs PLUS 1 NNRTI
  • 2 NRTIs PLUS 1 PI (boosted)
  • 2 NRTIs PLUS 1 INI