Anti-Virals and Anti-Retrovirals MOA

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Anti-Virals and Anti-Retrovirals MOA
2013-05-06 23:32:24
adamantanes neuraminidase inhibitors CMV antivirals HSV VAV NRTIs NNRTIs HCV Entry fusion protease integrase

adamantanes, neuraminidase inhibitors, CMV antivirals, HSV, VAV, NRTIs, NNRTIs, HCV, Entry/fusion inhibitors, protease inhibitors, integrase inhibitors
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  1. Adamantanes (amantadine & rimantadine) [influenza A]
    M2 channel inhibitor, causes failure of virus uncoating
  2. Neuraminidase inhibitors (oseltamivir & zanamivir) [influenza A & B tx+prophylaxis]
    bind sialic acid, inhibit cleavage, by neuraminidase, preventing release of newly formed viruses
  3. ganciclovir & valgancyclovir [CMV]
    competitive inhibitor of dGTP, intereferes with DNA polymerase, chain terminator
  4. foscarnet [CMV, HSV, VZV]
    blocks pyrophosphate binding site on DNA polymerase, prevents cleavage of pyrophosphate
  5. cidofovir [CMV, HSV, VZV last option]
    active DP form inhibits deoxycytidine TP and acts as sub for DNA polymerase, slows chain elongation
  6. acyclovir & valacyclovir [HSV, VZV]
    active TP form competes with deoxyguanosine TP for DNA polymerase, chain termination (lacks 3' hydroxyl)
  7. famciclovir [HSV, VZV]
    active TP form competes for viral DNA polymerase, but NOT a chain terminator! stays in cells long time
  8. docosanol [topical HSV]
    inhibits viral fusion to host cell membrane, prevents entry
  9. trifluridine [ophthalmic HSV]
    MP form inhibits thymidine synthetase; TP form inhibits viral DNA polymerase
  10. NRTIs (zidovudine, stavudine, lamivudine, emtricitabine, abacavir, didanosine, tenofovir) [HIV]
    compete with nucleoside TPs for reverse transcriptase active site, HIV binding blocked, RT cannot happen, chain termination
  11. NNRTIs (efavirenz, nevirapine, delaviridine, etravirine, rilpivirine) [HIV-1 only]
    allosteric, noncompetitive, reversible inhibitors of reverse transcriptase, cause conformational change, block RT
  12. enfuvirtide [HIV]
    peptide sequence that blocks gp41 binding, prevents fusion/cell entry
  13. maraviroc [HIV]
    CCR5 coreceptor antagonist that blocks binding of viral envelop protein to CCR5
  14. elvitrgravir & raltegravir [HIV]
    inhibit catalytic activity of HIV-1integrase, prevents insertion of HIV DNA into host cell genome
  15. interferons [HCV]
    activate ribonucleases, augment NK cell activity
  16. ribavirin [HCV]
    active TP form increases viral mutation frequency, affects host immune response
  17. NS3-4A inhibitors (boceprevir & telaprevir) [HCV]
    forms covalent bond b/w drug and protease active site, inhibits cleavage of HCV polyprotein into functional proteins