Antiviral

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fallcloud13
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170254
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Antiviral
Updated:
2012-09-11 21:49:35
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Antiviral
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Antiviral_Dr.Jarrahian
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  1. Amantadine (Symmetrel)
    • MOA: Blocks viral uncoating by interfering with influenza A M2 protein
    • BBB cross, renal unchanged.
    • Dopaminergic effect (agitated, parkinson's pt.)
    • Use: Influenza A
  2. Rimantadine (Flumadine)
    • MOA: Blacks viral uncoating by interfering with influenza A M2 protein
    • No BBB cross, metabolized and renal.
    • Use: Influenza A
  3. Zanamivir (Relenza)
    • MOA: Competitively blocks neuraminidases of influenza A and B
    • Inhaled or intranasal
    • Bronchospasm, acute deteriorations in lung function.
    • Use: Influenza A & B
  4. Oseltamivir (Tamiflu)
    • MOA: Competitively blocks neuraminidases of influenza A and B
    • Oral capsule
    • N/abdominal discomfort/emesis
    • Use: Influenza A & B
  5. Acyclovir (Zovirax)
    • MOA: Triphosphated form (TK and host cell enzymes) is incorporated into viral DNA missing 3' hydroxyle group. Irreversible inactivation of the DNA polymerase
    • IV (renal dysfunction and neurotox), Oral(diarrhea and headache), Topical, 15-20% bio
    • Use: Herpes
  6. Valacyclovir (Valtrex)
    • MOA: Triphosphated form (TK and host cell enzymes) is incorporated into viral DNA missing 3' hydroxyle group. Irreversible inactivation of the DNA polymerase
    • Oral(diarrhea and headache), 70% bio
    • Use: Herpes, CMv prophylaxis and chickenpox
  7. Ganciclovir (Cytovene)
    • MOA: Triphosphated form (UL97 and host cell enzymes) is incorporated into viral DNA missing 3' hydroxyle group. Irreversible inactivation of the DNA polymerase
    • Oral, topical, IV, bone marrow suppression(increased with zidovudine), leukopenia, thrombocytopenia, abnormal liver fxn
    • Use: CMV txn and prophylaxis
  8. Valganciclovir (Valcyte)
    • MOA: Triphosphated form (UL97 and host cell enzymes) is incorporated into viral DNA missing 3'
    • hydroxyle group. Irreversible inactivation of the DNA polymerase
    • Oral with food, IV, bone marrow suppression(increased with zidovudine), leukopenia, thrombocytopenia, abnormal liver fxn
    • Use: CMV txn and prophylaxis
  9. Penciclovir (Denavir)
    • MOA: Acyclic guanine nucleoside analog, Triphosphated form (TK and host cell enzymes) is incorporated into viral DNA missing 3' hydroxyle group.Inhibits viral DNA polymerase
    • Use: Topical for HSV and VZV
  10. Famciclovir (Famvir)
    • MOA: Acyclic guanine nucleoside analog, Triphosphated form (TK and host cell enzymes) is incorporated into viral DNA missing 3' hydroxyle group.Inhibits viral DNA polymerase
    • Use: oral for HSV and VZV
  11. Foscarnet (Foscavir)
    • MOA: Selectively inhibits CMV and herpes DNA polymerase by binding to its pyrophosphate binding site (blocks viral DNA synthesis), reversible binding to viral DNA polymerase and reverse transcriptase (NO PHOSPHORYLATION NEEDED, Not a nucleoside)
    • IV, some CNS, renal unchaged-tox (reversible), electrolyte imbalances hypocalcemia,magnesemia, seizures
    • Use: AIDS pts with CMV retinitis, acyclovir-resistant herpes simplex.
  12. Cidofovir (Forvade)
    • MOA: Acyclic nucleotide, analog of cytosine. diphophate form competes with dCTP
    • IV, long t1/2, nephrotox, topical, dose-related site reactions
    • Use: IV (CMV retinitis in HIVE-infected pt), Topical (effective in healing lesions in acyclovir-unresponsive mucocutaneous HSV infections with AIDS)
    • Once-weekly dose, with resistant CMV
  13. Trifluridine (Viroptic)
    • MOA: monophosphate irreversibly inhibits thymidylate snythetase, triphosphate is a competitive inihibitor of thymidine triphosphate incorporation into DNA by DNA polymerase, also incorporated in place of thymidine triphosphate creating fragile, poorly functioning DNA.
    • Intraocular, burning, stining, hypersensitivity
    • Use: No systemic (No specificity), Opthalmic treatment of primary Kerato-conjuctivitis and recureent epithelial keratitis due to Herpes simplex types 1 and 2
  14. Fomivirsen (Vitravene)
    • MOA: 21 mer phosphorothioate oligonuleotide, inhibits human CMV replication through an antisense mechanism, bingind of fomivirsen to the IE2 coding region of CMV mRNA inhibits protein synthesis and subsequently CMV replication
    • Intravitreal injection, iritis, vitritis, cataracts, increase in intraocular pressure. Active against CMV resistant to gan, foscarnet, and cidofovir
    • Use: CMV retinitis for pt intolerant of or unresponsive to other therapies
  15. Docosanol (Abreva)
    • MOA: inhibits the fusion between the plasma membrane and HSV envelope by modulating the host cell (STEP 1), active against lipid-enveloped virus
    • Topical, skin irritation, burning/stinging, no drug interaction
    • Use: Herpes labialis due to HSV1 or HSV2, also active against CMV, influenza, human herpes virus-6, RSV (all enveloped)
  16. Interferon a-2a & a-2b
    • MOA: potent cytokines that have antiviral, immuno-modulating, and antiproliferative actions.
    • IV, Flue-like syndrome, Leukopenia, bone marrow suppression, myalgia
    • Use: Hepatitis B and C, Condylomata acuminata (venereal warts, papilloma virus), Cancers
    • Ex) oligoadenylate synthetase-activates RNase decrades viral mRNA, Phyphodiesterase-degrades terminal nucleotides of tRNA
  17. Ribavirin (Virazole)
    • MOA: not fully understood, broad spectrum phosphorylated by host cell.
    • Mono-P inhibits inosine monophosphate dehydrogenase and thus GTP synthesis.
    • Tri-P inhibits viral RNA polymerases and GTP dependent capping of viral mRNA
    • Increases cytokines such as IL-2, TNF-a and IF-y
    • hepatic metabolism, PREG X
    • Aerosol, IV, Oral, anemia, bone marrow suppression, mutagenic
    • Use: aerosol-RSV children, influenza A and B, Oral-hepatitis, genital herpes, oral or IV- Lassa fever, Korean and Argentine hemorrhagic fevers
  18. Adefovir dipivoxil (Hepsera)
    • MOA: synthetic acyclic nucleotide analog of dAMP, phosphorylated by cellular kinases, replaces dAMP in hep B, DNA chain terminiation.
    • Oral, renal elimination, asthenia, HA, ab pain, N
    • Use: chronic hepatitis B
  19. Entecavir (Baraclude)
    • MOA: guanosince nucleoside analog hep B, inclulding lamivudine resistant. compete with dGTP.
    • Use: HIV and HBV
  20. Telbivudine (Tyzeka)
    • MOA: L-isomer of thymidine, 5'-triphosphate inhibits RT of HBW DNA polymerase. Incorporation of 5'-triphosphate into viral DNA causes DNA chain termination
    • Use: HIV and HBV
  21. Boceprevir (Victrelis)
    • MOA: Bloacks the proteolytic activity of HCV NS3/4A serine protease (Prevents replication of HCV)
    • Leukopenia, neutropenia, thrombocytopenia, rash; Stevens-Johnson syndrome
  22. Telaprevir (Incivek)
    • MOA: Bloacks the proteolytic activity of HCV NS3/4A serine protease (Prevents replication of HCV)
    • Leukopenia, neutropenia, thrombocytopenia, rash; Stevens-Johnson syndrome
  23. Imiquimod (Aldara)
    • MOA: Immune response modifier, mRNA encoding cytokines including IF-a at treatment site
    • erythema, itching, burning, flaking
    • Use: topical, condylomata acuminata, actinic keratosis
  24. Kunecatechins (Veregen)
    • MOA: antioxidants; enhance immune system function
    • 1st botanical drug for topical (green tea leaves)
    • Use: topical for condylomata acuminata in immunocompetent patient >18

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