Card Set Information

2011-10-11 23:25:47

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  1. acyclovir
    • U: HSV1 &2
    • A: competitive inhibition of HSV DNA polymerase and chain termination by adding onto the primer chain. since it does not have a 3' end, it can not be used for replication
    • R: most commonly alter the thymide kinase (that activates the drug and puts the 1st phosphate on) . Can also alter the HSV DNA polymerase. Can have cross resistance to Valcyclovir and Famciclovir.
  2. Valcyclovir
    • same as acyclovir but with L-valyl ester
    • rapidly converted to acyclovir and has 3-5x serum concentration than acyclovir
  3. Famciclovir
    • 1st pass metabolism: converted to penciclovir
    • penciclovir achieves higher intracellular concentrations
    • works the same as acyclovir and for same viruses
  4. Ganciclovir/Valganciclovir
    • U: treat cytomegalovirusz; CMV retinitis in immunocomprise patients
    • A: chain termination by acting on CMV polymerase
    • R: CMV loses its thymadine kinase that adds on phosphate
    • Admin: IV for 2 weeks
    • T: very toxic due to incorporation into host DNA.
    • AE: granulocytopenia, thrombocytopenia, renal impairment, seizures
  5. Cidofovir
    • U: treat CMV retinitis and broad spectrum anti-viral agent
    • A: direct inhibition of viral DNA polymerase and chain terminator
    • R: mutation in CMV DNA polymerase (with cross resistence to ganciclovir)

    Nucleotide analog = has phosphate on prodrug
  6. Foscarnet
    • U: broad spectrum anti-viral; CMV retinitis, colitis, esophagitis, acyclovir resistent HSV or VSV
    • A: Binds pyrophosphate binding site of viral DNA polymerases and inhibits pyrophosphate cleave of nucleotide triphosphates
    • T: very toxic
    • AE: Anemias, Renal toxicity, HYPOCALCEMIA due to Ca2+ chelation
    • Admin: IV

    Combine with ganciclovir to lower the toxicity
  7. Fomivirsen
    • U: Treat CMV retinitis
    • A: binds IE2 and directs it to be degraded by host RNases
    • Admin: direct injection into eye

    Antisense DNA Drug
  8. Interferon alpha
    • U: treat chronic hep B and C (also Human hepres virus type 8, AIDS associated Karposi's sarcoma)
    • A: works against both DNA and RNA viruses; inhibits transcription, translation, post-translational processing, virus maturation and virus release
    • Admin: subQ, no oral bioavailability

    pegylated improves bioavailbility by increasing t1/2
  9. Ribavirin
    • U: treat Hep C, respiratory syncytial virus
    • A: Guanosine analog and has multiple sites of action due to lowere GTP levels

    along with interferon alpha, this is the standard treatment for Hep C
  10. Adefovir
    • U: treat Hep B and HIV
    • A: same as the acyclovir (diphosphate = enzyme inhibitor, triphosphate = chain terminator)
    • Admin: prodrug
  11. Lamivudine
    • U: Hep B (and HIV but not as well)
    • A: HBV enzyme inhibition and chain termination; Nucleoside reverse transcriptase inhibitor for HIV
    • R: mutations of HBV polymerase
    • Admin: lower doses for HBV, therefore safer than when used for HIV
  12. Telbivudine
    • U: Hep B ONLY
    • A: enzyme inhibition & chain termination
    • R: mutation of HBV polymerase

    Potential cross resistance to other anti-HBV drugs
  13. Tenofovir
    • U: treat Hep B and HIV
    • A: prodrug that gtes phosphorylated and does enzyme inhibition and chain termination
    • R: mutations of HBV polymerase; Adefovir-resistant HBV has partial resistance to Tenofovir

    • Nucleotide drug
    • Long t1/2: once a day dosing
  14. Amantadine & Rimantadine
    • U: treat and prophalax influenza A
    • A: block the M2 ion channel; prevent fusion of the viral envelope with the phagolysosome membrane; prevent uncoating of virus
    • AE: CNS toxicity; alters dopamine metabolism; Rimantadine has higer oral bioavailability and fewer CNS effects
    • R: strains are resistant

    • anti-infectious: don't give for both treatment and prophylaxis in same household b/o resistance
    • Don't give to pregnant/nursing women or patients with psych problems
  15. Zanamivir
    • Neuraminidase inhibitor
    • U: both influenza A and B
    • A: act to decrease viral release, decrease viral spread, decrease viral entry, increase formation of viral aggregates
    • Admin: inhalation or IV (b/o poor oral bioavailibility)

    looks like sialic acid, fits into receptor, better because less likely to get resistence

    Both can be use to treat and prophylaxis
  16. Oseltamivir
    • Neuraminidase inhibitor
    • U: both influenza A and B
    • A: act to decrease viral release, decrease viral spread, decrease viral entry, increase formation of viral aggregates
    • Admin: oral as prodrug

    receptor has to spread out, easier to get resistence, makes pocket rigid

    Both can be use to treat and prophylaxis
  17. Palivizumab (as in Ab)
    • U: prophylaxis against respiratory syncytial virus
    • A: Ab against RSV F protein
    • Admin: IM (has long t1/2)