antiviral

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bshin
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85881
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antiviral
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2011-06-15 01:42:21
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antiviral
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  1. Acyclovir
    • anti-viral (herpes simplex, herpes zoster)
    • -Guanosine analog (no 3'-OH)
    • -prodrug-->phos-by host kinase-->phos by viral-Thymidine kinase (TK)-->incorp, terminate DNA chain
    • -short half life!

    • USE-HSV, VZV, EBV
    • -topical, oral, IV (encephalitis)
    • -reduce shedding, BUT only works on replicating stage (NOT dormant latency)
    • -prophylactic in immunocompromised
    • (for Herpes zoster, use similar agent Famciclovir)

    • SE- minor with oral , more with IV
    • -Crystalluria, neurotoxicity
    • -NOT hematotoxic (b/c activated by Herpes-specific TK!)

    Resistance- TK negative strains, changes in DNA pol.
  2. Famciclovir
    • anti-viral (herpes simplex, herpes zoster)
    • -Guanosine analog (no 3'-OH)-prodrug-->phos-by host kinase-->phos by viral-Thymidine kinase (TK)-->incorp, terminate DNA chain
    • -newer than Acyclovir, longer half life

    USE- HSV (acyclovir resistant ones)

    Resistance- TK negative strains.
  3. Valacyclovir
    • anti-viral (herpes simplex, herpes zoster)
    • -Guanosine analog (no 3'-OH)-prodrug-->phos-by host kinase-->phos by viral-Thymidine kinase (TK)-->incorp, terminate DNA chain
    • -newer than Acyclovir, longer half life

    USE- HSV (acyclovir resistant ones)

    Resistance- TK negative strains.
  4. Ganciclovir
    • anti-viral (herpes simplex, herpes zoster, CMV)
    • -Guanosine analog
    • -first phos by viral-specific (TK by HSV/VZV or phosphtransferase in CMV)
    • -but CAN be phos by cellular kinases
    • -similar to Acyclovir, but MORE toxic

    USE-CMV prophylaxis for AIDs!!

    • SE-dose-limiting hematotoxicity (leukopenia, thrombocytopenia), mucositis, fever, rash, crystalluria
    • -seizure in overdose
    • -nephrotoxicity
  5. Foscarnet
    • anti-viral
    • -NOT antimetabolite like acyclovir or gnaciclovir
    • -inhibit viral DNA and RNA polymerases(bind PPi binding site)
    • -does NOT req activation by viral kinase

    • USE- CMV retinitis in AIDS when ganciclovir fails.
    • -acyclovir-resistant HSV

    • SE- nephrotoxicity!!
    • do NOT use with Pentamidine (pneumocystis infection in AIDS)- also nephrotoxic so additive!--> ACN, hypocalcemia!!
  6. Cidofovir
    broad spectrum antiviral Cyt-analog- doesn't need to be phosphorylated
  7. HAART
    Highly active antiretroviral therapy
    started when paitients present with AIDs defining illness, CD4 < 350 or high viral load

    • -3 drugs
    • -2 nucleoside reverse transcriptase inhibitors (NRTIs) + 1 protease inhibitor
    • OR
    • -2 NRTIs + 1 non-nucleoside reverse-transcriptase inhibitor
  8. NRTIs
    • Nucleoside reverse transcriptase inhibitors
    • -prodrug--> phos by TK (or other)--> competitively inhibit nucleotide binding to reverse transcriptase--> chain termination
    • -used w/ protease inhibitors

    • SE- marrow suppression! (can be activated by nonspecific kinases)-reverse with GM-CSF
    • -peripheral neuropathy, lactic acidosis, megaloblastic anemia.

    - Zidovudine, Didanosine, Zalcitabine, Stavudine
  9. NNRTIs
    • non-nucleoside reverse transcriptase inhibitors
    • -NOT prodrug
    • -does NOT need to be phos
    • -inhibit reverse transcriptase
    • -additive/synergistic with NRTIs
    • -NOT marrow suppressant!

    -Nevirapine, Efavirenz, Declaviridine
  10. Nevirapine
    • non-nucleoside reverse transcriptase inhibitor
    • -NOT prodrug
    • -does NOT need to be phos -inhibit reverse transcriptase
    • -additive/synergistic with NRTIs
    • -NOT marrow suppressant!

    • USE- HIV/AIDS
    • -decrease vertical transmission by 50%!!

    SE-rash, induce CYP3A4, liver toxicity
  11. Efavirenz
    • non-nucleoside reverse transcriptase inhibitor
    • -NOT prodrug
    • -does NOT need to be phos
    • -inhibit reverse transcriptase
    • -additive/synergistic with NRTIs
    • -NOT marrow suppressant!

    USE- HIV/AIDS

    SE- insomnia, night mares!!
  12. Zidovudine
    • NRTI (anti-HIV)
    • -AZT
    • -Thymidine analog
    • -phos nonspecifically to triphosphate-->inhibit reverse transciptase

    • USE- HIV/AIDS
    • -prophylaxis dur pregnancy to reduce vertical transmission.

    SE- marrow suppression (most severe!),Megaloblastic anemia, myopathy, peripheral neuropathy

    Resistance- mutation in pol gene
  13. Didanosine
    • NRTI(anti-HIV)
    • -ddI
    • -Inosine analog (Inosine--> purine (A,G)
    • -phos nonspecifically to triphosphate-->inhibit reverse transciptase

    USE- HIV/AIDS

    SE-pancreatitis, peripheral neuropathy, hyperuricemia, liver toxic
  14. Zalcitabine
    • NRTI (anti-HIV)
    • -ddC
    • -Cytosine analog
    • -phos nonspecifically to triphosphate-->inhibit reverse transciptase

    USE- HIV/AIDS

    • SE-peripheral neuropathy (major!)
    • diarrhea, pancreatitis, neutropenia, rash
  15. Stavudine
    • NRTI (anti-HIV)
    • -d4T
    • -Thymidine analog like zidovudine
    • -phos nonspecifically to triphosphate-->inhibit reverse transciptase

    USE- HIV/AIDS

    • SE-peripheral neuropathy (major!)
    • myelosuppression less than Zidovudine
    • -do NOT use with Zidovudine!
  16. Lamivudine
    • NRTI (anti-HIV)
    • -3TC
    • -Cytosine analog
    • -phos nonspecifically to triphosphate-->inhibit reverse transciptase

    USE-HIV/AIDS, Hepatitis B!!

    • SE- least toxic! so least potent
    • GI effects, neutropenia.
  17. Abacavir
    • NRTI (anti-HIV)
    • -ABC
    • -phos nonspecifically to triphosphate-->inhibit reverse transciptase

    USE- HIV/AIDS

    SE-allergies!
  18. Combos of NRTIs to avoid
    ddI+ ddC- additive toxicity of peripheral neuropathy and pancreatitis

    d4T + AZT- competition b/c both Thymine analogs
  19. Saquinavir
    • protease inhibitor (anti-HIV)
    • -inhibit aspartate protease (pol gene encoded- cleave precursor viral protein to active ones)
    • -inhibit unique dipeptide structure on aspartate protease (absent in us)

    USE-HIV/AIDS

    • SE-least toxic, but very low bioavailability. TOO much resistance now, so doens't work..
    • -Hyperglycemia, DM, nausea, diarrhea

    Resistance-point mutation in pol gene
  20. Ritonavir
    • protease inhibitor (anti-HIV)
    • -inhibit aspartate protease (pol gene encoded- cleave precursor viral protein to active ones)
    • -inhibit unique dipeptide structure on aspartate protease (absent in us)

    USE- HIV/AIDS

    • SE-CYP activate, inhibit!! so much drug interactions!!
    • Hyperglycemia, nausea, diarrhea
  21. Indinavir
    • protease inhibitor (anti-HIV)
    • -inhibit aspartate protease (pol gene encoded- cleave precursor viral protein to active ones)
    • -inhibit unique dipeptide structure on aspartate protease (absent in us)

    USE- HIV/AIDS

    SE-Hyperglycemia, crystalluria, thrombocytopenia
  22. Nelfinavir
    • protease inhibitor (anti-HIV)
    • -inhibit aspartate protease (pol gene encoded- cleave precursor viral protein to active ones)
    • -inhibit unique dipeptide structure on aspartate protease (absent in us)

    USE- HIV/AIDS

    SE-Hyperglycemia, nausea, diarrhea
  23. Amprenavir
    • protease inhibitor (anti-HIV)
    • -inhibit aspartate protease (pol gene encoded- cleave precursor viral protein to active ones)
    • -inhibit unique dipeptide structure on aspartate protease (absent in us)

    USE- HIV/AIDS

    SE-Hyperglycemia, diarrhea, nausea
  24. Atazanavir
    • protease inhibitor (anti-HIV)
    • -inhibit aspartate protease (pol gene encoded- cleave precursor viral protein to active ones)
    • -inhibit unique dipeptide structure on aspartate protease (absent in us)
    • newer! NO hyperglycemia DM SE!

    USE- HIV/AIDS
  25. Enfuvirtide
    • Fusion inhibitor (anit-HIV)
    • -bind, inhibit gp41-->steric hindrance so gp120 cannot bind CD4
    • -gp120 mutates much more frequent than gp41

    USE-early HIV/AIDS drug!

    SE-hypersensitivity, increase risk of bacterial pneumonia
  26. Maraviroc
    • Fusion inhibitor (anit-HIV)
    • -block CCR5 on Tcell

    USE-early HIV/AIDS drug!

    SE-hypersensitivity, increase risk of bacterial pneumonia
  27. Raltegravir
    Integrase inhibitor (anti-HIV)
  28. Amantadine
    • DA-reuptake blocker+releaser+ antimuscarinic+ anti-viral!!
    • -block attachment, penetration, uncoating of Influenza A

    • USE- Prophylaxis for Influenza A
    • Parkinson's disease

    • SE-Ataxia, dizziness, slurred spech
    • nervousness, insomnia
    • -atropine-like, livedo reticularis~!!

    Resistance-mutated M2 (most Influenza viruses are resistant!)
  29. Rimantidine
    • derivative of Amantadine with fewer SE
    • -does NOT cross CNS, so less atropine-like CNS effects
  30. Zanamivir, Oseltamivir
    • antiviral
    • -inhibit neuraminidase of Influenza A,B
    • (decrease relesase of progeny of virus)

    USE- prophylaxis

    SE- flu-like symptoms!
  31. Ribavirin
    • antiviral
    • -nucleoside analog
    • -mono-phos form-->inhibit IMP dehydrogenase (block Guanine syn)
    • -tri-phos form-->inhibit RNA pol

    USE- RSV (infant bonchiolitis!) , Hep-C (w/ alpha-IFN)

    SE-Hemolytic anemia, upper airway irrtation, teratogen!!
  32. IFN alpha
    antiviral

    • USE- Hepatitis B, C, D
    • -Kaposi sarcoma, CML, renal cell carcinoma

    note- Lamivudine also used for Hep B

    SE- neutropenia
  33. IFN beta
    immunoregulatory

    USE- Multiple sclerosis

    SE- neutropenia
  34. IFN gamma
    USE- NADPH oxdiase deficiency (chronic granulomatous disease)

    SE- neutropenia
  35. Antibiotics to avoid in pregancy
    • Sulfonamides--> kernicterus
    • Aminoglycosides--> ototoxcity
    • Fluoroquinolones--> cartilage damage
    • Erythromycin-->acute cholestatic hepatitis in mom
    • Clarithromycin-->embryotoxic
    • Metronidazole-->mutagenesis
    • Tetracyclline-->discolor teeth, inbibit bone growth
    • Ribavirin-->teratogenic
    • Griseofulvin-->teratogenic
    • Chloramphenicol-->"gray baby"

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