antifungals, antivirals

  1. super saturated potassium iodide and other iodides treat what?
    Sporothrix schenckii. skin sporotrichosis (gardener)
  2. Disrupts mitotic spindle, binds microtubules, like colchicine. treats tinea capitis
  3. Blocks ergosterol synthesis. topical & po for skin & nail infections.
  4. Blocks beta glucan synthase, disturbing integrity of fungal cell wall
    Caspofungin (echinocardins class)
  5. 95% bioavail. No acid concern. Good distribution, good CNS penetration.
    Look for P450 interaction. Photosensivity. (triazole 2nd generation).
  6. GI must be pH 4 to absorb. Liver metabolism. No kidney concern. Not so good CNS penetration. Triazole (2nd generation)
  7. good absorption, 97% bioavail., CNS/CSF 70%, all compart. 90% out of kidney. Trizaole (2nd generation azole)
  8. Inhibit enzyme – lanosterol demethylase (P450-dependent enzyme) --> blocks ergosterol synthesis
  9. 1st generation azoles, topical only
    Imidazoles: Ketoconazole & Clotrimazole & Miconazole
  10. Needs low pH (3.0) to dissolve. Less selective for fungal P450 -->
    more toxic to humans. Poor CNS distribution. Blocks host steroid
  11. Skin cream, lotion. Topical for Tinea skin infection. Imidazole (1st generation)
    Clotrimazole & Miconazole
  12. Binds ergosterol in fungal cell membrane
    Nystatin, amphotericin B, ambisome
  13. Similar to Amphotericin B – more toxic. Topical only.
  14. Protease inhibitors
    Fosamprenavir, Lopinavir/Ritonavir, Atazanavir
  15. Protease inhibitors are not preferred due to ...
    • most are not preferred due to short serum t1/2 and All drugs in this
    • class are inducers or inhibitors of this CYP450 system. Therefore, a
    • high chance of drug-drug interactions
  16. Integrase inhibitor. Active against virus with resistance to NRTIs, NNRTIs, and PIs
  17. Eliminated by glucuronidation. no induction or inhibition of P450
    Integrase inhibitor, Raltgravir
  18. Non-Nucleoside Reverse Transcriptase Inhibitor
  19. bind directly to enzyme, block RNA-dependent DNA Polymerase action
    NNRTI - Efavirenz
  20. t1/2 40-55 hr, inducer of CYP3A
  21. Nucleoside Reverse Transcriptase Inhibitors - long half life
    Zidovudine, Lamivudine, Tenofovir and Emtricitabine
  22. incorporated into the growing nucleic acid, cause DNA chain termination
    NRTIs : Zidovudine, Lamivudine, Tenofovir and Emtricitabine
  23. NRTIs toxicity
    Mitochondrial toxicity, Lactic Acidosis, Hepatic Steatosis, hepatotoxicity, Multiorgan failure and Death
  24. Fusion inhibitor. binds to the viral surface glycoprotein gp41 and
    prevents fusion. Used w/ viruses resistant to NNRTIs and NRTIs and PIs
  25. Enfuvirtide effect on P450 system
  26. CCR5 receptor inhibitor. Active against virus with resistance to PIs, NRTIs and NNRTIs
  27. CCR5 receptor inhibitor. Blood conc will change depending on inducer/inhibitor of CYP3A4
  28. DNA polymerase inhibitors for anti herpes. IV or topical
    Acyclovir, Valcyclovir, Famciclovir, Ganciclovir, Cidofovir and Foscarnet
  29. nucleoside analog incorporated into herpes DNA replication
  30. Acyclovir, Valcyclovir, Famciclovir, Ganciclovir, Cidofovir and Foscarnet toxicities
    Nephrotoxicity, neurotoxicity
  31. Side effect of antiherpes Trifluridine.
    burning sensation and edema of eye
  32. Blocks DNA polymerase of virus (hepatitis & herpes)
    Famciclovir - treats Hep B
  33. side effects of Famciclovir
    not remarkable
  34. inhibitors reverse transcriptase treating Hep B
  35. side effects of Lamivudine
    GI, headache, fatiqgue, pancreatitis, lactic acidosis. Hypersensitivity
  36. Inhibits DNA, RNA synthesis, treating Hep C
  37. Side effects of Ribavirin
    hemolytic anemia, elevated uric acid, teratogenic
  38. Interferon is used to treat
    Hep B & C
  39. Interferon toxicity
    Flu like, bone marrow, neurotoxicity, liver toxicity
  40. prodrug that inhibits HBV DNA polymerase
    Adefovir DP
  41. Adefovir DP side effects
    Nephrotoxicity, bone loss, lactacidosis, hepatic steatosis
  42. H+ must enter virus via M2 ionic channel to change pH and cause
    uncoating and release of RNA. Drugs block ion channel, prevent release
    amantadine & rimantadime
  43. Side effects of Amantadine & Rimantadine
    CNS: insomnia, poor concentration, nervous, hallucination, depression
  44. Which one is more prone to resistance for flu virus? Amantadine or Rimantadine?
    Amantadine. Due to farmers feeding to chickens
  45. Blocks neuraminidase
    Oseltamivir and Zanamivir
  46. Side effects of Oseltamivir
    nausea, vomiting
  47. side effects of zanamivir
    bronchospasm in asthmatics
  48. guanosine analog. blocks dna and rna synthesis
  49. Ribavirin is used in
    flu & hepatitis
Card Set
antifungals, antivirals
antifungals, antivirals