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  1. Antifungal 3 main MOA
    • 1. alter cell membrane permeability
    • 2. block nucleic acid synthesis
    • 3. disrupt microtubule function
  2. Antifungals that effect cell wall permeability (4)
    • 1. Azoles
    • 2. Allylamines 
    • 3. Polyenes 
    • 4. Glucan synthesis inhibitor
  3. Antifungals that block nucleic acid synthesis  (1)
    pyrimidine analogs
  4. Antifungals that disrupt microtubule function
  5. Azoles

    A. Imidazoles (3)
    B. Triazoles (4)
    • A.
    • 1. ketoconazole
    • 2. miconazole (topical)
    • 3. clotrimazole(topical)

    • B.
    • 1. Itraconazole
    • 2. fluconazole
    • 3. voriconazole
    • 4. Posiconazole
  6. Fluconazole
    • -only azole drug to penetrate CNS
    • -IV & PO

    -used for candida infections and cryptococcal meningitis

    -150mg stat dose for vulvovaginal candidiasis
  7. Ketoconazole
    - PO, Topical

    - for mucocutaneous candidiasis, seborhea, tinea versicolor, tinea skin infections

    - less selective for fungal CYP P450 so AE and DI (drug interactions)

    - hepatotoxicity (monitor LFTs)

    - GI side effects ARE COMMON

    -endocrine effects
  8. Itraconazole
    -IV, PO

    -is most potent with widest spectrum

    -for onychomycosis, tx of endemic histoplasmosis and blastomycosis

    -watch DI

    -AE: GI, edema, rash, hepatotoxicity, so mointor LFTs
  9. Voriconazole (Vfend)
    - new Triazole agent

    - for invasive aspergillosis, candidemia, esophageal candidiasis

    AE: well tolerated; occasional elevated LFTs, rash, visual disturbances

    DI: metabolized by CYT P450 so many drug interactions
  10. Posiconazole
    Newest Azole

    Oral Triazole for IC (Immunocompromised) pts w/ aspergillus and candida prophylaxis for severe IC pts

    AE: N/V and liver dmg
  11. Topical azoles (3)
    • 1. Clotrimazole
    • 2. Miconazole 
    • -both for vulvovaginal candidiasis, tinea infections

    3. ketoconazole cream, shampoo for tinea skin infections and seborrhea
  12. Caspofungin acetate
    -new glucan inhibitor

    -MOA: inhibits beta 1,3 D-glucan in fungal cell wall

    -IV for REFRACTORY invasive aspergillosis infections

    • AE:
    • -allergic rxns with feve, flushing, GI effects
    • -infusion vein inflammation (phlebitis)
  13. Anidulafungin (Eraxis)
    • -IV
    • -for severe esophageal candidiasis (2nd to fluconazole), candidemia, and other Candidida

    • AE:
    • -diarrhea
    • -hypokalemia
    • -evelated ALT
  14. Micafungin (Mycamine)
    -IV for Candida prophylaxis in pts undergoing stem cell transplant

    -2nd for esophageal candidiasis
  15. Amphotericin B
    • -Polyene antibiotic
    • broadest spectrum antifungal
    • -drug choice for life threatening fungal infections

    MOA: binds to ergosterol in fingal membrane and alters permability

    Toxicity: ampho "terrible" infusion related; fever, chills, muscle spasms, HA, hypotension; Slower toxicities: renal dmg common
  16. Nystatin
    • -Polyene antibiotic
    • -mostly used for topical application
Card Set:
2013-01-16 00:49:26
Pharm B3

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