antifungals Flashcards
amphotericin B
binds ergesterol in mbrn opening pores
IV, TOP, Renal. seqester in lung, spleen, liver, little CNS
broad spectrum, life threatening fungal, like in immunosuppresed
nephrotoxic, anemia, fever vomit rigor (IV)
nystatin
binds ergesterol in mbrn opening pores
TOP,
broad spectrum, life threatening fungal, like in immunosuppresed
toxicity
ketocanazole
inhibit fungal p450 causing decreased levels of ergosterol, changing mbrn permeability. excreted in breast milk, placenta
TOP, PO, IV. HEPATIC
chronic mucocutaneous candidiasis. can antagonize ampho
hepatotoxic, jaundice, pruritus, teratogenic, stops testosterone. interacts with antacids, 3A4 inhibitors
clotrimazole
inhibit fungal p450 causing decreased levels of ergosterol, changing mbrn permeability. excreted in breast milk, placenta
TOP, hepatic
oral and vaginal candidiasis
hepatotoxic, jaundice, pruritus, teratogenic, stops testosterone. interacts with antacids, 3A4 inhibitors
miconazole
inhibit fungal p450 causing decreased levels of ergosterol, changing mbrn permeability. excreted in breast milk, placenta
TOP, hepatic
oral and vaginal candidiasis
hepatotoxic, jaundice, pruritus, teratogenic, stops testosterone. interacts with antacids, 3A4 inhibitors
fluconazole
inhibit 14 alpha demethylase (funal p450) fungistati
PO renal, can enter CNS
vaginal, oropharyngeal, esophageal candidiasis
adverse effects in HIV pts,
itraconazole
inhibit 14 alpha demethylase (funal p450) fungistatic
PO, hepatic
aspergillosis, histoplasmosis, sporotrichosis. Dermatophytoses, onychomycosis if need a systemic therapy.
adverse issues in HIV pts
teroconazole
inhibit 14 alpha demethylase (funal p450) fungistatic
PO,
adverse issues in HIV pts
Voriconazole
inhibit 14 alpha demethylase (funal p450) fungistatic
PO,
serious invasive aspergillosis,
adverse issues in HIV pts. less toxic than ampho
Terbinafine
inhibits ergesterol synthesis by inhibiting squalene oxidase, and toxic effects from accumulation of squalene.
PO, TOP
tinea cruris and caporis, onychomycosis. fingernail, toe infection, athletes foot
GI upset, headache, rash, interferes with p450
caspofungin
echinocandins. inhibits beta 1,3, D glycan which is part of cell walls
IV, hepatic,
invasive aspergilosis that is resistant to amph and itra
histamine mediated symptoms, (rash, swelling, pruitus, fever, nausea
flucytosine
converted to 5 fluorouracil via cytosine deaminase interfering with DNA synth. (high selectivity)
PO, renal. excellent distribution including CNS
cryptococcosis. Candidiasis, chromoblastomycosis. given with amphiteracin
resistance in fungi that don’t have cytosine deaminase. nausea, vomiting, and w/ prolonged use, bone marrow depression, hair loss
griseofulvin
inhibits protein and nucleic acid synth
IV/IM/inhale
protozoa, P jirovici.
leukopenia, hypoglycemia, hypotension, nephro/hepatotoxicity.