Antifungals Flashcards
amphotericin B MOA
cidal
interacts with ergosterol in fungal membrane, results in pore formation that increases permeability which leads to cell death
DOC for most systemic fungal infections
Amphotericin B
amphotericin B infusion toxicites
chills, fevers, muscle spasms, vomiting, headache
amphotericin B cumulative toxicities
powerful nephrotoxic agent (azotemia, BUN and crea)
can lead to irreversible kidney damage
MOA for flucytosine
metabolic antagonism of fungal DNA and RNA
converted to 5-fluorouracil which interferes with synthesis
DOC for cryptococcus infections
Flucytosine + Amp B (synergistic)
Does flucytosine penetrate CNS?
Yes
All flu drugs are good CNS penetrators
toxicities of flucytosine
depression of bone marrow, GI disturbances, elevation of AST or ALT
MOA for “azole” antifungals
static
inhibits synthesis of ergosterol and eventually inhibition of fungal growth
spectrum for ketoconazole
broad spectrum, good for topical infections
ketoconazole toxicities
inhibitor of P450 system, gynecomastia and impotence, prolonged QT
ketoconazole contraindications
acute or chronic hepatic disease
fluconazole penetration
penetrates well into other bodily fluids, particularly CSF
Fluconazole in HIV patients?
good for suppressive and/or prophylactic therapy in HIV patients
Toxicities of fluconazole
potent inhibitor of CYP2C9, but less drug interactions than other azoles, headache (due to CNS penetration)