Antifungals Flashcards
What is the mechanism for Amphociterin B, and is there anything unique about it?
binds to ergosterol and creates membrane pores.
good for yeasts. Broadest spectrum antifungal.
Highly protein bound.
What is the mechanism for Flucytosine (5-FC), and is there anything unique about it?
inactive until taken up by fungal cytosine permease. Inhibits DNA and RNA synthesis.
Only usefor for crypt neoformans and chromoblastomycosis by molds.
Bone marrow toxicity and narrow therapeutic window.
Often synergized with other antifungals
What is the mechanism for Azoles class drugs, and is there anything unique about it?
inhibits ergosterol synthesis by inhibiting fungal P450s.
Not very toxic to humans.
What is the mechanism for ketoconazole, and is there anything unique about it?
inhibits ergosterol production by inhibiting fungal P450s.
Strongly inhibits human P450 as well and causes impotence. Not commonly used anymore.
What is the mechanism for itraconazole, and is there anything unique about it?
inhibits ergosterol synthesis by inhibition of fungal P450s.
Choice for histoplasma and other dimorphic fungi.
What is the mechanism for fluconazole, and is there anything unique about it?
inhibits ergosterol synthesis by inhibition of fungal P450s.
Few drug interactions. Commonly used as a prophylactic or to treat crypto meningitis
What is the mechanism for voriconazole, and is there anything unique about it?
inhibits ergosterol synthesis by inhibition of fungal P450s.
inhibits human CYP 3A4 and causes rash and visual disturbances.
What is the mechanism for posaconazole, and is there anything unique about it?
inhibits ergosterol synthesis by inhibition of fungal P450s.
Liquid oral form, absorbed with high fat meals. Broadest spectrum azole.
Inhibits CYP3A4
What is the mechanism for echinocandin class drugs, and is there anything unique about it?
(-fungins) Inhibit synthesis of beta(1-3) glucan, which disrupts fungal cell walls to kill. Cause GI irritation.
What is the mechanism for caspofungin, and is there anything unique about it?
echinocandin, Inhibit synthesis of beta(1-3) glucan, which disrupts fungal cell walls to kill.
Highly protein bound. Only used if amph B not working.
What is the mechanism for micafungin, and is there anything unique about it?
echinocandin, Inhibit synthesis of beta(1-3) glucan, which disrupts fungal cell walls to kill.
CYP inhibition
What is the mechanism for anidulfungin, and is there anything unique about it?
echinocandin, Inhibit synthesis of beta(1-3) glucan, which disrupts fungal cell walls to kill.
Histamine release with IV.
What is the mechanism for griseofulvin, and is there anything unique about it?
oral systemic drug, binds to keratin in developing skin to protect from new infections.
Causes allergic syndrome like serum sickness.
Interactions with warfarin.
What is the mechanism for terbinafine, and is there anything unique about it?
oral systemic drug, binds to keratin and inhibits squalene epoxidase and blocks ergosterol synthesis.
Few interactions or adverse effects
What is the mechanism for nystatin, and is there anything unique about it?
topical antifungal, used for candida.
Extremely toxic by any delivery besides topical.
