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Antifungals
Drugs
21
Chemistry
12th Grade
12/11/2012

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Cards

Term
Polyenes (have a lot of double bonds)
Definition
Amphotericin B, Nystatin
Term
isolated from Streptomyces nodosus (used systemically)
Definition
Amphotericin B
Term
isolated from S. noursei (not used systemically)
Definition
Nystatin
Term
Imidazole antifungals
Definition
Clotrimazole, Miconazole, Econazole, Tioconazole, Ketoconazole
Term
Only Imidazole that is available for systemic use (others are for topical)
Definition
Ketoconazole
Term
Inhibit fungal C-14 demethylase in ergosterol biosynthesis (A P450 enzyme, accumulation of lanosterol
Definition
Imidazoles and triazoles
Term
five membered ring with 2 nitrogens in it
Definition
imazole
Term
five membered ring with 3 nitrogens in it
Definition
triazole
Term
Most commonly used to treat candidiasis resistant to nystatin; non-meningeal crytococcal disease
Definition
Ketoconazole
Term
Triazole antifungals
Definition
Traconazole, Terconzole, Fluconazole
Term
Lack of pH dependence on oral bioavailability, less effect on human steroid metabolism
Definition
1,2,4-Triazoles
Term
much weaker base than imidazole (pKa ~2)
Definition
1,2,4- Triazoles
Term
single-dose treatment for vaginal candidiasis; step-down therapy after amphotericin B
Definition
Fluconazole
Term
"Pulse" treatment for onychomycosis
Definition
Itraconazole
Term
Vaginal suppository for candidiasis
Definition
Terconazole
Term
Allylamines and related amines
Definition
Terbinafine, Naftidine, Butenafine
Term
A benzylamine
Definition
Butenafine
Term
Inhibit squalence epoxidase (SQLE) in ergosterol synthesis; fungistatic activity limited to dermatophytes (not active against Candida sp)
Definition
Allylamines and related amines
Term
oral formulation available; requires LFTs to monitor hepatotoxicity
Definition
terbinafine
Term
converted by yeast cytosine deaminase then activated to 5-FdUMP; Irreversible inhibition of thymidylate synthase
Definition
Flucytosine
Term
Flucytosine (5-FC)
Definition
fungistatic against Candida and Crytococcus; secondary resistance develops rapidly
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