Flashcards in Antifungfal Drugs Deck (24)
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1
amphotericin B: use, mechanism, side effect
-broad spectrum for most systemic mycoses
-binds ergosterol in fungal membranes producing membrane instability/leakage
-side effect: nephrotoxicity
2
flucytosine: use, mechanism, side effect
-serious infections due to Candida and Cryptococcus
-converted by fungal enzyme to 5-FU, whose metabolites then bock nucleic acid synthesis
-side effect: nephrotoxicity
3
imidazoles/triazoles: mechanism, drug names
-inhibit enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
-FIV: fluconazole, itraconazole, voriconazole
4
fluconazole: mechanism, candida spectrum (sites, species), use other than Candida
-inhibits enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
-sites: CNS and urinary
-least: some albicans and glabrata, no krusei
-Cryptococcus meningitis
5
itraconazole: mechanism, candida spectrum (sites, species), uses other than Candida
-inhibits enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
-sites: esophageal and oropharyngeal
-intermediate: albicans, glabrata, some krusei
-Blastomyces, Histoplasma
6
voriconazole: mechanism, candida spectrum (sites, species), use other than Candida
-inhibits enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
-sites: not urinary
-broad: covers many species
-invasive Aspergillus
7
list imidazoles/triazoles from broadest to least broad candida spectrum
voriconazole, itraconazole, fluconazole
8
imidazole/triazole with CNS penetration
fluconazole
9
which antifungals can cause nephrotoxicity?
amphotericin B and flucytosine
10
imidazole/triazole used against crpytococccus meningitidis
fluconazole
11
imidazole/triazole used against blastomyces and histoplasma
itraconazole
12
antifungals used to treat invasive Aspergillus
voriconazole, caspofungin
13
imidazole/triazole that has risk of serious cardiovascular events/death?
itraconazole
14
side effects of imidazole/triazoles?
-mild hepatotoxicity
-potent inhibitors of many CYP enzymes
15
caspofungin: uses, mechanism
-invasive Aspergillus, Candida (esophageal and systemic)
-inhibits fungal cell wall synthesis by blocking synthesis of beta(1,3)-D-glucan
16
drugs used to treat superficial Candida infections
FACIN: fluconazole, clotrimazole, itraconazole, nystatin, amphotericin B
17
nystatin: use, mechanism
-superficial Candida infections
-mechanism similar to amphotericin B: binds ergosterol in fungal membranes producing membrane instability/leakage
18
treatment of ophthalmic fungal infections
natamycin
19
natamycin: use, mechanism
-treatment of ophthalmic fungal infections
-mechanism similar to amphotericin B: binds ergosterol in fungal membranes producing membrane instability/leakage
20
only FDA-approved topical Rx for fungal nail infections
ciclopirox
21
terbinafine: use, mechanism
-oral preparation for severe dermatophyte infections refractory to topical therapy
-inhibits fungal squalene epoxidase; fungicidal
22
inhibits fungal squalene epoxidase
terbinafine
23
inhibit enzyme that converts lanosterol to ergosterol, depriving membranes of ergosterol
imidazole/triazoles: fluconazole, itraconazole, voriconazole
24