Unit 3: K48.Antifungals Flashcards
Downside of antifungals
Lots of side effects
Why do antifungals have so many side effects?
Fungi are eukaryotes, just like human cells
Antifungals that alter cell membrane permeability
Azoles
Polyenes
Terbinafine
What antifungals are used for more serious fungal infections?
Echinocandins
What antifungals are used for severe fungal infections, especially of the scalp?
Griseofulvin
First antifungal available?
Amphotericin B
Amphotericin B has a ______ spectrum
WIDE
Nickname for Amphotericin B…and why?
“Amphoterrible”
Chills, fever, muscle spasms, hypotension
Nephrotoxic
Flucytosine is related to which cancer drug?
5-FU
Flucytosine has a ______ spectrum
NARROW
Side effects for flucytosine (5-FC)
Bone marrow depression
Alopecia
Liver dysfunction
Name some Azoles
Ketoconazole Itraconazole Fluconazole Voriconazole Posaconazole* Isavuconazole*
*rarely used
Azoles: MOA
Interfere with fungal cell membrane permeability
Ketoconazole has a _____ spectrum
NARROW
Ketoconazole can cause _____ when used topically, so it must be used with caution
Hypersensitivity reactions
Angioedema
Fluconazole’s brand name is _____
Diflucan
Fluconazole is
EASY or HARD
to take?
EASY
Fluconazole can be used for
candidiasis, yeast infections, thrush
What antifungal is used for rose thorn scratches?
Itraconazole
What is voriconazole used for?
Candidemia
Invasive aspergillosis
Azole toxicity
Lots of drug interactions
Vomiting, diarrhea, rash
Hepatotoxicity —> monitor liver function
Why are there so many drug interactions with Azoles?
Inhibitor if P450 isozymes; increases levels of many other drugs
Voriconazole can cause…
Visual blurring (immediate but transient)
Griseofulvin is given via what route for what indication?
PO Skin infections (e.g. tinea of the scalp)
Terbinafine is used to treat _____
Nail fungus
Monitor what with Terbinafine?
Liver function
How is Amphotericin B usually given and why?
poorly absorbed through GI tract –> given via IV
Name antifungals that block beta-glucan synthesis
echinocandins
name antifungals that block nucleic acid synthesis
flucytosine
what are the primary drugs for systemic infections?
azoles
Amphotericin B
Echinocandins
Name the steroid unique to fungal cell membranes
ergosterol
How does amphotericin B work?
alters fungal membrane permeability
Name the azole with the broadest spectrum
posoconazole
What azole has a spectrum similar to Posoconazole?
Isavuconazole
What is the mechanism of action for the azoles?
interfere with fungal cell membrane permeability by inhibiting ergosterol synthesis
What anti fungal is related to the anti-cancer drug 5-FU?
flucytosine (5-Fluorocytosine, 5-FC)
Name some topical azoles
clotrimazole
miconazole
ketoconazole
name some topical allyamines
terbinafine
naftilfine