Pharm - Antifungals - General Flashcards
polyenes
amphotericin B
nystatin
azoles
fluconazole
voriconazole
posconazole
itraconazole
echinocandins
caspofungin
pyrimidine inhibitors
flucytosine
allylamines
terbinafine
Amphotericin B
MOA
binds ergosterol in cell membrane –> pore formation and efflux of K –> cell death
Amphotericin B
use
BROADEST spectrum
- mucorales infections
- candida
- cryptococcal meningitis
- severe endemic mycoses
Amphotericin B
AE
2 major toxicities
- infusion related (CK release)
- nephrotoxicity (distal RTA)
- fever/chills
- phlebitis
- hypOtension
- arrythmias
- nephrotoxicity
- hypOMg
- hypOkalemia
- nephrogenic DI
Nysatin
MOA/USE/AE
MOA: binds ergosterol
USE: thrush/diaper rash
AE: tox when IV, use topical only
terbinafine
MOA/USE/AE
MOA: blocks squalene epoxidase (essential for ergosterol synthesis)
USE: dermatophyte infec (skin, nails)
AE: HA hepatotoxicity blurry vision taste change
which azole is least used due to tox
ketoconazole
-azoles
MOA
MOA: block ergosterol synthesis, inhibit p450 enzyme that converts lanosterol to ergosterol
-azoles
AE
- metabolized by p450 (drug interactions)
- hepatotoxicity
- transaminitis
- QT prolong
fluconazole
use
- excellent against cryptococcus neoformans
- active against Candida, coccidiodes
voriconazole
AE:
- if CYP2C19 polymorphism –> can vary metabolism
- inhibits CYP43A4 –> drug interactions
- visual changes
- hallucinations
- photosensitivity rash
- QT prolongation