Antifungals Flashcards
Griseofulvin
-Acts on microtubules
MOA: interferes with fun and disrupts mitosis
Adverse: teratogenic, carcinogen, confusion, disulfiram-like rxn, increase cytochrome P450 and warfarin metabolism
Use: oral treatment of superficial and inhibits growth of dermatophytes
Nystatin
Target: ergosterol
MOA: creates pores to cause rapid leakage of monovalent ions
Adverse: topical only because its toxic
Use: swish and spit for oral thrush, topical for diaper rash or vaginal candidiasis
Azoles
Target: 14-alpha-demethylase
MOA: inhibits fungal ergosterol synthesis
MOR: with prolonged use and immunocompromised host
Adverse: testosterone synthesis inhibition, CYP450 inhibition, QT prolongation, itraconazole - cardiomyopathy, voriconazole - CNS and visual disturbances
Use: fluconazole is best for CNS infection
Isavuconazole for aspergillus and mucorales
Voriconazole is choice for aspergillus and candida
Ketoconazole was first gen and not used now
Echinocandins
-caspofungin and micafungin
Target: B Glucan
MOA: inhibition of cell wall synthesis
MOR: alteration to glucan synthase and efflux pump in candida
Adverse: some histamine release with infusion
Use: invasive aspergillosis, candida spp.
-can penetrate to eyes and CNS
Terbinafine
Target: squalene epoxidase
MOA: inhibition of ergosterol
Adverse: GI upset, h/a, hepatotoxic, taste disturbance
Use: dermatophytes
5-Flucytosine
MOA: inhibits DNA and RNA synthesis by converting 5-FC by cytosine deaminase
MOR: increased pyrimidine salvage
Adverse: GI symptoms, hepatoxicity, bone marrow suppression
Use: with Amphotericin B for cryptococcal meningitis
Amphotericin B
Target: ergosterol
MOA: pore generation to cause rapid leakage of monovalent ions
Adverse: Shake and bake, infusion rigors, fever - use meperidine and acetaminophen for prophylaxis, nephrotoxic that can be irreversible, muscle and joint pain
Spectrum: broadest and most use, serious systemic mycoses
Liposomal Amphotericin B
-can more easily access CNS than AmB
