Antifungals Flashcards
what do echinocandins target
B-1,3-glucan synthase (part of the cell wall)
give some examples of echinocandins and state side effects
end in FUNGIN micafungin caspofungin anidulafungin minimal side effects
what are echinocandins used for
aspergillus
candida
not certain moulds like Cryptococcus
parenteral administration for systemic infections
what do polyenes target
directly target ergosterol in the cell membrane
form an association–> pore like molecular aggregates –> potassium leakage and death
give 2 types of polyenes
amphotericin B and nystatin
what is nystatin used for
only superficial not systemic (as toxic)
oral/ vaginal candidiasis
what is amphotericin B used for
v. broad spectrum
systemic infections such as crypotoccus, aspergillus, candida
parenteral not oral administration
how is amphotericin B often given
as lipid associated Amphotericin B formulations to decrease nephrotoxicity
what are the negatives of amphotericin B
nephrotoxicity and allergic reactions
what is the target of allylamines
squalene epoxidase –> needed for formation of ergosterol in cell membrane
what are the uses of allylamines
dermatophyte infections
give an example of an allylamine
terbinafine
which infections is terbinafine administered topically for
tinea corporis
tinea pedis
tinea cruris
which infections is terbinafine administered orally
onychomycosis
tinea capitis
what do azoles target
lanosterol 14a demethylase
what are the 2 types of azole
imidazoles (2n) and triazoles (3n)
what are the main side effects of allyamines
hepatotoxicity
jaundice hepatitis
what are the main side effects of azoles
hepatotoxicity
what are the drug interactions of azoles
inhibit CP450 enzymes
name some imidazoles
clotrimazole
miconazole
ketoconazole
what are imidazoles used to treat
rarely systemic infections
superficial infections e.g. candidiasis, dermatophyte infections
name some triazoles
fluconazole itraconazole voriconazole posaconazole isavuconazole
what is the spectumof fluconazole
yeasts not aspergillus
what is the spectrum of itraconazole and voriconazole
yeasts and aspergillus
what is the spectrum of posaonaole and isavuconazole
yeasts aspergillus mucoraceous moulds
which antifungals need therapeutic drug monitoring
itraconaole
coriconazole
5-fluorocytosine
what is 5-fluorocytosine
developed as an anti-cancer drug
targets DNA synthesis (and RNA/ protein synthesis)
cytosine permease uptake means selective toxicity
what is the negative of 5-fluorocytosine
BM suppression
what is 5-flurocytosine used for
only yeasts such as candida and cryptococcus
what is used to treat cryptococcal meningitis
5-fluorocytosine and amphotericin B
what targets mitosis
griseofulvin
what side effects does griseofulvin have
minimal side effects
what is griseofulvin used for
dermatophyte infections in children requiring systemic treatment
kerion (fungal abscess)
onychomycosis