antifungals Flashcards
(90 cards)
what type of fungal infections are life threatening
systemic infections
what populations are often affected by fungal infections
immunosuppressed
chronic immune suppression
undergoing chemotherapy
HIV/AIDS
etc
what are the superficial fungal infections
pityriasis versicolor
tinea nigra
what are cutaneous fungal infections
dermatophytosis (skin, hair and nails) (tineas)
candidiasis of skin (breast, armpits, inguinal folds)
what are subcutaneous fungal infections
sporotrichosis (rose-gardeners)
chromomycosis
what are systemic fungal infections
coccidioidomycosis
histoplasmosis
blastomycosis
cryptococcosis
systemic candidiasis
aspergillosis
zygomycetes (mucorales)
what are the different categories of antifungal drugs
Polyenes
Zadoles
Echinocandins
allylamines
other
what are the polyene antifungal medications
amphotericin B
Nystatin (potent)
what are the Zoles antifungal medications
clotrimazole
ketoconazole
fluconazole
itraconazole
posaconazole
posaconazole
voriconazole
what are echinocandin medications
caspofungin
what are allylamines
terbinafine
what are the other antifungal drugs
flucytosine
griseofulvin
what is the MOA for amphotericin B
lipophilic rod-like molecule disrupts fungal cell wall synthesis by binding to sterols, primarily ergosterol, leading to formation of pores in the cell membrane. K+ leaks out of cell resulting in cell death.
what is amphotericin B produced by
streptomyces nodosus
when is amphotericin B used
treatment of severe invasive fungal infection
widest spectrum of activity of all antifungals
rapid onset
resistance is rare
what are the pharmacokinetics of amphotericin B
metabolism poorly understood
poor PO absorption. Used IV - wide tissue distribution
little CSF penetration; intrathecal sometimes used
low TI
Nephrotoxicity - azotemia due to dose-dependent decrease in GFR
what are the AE of amphotericin B
infusion related reactions:
fever and rigors
decreased incidence following multiple doses
pre-medicate with Tylenol or Benadryl recommended
may treat rigors with low-dose meperidine
Nausea/vomiting, anemia, phlebitis
What is flucytosine
5-FC
synthetic pyrimidine analog (false nucleotide)
what is the MOA for Flucytosine
inhibits thymidylate synthase and incorporates into fungal RNA disrupting nucleic acid and protein synthesis
NOT used as monotherapy; resistance too high
what is the spectrim of activity for flucytosine
used in combo with ampotericin B (synergistic) for tx of systemic mycoses and meningitis caused by cryptococcus and candida spp.
used in combo with itraconazole for treatment of chromoblastomycosis infections
What needs to be monitored when using amphotericin B
K+, Mg++; replete aggressively in the presence of decreased GFR
What are the pharmacokinetics of Flucytosine
good PO absorption, penetrates CSF
dose adjustment required in renal impairment
what are the AE of flucytosine
reversible neutropenia, thrombocytopenia
dose-related bone marrow suppression
reversible hepatic dysfunction
more common: GI upset, N/V, diarrhea
What are the two groups of azoles
imidazole and triazoles