B3-046 Antifungal Chemotherapy Flashcards
mechanism flucytosine
inhibits DNA/RNA synthesis by converting flucytosine to 5-fluorouracil
used with amphotericin B for cryptococcus menigitis
flucytosine
**resistance develops rapidly with monotherapy
PK: flucytosine
orally effective, spreads to CNS
adverse effects: flucytosine
low toxicity as it is not activated in mammalian cells
mechanism: amphotericin B
binds to ergosterol, forms holes in plasma membrane
amphotericin B can be given _______ to CNS
intrathecal
amphotericin B is typically administered
IV
the 1/2 life of amphotericin B is _______
2 weeks
amphotericin B is used for
severe systemic mycoses
**use initially, then switch
adverse effects: amphotericin B
shake and bake
chills, fever, nausea, vomiting, headache
nystatin is _______ for systemic use
too toxic
treatment for oral candidiasis
nystatin
inhibitors of ergosterol synthesis are ________ catalyzed
fungal CYP
mechanism: terbinafine
inhibits squalene epoxidase (ergosterol synthesis)
mechanism: azoles
inhibit ergosterol synthesis by blocking fungal CYPs
adverse effects: ketoconazole
blocks adrenal steroidgenesis [gynecomastia]
inhibits CYP3A4
used as adjunct therapy for prostate cancer
ketoconazole
itraconazole is used for
histo, blasto, sporothrix
most widely used antifungal
fluconazole
fluconazole is administered
oral or IV
fluconazole is ________ for fungal CYPs
more selective
as the newest triazole, voriconazole has improved _______ and __________
bioavailability; less mammalian CYP inhibition
more effective than ampho B against invasive aspergillus
voriconazole
adverse effects: voriconazole
visual disturbances
mechanism: caspofungin
inhibitor of cell wall synthesis
caspofungin is administered
IV
**highly protein bound, slow metabolism
concentrates in keratinized tissue
griseofulvin
mechanism: grisofulvin
block mitosis?
adverse effects: griseofulvin
teratogenic
CYP inducer
hepatotoxic
topical antifungals
griseofulvin
terbinafine
mechanism: co-trimoxazole
DHFR/dihydropteroate synthase inhibitors
prophylactic use agains P. jiroveci
trimethoprim-sulfamethoxazole
only ______ affects tissue shizonts
primaquine
mechanism: chloroquine
alters metabolism of heme by parasite
PK: choloquine
loading dose necessary for acute treatment
clears parasitemia from all four+ plasmodium
chloroquine
used with primaquine form P. ovale and P. vivax
chloroquine
preferred drug for prophylaxis for all four species
chloroquine
**loading dose 1 week before travel, continue 4 weeks after return
adverse effect: chloroquine
pruritis
primaquine mechanism
unsure
tissue schizonticide
PK: primaquine
metabolites are intracellular oxidants
used in combination with chloroquine for prophylaxis or cure of P. vivax, P. ovale
primaquine
adverse effects: mefloquine
psychotropic effects
clinical use: mefloquine
chloroquine resistant malaria
used for chloroquine resistant P. falciparum
proguanil or fansidar
adverse effect: proguanil
SJS
effective blood schizonticide for P. falciparum
fansidar
mechanism: metronidazole
amebicid
activated by electron donation, effective for anaerobic/ hypoxic stress
used for extraintestinal, intestinal, and urogenital protozoal infections
metronidazole
used for anaerobic infections
metronidazole
causes disulfiram effect
metronidazole
mechanism: pentamidine
unknown
can be administered via aerosol
pentamidine
aerosol used for treatment/prophylaxis against pneumocystis
pentamidine
used for leishmaniasis, sleeping sickness
pentamidine
given orally, less than 10% absorbed
mebendazole
rapidly metabolized, secreted in urine
mebendazole
wide spectrum anti helmintic
mebendazole
oral treatment for all intestinal strongyloidiasis and onchoceriasias
[head lice, scabies]
ivermectin
MDR1 substrate
ivermectin