B3-046 Antifungal Chemotherapy Flashcards

1
Q

mechanism flucytosine

A

inhibits DNA/RNA synthesis by converting flucytosine to 5-fluorouracil

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2
Q

used with amphotericin B for cryptococcus menigitis

A

flucytosine

**resistance develops rapidly with monotherapy

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3
Q

PK: flucytosine

A

orally effective, spreads to CNS

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4
Q

adverse effects: flucytosine

A

low toxicity as it is not activated in mammalian cells

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5
Q

mechanism: amphotericin B

A

binds to ergosterol, forms holes in plasma membrane

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6
Q

amphotericin B can be given _______ to CNS

A

intrathecal

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7
Q

amphotericin B is typically administered

A

IV

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8
Q

the 1/2 life of amphotericin B is _______

A

2 weeks

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9
Q

amphotericin B is used for

A

severe systemic mycoses

**use initially, then switch

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10
Q

adverse effects: amphotericin B

A

shake and bake
chills, fever, nausea, vomiting, headache

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11
Q

nystatin is _______ for systemic use

A

too toxic

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12
Q

treatment for oral candidiasis

A

nystatin

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13
Q

inhibitors of ergosterol synthesis are ________ catalyzed

A

fungal CYP

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14
Q

mechanism: terbinafine

A

inhibits squalene epoxidase (ergosterol synthesis)

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15
Q

mechanism: azoles

A

inhibit ergosterol synthesis by blocking fungal CYPs

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16
Q

adverse effects: ketoconazole

A

blocks adrenal steroidgenesis [gynecomastia]

inhibits CYP3A4

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17
Q

used as adjunct therapy for prostate cancer

A

ketoconazole

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18
Q

itraconazole is used for

A

histo, blasto, sporothrix

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19
Q

most widely used antifungal

A

fluconazole

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20
Q

fluconazole is administered

A

oral or IV

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21
Q

fluconazole is ________ for fungal CYPs

A

more selective

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22
Q

as the newest triazole, voriconazole has improved _______ and __________

A

bioavailability; less mammalian CYP inhibition

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23
Q

more effective than ampho B against invasive aspergillus

A

voriconazole

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24
Q

adverse effects: voriconazole

A

visual disturbances

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25
mechanism: caspofungin
inhibitor of cell wall synthesis
26
caspofungin is administered
IV **highly protein bound, slow metabolism
27
concentrates in keratinized tissue
griseofulvin
28
mechanism: grisofulvin
block mitosis?
29
adverse effects: griseofulvin
teratogenic CYP inducer hepatotoxic
30
topical antifungals
griseofulvin terbinafine
31
mechanism: co-trimoxazole
DHFR/dihydropteroate synthase inhibitors
32
prophylactic use agains P. jiroveci
trimethoprim-sulfamethoxazole
33
only ______ affects tissue shizonts
primaquine
34
mechanism: chloroquine
alters metabolism of heme by parasite
35
PK: choloquine
loading dose necessary for acute treatment
36
clears parasitemia from all four+ plasmodium
chloroquine
37
used with primaquine form P. ovale and P. vivax
chloroquine
38
preferred drug for prophylaxis for all four species
chloroquine **loading dose 1 week before travel, continue 4 weeks after return
39
adverse effect: chloroquine
pruritis
40
primaquine mechanism
unsure tissue schizonticide
41
PK: primaquine
metabolites are intracellular oxidants
42
used in combination with chloroquine for prophylaxis or cure of P. vivax, P. ovale
primaquine
43
adverse effects: mefloquine
psychotropic effects
44
clinical use: mefloquine
chloroquine resistant malaria
45
used for chloroquine resistant P. falciparum
proguanil or fansidar
46
adverse effect: proguanil
SJS
47
effective blood schizonticide for P. falciparum
fansidar
48
mechanism: metronidazole
amebicid activated by electron donation, effective for anaerobic/ hypoxic stress
49
used for extraintestinal, intestinal, and urogenital protozoal infections
metronidazole
50
used for anaerobic infections
metronidazole
51
causes disulfiram effect
metronidazole
52
mechanism: pentamidine
unknown
53
can be administered via aerosol
pentamidine
54
aerosol used for treatment/prophylaxis against pneumocystis
pentamidine
55
used for leishmaniasis, sleeping sickness
pentamidine
56
given orally, less than 10% absorbed
mebendazole
57
rapidly metabolized, secreted in urine
mebendazole
58
wide spectrum anti helmintic
mebendazole
59
oral treatment for all intestinal strongyloidiasis and onchoceriasias [head lice, scabies]
ivermectin
60
MDR1 substrate
ivermectin