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
Q

mechanism: caspofungin

A

inhibitor of cell wall synthesis

26
Q

caspofungin is administered

A

IV

**highly protein bound, slow metabolism

27
Q

concentrates in keratinized tissue

A

griseofulvin

28
Q

mechanism: grisofulvin

A

block mitosis?

29
Q

adverse effects: griseofulvin

A

teratogenic
CYP inducer
hepatotoxic

30
Q

topical antifungals

A

griseofulvin
terbinafine

31
Q

mechanism: co-trimoxazole

A

DHFR/dihydropteroate synthase inhibitors

32
Q

prophylactic use agains P. jiroveci

A

trimethoprim-sulfamethoxazole

33
Q

only ______ affects tissue shizonts

A

primaquine

34
Q

mechanism: chloroquine

A

alters metabolism of heme by parasite

35
Q

PK: choloquine

A

loading dose necessary for acute treatment

36
Q

clears parasitemia from all four+ plasmodium

A

chloroquine

37
Q

used with primaquine form P. ovale and P. vivax

A

chloroquine

38
Q

preferred drug for prophylaxis for all four species

A

chloroquine

**loading dose 1 week before travel, continue 4 weeks after return

39
Q

adverse effect: chloroquine

A

pruritis

40
Q

primaquine mechanism

A

unsure
tissue schizonticide

41
Q

PK: primaquine

A

metabolites are intracellular oxidants

42
Q

used in combination with chloroquine for prophylaxis or cure of P. vivax, P. ovale

A

primaquine

43
Q

adverse effects: mefloquine

A

psychotropic effects

44
Q

clinical use: mefloquine

A

chloroquine resistant malaria

45
Q

used for chloroquine resistant P. falciparum

A

proguanil or fansidar

46
Q

adverse effect: proguanil

A

SJS

47
Q

effective blood schizonticide for P. falciparum

A

fansidar

48
Q

mechanism: metronidazole

A

amebicid

activated by electron donation, effective for anaerobic/ hypoxic stress

49
Q

used for extraintestinal, intestinal, and urogenital protozoal infections

A

metronidazole

50
Q

used for anaerobic infections

A

metronidazole

51
Q

causes disulfiram effect

A

metronidazole

52
Q

mechanism: pentamidine

A

unknown

53
Q

can be administered via aerosol

A

pentamidine

54
Q

aerosol used for treatment/prophylaxis against pneumocystis

A

pentamidine

55
Q

used for leishmaniasis, sleeping sickness

A

pentamidine

56
Q

given orally, less than 10% absorbed

A

mebendazole

57
Q

rapidly metabolized, secreted in urine

A

mebendazole

58
Q

wide spectrum anti helmintic

A

mebendazole

59
Q

oral treatment for all intestinal strongyloidiasis and onchoceriasias

[head lice, scabies]

A

ivermectin

60
Q

MDR1 substrate

A

ivermectin