antifungal medchem Flashcards

1
Q

2 most common mechanisms of antifungal agents

A
  • prevention of biosynthesis

- binding of ergosterol

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2
Q

secondary mechanisms of antifungals

A
  • cell wall disruption

- similar to cancer drugs

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3
Q

amphotericin B MoA

A

binds ergosterol

*conjugated double bonds increases specificity

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4
Q

amphotericin class

A

polyene membrane disrupter, increasing leakiness

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5
Q

nystatin MoA

A

binds ergosterol

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6
Q

nystatin class

A

polyene membrane disrupter, increasing leakiness

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7
Q

amphotericin use

A

systemic fungal infection

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8
Q

nystatin use

A

topical or oral (thrush)

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9
Q

two enzymes involved in biosynthesis

A

squalene epoxide

14alpha demethylase

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10
Q

fluconazole MoA

A

14alpha demethylase inhibitor

triazole rings bind to p450 heme

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11
Q

ketoconazole MoA

A

14alpha demethylase inhibitor

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12
Q

avoid what with ketoconazole

A

divalent cations

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13
Q

terconazole MoA

A

14 alpha demethylase inhibitor

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14
Q

terconazole route

A

topical

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15
Q

itraconazole route

A

oral

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16
Q

voriconazole MoA

A

14 alpha demethylase inhibitor

17
Q

issue with voriconazole

A

extensive p450 metabolism so many drug interactions

18
Q

14 alpha demethylase inhibitor that is prodrug

A

isavuconazonium sulfate

19
Q

squalene epoxidase inhibitors

A

naftifine
butenafine
terbinafine

20
Q

squalene epoxidase inhibitor SAR

A

allyl amines with napthalene group to mimic squalene

21
Q

caspofungin MoA

A

inhibits cell wall biosynthesis

1,3-beta-D-glucan synthase

22
Q

flucytosine MoA

A

converted to 5-FUMP and/or 5-FdUMP which inhibits protein/DNA synthesis

23
Q

flucytosine use

A

in conjunction with amphotericin B

24
Q

flucytosine side effects

A

GI due to gut flora also being affected

25
Q

Griseofulvin MoA

A

binds tubulin to prevent mitosis

26
Q

griseofulvin use

A

skin and nail infections because it gets taken into keratin

oral