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PHRM 865 > Stahlein > Flashcards

Stahlein Flashcards

1
Q

difference in cell membranes of fungal and human cells

A

fungal cells have ergosterol
human cells have cholesterol

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2
Q

why do we target ergosterol synthesis?

A

antifungal drugs target ergosterol and its biosynthesis to selectively affect fungal cells without harming human cells

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3
Q

which enzyme do allylamines (terbinafine) inhibit

A

squaline epoxidase

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4
Q

which enzyme do azoles inhibit

A

CYP450 14-alpha demethylase

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5
Q

amphotericin B class and MOA

A

polyenes
binds ergosterol and forms pores in membrane

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6
Q

amphotericin B selectivity

A

binds ergosterol better than cholesterol

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7
Q

amphotericin B toxicities

A

infusion related toxicities
renal damage

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8
Q

reversible amphotericin B toxicity

A

reduced renal perfusion

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9
Q

irreversible amphotericin B toxicity

A

renal tubular injury

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10
Q
A

amphotericin B
polyenes
binds ergosterol and forms pores in membrane

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11
Q

nystatin MOA and class

A

polyene
binds ergosterol and forms pores in membrane

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12
Q

nystatin dosage form

A

topical

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13
Q

terbinafine MOA and class

A

allylamines
inhibit squaline epoxidase to disrupt ergosterol synthesis

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14
Q

terbinafine selectivity

A

selective for fungal enzyme over mammalian

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15
Q
A

terbinafine
inhibits squaline epoxidase

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16
Q

azoles MOA

A

inhibition of 14-alpha demethylase by nitrogen binding iron in CYP450
inhibits conversion of lanosterol to ergosterol

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17
Q

azole structure

A
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18
Q
A

ketoconazole
dioxy ring and azole ring

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19
Q
A

itraconazole
triazole (3Ns)

20
Q
A

fluconazole
2Fs and OH
2 triazoles

21
Q
A

voriconazole
one F
triazole

22
Q
A

posconazole
furan ring

23
Q
A

isavuconazole
prodrug
has sulfur group

24
Q
A

osteoconazole
3 Fs

25
Q

caspofungin, micafungin, anidulafungin, rezafungin MOA and class

A

echinocandins
inhibit synthesis of beta 1-3 glucan cell wall component

26
Q

echinocandins selectivity

A

no enzyme in mammalian cells like beta glucan

27
Q
A

echinocandins
inhibit synthesis of beta 1-3 glucan synthesis

28
Q

rezafungin considerations

A

once weekly IV injection
long half life
BIG structure

29
Q
A

rezafungin

30
Q

ibrexafungerp MOA

A

small molecule inhibitor of glucan synthase enzyme

31
Q
A

ibrexafungerp
small molecule inhibitor of glucan synthase enzyme

32
Q

flucytosine class and MOA

A

antimetabolite
inhibits thymidylate synthase which interferes with protein synthesis

33
Q

flucytosine selectivity

A

metabolized in fungal cells to 5-FU by cytosine deaminase which we lack

34
Q
A

flucytosine
inhibits thymidylate synthase which interferes with protein synthesis

35
Q

tavaborole MOA

A

inhibits leucyl transfer RNA synthase (LeuRS) which inhibits protein synthesis

36
Q
A

tavaborole
inhibits leucyl transfer RNA synthase (LeuRS) which inhibits protein synthesis

37
Q

amphotericin B and flucytosine toxicity consideration

A

both have renal tox but when used in combo we can use lower doses of amphotericin B

38
Q

how does amphotericin B help flucytosine concentrations

A

amphotericin B creates pores in membrane which allows more flucytosine in

39
Q

which antifungal has CYP450 interactions

A

azoles! - inhibitors and substrates

40
Q

how do CYP3A4 interactions work with azoles

A

increase concentrations of other drugs
CYP inducers would decrease azole concentrations

41
Q

which drug is a potent CYP3A4 inhibitor

A

ketoconazole
increases half life of cyclosporine and triazolam

42
Q

which drug is a 2C19 substrate

A

voriconazole

43
Q

what does the azole functional group do

A

nitrogen binds with iron to prevent formation of the intermediate

44
Q

what reaction does thymidylate synthase catalyze

A

dUMP to fDUMP

45
Q

how does flucytosine decrease DNA synthesis

A

inhibits thymidylate synthase so dTMP can not be formed

PHRM 865 (31 decks)

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