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Pharmacology > Antifungals > Flashcards

Antifungals Flashcards

1
Q

What antifungal class does amphotericin B belong to?

A

polyene antifungal

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2
Q

How does amphotericin B achieve its cidal activity?

A

binds to ergosterol to form pores

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3
Q

What is the DOC for most systemic antifungal infections?

A

amphotericin B

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4
Q

Does amphotericin B have CNS activity?

A

No

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5
Q

If a patient is receiving an amphotericin B infusion, what immediate side effects would you expect to see?

A

Shake and bake sxs

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6
Q

does the presence of acute side effects during amphotericin B infusion warrant a dose change?

A

no, you can lower the rate

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7
Q

how long is the course of tx for amphotericin B?

A

6wks to 4 months

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8
Q

describe the long-term side effects of amphotericin b…

A

extremely nephrotoxic

elevated BUN and serum creatinine (azotemia)

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9
Q

What is flucytosine converted to in the body, and what does it act against?

A

converted to 5-F-U, acts against DNA/RNA synthesis

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10
Q

What is the DOC for cryptococcus infections?

A

Flucytosine + amphotericin B

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11
Q

Flucytosine acts against cryptococcus neoformans. What else is it active against?

A

candida, aspergillus fumigatus, sporotrichum

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12
Q

What is a serious side effect of flucytosine?

A

depression of bone marrow

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13
Q

What labs could be elevated during flucytosine tx? Are they concerning? Why?

A

ALT, AST elevation

Reversible upon discontinuation of drug

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14
Q

What do Azole drugs inhibit? does this lead to static or cidal activity?

A

inhibit ergosterol

static

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15
Q

describe the tissue distribution of ketoconazole

A

widely distributed

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16
Q

describe the spectrum of ketoconazole…

A

broad spectrum antifungal

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17
Q

what does ketoconazole inhibit, leading to what adverse effects?

A

P450 inhibitor, has many drug interactions

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18
Q

what are 2 major adverse effects of ketoconazole?

A
  1. gynecomastia and impotence due to inhibited adrenal and testicular fx
  2. prolonged QT
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19
Q

What contraindicates the administration of ketoconazole?

A

acute or chronic hepatic disease

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20
Q

under what circumstances should oral ketoconazole administration be considered?

A

only when no other antifungal therapy can be used

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21
Q

does fluconazole have good CNS penetration?

A

yes

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22
Q

Which azole antifungal makes a good suppressive or prophylactic therapy for HIV/AIDS patients?

A

fluconazole

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23
Q

which CYP does fluconazole inhibit, and should that concern you?

A

CYP2C9. not concerning due to limited nature of CYP2C9 activity compared to ketoconazole’s CYP450 activity

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24
Q

Can amphotericin B be administered w/ aminoglycosides? why?

A

with caution due to synergistic nephrotoxicity

25
Q

when giving fluconazole for suppresive therapy, describe the duration of tx.

A

lifelong or until CD4 count elevates

26
Q

what is the most common side effect of fluconazole?

A

headache

27
Q

what is the DOC for aspergillus infection?

A

Voriconazole + ampho B

“VORacious AMPHOtite for asparagus”

28
Q

voriconazole + ampho B is the DOC for aspergillosis. what else does voriconazole treat?

A

esophageal candidiasis

salvage tx of scedosporium and fusarium sp.

29
Q

Voriconazole is metabolized greatest by CYP2C19. But Voriconazole also inhibits P450s. explain how it can still be metabolized by P450 enzymes…

A

CYP2C19 has the greatest action against voriconazole, least inhibited by voriconazole

30
Q

What is a major adverse effect of voriconazole?

A

Can cause reversible visual impairment

31
Q

Describe the spectrum of itraconazole

A

similar spectrum to ketoconazole and fluconazole but with greater activity against aspergillus

32
Q

what are the adverse reactions of itraconazole?

A

GI upset, NV…

CYP3A4 inhibition

33
Q

Describe the bioavailability of itraconazole as capsules…

A

40-55% on empty stomach, 90-100% w/ meal or cola

34
Q

describe the bioavailability of itraconazole as an oral solution

A

55% w/ meal, and 72% under fasting conditions

35
Q

What 3 species of

fungus does isavuconazonium tx?

A

aspergillus, mucor, rhizopus

36
Q

Does isavuconazonium have drug interations?

A

yes, substrate for and moderate 3A4 inhibition

37
Q

What 2 adverse effects can occur w/ isavuconazonium administration…

A

Nephro

decrease QT

38
Q

When is isavuconazonium contraindicated?

A

pt. c family hx of short QT syndrome

39
Q

describe the sprectrum of posaconazole…

A

tx of aspergillus and candida

40
Q

does posaconazole interact w/ other drugs?

A

yes–3A4 substrate and inhibitor

41
Q

what antibiotic can echinocandins be compared to?

A

these drugs are the “fungal PCN”

42
Q

why is caspofungin known as a “penicillin of antifungals”

A

because it is cidal and inhibits cell wall synthesis

43
Q

does caspofungin come w/ drug interactions or nephrotoxicity?

A

no

44
Q

when should you consider caspofungin in refractory patients?

A

for invasive aspergillosis w/ azole/ampho b resistant fungi

45
Q

what side effects should you educate pts on w/ caspofungin administration?

A

elevated AST/ALT, histamine release/flushing, HA, Chills, GI

46
Q

how do echino candins work?

A

inhibit cell wall synthesis of b(1,3)-D-glucan

47
Q

What are the topical antifungals?

A

grisofulvin, terbinafine, nystatin

48
Q

What diseases do topical antifungals like griseofulvin, terbinafine and nystatin treat?

A

dermatophytosis, onychomycosis

49
Q

what is the DOC for onychomycosis and why?

A

griseofulvin–binds to keratin

50
Q

what are major adverse effects of griseofulvin?

A

Disulfiram-like effects, ohotosensitivity, GI sxs, headache, CNS

51
Q

what contraindicates the use of griseofulvin?

A

acute intermittent porphyria

hepatocellular failure

pregnancy, men 6 months prior to fathering child

52
Q

what is the moa of terbinafine?

A

inhibits ergosterol synthesis by inhibiting squalene epoxidase

53
Q

where does terbinafine tend to concentrate?

A

the nail

54
Q

what other drug can nystatin be compared to and why?

A

ampho b, both polyenes

55
Q

what is the most common use for nystatin?

A

candidal infx

56
Q

nystatin is not absorbed where?

A

GI tract, skin, or mucous membranes

57
Q

Because nystatin has poor GI and skin absorption, what can it be used for?

A

PO adminstration for GI and skin candida infx

58
Q

which antifungals are cidal?

A

ampho b
nystatin
terbinafine
caspofungin

Pharmacology (6 decks)

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