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FPT > Antifungals > Flashcards

Antifungals Flashcards

1
Q

Which antifungals target ergosterol?

A

Polyenes, triazoles and imidazoles.

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2
Q

Which antifungals inhibit ergosterol synthesis?

A

Allymines.

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3
Q

Which antifungals block the production of the beta-(1,3)-glucan protein damaging the cell wall?

A

B-3-glucan synthase inhibitors.

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4
Q

Which antifungals target chitin synthase?

A

Nikkomycin and polyoxin.

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5
Q

Which antifungals inhibit DNA/RNA synthesis?

A

Flucytosine.

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6
Q

Which antifungals inhibit fungal cell mitosis?

A

Griseofulvin.

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7
Q

List polyenes?

A

Nystatin.
Amphotericin B.

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8
Q

How is nystatin used?

A

Mostly topical and local treatment (oral thrush).

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9
Q

What is the effectiveness of absorption of nystatin?

A

Poor systemic absorption.
Poor oral bioavailability.
No drug interaction.

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10
Q

List MOA of amphotericin B?

A

binds to ergosterols to form pores, leading to leakage of molecules causing oxidative damage.

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11
Q

List the spectrum of activity of amphotericin B?

A

Candida, Aspergillus, Histoplasma, cryptococcus, and blastomyces.

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12
Q

What is the excretion method of polyenes?

A

Excreted by kidney slowly through months.

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13
Q

List the side effects of amphotecirin B?

A

Fever, chills, electrolyte abnormalities (hypokalemia), renal dysfunction, hematologic toxicity.

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14
Q

Give an example of fluorocytosine?

A

5-fluorocytosine.

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15
Q

List MOA of 5-fluorocytosine?

A

Inhibits thymidylate synthase and DNA synthase.

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16
Q

List spectrum of activity of 5-fluorocytosine?

A

Candida and crptococcus.

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17
Q

Resistance is common for which antifungal and how to fix it?

A

5-fluorocytosine.

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18
Q

List the adverse effects of 5-fluorocytosine?

A

Bone marrow toxicity - pancytopenia - reversible.

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19
Q

What is the mechanism of azoles?

A

Binds to ergosterol to form pores.

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20
Q

List the spectrum of activity of azoles?

A

Candida, aspergillus, histoplasma, cyptococcus, blastomyces, coccidiode, dermatophytes.

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21
Q

________ newer azoles with fewer side effects?

A

Triazoles.

22
Q

Which antifungals work by inhibiting sterol 14 alpha- demethylase?

A

The azoles.

23
Q

Adverse effects of the azoles are due to what?

A

Inhibition of mammalian steroid synthesis.

24
Q

Drug interactions with azoles are due to what?

A

Inhibition of cyt.P450 enzymes.

25
Q

Triazoles cause what?

A

Decrease potassium.

26
Q

What is the MOA of echinocandins?

A

Inhibits 1,3-B-D-glucan synthase.

27
Q

Echinocandins are used for what?

A

Aspergillosis and candidiasis.

28
Q

What are echinocandins used for?

A

Empiric antifungal therapy.

29
Q

What are the adverse effects of echinocandins?

A

Fever, histamine release, hypokalemia.

30
Q

Give an example of echinocandins?

A

Capsofungin.

31
Q

Echinocandins are metabolized by what?

A

Hydrolysis and N-acetylation.

32
Q

Which antifungal is not an inhibitor/inducer/substrate of CYP?

A

Echinocandins.

33
Q

List allylamines?

A

1- naftifine.
2- terbinafine.
3- butenafine.

34
Q

List properties of naftifine?

A
  • only available as gel or cream. (Poor systemic absorption 4-6%).
  • no interactions found.
35
Q

What are the substrates for terbinafine?

A

1A2, 2C9/19, 3A4.

36
Q

_______ decreases terbinafine clearance by 33%

A

Cimetidine.

37
Q

________ increases terbinfine clearance by 100%?

38
Q

What is the inhibitor of terbinafine?

A

2D6 strong.

39
Q

Terbinafine Increases ________ leavels, ________ (Cmax up 1.9 folds), ________ (t1/2 up to 400 hours), __________ (Cmax up 2 folds)

A

Nortriptyline, paroxetine, amitriptyline, desipramine.

40
Q

What is the inducer of terbinafine?

41
Q

terbinafine increases metabolism of ________ by 15%?

A

Cyclosporine.

42
Q

Which antifungal binds to microtubules/ disrupts mitosis?

A

Griseofulvin.

43
Q

Griseofulvin deposits where?

A

In keratin layers.

44
Q

__________ actively concentrate griseofulvin

A

Dermatophytes.

45
Q

Griseofulvin is used for what?

A

Infections of the skin, hair, nails; prolonged therapy.

46
Q

List toxicity of griseofulvin?

A

Headache, neuro and hepatotoxicity, photosensitivity, carcinogenic.

47
Q

List topical antifungals?

A

1- tolnaftate.
2- nystatin.
3- naftifine.
4- terbinafine.

48
Q

Topical antifungals are used for what?

A

Stratum corneum mucosa, cornea by dermatophytes and candida.

49
Q

Topical antifungals are not used for what?

A

Subcutaneous, nail or hair infections.

50
Q

Whitfields ointment contains what?

A

Benzoic + salicylic acid.

FPT (17 decks)

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