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Boards First Aid and Kaplan > Antifungal agents > Flashcards

Antifungal agents Flashcards

1
Q

What is the MOA of capsofungin?

A

Inhibits the synthesis of beta glucan (component of the fungal cell wall)

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2
Q

What is the MOA of the “-azoles”?

A

Inhibit 14-alpha-demethylase (enzyme used to convert lanosterol ergosterol(cell membrane component))

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3
Q

What is the MOA of terbinafine?

A

Inhibits squalene epoxidase (converts squalene to squalene epoxide)

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4
Q

What is the MOA of amphotericin B?

A

Binds to ergosterol (a component of the fungal cell membrane) to form artificial pores which disrupt membrane permeability

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5
Q

Name examples of polyenes

A
  • Amphotericin B

- Nystatin

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6
Q

What is the mechanism of resistance to amphotericin B?

A

Low ergosterol content

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8
Q

What are the clinical uses of the polyenes?

A
  • Amphotericin B has wide spectrum-DOC (or co-DOC) for severe infx caused by cryptococcus or mucor
  • Nystatin-too toxic for systemic use-used topically for localized infx (candidiasis)
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9
Q

What other antifungal is synergistic with amphotericin B and what is this combo used to treat?

A

Amphotericin B is synergistic with flucytosine in cryptococcoses

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10
Q

What are the possible side effects of amphotericin B?

A
  • Infusion related-fever, chills, muscle rigor, hypotension, occur during IV infusion
  • Dose-dependent-nephrotoxicity, tubular acidosis
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11
Q

What is ketoconazole used for?

A
  • Co-DOC for paracoccidioides and backup for blastomycoses and histoplasma
  • Oral use in mucocutaneous candidiasis or dermatophytoses
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12
Q

What is fluconazole used for?

A
  • DOC for esophageal and invasive candidiasis and coccidioidomycoses
  • Prophylaxis and suppression in cryptococcal meningitis
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13
Q

What are itraconazole and voriconazole used for?

A
  • DOC in blastomycoses and sporotrichoses

- Backup for several other mycoses and candidiasis

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14
Q

What is voriconazole used for specifically?

A

Aspergillosis

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15
Q

What are clotrimazole and and miconazole used for?

A

Used topically for candida and dermatophyte infx

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16
Q

What is the only “-azole” that penetrates the CSF (can be used for meningeal infx)?

A

Fluconazole

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17
Q

How is fluconazole eliminated from the body?

A

Eliminated in the urine (largely unchanged)

18
Q

How are ketoconazole and itraconazole eliminated from the body?

A

Metabolized by liver enzymes

19
Q

Which “-azole” is a p450 inhibitor?

A

Ketoconazole

20
Q

What are the possible side effects of the “-azoles”?

A
  • Decreased synthesis of steroids, including cortisol and testosterone -> decreased libido, gynecomastia, and menstrual abnormalities
  • Increased LFTs and hepatotoxicity
21
Q

What is the MOA of flucytosine?

A

Flucytosine is activated by fungal cytosine deaminase to 5-FU which is incorporated in fungal RNA
-5-FU also forms 5-FdUMP which inhibits thymidylate synthase -> decreased thymine

22
Q

What happens if flucytosine is used alone?

A

Resistance develops quickly

23
Q

What is flucytosine used for?

A

Use in combination with amphotericin B in severe candidal and cryptococcal infx-enters CSF

24
Q

What is the main side effect of flucytosine?

A

Bone marrow suppression

25
Q

What is the MOA of terbinafine?

A

Inhibits squalene epoxidase -> decreased ergosterol

26
Q

What is terbinafine used for?

A

Dermatophytes and onychomycoses

27
Q

What are the possible side effects of terbinafine?

A

GI distress, rash, headache, inc LFTs

28
Q

What are examples of echinocandins?

A

Capsofungin and other “-fungins”

29
Q

What is the MOA of the echinocandins?

A

Inhibit the synthesis of beta-1,2 glucan (critical component of fungal cell walls)

30
Q

What are the echinocandins used for?

A

Backup drugs given IV for disseminated and mucocutaneous candida infx or invasive aspergillosis

31
Q

What is the mechanism of resistance to “-azoles”?

A

Decreased intracellular accumulation

Boards First Aid and Kaplan (19 decks)

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