Antifungals Flashcards

To review the 5 major classes of antifungal drugs and their common side effects.

1
Q

What do the echinocandins work on? What is their mechanism of function?

A

They work on the cell wall and inhibit the enzyme 1,3 D-glucan synthase.

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2
Q

Caspofungin and Micafungin belong to what class of antifungals?

A

The Echinocandins.

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3
Q

What side effect is associated with the echinocandins?

A

Flushing due to histamine release (vasodilation of superficial microvasculature).

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4
Q

What administrative routes can the Polyenes been given through?

A
  • Amphotericin B can only be given through IV.

- Nystatin can be given orally and topically.

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5
Q

Amphotericin B

A
  • Member of the polyenes.
  • Works on most fungi.
  • Binds to ergosterol and punches holes in the membrane.
  • Fungicidal.
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6
Q

What is one side effect of Amphotericin B?

A

Nephrotoxicity

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7
Q

Nystatin

A
  • Member of the polyenes.
  • Oral and topical formulation.
  • Not absorbed from the GI, it acts topically.
  • No clinical side effects.
  • Binds to ergosterol and punches holes in the membrane.
  • Fungicidal
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8
Q

What are the primary substances in the fungal cell wall?

A

Glucan (the polysaccharide component) and chitin.

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9
Q

How do the allylamines function?

A

They block ergosterol synthesis by inhibiting squalene epoxide.

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10
Q

What is the main side effect of the allylamines?

A

Reversible agranulocytosis (neutropenia).

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11
Q

What are the names of two allylamines?

A

Fluconazole and Terbinafine

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12
Q

What are the two groups of azoles?

A

Imidazoles and Triazoles

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13
Q

What are two benefits of the azoles?

A
  • Excellent oral absorption.

- Low toxicity.

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14
Q

Mechanism of action of the azoles?

A

Block ergosterol synthesis by inhibiting 14alpha demethylase.

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15
Q

Give an example of an antifungal anti-metabolite.

A

Flucytosine (5-FU)

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16
Q

Which class is not often used due to resistance and toxicity issues?

A

The anti-metabolite Flucytosine (5-FU).

17
Q

How does the antifungal anti-metabolite act?

A

Inhibits DNA/RNA synthesis.

18
Q

What is the only administrative route to give the Echinocandins?

A

Through IV formulation only.

19
Q

Summarize the main actions of the antifungals.

A

Azoles & Allylamines: Inhibit ergosterol synthesis.
Polyenes: Attach to ergosterol and punch holes in the membrane.
Echinocandins: Inhibit glucan synthesis.
Antimetabolites: Inhibit DNA/RNA synthesis.

20
Q

What are the symptoms of Flucytosine (anti-metabolite)?

A

Bone marrow suppression, nausea, vomiting, and diarrhea.