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Pharm Block 3 > Antifungals > Flashcards

Antifungals Flashcards

1
Q

What is the action of Amphotericin B?

A

binds ergosterol to form pores in membrane that leaks potassium

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2
Q

What fungi is Amphotericin B active against?

A
  1. Candida albicans 2. Histoplasma 3. Cryptococcus 4. Coccidioides 5. Blastomyces
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3
Q

What are the adverse effects of Amphotericin B

A

Acute Kidney Injury (accumulates in PCT affecting absorption of Na, Cl), hypotension, anemia. Does not cross BBB or placenta

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4
Q

How is Amphotericin B administered?

A

Slow IV infusion, given with sodium flush before and after to avoid kidney toxicity

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5
Q

What is the action of Flucytosine

A

Converted to 5-flurodeoxyuridine monophosphate in fungal cells, inhibits DNA synthesis by inhibiting thymidylate synthase and RNA synthesis by inhibiting F-deoxyUTP.

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6
Q

What are adverse effects of Flucytosine?

A

Falling neutrophils
Liver dysfunction
Upchuck
Clotting

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7
Q

How is Flucytosine used?

A

Combined with other agents, systemic fungal infections -> broad spectrum agent, can cross BBB

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8
Q

What are the 4 azoles?

A

ketoconazole, fluconazole, voriconazole, posaconazole - AZOLES are assholes! lots of side effects and all teratogenic

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9
Q

What azole is used for aspergillus?

A

voriconazole

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10
Q

Which azole has the fewest side effects?

A

fluconazole

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11
Q

What is the mechanism of the azoles?

A

inhibit C14-alpha-demethylase, which blocks conversion of lanosterol to ergosterol (membrane structure)

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12
Q

What are side effects of Fluconazole?

A

teratogenic, GI effects and skin rash

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13
Q

What are side effects of ketonazole?

A

sex related, hepatotoxicity

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14
Q

What are side effects of Voriconazole?

A

frequent drug interactions (p450), visual and auditory hallucinations

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15
Q

What are side effects of posaconazole?

A

Liver dysfunction, give with high fat meal

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16
Q

How is resistance to azoles conferred?

A

mutation in C14-alpha-demethylase gene so drug can no longer bind to it

17
Q

What are the echinocandins?

A

caspofungin, anidulafungin

18
Q

What is the mechanism of the echinocandins?

A

inhibit Beta(1,3)-D-glucan (inhibits cell wall synthesis) which leads to cell lysis

19
Q

What are capsofungin and anidulafungin useful against?

A

A for aspergillis and C for candida

20
Q

What are adverse effects of echinocandins?

A

The F’s: fever, flebitis, flushing, and Rash

21
Q

What is the mechanism of Griseofluvin?

A

accumulates in keritin-containing tissues, disrupts mitotic spindle and fungal mitosis

22
Q

What are the uses of Grisofluvin?

A

ringworm, dermatophytosis of skin and hair. Give with Grease

23
Q

What are adverse effects of Griseofluvin?

A

induces P450 drugs, increases metabolism of many drugs

24
Q

How is Griseofluvin administered?

A

With “grise” – grease. Take with high fat meal

25
Q

What is the mechanism of Terbinafine?

A

inhibits squalene epoxidase, which block synthesis of ergosterol in cell membrane. “Fungicidal”

26
Q

What are the clinical uses of Terbinafine?

A

dermatophytoses, onchyomycoses (nails)

27
Q

What are the adverse effects of Terbinafine?

A

The T’s. Taste, Toilet, transaminases (+ visual)

28
Q

What is Nystatin used for?

A

topical treatment of candida or oral treatment with swishing and spit (minimal oral absorption)

29
Q

What is the mechanism of nystatin?

A

forms pores in membranes allowing potassium efflux

30
Q

What is the mechanism of Cilopirox?

A

inhibits transport, leads to decrease in DNA, RNA, and protein synthesis

31
Q

What is Cilopirox used to treat?

A

Topical use: seborrheic dermatitis (1% solution), tina pedis, tinea corporis, onchyomycoses (8% solution)

Pharm Block 3 (4 decks)

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