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Flashcards in Antifungals Deck (50):
1

MOA of amphotericin B

  • Binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes 

2

  • Binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes 

MOA of amphotericin B

3

Use of amphotericin B

  • Serious, systemic mycoses. Cryptococcus (amphotericin B with/without flucytosine for cryptococcal meningitis), Blastomyces, Coccidioides, Histoplasma, Candida, Mucor.
  • Intrathecally for fungal meningitis.
  • Supplement K+ and Mg2+ because of altered renal tubule permeability. 

4

  • Serious, systemic mycoses. Cryptococcus (amphotericin B with/without flucytosine for cryptococcal meningitis), Blastomyces, Coccidioides, Histoplasma, Candida, Mucor.
  • Intrathecally for fungal meningitis.
  • Supplement K+ and Mg2+ because of altered renal tubule permeability. 

Use of amphotericin B

5

toxicity of amphotericin B

  • Fever/chills (“shake and bake”), hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis (“amphoterrible”). Hydration decreases nephrotoxicity. Liposomal amphotericin decreases toxicity. 

6

  • Fever/chills (“shake and bake”), hypotension, nephrotoxicity, arrhythmias, anemia, IV phlebitis (“amphoterrible”). Hydration decreases nephrotoxicity. Liposomal amphotericin decreases toxicity. 

toxicity of amphotericin B

7

MOA of nystatin

  • Binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes. 
  • Topical form because too toxic for systemic use.

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  • Binds ergosterol (unique to fungi); forms membrane pores that allow leakage of electrolytes. 
  • Topical form because too toxic for systemic use.

MOA of nystatin

9

Use of nystatin

“Swish and swallow” for oral candidiasis (thrush); topical for diaper rash or vaginal candidiasis. 

10

“Swish and swallow” for oral candidiasis (thrush); topical for diaper rash or vaginal candidiasis. 

Use of nystatin

11

Azole drugs

Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole. 

12

Fluconazole, ketoconazole, clotrimazole, miconazole, itraconazole, voriconazole. 

Azole drugs

13

MOA of azoles

Inhibit fungal sterol (ergosterol) synthesis, by inhibiting the cytochrome P-450 enzyme that converts lanosterol to ergosterol. 

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Inhibit fungal sterol (ergosterol) synthesis, by inhibiting the cytochrome P-450 enzyme that converts lanosterol to ergosterol. 

MOA of azoles

15

Use of Azoles

  • Local and less serious systemic mycoses.

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  • Local and less serious systemic mycoses.

Use of Azoles

17

Use of Fluconazole

chronic suppression of cryptococcal meningitis in AIDS patients and candidal infections of all types 

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chronic suppression of cryptococcal meningitis in AIDS patients and candidal infections of all types 

Use of Fluconazole

19

Use of Itraconazole

Tx: Blastomyces, Coccidioides, Histoplasma. 

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Tx: Blastomyces, Coccidioides, Histoplasma. 

Use of Itraconazole

21

Use of Clotrimazole and miconazole 

topical fungal infections

22

topical fungal infections

Use of Clotrimazole and miconazole 

23

Toxicity of azoles

Testosterone synthesis inhibition (gynecomastia, esp. with ketoconazole), liver dysfunction (inhibits cytochrome P-450) 

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Testosterone synthesis inhibition (gynecomastia, esp. with ketoconazole), liver dysfunction (inhibits cytochrome P-450) 

Toxicity of azoles

25

MOA of Flucytosine

Inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase. 

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Inhibits DNA and RNA biosynthesis by conversion to 5-fluorouracil by cytosine deaminase. 

MOA of Flucytosine

27

Use of Flucytosine

Systemic fungal infections (esp. meningitis caused by Cryptococcus) in combination with amphotericin B. 

28

Systemic fungal infections (esp. meningitis caused by Cryptococcus) in combination with amphotericin B. 

Use of Flucytosine

29

Toxicity of flucytosine

Bone marrow suppression 

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Bone marrow suppression 

Toxicity of flucytosine

31

echinocandins

Caspofungin, micafungin, anidulafungin

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Caspofungin, micafungin, anidulafungin

echinocandins

33

MOA of echinocandins

Inhibits cell wall synthesis by inhibiting synthesis of β-glucan. 

34

Inhibits cell wall synthesis by inhibiting synthesis of β-glucan. 

MOA of echinocandins

35

Use of echinocandins

Invasive aspergillosis, Candida.

36

Invasive aspergillosis, Candida.

Use of echinocandins

37

Toxicity of echinocandins

GI upset, flushing (by histamine release). 

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GI upset, flushing (by histamine release). 

Toxicity of echinocandins

39

MOA of terbinafine

Inhibits the fungal enzyme squalene epoxidase.

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Inhibits the fungal enzyme squalene epoxidase.

MOA of terbinafine

41

Use of Terbinafine

Dermatophytoses (especially onychomycosis—fungal infection of finger or toe nails). 

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Dermatophytoses (especially onychomycosis—fungal infection of finger or toe nails). 

Use of Terbinafine

43

Toxicity of Terbinafine

GI upset, headaches, hepatotoxicity, taste disturbance. 

44

GI upset, headaches, hepatotoxicity, taste disturbance. 

Toxicity of Terbinafine

45

MOA of griseofulvin

Interferes with microtubule function; disrupts mitosis. Deposits in keratin-containing tissues (e.g., nails). 

46

Interferes with microtubule function; disrupts mitosis. Deposits in keratin-containing tissues (e.g., nails). 

MOA of griseofulvin

47

Use of griseofulvin

Oral treatment of superficial infections; inhibits growth of dermatophytes (tinea, ringworm). 

48

Oral treatment of superficial infections; inhibits growth of dermatophytes (tinea, ringworm). 

Use of griseofulvin

49

Toxicity of griseofulvin

Teratogenic, carcinogenic, confusion, headaches, increases P-450 and warfarin metabolism. 

50

Teratogenic, carcinogenic, confusion, headaches, increases P-450 and warfarin metabolism. 

Toxicity of griseofulvin