Antifungal drugs Flashcards

1
Q

What are the pharmacokinetics of Amphoterecin B?

A

IV, topical, oral and intrathecal admin

**Broad spectrum of action including aspergillus, blastomyces, candida, coccidiodes, cryptococcus, histoplasma

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2
Q

What is the MOA of Amphoterecin B?

A

Selectively bind fungal ergosterol-> form polyene associated pores in cells membrane -> leakage of intracellular ions and macromolecules

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3
Q

What are the main uses of Amphoterecin B?

A
  • used in all life threatening mycoses
  • disseminated infections
  • fungal pneumonia and cryptococcal menigitis
  • mycoses are rapidly progressing in IC patients
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4
Q

What are the AE of Amphoterecin B?

A

nephrotoxicity- K+ supplements and normal saline infusions req

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5
Q

What is the MOA of Nystatin?

A

Selectively bind fungal ergosterol-> form polyene associated pores in cells membrane -> leakage of intracellular ions and macromolecules

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6
Q

What is the pharmacokinetics of flucytosine?

A

water soluble, oral/IV admin, renal excretions

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7
Q

What is the MOA of flucytosine?

A

taken up into fungal cells via membrane bound cytosine perm ease -> converted into 5FU will inhibit either DNA synthesis or RNA synthesis

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8
Q

What are the clinical uses of Flucytosine?

A

Current use is confined to combination therapy

-deep candidal infections, cryptococcal meningitis and chromoblastomycosis

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9
Q

What are the adverse effects of flucytosine?

A

arise from 5FC metabolism by intestinal flora to toxic antineoplastic 5FU
** black box warning regarding renal impairment

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10
Q

What is the MOA of Fluconazole, Itraconazole, and miconazole?

A

Inhibition of fungal ergosterol biosynthesis

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11
Q

What are the clinical uses of itraconazole?

A

scalp ringworm, jock itch, athletes foot

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12
Q

What are the clinical uses of ketoconazole?

A

tinea versicolor, seborrheic dermatitis

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13
Q

What are the clinical uses of Fluconazole?

A

candida infections!

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14
Q

What is the MOA of anidulafungin, caspofungin and micafungin?
Resistance?

A

noncompetitive inhibition of fungal B (1-3) D glucan synthase-> fungicidal effect
***resistance from mutations in FKS1

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15
Q

What are the uses for anidulafungin?

A

invasive candidiasis, esophageal candidiasis, candidemia

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16
Q

What are the uses for caspofungin?

A

disseminated and mucocutaneous candidiasis and for invasive aspergillosis

17
Q

Whata re the uses for micafungin?

A

prophylaxis for candida infections in BM transplants

18
Q

What is the MOA of Griseofulvin?

A

inhibits fungal mitosis (disrupts mitotic spindle by interacting with polymerized microtubules)
**fungistatic

19
Q

What are the clinical uses Griseofulvin?

A

Dermatophyte infections of skin, hair and nails

20
Q

What are the AE of griseofulvin?

A

hypersensitivity and rash!

21
Q

What are the pharmacokinetics of griseofulvin?

A

oral and is distributed in heratinized tissues

22
Q

What are the pharmacokinetics of terbinafine?

A

oral and topical

-distributed in keratinized tissue and fat

23
Q

What is the MOA of Terbinafine?

A

inhibits ergosterol synthesis by inhibiting squalene epoxidase -> accumulation of squalene is toxic to fungi
*** fungicidal

24
Q

What are the clinical uses for terbinafine?

A

fungal infections of skin, hair and nails.

onychomycosis - tinea cruris and tinea corporis

25
Q

What are the AE of terbinafine?

A

hepatotoxicity, agranulocytosis, pancytopenia, anemia

26
Q

What is the MOA of tolnaftate??

A

thought to inhibit fungal squalene epoxidase

27
Q

What are the clinical uses of tolnaftate?

A

cutaneous mycoses caused by dermatophytes and M furfur

28
Q

What are the clinical uses of ciclopirox?

A

candidiasis, tinea corporis, tinea cruris, tinea pedis, tinea versicolor, onychomycosis and seborrheic dermatitis

29
Q

What are the clinical uses of undecylenic acid?

A

dermatophytoses esp tinea pedis **athletes foot!