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DD/BL Final > Antifungal Agents > Flashcards

Antifungal Agents Flashcards

1
Q

Amphotericin MoA?

A

binds ergosterol –> forming pores in membranes with loss of vital intracellular constituents

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2
Q

Nystatin MoA?

A

[same as Amphotericin]

binds ergosterol –> forming pores in membranes with loss of vital intracellular constituents

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3
Q

Amphotericin Pharmacokinetics?

A
  1. IV or topical only
  2. Slow excretion by kidney & hepato-biliary
  3. 1/2 life = 15 d
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4
Q

Amphotericin Spectrum

A

broad spectrum!!

  • life threatening
  • systemic infection
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5
Q

Amphotericin Adr?

A
  1. Nephrotoxicity
  2. acute fever/chill
  3. Anemia
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6
Q

Nystatin Pharmacokinetics?

A

Topical only!!

NO orally absorption

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7
Q

Nystatin Spectrum

A

Superficial Candidal infection

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8
Q

Nystatin Adr?

A
  1. Topically: well-tolerated

2. Oral: mild GI upset

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9
Q

Caspofungin MoA?

A

inhibits synthesis of cell wall component

–> disrupting assembly

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10
Q

Caspofungin Pharmacokinetics?

A

IV only!!

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11
Q

How P450 inducers affect Caspofungin?

A

decreasing level

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12
Q

Caspofungin spectrum?

A

aspergillosis (infection with aspergillus), if resistant to ampho B

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13
Q

Caspofungin Adr?

A

infusion related symptoms

* histamine –> rash, pruritus, n/v

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14
Q

Triazoles MoA?

A

[like imidazole]

* inhibit P450 ergosterol synthesis –> altering membrane permeability

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15
Q

How Triazole comparing with Imidazole?

A

more selective inhibition of fungal P450

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16
Q

Representing Triazole drug?

A
  1. Fluconazole
  2. Intraconazole
  3. Terconazole
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17
Q

Fluconazole Pharmacokinetics?

A
  1. IV/po
  2. renal excretion
  3. enter CNS
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18
Q

Fluconazole Spectrum

A
  1. oropharyngeal/esophageal candidiasis
    2 vulvovaginal candidiasis (single dose)
  2. cryptococcal meningitis
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19
Q

Fluconazole Adr?

A
  1. GI upset : well-tolerated

2. Lesser effect on CYP450 metabolism

20
Q

Intraconazole Pharmacokinetics?

A
  1. IV/po

2. hepatic metabolism

21
Q

Intraconazole Spectrum?

A
  1. superficial dermatophytosis

2. onychomycosis

22
Q

Intraconazole Adr?

A
  1. inhibits CYP450 metabolism

2. n/v, diarrhea, headache

23
Q

Terconazole Pharmacokinetics?

A

Topical only

24
Q

Terconazole Spectrum?

A

vulvovaginal candidiasis

25
Q

Terconazole Adr?

A

None

26
Q

Imidazole MoA?

A

inhibit CYP450 ergosterol synthesis –> altering membrane permeability

27
Q

Imidazole representing drug?

A
  1. Ketoconazole

2. Clotrimazole/Miconazole

28
Q

Ketoconazole Pharmacokinetics?

A
  1. IV/po/topical

2. Hepatic metabolism

29
Q

Ketoconazole Spectrum?

A
  1. System infection (candidiasis)

2. wide use in dermatologic indications

30
Q

Why Ketoconazole use for systemic treatment declines?

A

Due to toxicity

31
Q

Ketoconazole Adr?

A
  1. Hepatotoxicity, anorexia, n/v
  2. Inhibits CYP450
  3. Inhibits Androgen-GC biosynthesis
32
Q

Clotrimazole Pharmacokinetics?

A

Topical only

33
Q

Clotrimazole Spectrum?

A

Oral & vaginal candidiasis

34
Q

Clotrimazole Adr?

A

None

35
Q

Terbinafine MoA?

A

inhibits squalene oxidase reducng ergosterol synthesis

36
Q

Terbinafine Pharmacokinetics?

A
  1. po & topical

2. Metabolized by P450

37
Q

Terbinafine Spectrum

A
  1. po: onychomycosis of finger/toe nails

2. topical: athlete’s foot

38
Q

Terbinafine Adr?

A
  1. Inhibition CYP450

2. headache, diarrhea, rash

39
Q

Flucytosine MoA?

A

converted to 5FU in fungi –> inhibit thymidylate synthetase & DNA synthesis

40
Q

Flucytosine Pharmacokinetics?

A
  1. well-absorbed & distributed

2. renal elimination –> decrease dose if renal impair

41
Q

Flucytosine Spectrum?

A

cryptococcosis & candidiasis serious infections

42
Q

Flucytosine Adr?

A
  1. n/v, skin rashes

2. prolonged use –> bone marrow depression

43
Q

Griseofulvin MoA?

A

binds to fungal microtubules inhibiting mitosis

44
Q

Griseofulvin Pharmacokinetics?

A
  1. po: poor

- -> improving with: microsizing particle, fatty meal

45
Q

Griseofulvin Spectrum?

A

Severe dermatophytosis of skin, hair, finger/toe nails

46
Q

Griseofulvin Adr?

A
  1. hypersensitivity reactions

2. GI distress, headache, confusion

DD/BL Final (11 decks)

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