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DD/BL Final > Antifungal Agents > Flashcards

Antifungal Agents Flashcards

(46 cards)

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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?

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A
  1. GI upset : well-tolerated

2. Lesser effect on CYP450 metabolism

20
Q

Intraconazole Pharmacokinetics?

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A
  1. IV/po

2. hepatic metabolism

21
Q

Intraconazole Spectrum?

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A
  1. superficial dermatophytosis

2. onychomycosis

22
Q

Intraconazole Adr?

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A
  1. inhibits CYP450 metabolism

2. n/v, diarrhea, headache

23
Q

Terconazole Pharmacokinetics?

24
Q

Terconazole Spectrum?

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A

vulvovaginal candidiasis

25
Terconazole Adr?
None
26
Imidazole MoA?
inhibit CYP450 ergosterol synthesis --> altering membrane permeability
27
Imidazole representing drug?
1. Ketoconazole | 2. Clotrimazole/Miconazole
28
Ketoconazole Pharmacokinetics?
1. IV/po/topical | 2. Hepatic metabolism
29
Ketoconazole Spectrum?
1. System infection (candidiasis) | 2. wide use in dermatologic indications
30
Why Ketoconazole use for systemic treatment declines?
Due to toxicity
31
Ketoconazole Adr?
1. Hepatotoxicity, anorexia, n/v 2. Inhibits CYP450 3. Inhibits Androgen-GC biosynthesis
32
Clotrimazole Pharmacokinetics?
Topical only
33
Clotrimazole Spectrum?
Oral & vaginal candidiasis
34
Clotrimazole Adr?
None
35
Terbinafine MoA?
inhibits squalene oxidase reducng ergosterol synthesis
36
Terbinafine Pharmacokinetics?
1. po & topical | 2. Metabolized by P450
37
Terbinafine Spectrum
1. po: onychomycosis of finger/toe nails | 2. topical: athlete's foot
38
Terbinafine Adr?
1. Inhibition CYP450 | 2. headache, diarrhea, rash
39
Flucytosine MoA?
converted to 5FU in fungi --> inhibit thymidylate synthetase & DNA synthesis
40
Flucytosine Pharmacokinetics?
1. well-absorbed & distributed | 2. renal elimination --> decrease dose if renal impair
41
Flucytosine Spectrum?
cryptococcosis & candidiasis serious infections
42
Flucytosine Adr?
1. n/v, skin rashes | 2. prolonged use --> bone marrow depression
43
Griseofulvin MoA?
binds to fungal microtubules inhibiting mitosis
44
Griseofulvin Pharmacokinetics?
1. po: poor | - -> improving with: microsizing particle, fatty meal
45
Griseofulvin Spectrum?
Severe dermatophytosis of skin, hair, finger/toe nails
46
Griseofulvin Adr?
1. hypersensitivity reactions | 2. GI distress, headache, confusion

DD/BL Final (11 decks)

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