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Principles of Therapy Core Drugs > Antifungal Drugs > Flashcards

Antifungal Drugs Flashcards

1
Q

What is the classification of Amphotericin B?

A

Polyene antibiotic
Systemic use
anti fungal

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2
Q

What is the mechanism of action of Amphotericin B?

A

Binds selectively to ergosterol, which alters permeability of cell by forming pores in cell membrane, results in the loss of intracellular ions + macromolecules which leads to cell death.

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3
Q

What are the therapeutic indications of Amphotericin B?

A

most organisms responsible for systemic mycoses

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4
Q

What is the solubility of Amphotericin B?

A

soluble in water

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5
Q

How is Amphotericin B administered?

A

IV, oral for candidiasis infections within the lumen of GIT, topically

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6
Q

What are the 2 formulations of Amphotericin B?

A
  • colloidal suspension of amphotericin B and sodium deoxycholate (IV)
  • amphotericin complexed with lipids or encapsulated in liposomes
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7
Q

What % of Amphotericin B is bound to plasma proteins?

A

> 90%

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8
Q

Describe the distribution of Amphotericin B

A

widely distributed in tissues, crosses BBB poorly (except when meninges are inflamed)

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9
Q

What is the half-life of Amphotericin B?

A

24-hours, up to 15 days with repeated dosages

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10
Q

How is Amphotericin B excreted?

A

excreted very slowly via the urine, 2-5% in an active form

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11
Q

What are the adverse effects of Amphotericin B?

A
  • fever, headache, tinnitis, nausea
    and vomiting and chills (immediate)
  • renal toxicity (slower)
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12
Q

What is the classification of Ketoconazole?

A

Imidazole
Systemic use
anti fungal

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13
Q

What is the mechanism of action of Ketoconazole?

A

inhibits of the cytochrome P450 enzyme system of fungal cells

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14
Q

What are the therapeutic indications of Ketoconazole?

A

yeast and dermatophyte infections

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15
Q

Describe the absorption of Ketoconazole

A

Oral absorption (varies among individuals)

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16
Q

What % of Ketoconazole is bound to plasma proteins?

A

99%

17
Q

Describe the distribution of Ketoconazole

A

widely distributed in tissues and body fluids

18
Q

What is the half-life of Ketoconazole?

A

8 hours

19
Q

How is Ketoconazole metabolised and excreted?

A

metabolized in the liver and excreted in bile, a small amount is also excreted in urine

20
Q

What are the adverse effects of Ketoconazole?

A
  • fatal liver damage
  • gynecomastia, infertility, and menstrual irregularities
  • alters metabolism of other drugs (increases concentration and toxic effects)
21
Q

What is the classification of Fluconazole?

A

Triazole
Systemic use
Antifungal

22
Q

What is the mechanism of action of Fluconazole?

A

inhibits of the cytochrome P450 enzyme system of fungal cells

23
Q

What are the therapeutic indications of Fluconazole?

A
  • Orally: oropharyngeal and eosophageal candidiasis
  • IV: systemic candidiasis and cryptococcal infections including cryptococcal meningitis
  • Mainly candida and cryptococcus
24
Q

How is Fluconazole administered?

A

Orally and IV

25
Q

Describe the distribution of Fluconazole

A

Crosses BBB

26
Q

What are the adverse effects of Fluconazole? (5)

A
  • nausea
  • vomiting
  • abdominal pain
  • diarrhea
  • headache
27
Q

What is the classification of Griseofulvin?

A

Antibiotic
Systemic use
antifungal

28
Q

What is the mechanism of action of Griseofulvin?

A

inhibits mitosis in fungal cells by binding to tubulin

29
Q

What are the therapeutic indication of Griseofulvin?

A

dermatophyte (micosporum) infections of the skin, hair and nails

  • fungistatic
  • fungicidal
30
Q

What is the spectrum of activity of Griseofulvin?

A

narrow

31
Q

How is Griseofulvin administered?

A

orally

32
Q

Describe the absorption of Griseofulvin

A

poorly soluble in water and absorption is improved when the agent is taken with a fatty meal

33
Q

What is the half life of Griseofulvin?

A

24 hours, detectable in the skin for longer

34
Q

What are the adverse effects of Griseofulvin?

A
  • GIT disturbances
  • headache
  • photosensitivity
  • induces cytochrome P450 enzymes (causes drug interactions)
35
Q

What is the classification of Nystatin?

A

Polyene antibiotic
topical use
anti fungal

36
Q

What is the classification of Clotrimazole?

A

Topical Use
Imidazoles
anti fungal

Principles of Therapy Core Drugs (8 decks)

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