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Infectious Disease > Azole - Antifungal Class > Flashcards

Azole - Antifungal Class Flashcards

1
Q

(T/F) - Azoles have become mainstay of antifungal therapy

A

TRUE

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2
Q

What is the MOA of azoles?

A

Inhibits fungal cytochrome P450, decreasing ergosterol production

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3
Q

Itraconazole has a good spectrum in which fungi organisms?

A
  • C. albicans
  • C. lusitaniae
  • C. tropicalis
  • C. parapsilosis
  • Cryptococcus neoformans
  • Aspergillus spp
  • Many dimorphic fungi
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4
Q

What AEs can occur in itraconazole?

A
  • Hepatotoxicity
  • QTc prolongation
  • Negative inotrope
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5
Q

Itraconazole is contraindicated in what?

A

Heart failure patients

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6
Q

Itraconazole strongly inhibits what?

A

CYP3A4

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7
Q

What are the popular itraconazole formulations?

A
  • Capsules

- Solution

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8
Q

Which itraconazole formulation has a lower bioavailability?

A

Capsules

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9
Q

Which itraconazole formulation is less preferred for systemic fungal infections?

A

Capsules

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10
Q

Which itraconazole formulation should be taken with a full meal?

A

Capsules

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11
Q

Which itraconazole formulation should be taken on an empty stomach?

A

Solution

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12
Q

If someone wants to lower the absorption levels of itraconazole, how can it be lowered?

A

With PPIs; or take itraconazole with a soda

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13
Q

What is the drug of choice for itraconazole?

A

Histoplasmosis; a dimorphic infection

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14
Q

Fluconazole has a good spectrum in which fungi organisms?

A
  • C. albicans
  • C. tropicalis
  • C. parapsilosis
  • C. lusitaniae
  • Cryptococcal neoformans
  • Coccidioides immitis
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15
Q

What AEs can occur with fluconazole?

A
  • Rash
  • Hepatotoxicity
  • QTc prolongation
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16
Q

Fluconazole strongly inhibits what?

A
  • CYP2C19

- CYP2C9

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17
Q

Fluconazole moderately inhibits what?

A

CYP3A4

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18
Q

(T/F) - Fluconazole has a high bioavailability, regardless of formulation

A

TRUE

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19
Q

(T/F) - Fluconazole needs to adjust doses in renal insufficient patients

A

TRUE

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20
Q

(T/F) - Fluconazole has a strong activity against C. krusei and C. glabrata

A

FALSE - poor activity against those fungi organisms

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21
Q

If fluconazole will be used for C. krusei or C. glabrata, what should be done before giving fluconazole and at what dose should fluconazole be given?

A

Check susceptibilities; 800 mg/day

22
Q

What is the drug of choice for fluconazole?

A

Susceptible fungal infections

23
Q

Voriconazole has a good spectrum in which fungi organisms?

A
  • C. albicans
  • C. tropicalis
  • C. parapsilosis
  • C. lusitaniae
  • C. krusei
  • Aspergillus spp
  • Many other moulds
24
Q

What AEs can occur with voriconazole?

A
  • Hepatotoxicity
  • Rash
  • QTc prolongation
  • Visual and auditory hallucinations
  • Visual effects
  • Photosensitivity
25
Q

What kind of visual effects can occur with voriconazole?

A
  • Wavy lines

- Flashing

26
Q

Voriconazole moderately inhibits what?

A
  • CYP2C9

- CYP3A4

27
Q

(T/F) - The IV formulation of voriconazole can be nephrotoxic

A

TRUE - it contains a cyclodextrin vehicle which can accumulate in renal dysfunction patients

28
Q

Voriconazole IV is contraindicated in what?

A

CrCl < 50 mL/min

29
Q

Can another formulation of voriconazole be used for renal dysfunction patients?

A

Oral formulations

30
Q

Voriconazole is not useful for what treatment?

A

Candiduria

31
Q

Voriconazole is eliminated where?

A

Hepatically

32
Q

What is the drug of choice for voriconazole?

A

Invasive aspergillus

33
Q

Posaconazole has a good spectrum in which fungi organisms?

A
  • C. albicans
  • C. parapsilosis
  • C. tropicalis
  • C. lusitaniae
  • C. krusei
  • Aspergillus spp
  • Many moulds
  • Dimorphic fungi
  • Mucorales (Zygomycetes spp)
34
Q

What AEs can occur with Posaconazole?

A
  • Hepatotoxicity
  • Rash
  • Possible QTc prolongation
  • GI disturbances
35
Q

Posaconazole is a strong inhibitor of what?

A

CYP3A4

36
Q

What are the formulation of Posaconazole in the market?

A
  • Oral delayed release tablets
  • Oral suspension
  • IV injection
37
Q

Which formulations are not interchangeable with posaconazole?

A

Oral delayed release tablets and oral suspension

38
Q

Which formulations need to be taken with a meal with posaconazole?

A

Oral formulations

39
Q

What is the indicated choice for PO tabs, suspension and IV posaconazole formulations?

A
  • Prophylaxis of candida

- Aspergillus in high-risk patients

40
Q

What is the indicated choice for PO suspension of posaconazole formulation?

A
  • Oropharyngeal candidiasis

- Resistance of fluconazole and/or itraconazole

41
Q

Isavuconazole has a good spectrum in which fungal organisms?

A
  • Candida spp
  • Aspergillus spp
  • Mucorales (zygomycetes spp)
  • Other moulds
  • Dimorphic fungi
42
Q

What AEs can occur with isavuconazole?

A
  • Hepatotoxicity
43
Q

Isavuconazole is a substrate from what?

A

CYP3A4

44
Q

Isavuconazole is an inhibitor of what?

A
  • CYP4A4
  • P-gp
  • Organic cation transporter 2
45
Q

What are the formulations available with isavuconazole?

A
  • Capsules

- IV

46
Q

(T/F) - Isavuconazole capsules need to be taken with food

A

FALSE - can be taken with or without food

47
Q

(T/F) - Isavuconazole is supplied as a prodrug

A

TRUE

48
Q

(T/F) - Isavuconazole is a narrow spectrum drug

A

FALSE - broad spectrum

49
Q

(T/F) - Isavuconazole has a very long t 1/2

A

TRUE

50
Q

Does the loading dose of isavuconazole need extensive dosing?

A

Yes; q8h for 48h then 24h

51
Q

What is the drug of choice for isavuconazole?

A

Invasive mold infections

Infectious Disease (41 decks)

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