Antifungals Flashcards

1
Q

Which vehicle of application for a topical drug is the best for drug delivery?

A

ointment

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2
Q

What is the typically therapy for widespread tinea infections?

A

In order of effectiveness: All oral

  1. Terbinafine
  2. Itraconazole
  3. Fluconazole
  4. Griseofulvin
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3
Q

What is the typical therapy for localized tinea infections?

A
Topical:
Azoles
Terbinafine
Naftifine
ciclopirox
*Acronym: CANT
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4
Q

What is the typical therapy for Onychomycosis?

A
  1. Terbinafine
  2. Griseofulvin
  3. Itraconazole
  4. Fluconazole

(griseofulvin jumps from 4 to 2 for onychomycosis)
*Acronym: TGIF!

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5
Q

What topical therapy is used for onychomycosis?

A

Ciclopirox

Amorolfine

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6
Q

What is the MOA of ciclopirox?

A

Ciclopirox blocks fungal transmembrane transport, as a result important things cannot be taken into the cell by the fungus. Furthermore, high concentrations may destabilize the fungal membrane and lead to leakage

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7
Q

What ADEs should be considered with itraconazole?

A
  1. negative inotropic action
  2. hepatotoxicity (watch those LFTs)
  3. Cat C and breast milk (probably shouldn’t take
    with babies)
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8
Q

What is the MOA of itraconazole?

A

Same as the other azoles it inhibits the synthesis of ergosterol (blocks fungal P450s).

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9
Q

T or F Itraconazole has relatively few drug-drug interactions?

A

F - Itraconazole is known to have CYP interactions therefore use with other drugs should be minimized. (CYP3A4)

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10
Q

Which 3 anti-fungal drugs are known to cause QT prolongation?

A

Fluconazole
Psoaconazole
Voriconazole

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11
Q

Which anti-fungal is associated with visual disturbances?

A

Voriconazole

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12
Q

Which 4 anti-fungals cause hepatotoxicity?

A

Fluconazole
Posaconazole
Voriconazole
Itraconazole

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13
Q

What makes taking Posaconazole inconvenient?

A

Posaconazole must be administered with full meal or acidic carbonated drink for adequate bioavailability

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14
Q

Can fluconazole, Posaconazole, and voriconazole be taken during pregnancy?

A

All three are contraindicated in pregnancy:
Fluconazole-Cat D
Voriconazole-Cat D
Posaconazole-Cat C

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15
Q

Which anti-fungal requires dose adjustment with renal failure?

A

Fluconazole

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16
Q

Which antifungals undergo hepatic elimination?

A

Posaconazole

Voriconazole

17
Q

What factor is necessary for the azoles to enter the CSF?

A

P-gp

18
Q

Which antifungals enter the CNS?

A

Fluconazole > voriconazole > Itraconazole

19
Q

What is important to remember about the metabolism of Griseofulvin?

A

It undergoes extensive hepatic metabolism resulting in 4 effects:

  1. decreases effect of anticoagulants (warfarin)
  2. decreases contraceptive effect
  3. decreases cyclosporin serum levels
  4. increases alcohol effects

(Gets you drunk, gets you knocked up, then makes you bleed)

20
Q

What is the MOA of terbinafine?

A

terbinafine inhibits ergosterol synthesis by inhibiting squalene epoxidase, an enzyme that is part of the fungal cell membrane synthesis pathway

21
Q

What is special about terbinafine?

A

Typically well tolerated. Some neutropenia and lymphopenia may be noted especially in immunocompromised patients. Cat B

22
Q

What is the MOA of Naftifine?

A

unknown

23
Q

What is different about naftifine’s utility when compared with other antifungals?

A

naftifine is locally bactericidal

It is also anti-inflammatory

24
Q

T or F: One should not mix Naftifine with the Azoles?

A

T: Naftifine inhibits sterol synthesis at an earlier stage thus causing pharmacodynamic interference and reducing the effectiveness of the azoles.

25
Q

What is Ciclopirox?

A

A topical anti-fungal

May cause hypersensitivity or allergy to drug or co-formulated materials.

26
Q

What is the MOA of Amorolfine?

A

It inhibits ergosterol synthesis.

27
Q

Which two anti-fungals may irritate skin if applied to abrasions?

A

ciclopirox

Amorolfine