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Pharmacology II Final Exam > Antifungals > Flashcards

Antifungals Flashcards

1
Q

What are some examples of local fungal infections?

A

Dermatophytosis (Ringworm) due to Trichophyton, Microsporum, and Epidermophyton.

Candida (yeast, Moilia)

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2
Q

What are some examples of systemic mycoses?

A

Histoplasmosis, Aspergillosis, Coccidiomycosis, Blastomycosis, Crytococcus, Sporotrichosis, etc.

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3
Q

What are examples of polyene antifungals?

A

Amphotericin B, Nystatin, and Natamycin.

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4
Q

What are some examples of azole anti fungal drugs?

A

Ketoconazole, Clotrimazole, Miconazole, Enilconazole, and Thiabendazole.

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5
Q

Which anti fungal drugs are broad-spectrum?

A
  1. Ciclopirox olamine
  2. Cuprimyxin
  3. Haloprogin
  4. Polyenes
  5. Azoles
  6. Terbinafine
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6
Q

What is the most common narrow-spectrum anti fungal and what does it treat?

A

Tolnaftate. It treats Malassezia canis.

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7
Q

What are some topical anti fungal drugs?

A
  1. Iodides
  2. Organic acids (Salicylic acid, Benzoic acid, fatty acids, etc.)
  3. Lime sulfur
  4. Thymol
  5. Hexachlorphene
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8
Q

What are some systemic anti fungal drugs? (6)

A
  1. Griseofulvin
  2. Amphotericin B
  3. Flucytosine
  4. Azoles (Ketoconazole)
  5. Allylamines (Terbinafine)
  6. Lufenuron
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9
Q

Which three systemic anti fungal drugs are most commonly used?

A
  1. Griseofulvin
  2. Amphotericin B
  3. Ketoconazole
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10
Q

What are polyenes?

A

Polyenes are broad spectrum topical anti fungal drugs.

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11
Q

Name three polyenes.

A
  1. Nystatin
  2. Amphotericin B
  3. Natamycin
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12
Q

What is the MOA of polyenes?

A

Fungicidal due to rapid alteration of fungal cell membrane permeability by binding irreversibly to ergosterol.

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13
Q

What are azoles?

A

Broad spectrum topical and systemic anti fungal drugs.

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14
Q

Which azoles are administered topically? (4)

A
  1. Clotrimazole
  2. Miconazole
  3. Enilconazole
  4. Thiabendazole
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15
Q

Which azole is administered both topically and systemically?

A

Ketoconazole

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16
Q

Which azoles are administered systemically? (2)

A
  1. Itraconazole

2. Fluconazole

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17
Q

What is the MOA of azoles?

A

Fungistatic due to alteration of fungal cell permeability by blocking conversion of lanosterol to ergosterol, which is catalyzed by 14-a demethylase.

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18
Q

What are allylamines?

A

Systemic antifungals

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19
Q

What is the most commonly used allylamine?

A

Terbinafine

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20
Q

What is the MOA of Allylamines?

A

Fungicidal due to inhibition of ergosterol synthesis by inhibiting squalene-epoxidase that converts squalene to squalene-epoxide resulting in accumulation of squalene.

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21
Q

What is Griseofulvin, how is it administered, and what does it treat?

A

Griseofulvin is a systemic anti fungal that is given orally for treatment of dermatophytes because of selective deposition in new keratin.

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22
Q

What is the MOA of Griseofulvin?

A

Fungistatic due to interference with microtubule function and inhibiting mitosis.

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23
Q

How is Griseofulvin absorbed?

A

GI absorption is low and is enhanced by decreasing particle size and a high fat meal.

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24
Q

How long does Griseofulvin have to be given to provide a successful treatment?

A

Treatment takes 3-6 weeks in small animals.

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25
Q

T/F: Griseofulvin is a hepatic enzyme inducer.

A

True

26
Q

What are some adverse effects of Griseofulvin?

A

Causes GI irritation and cats are sensitive to its toxicity (idiosyncratic reactions.)

27
Q

What toxic effects does Griseofulvin have in cats?

A

It is teratogenic, hepatotoxic, and causes idiosyncratic bone marrow suppression (neutropenia, anemia, and pancytopenia.)

28
Q

What is Amphotericin B?

A

Part of the polyene class of antifungals and can be topical or systemic.

29
Q

How is Amphotericin B administered?

A

Given IV because it has poor oral absorption. It has a wide distribution, except to the CNS.

30
Q

What does Amphotericin B treat?

A
  • Most effective drug for treatment of systemic mycoses in immunocompromised animals.
  • Combined with Flucytosine for cryptococcal meningitis in cats or with azoles for treatment of systemic mycoses.
  • Used topically for Candida
31
Q

What is Amphotericin B not effective against?

A

Aspergillus

32
Q

What are some toxic effects of Amphotericin B?

A
  1. Nephrotoxicity (narrow safety margin.)
  2. Hypokalemia
  3. Hypotension
  4. Cardiac arrhythmias

Liposoma encapsulated preparation is less toxic than colloidal suspension preparation.

33
Q

What kind of drug is Flucytosine?

A

Systemic antifungal

34
Q

What is the MOA for Flucytosine?

A

Fungicidal due to inhibition of nucleic acid synthesis by inhibiting thymidylate synthase.

35
Q

How is Flucytosine administered and how is it distributed in the body?

A

Readily absorbed orally and has a wide distribution, including the CNS.

36
Q

What are three adverse effects of Flucytosine?

A
  1. GI irritation
  2. Bone marrow suppression
  3. Liver dysfunction
37
Q

How is Ketoconazole administered?

A

It is given orally for broad-spectrum activity. Requires acidic pH for dissolution and oral absorption.

38
Q

T/F: Ketoconazole has good penetration in the CNS.

A

False. Ketoconazole has poor penetration in the CNS.

39
Q

How long does it take for Ketoconazole to work?

A

It has a slow effect. It takes 3-6mo to take effect.

40
Q

What is Ketoconazole not very effective against?

A

Aspergillosis

41
Q

What are the adverse effects of Ketoconazole?

A
  1. Inhibits cortisol and testosterone synthesis in small animals.
  2. Inappetence
  3. Pruritus and alopecia in dogs
  4. Should not be give to pregnant animals (teratogenic!)
42
Q

Who is more sensitive to Ketoconazole, dogs or cats?

A

Cats are more sensitive than dogs to toxicity, but large doses cause hepatotoxicity in cats and dogs.

43
Q

How is Itraconazole similar to Ketoconazole?

A

They have similar pharmacokinetics and therapeutic uses. They are both contraindicated during pregnancy.

44
Q

What is are three differences between Itraconazole and Ketoconazole?

A

Itraconazole’s oral absorption does not depend on acidity, it is effective against Aspergillus, and it does not inhibit cortisol or testosterone synthesis at therapeutic doses.

45
Q

What is the preferred drug for treating systemic Blastomycosis and Histoplasmosis?

A

Itraconazole

46
Q

What is the drug of choice for treating Sporotrichosis?

A

Itraconazole

47
Q

What is Fluconazole effective at treating?

A

Acute cryptococcal meningitis

48
Q

How is Fluconazole administered?

A

IV

49
Q

What are the differences between Fluconazole and Ketoconazole?

A

Fluconazole’s oral absorption does not depend on acidity and it has more penetration to tissues than Ketoconazole (and Itraconazole) and crosses the CNS at therapeutic levels.

50
Q

How serious are the side effects of Fluconazole?

A

Minimal

51
Q

What kind of drug is Terbinafine?

A

Broad-spectrum topical antifungal.

52
Q

What is Terbinafine used to treat and how is it administered?

A

Terbinafine is a safe and effective drug against dermatohytosis. It is available as tablets and topical cream.

53
Q

What is one side effect of Terbinafine?

A

May elevate ALT in cats

54
Q

What is the MOA of Lufenuron?

A

Inhibits cell wall synthesis due to inhibiting chitin synthesis by inhibiting chitin synthetase.

55
Q

What kind of drug is Lufenuron?

A

Systemic antifungal

56
Q

How is Lufenuron administered in cats and dogs?

A

Dogs: Orally
Cats: Injection

57
Q

T/F: Large doses are safe and effective in treating dermatophytosis in dogs and cats.

A

True

58
Q

What drug is used to treat keratitis in horses?

A

Clotrimazole

59
Q

What two drugs are used to treat canine nasal aspergillosis?

A

Clotrimazole and Enilconazole

60
Q

What drug is used to treat systemic aspergillosis?

A

Itraconazole PO for 2-3 months

Pharmacology II Final Exam (4 decks)

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