PHARMACOLOGY - Antifungal Drugs Flashcards

1
Q

Why are fungal infections increasing?

A

Antibiotics disrupt the host microbiome allowing fungi to infect as fungi are resistant to antibiotics. The increased use of immunosuppressive drugs has also predisposed animals to fungal infections

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2
Q

Define fungicidal anti-fungal drugs

A

Fungicidal drugs kill fungi

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3
Q

Define fungistatic anti-fungal drugs

A

Fungistatic drugs inhibit fungal growth

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4
Q

What are the six main classes of anti-fungals use in veterinary medicine?

A

Allylamines
Azoles
Polyenes
Echinocandins
Antimetabolites
Griseofulvin

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5
Q

What is the mechanism of action for the allylamine anti-fungals?

A

Allylamines inhibit ergosterol biosynthesis through the inhibition of the squalene epoxidase enzyme

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6
Q

What is the spectrum of activity for allylamines?

A

Dermatophytes

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7
Q

How should allylamines be administered?

A

Oral
Topical

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8
Q

Why do allylamines persist within the skin when administered topically?

A

Allylamines are highly lipophilic so persist well in the skin

Lipophilic (dissolves in lipid)

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9
Q

Give an example of an allylamine

A

Terbinafine

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10
Q

What is the mechanism of action for azole anti-fungal drugs?

A

Azoles inhibit ergosterol biosynthesis through the inhibition of the 1,4 sterol-methylase enzyme

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11
Q

What is the spectrum of activity for azoles?

A

Broad spectrum

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12
Q

How should most azoles be administered?

A

Topical

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13
Q

Which group of azoles is available for systemic use?

A

Triazoles

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14
Q

Give a specific example of a triazole

A

Flucanozole

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15
Q

How should systemic azoles such as the triazoles be administered?

A

Intravenous (IV)
Oral

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16
Q

What are the three main mechanisms of resistance to azole anti-fungal drugs?

A

Mutation of the 1,4 sterol-methylase enzyme
Drug efflux
Biofilm formation

17
Q

What is the mechanism of action for polyene anti-fungal drugs?

A

Polyenes bind to ergosterol and form pores in the fungal plasma membrane, disrupting the osmotic integrity of the cell causing the fungal cell to burst or undergo oxidative damage

18
Q

What is the spectrum of activity for the polyenes?

A

Broad spectrum

19
Q

How should polyenes be administered?

A

Intravenous (IV)
Topical

20
Q

Give two examples of polyenes

A

Amphoterecin B
Nystatin

21
Q

Why should nystatin only be administered topically and not intravenously (IV)?

A

Nystatin is toxic and can cause side affects such as nephrotoxicity, hypokalaemia and thrombophlebitis

Thrombophlebitis (inflammtion causing blood clots)

22
Q

What is the mechanism of action for echinocandin anti-fungal drugs?

A

Echinocandins inhibit glucan synthesis through the inhibition of the beta 1,3 glucan synthase enzyme, causing the fungal cell wall to lose its structural integrity and undergo fungal cell lysis

23
Q

What is the spectrum of activity for the echinocandins?

A

Candida
Aspergillus

24
Q

How should echinocandins be administered?

A

Intravenous (IV)

25
Q

What are the two main mechanisms of resistance to echinocandin anti-fungal drugs?

A

Mutation of the beta 1,3 glucan synthase enzyme
Up-regulation of chitin synthesis

26
Q

What is the spectrum of activity for antimetabolite anti-fungal drugs?

A

Cryptococcus
Candida

27
Q

How should antimetabolites be administered?

A

Oral

28
Q

Give an example of an antimetabolite

A

Flucytosine

29
Q

Why should antimetabolites never be given alone?

A

Antimetabolites only require a one step mutation for fungi to develop resistance and thus antimetabolites should always be given with another anti-fungal drug

30
Q

What is the mechanism of action for griseofulvin anti-fungal drugs?

A

Griseofulvin inhibits fungal mitosis through disrupting microtubule formation

31
Q

What is the spectrum of activity for griseofulvin?

A

Dermatophytes

32
Q

How should griseofulvin be administered?

A

Oral

33
Q

What are the side affects of griseofulvin seen in cats?

A

Griseofulvin has an idiosyncratic reaction in cats meaning each individual cat can have unique, unpredictable reactions to this drug

34
Q

Can griseofulvin be used in pregnant animals?

A

No as griseofulvin is teratogenic

35
Q

(T/F) Although there has been debate, griseofulvin is still licensed for food producing animals in the UK

A

FALSE. Griseofulvin is no longer licensed for food producing animals in the UK