Antifungals Flashcards

1
Q

3 forms of fungi

A

Filamentous fungi
Yeasts
dimorphic- either year or filamentous fungi

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2
Q

what distinctive features do filamentous fungi have

A

hair like hyphae
mycelium which holds hyphae together
septae
produce spores

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3
Q

what distinctive feature do yeasts have

A

divide by budding

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4
Q

Antifungal targets

A

cell membrane- ergesterol

cell wall- B 1,3 glucan.

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5
Q

Are fungi prokaryotic or eukaryotic

A

eukaryotic

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6
Q

function of ergesterol

A

regulate membrane permeability.

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7
Q

mechanism of egesterol synthesis.

A

Squalene is converted to lansterol which is converted to ergesterol.
• Ist conversion requires enzyme squalene epoxidase
• 2nd conversion requires enzyme Lanosterol 14a demethylase.

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8
Q

what part of a fungi is ergesterol part of

A

cell membrane

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9
Q

what part of a fungi is B1, 3 glucans part of

A

cell wall.

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10
Q

what are the 4 main anti fungal classes

A

Polyenes
Allyamines
Azoles
Echinocandins.

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11
Q

what is the mode of action of polyenes

A

– Association with ergosterol- binds to it.

– Formation of pore-like molecular aggregates

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12
Q

Main examples of polyenes

A

Amphotericin B
lipid associated Amphotericin B
Nystatin

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13
Q

side effects of Amphotericin B

A

Nephrotoxicity

allergic reactions

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14
Q

Why is lipid amphotercin better than normal amphotericin b

A

• Minimize delivery of AmB to kidney cells- more selective toxicity.
redeuced nephroroxicity.

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15
Q

How is nystatin prescribed

A

parenterally.

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16
Q

How is amphotericin b prescribed

A

parenterally.

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17
Q

What is the mode of action of allyamines

A

inhibit egosterol synthesis

acts on squalene epoxidase.

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18
Q

Example of allyamines

A

Terbinafine

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19
Q

Is amphotericin broad or narrow spectrum

A

broad

20
Q

Are allyamines broad or narrow spectrum

A

broad

21
Q

What are the side effects of allylamines

A

liver toxicity.

22
Q

clinical use of allyamines

A

Dermatophyte infections (superficial fungal infections)-caused by fungi which like to eat keratin.

23
Q

What conditions are allyamines used for

A

• Topical use
– Athletes foot , fungal groin infection, (tinea pedis), tinea corporis, tinea cruris.
• Systemic (oral) use
– Scalp ringworm, nail fungal infection (tinea capitis), onychomycosis

24
Q

what are the 2 types of azoles.

A

Imidazole- toxic

Triazole- non toxic

25
Q

how many nitrogen atoms sides imidazole have

A

2

26
Q

how many nitrogen atoms do triazoles have

A

3

27
Q

What is the mode of action of azoles

A

• Mode of action
– Inhibit ergosterol synthesis
Lanosterol 14α-demethylase

28
Q

Are azoles broad or narrow spectrum

A

depends on drug but mainly broad

29
Q

which is the only azole which does;t work against Aspergillus

A

Fluconazole.

30
Q

Most commonly used imidazole

A

Clotrimazole- vaginal thrush

31
Q

Most commonly used Triazoles

A

Fluconazole
Itraconazole
Voriconazole.

32
Q

What are the side effects of azoles

A

hepatotoxicity- mild liver enzyme abnormalities.

33
Q

what drugs do azoles commonly interact with

A

Inhibit cytochrome P450 enzymes.

34
Q

what are type of infections are imidozoles used for

A

superficial infections

35
Q

What type of infections are triazoles used for

A

severe fungal infections

36
Q

What is the mode of action of Echinocandins

A

Inhibition of β-1,3-glucan synthase

37
Q

Most commonly used Echinocandins

A

Anidulafungin

38
Q

Are echinocandins broad or narrow spectrum

A

broad- although it misses out cryptococcus.

39
Q

What are the side effects of enchinocandins

A

Minimal effects

skin rash, nausea, vomiting, headache, diarrhoea in common with any other drug

40
Q

Clincial use of enchicandins

A

Systemic infections

41
Q

what type of drug is 5-fluorocytosine (5-FC)

A

Synthetic analogue of cytosine

42
Q

What is the mode of action of 5-fluorocytosine (5-FC)

A

Entry into cell requires fungal cytosine perm ease.

• Inhibit RNA/protein synthesis and DNA synthesis

43
Q

What spectrum of fungi does 5-fluorocytosine (5-FC) act against.

A

Yeasts only

44
Q

What are the side effects of 5-fluorocytosine (5-FC

A

Bone marrow suppression

45
Q

Clinical use of 5-fluorocytosine (5-FC)

A

Limited

Cryptococcal meningitis

46
Q

What are the reasons for therapeutic drug monitoring

A

to minimize efficacy

to minimize toxicity

47
Q

what 3 drugs are therapeutically monitored

A

Itraconazole
5-fluorocytosine
Voriconazole.