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BMSC2210 - Chemotherapy > L12 - echinocandins and terbinafine > Flashcards

L12 - echinocandins and terbinafine Flashcards

1
Q

What are the 3 echinocandins?

A

Caspofungin
Anidulafungin
Micafungin

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2
Q

How are echinocandins administered?

A

IV as too big for oral

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3
Q

What can caspofungin treat?

A

invasive candidosis
aspergillosis
empiric therapy

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4
Q

What can Anidulafungin treat?

A

Invasive candidosis

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5
Q

What can Micafungin treat?

A

Invasive candidosis
oesophageal candidosis
candidosis prophylaxis

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6
Q

What is used to treat aspergillosis if ambisome does not work?

A

Caspofungin

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7
Q

What do echinocandins inhibit?

A

glucan synthase

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8
Q

Mode of action of echinocandins?

A

bind to Fks1p subunit - block beta1,3-D-glucan synthesis

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9
Q

What are echinocandins not active against?

A

Cryptococcus
Mucoraceous moulds
Dimorphic fungi

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10
Q

Are echinocandins fungistatic or fungicidal?

A

mainly fungistatic

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11
Q

What causes less toxicity, caspofungin or amphotericin B, when treating candidaemia?

A

Caspofungin (slightly)

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12
Q

What is superior when treating candidaemia , andulafungin or fluconazole?

A

andulafungin

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13
Q

What is superior when treating candidaemia, Micafungin or Ambisome?

A

similar

but micafungin has FEWER SIDE EFFECTS

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14
Q

Toxicity associated with caspofungin?

A

hypokalemia
fever
deranged liver function

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15
Q

Toxicity associated with andulafungin?

A

headache
nausea
deranged liver function

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16
Q

Toxicity associated with Micafungin?

A

headache

deranged liver function

17
Q

Do echinocandins undergo hepatic metabolism?

A

some metabolism,

but NOT through CYP450

18
Q

Does caspofungin interact with other durgs?

A

some immunosuppressants
child steroids
some anti-microbials

19
Q

Does andulafungin interact with other drugs?

A

none known

20
Q

Does micafungin interact with other drugs?

A

some immunosuppressant

21
Q

How can Candida albicans be resistant to Echinocandins?

A

mutations in gene for FSK1 of beta 1-3 glucan synthase complex

codon 645 serine is mutated

22
Q

What other fungi are resistant to echinocandins?

A

C. glabrata

Cryptococcus?

23
Q

What is the paradoxical effect seen in echinocandins?

A

at high conc., anti fungal stops working - forces cells to respond rapidly and bypasses effects of drugs

24
Q

How does the paraodoxical effect occur in echinocandins?

A

up regulation of chitin biosynthesis

up regulation of cell wall integrity pathway

25
Q

Is there an upregulation of chitin in response to caspofungin?

A

yes

26
Q

What class of drug is Terbinafine?

A

allylamine

27
Q

What is the mode of action of terbinafine?

A

inhibition of squalene epoxidase - usually catalyses step in ergosterol synthetic pathway

28
Q

What can terbinafine be used against?

A

moulds - dermatophytes, dematiacous fungi, apergillus-like moulds

some yeasts

29
Q

What are the formulations of terbinafine?

A

Tablets
Gel/ cream
Spray

30
Q

What are the indications of Terbinafine?

A

dermatophyte infections of skin/nail

yeast skin infection

31
Q

What is more effective at pulse therapy - terbinafine or itraconazole?

A

terbinafine

32
Q

Does terbinafine bind to proteins?

A

yes, >90%

33
Q

What is Terbinafine metabolised by?

A

CYP enzymes

34
Q

Toxicity of terbinafine?

A

occasional liver dysfunction

altered taste perception

35
Q

drug interactions of terbinafine?

A

lots due to metabolism by CYP450

similar to azoles but other antifungals and anti-depressants too

36
Q

Is there resistance to terbinafine?

A

rare

substitution mutation in squalene epoxidase gene in Trichophyton rubrum

also issues with T. interdigitale

37
Q

What is Ibrexfungerp?

A

NEW ANTI-FUNGAL

Terpenoid glycoside inhibitor

38
Q

What is Ibrexafungerp active against?

A

Candida

Aspergillus

BMSC2210 - Chemotherapy (17 decks)

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