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eDeN_cArDs > Anti-Fungal / Anti-Protozoal > Flashcards

Anti-Fungal / Anti-Protozoal Flashcards

1
Q

Unlike bacteria, fungi are _____, with rigid cell walls composed largely of ____

A

eukaryotic , chitin

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2
Q

What does fungal cell membranes contain?

A

ergosterol

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3
Q

Name the 4 drug classes for subcutaneous and systemic mycotic infections

A

Amphotericin B
Antimetabolite antifungals (Flucytosine)
Echinocandins (Caspofungin)
Azole Antifungals (Triazoles)

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4
Q

Name the 3 drug classes for cutaneous mycotic infections

A

Nystatin
Squalene epoxidase inhibitors (Terbinafine)
Azole antifungals (Imidazoles)

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5
Q

Amphotericin B is a naturally occurring ______ anti fungal produced by Stroptomyces nodosus

A

polyene

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6
Q

Amphotericin B MOA

A

binds to ergosterol in plasma membranes of sensitive fungal cells to forms pores –> disrupt membrane function, allowing electrolytes and small molecules to leak from the cell, resulting in cell death

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7
Q

Amphotericin B is fungicidal or fungistatic?

A

fungicidal: high conc
fungistatic: low conc

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8
Q

Amphotericin B is active against

A

Candida albicans (Candidiasis)
Histoplasmosis
cryptococcus neoformans
aspergillus (Aspergilloses)

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9
Q

Common indiction for Amphotericin B

A

oral candidiasis alongside nystatin

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10
Q

Amphotericin B administration

A

Topical or slow IV infusion as GI absorption is negligible for all formulations

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11
Q

Amphotericin B is ____ in water

A

insoluble

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12
Q

Amphotericin B excretion

A

Urine and some via bile

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13
Q

Amphotericin B dose adjustment for renal dysfunction

A

TDD 50%

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14
Q

Amphotericin B ADR (Name 4)

A 
Fever and chills
nephrotoxicity 
hypotension 
thrombophlebitis 
ototoxicity
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15
Q

Amphotericin B Preggo?

A

Cat B

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16
Q

Name an antimetabolite Antifungals

A

5-Flucytosine

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17
Q

5-Flucytosine is _____-soluble

A

water

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18
Q

5-Flucytosine MOA

A

enters fungal cells through cytosine specific permeases –> converted by cytosine deaminase to 5-fluorouracil –> incorporated into fungal RNA –> 5-fluorodeoxyuridine monophosphate (a potent inhibitor of thymidylate synthase)

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19
Q

5-FC is fungi_____

A

static

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20
Q

5-Flucytosine is effective in combination with ___ for treating __________ and _________

A

amphotericin B, Candidiasis, cryptococcosis

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21
Q

5-Flucytosine absorption

A

oral

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22
Q

5-Flucytosine CSF?

A

yes

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23
Q

mechanism of resistance for 5-Flucytosine

A

Decreased levels of any of the enzymes in conversion to 5-FC

Used in combination with amphotericin B

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24
Q

5-Flucytosine ADR

A

GI
bone marrow suppression (monitor leukocytes and platelets weekly
hepatotoxicity

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25
Q

5-Flucytosine preggo

A

Cat C

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26
Q

Name 3 echinocandins

A

caspofungin
micafungin
anidulafungin

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27
Q

MOA of Echinocandins

A

inhibit the activity of the gluten synthase complex, resulting in the loss of the structural integrity of the cell wall

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28
Q

Echinocandins oral bioavailability

A

poor

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29
Q

Echinocandins CSF?

A

yes

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30
Q

Echinocandins broad or narrow activity?

A

broad spectrum

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31
Q

Echinocandins have potent activity against which species

A

aspergillus and most candidia species including those species resistant to azaleas

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32
Q

Echinocandins preggo

A

cat C

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33
Q

Caspofungin administration

A

IV

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34
Q

Caspofungin use

A

first line option for patients with invasive candidiasis including candidemia
second line option for invasive aspergillosis in patients who have failed or cannot tolerate amphotericin B or an azalea

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35
Q

Caspofungin elimination

A

urine and faeces

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36
Q

Caspofungin metabolised by CYP450?

A

no

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37
Q

Caspofungin metabolised by…..

A

hydrolysis and N-acetylation

38
Q

Caspofungin ADR

A

GIT, fever, chills, rashes, skin flushing

thrombocytopenia

39
Q

Name the Triazoles

A

Fluconazole
Itraconazole
Voriconazole

40
Q

What are the 2 different classes of azalea antifungals?

A

imidazole and triazoles

41
Q

Imidazole are given ______ while triazoles are given ______

A

topically, systematically

42
Q

Azoles are fungi___

A

static

43
Q

Azoles MOA

A

inhibit C-14 alpha-demethylasse, blocking the demethylation of lanosterol to ergosterol
inhibition of ergosterol biosynthesis disrupts membrane structure and function and inhibits fungal cell growth

44
Q

Fluconazole administration

A

oral, IV

45
Q

Fluconazole indications

A

Candidemia and most forms of mucocutaneous candidiasis
cryptococcal meningitis
histoplasmosis
blastomycosis
single dose for vulvovaginal candidiasis
fungal meningitis

46
Q

Fluconazole CSF?

A

yes

47
Q

Fluconazole cross into breast milk?

A

yes

48
Q

Fluconazole clearance

A

renal

49
Q

Fluconazole ADR

A 
N/V
headache
skin ashes 
hepatotoxicity 
QT prolongation
50
Q

Itraconazole administration

A

oral

oral solution on empty stomach

51
Q

Itraconazole advantage

A

broad spectrum

52
Q

Itraconazole indications

A

blastomycosis and aspergillosis in patients intolerant to Amphotericin B
onychomycosis in non immunocompromised patients

53
Q

Itraconazole CSF?

A

no

54
Q

absorption of Itraconazole decreased with…..

A

antacids and ppi

55
Q

Itraconazole metabolised in…

A

liver

56
Q

Itraconazole excreted in…

A

feces and urine

57
Q

Itraconazole ADR

A

N/V, HA, skin rashes
Hepatotoxicity
QT prolongation
Itraconazole is associated with cardio toxicity

58
Q

Voriconazole ADR

A

N/V, HA, skin rashes
Hepatotoxicity
QT prolongation
Neuro toxicity (visual disturbances)

59
Q

Voriconazole administration

A

oral, IV

60
Q

Voriconazole indications

A

invasive asperigillosis

candida

61
Q

Voriconazole CSF?

A

yes

62
Q

Voriconazole metabolism

A

CYP450

63
Q

Voriconazole elimination

A

80% of inactive metabolites are exerted via urine

64
Q

What does imidazole have activity against

A 
epidermophyton
microsporum
Trichophyton
Candida
Malassezia
65
Q

Name the 2 imidazole

A

Clotrimazole

Miconazole

66
Q

Imidazole ADR

A

Contact dermatitis, vulvar irritation and edema

67
Q

Clotrimazole administration

A

topical

68
Q

Clotrimazole;s therapeutic uses

A

dermatophyte infections

vulvovaginal candidiasis

69
Q

Miconazole administration

A

topical

70
Q

Miconazole persists in skin for ____ days after application

A

> 4

71
Q

Miconazole Indications

A

tinea pedis, tinea curries and tineaa versicoloured

vulvovaginal candidiasis

72
Q

Imidazole ADR

A

topical: contact dermatitis, vulvar irritation and deem

GI (for oral admin)

73
Q

What is nystatin?

A

polyene anti fungal

74
Q

Nystatin MOA

A

similar to amphotericin B
binds to ergosterol in plasma membranes of sensitive fungal cells to forms pores –> disrupt membrane function, allowing electrolytes and small molecules to leak from the cell, resulting in cell death

75
Q

Nystatin administration

A

oral, cream, pessary

76
Q

Nystatin can be administered as an oral agent for the treatment of…..

A

oropharyngeal candidiasis

77
Q

is Nystatin used parenterally?

A

no

systemic toxicity

78
Q

Nystatin spectrum

A

broad
oral or gi
vulvovaginal candidiasis

79
Q

What is Nystatin commonly used for

A

cutaneous and oral candida infections

80
Q

Nystatin ADR

A

rare. may cause skin irritation

81
Q

Name a squalene epoxidase inhibitor

A

terbinafine

82
Q

Terbinafine MOA

A

inhibiting squalene epoxidase –> block its conversion to lanosterol and biosynthesis of ergosterol
increased membrane perm and death of the fungal cell

83
Q

Terbinafine Administration

A

oral and topical

84
Q

Terbinafine is active against

A

richophyton

85
Q

oral Terbinafine is used to treat

A

dermatophyte onychomycoses and tinea capitis

86
Q

Terbinafine oral bioavailability

A

40%

87
Q

Terbinafine (oral) is extensively metabolised by _________ enzymes and excreted mainly via _____

A

CYP450, urine

88
Q

Terbinafine ADR

A

GI, HA, rash
hepatic failure
exacerbation of SLE

89
Q

Terbinafine preggo

A

cat B (oral) cat A (vaginal)

90
Q

Terbinafine breastfeeding

A

no

eDeN_cArDs (5 decks)

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