Lecture 6-7 - Anti-fungals (Cooke) Flashcards

1
Q

natural (derived from other fungi) anti-fungal drugs

A

amphotericin B

griseofulvin

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2
Q

synthetic anti-fungal drugs

A

azoles
allylamines
flucytosine

(only going over most commons)

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3
Q

derived from Penicillium mold and MOA disrupts mitosis

A

griseofulvin

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4
Q

topical griseofulvin is old treatment for

A

dermatophytosis (have better drugs with less SE now)

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5
Q

if giving griseofulvin orally should it be given with or w/o food

A

with a fatty meal

*azoles are used more commonly now

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6
Q

SE of griseofulvin

A

BM Suppression
teratogenic (not safe for pregos)
V/D
anorexia

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7
Q

derived from streptomyces

A

amphotericin B

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8
Q

MOA amphotericin B

A

binds sterols (cholesterols specific to fungi wall)

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9
Q

route of admin for amphotericin B

A

almost always IV, however there is a SC protocol for use PRN

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10
Q

amphotericin B oral absorption

A

POOR

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11
Q

Amphotericin B is __ toxic

A

nephrotoxic, must monitor renal values and give IVF

liposome form can reduce toxicity

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12
Q

CS of acute amphotericin B toxicity

A

vomiting
myalgia
fever
anaphylaxis

this is why give IV injection SLOWLY and D/C if there are any SE

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13
Q

amphotericin B spectrum

A

most fungi, some resistance is emerging

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14
Q

amphotericin B has poor penetration of

A

bone, brain/CSF, eye

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15
Q

what can you dilute amphotericin with

A

sterile H2O or D5W, NOT saline bc will precipitate

should always check renal values before, give IVF before and after administered

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16
Q

2 reasons would use SC route for amphotericin

A

cheaper

may reduce nephrotoxicity

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17
Q

benefits to amphotericin lipid complex drug

A

taken up by macs to the site of inflamm/fungus
greatest concentrations in liver, spleen, and lung = decreaed renal accumulation/toxicity
still need to monitor renal values and hydrate patient

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18
Q

benefit to liposome encapsulated AmB

A

small size, high concentration in CSF and kidneys (good for renal asper)

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19
Q

fluorinated pyrimidine

A

flucytosine

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20
Q

MOA flucytosine

A

interferes w DNA

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21
Q

absorption and penetration abilities of flucytosine

A

good oral absorption

penetrates CSF/BBB

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22
Q

Flucytosine can be used to tx

A

cryptococcus

candidiasis

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23
Q

flucystosine is synergistic with

A

amphotercin B

combo used for CNS dz/very sick p

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24
Q

cutaneous SE of flucytosine reported in dogs

A

drug eruptions

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25
Q

CBC SE of flucytosine reported in cats

A

thrombocytopenia

26
Q

flucystosine __ toxic

A

nephrotoxic

27
Q

most common antifungals used in vet med

A

azoles; imidazoles (ketoconazole) and triazoles (itra, flucon, posocon, voricon)

28
Q

MOA azoles

A

inhibit cytochrome P450 and inhibit ergosterol synthesis (disrupts cell membrane syn), can’t transport ATP = growth inhibition

***fungiSTATIC

29
Q

azoles are metabolized by the

A

liver (cytochrome P450) = drug interactions!

30
Q

azoles require __ for absorptions

A

acid

can use antinausea drug for SE but not a PPI/H2 bc need the acid!

31
Q

ketoconazole orally should be given with

A
fatty meal
no antacids (need acid)
32
Q

penetration of ketoconazole

A

poor penetration of brain/eye

33
Q

topical ketoconazole can be used to tx

A

candida, malassezia

oral can tx blasto but not asper, cryptococcus, sporothrix

34
Q

SE ketoconazole

A
nausea
vomiting 
anorexia 
hepatotoxicity 
cortisol suppression (old school tx for cushing's)
35
Q

ketoconazole is __ toxic

A

hepatotoxic (ALT, AST, ALP will go up, esp if ALT over ALP) = d/c drug

36
Q

oral itraconazole capsules should be given with __ meal and liquid with a __ meal

A

fatty meal, acidic environment

fasted

37
Q

distribution/penetration of itraconazole

A

no CNS

minimal urine excretion

38
Q

SE itraconazole

A
less toxic than keto 
same SE (nausea, vomit, inapp, hepatotoxic, cutaneous drug reaction)
39
Q

spectrum of itraconazole

A

broad;

histo, blasto, crypto, coccidioides, aspergillus

40
Q

fluconazole oral bioavailability and distribution

A

high oral bioavailability
water soluble = wide distribution including BRAIN/EYE
renal excretion of active drug also makes it good for fungal UTI (ie DM p)

41
Q

cryptococcus in the eye/CNS drug of choice

A

fluconazole

42
Q

fluconazole derivative that is more potent than flu and itraconazole

A

voriconazole

43
Q

itraconazole analoge that is as good or better than flu or itra for candida, crypto, asper, blasto, histo but is very very expensive

A

posaconazole

too expensive for vet med, 1 vial (100ml) = $1400 :0

44
Q

topical azoles

A

clotrimazole and enilconazole

45
Q

primary treatment for nasal aspergillus

A

clotrimazole

46
Q

SE of topical clotrimazole

A

irritation
erythema
aspiration pneumonia
airway obstruction (larynx swelling)

47
Q

non-responsive candida cystitis and renal aspergillosis possible treatment option

A

clotrimazole via infusion

SE caustic

48
Q

allylamine that inhibits ergosterol synthesis

A

terbinafine; similar to azoles but acts at different spot in ergosterol synth pathway

49
Q

most common tx for dermatophytosis

A

terbinafine

50
Q

oral bioavailability of terbinafine

A

good!

51
Q

3 anti-fungals that have good oral bioavailability

A

terbinafine
fluconazole
flucytosine

52
Q

SE terbinafine

A

V/D
hepatotoxic
pancytopenia

53
Q

__ seems to have some efficacy for treating pythium

A

terbinafine

54
Q

__ is an agricultural fungicide that inhibits RNA polymerase that may be effective against plant pathogen oomycetes

A

mefenoxam

seems to be good but NOT available for use in animals yet (case report of pythium being tx with itra + terbinafine + mefenoxam)

55
Q

terbinafine seems to be synergistic with

A

azoles

56
Q

lowest concentration of drgu that inhibits growth of the organism cultured in vitro (not in vivo) (NOT the concentration required to KILL the organism)

A

MIC; minimum inhibitory concentration

57
Q

when to consider sensitivity testing for fungal dz

A

systemic aspergillosis
non-responsive infection
minimal financial constraints

58
Q

first and second choice for blastomycosis, histoplasmosis, and systemic aspergillosis

A

itraconazole

amphotericin B

59
Q

first and second choice for cryptococcosis of CNS

A

Fluconazole

itraconazole

60
Q

first and second choice for coccidioidomycosis

A

itraconazole

fluconazole

61
Q

first and second choice for nasal aspergillosis

A

topical clotrimazole

topical enilconazole

62
Q

first and second choice for sporothrix

A

itraconazole

terbinafine