antifungals Flashcards

1
Q

list the antifungal classes

A
  1. polyenes
  2. azoles
  3. echinocandins
  4. terbinafine
  5. griseofulvin
  6. topical antifungals
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2
Q

list the polyenes

A

amphotericin B

nystatin

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3
Q

list the azoles

A

fluconazole

itraconazole

voriconazole

prosaconazole

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4
Q

list the echinocandins

A

corspofungin

andidulafungin

micafungin

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5
Q

list the topical antifungals

A

azoles: cotrimazole
hydroxy pyridones: ciclopirox
thiocarbamate: tolnafate

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6
Q

azoles MOA

A

inhibit synthesis of ERGOSTEROL via inhibition of lanosterol C14-demethylase

inhibits CELL WALL SYNTHESIS

protens CYP450 INHIBITOR

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7
Q

indications for azoles

A

UNCOMPLICATED systemic infections in immunocompromised patients

CANDIDA (fungistatic)
aspergillus (fungicidal)
CRYPTOCOCCUS 
blastomycosis 
coccidioimycosis 
histoplasmosis
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8
Q

why is fluconazole good for UTIs?

A

because it is renally eliminated and achieves reliable urinary concentration

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9
Q

which drug causes phototoxicity

A

voriconazole (azole)

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10
Q

what is a consideration with azoles RE: interactions

A

azoles are potent CYP3A4 inhibitors

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11
Q

echinocandin MOA

A

inhibit synthesis of GLUCAN SYNTHASE which is an essential component of cell wall synthesis

inhibition of glucan synthase weakens the fungal cell wall and results in lysis

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12
Q

echinocandin indications

A

for SEVERE INVASIVE CANDIDA (on which it is fungicidal)

aspergillis infection (fungistatic)

NOT renally eliminated
IV admin only
caspofungin requires hepatic dosage adjustment

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13
Q

polyenes MOA

A

bind to ERGOSTEROL in cell membrane resulting in development of PORES in fungal membrane

this disrupts the cell wall permeability and results in cell death

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14
Q

polyenes indications

A

serious, INVASIVE/SYSTEMIC fungal infections

Amphotericin B: poor CSF penetration but effective for aspergillus, invasive candida and cryptococcal meningitis

Amphotericin B: vitreal and urine penetration–NOT renally eliminated–IV only

Nystatin: good for candida–local/topical only because HIGHLY TOXIC in IV form

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15
Q

terbinafine MOA

A

inhibits ERGOSTEROL synthesis via inhibition of SQUALENE OXIDASE

distrubutes mainly to sebum and skin

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16
Q

terbinafine indications

A

ONCHOMYCOSIS

used for fungal nail infections

17
Q

what is a consideration with terbinafine RE: interactions

A

it is a potent CYP2D6 inhibitor

18
Q

griseofulvin MOA

A

binds to TUBULIN and therefore interferes with microtubule formation and INHIBITS MITOSIS

binds to KERATIN in keratin precursor cells making them resistant to fungal infections

19
Q

griseofulvin site of action/administration

A

ORAL ONLY

no topical action

20
Q

what is a consideration with griseofulvin RE: interactions

A

it is a potent CYP450 INDUCER

21
Q

how do topical azoles work

A

i.e cotrimazole

inhibits ergosterol synthesis

22
Q

how do topical hydroxypyridones work

A

i.e ciclopirox

inhibits transport and uptake of essential substrates into the fungal cell

23
Q

how do topical thiocarbamates work

A

i.e tolnafate

inhibits ergosterol synthesis via inhibition of squalene oxidase