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Spring 2018 Pharm Exam 4 > #5: Antifungals > Flashcards

#5: Antifungals Flashcards

1
Q

What is the MOA of Amphotericin B

A

Binds to ergosterol and disrupts membrane integrity

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2
Q

ADME of Amphotericin B

  1. how is it excreted and therefore it causes
  2. How must it be given for fungal meningitis and why
A

ADME of Amphotericin B

  1. slowly excreted –> toxicity
  2. must be given intrathecal fungal meningitis b/c poor BBB penetration
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3
Q

Amphotericin B AEs

  1. what the immediate AE occurs when giving drug
  2. what is the long term/dosing limiting AE
A

Amph B AEs

  1. immediate AE = infusion rxn
  2. long term AE = renal damage
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4
Q

Amphotericin B AEs: infusion + renal

  1. how can you decr a immed infusion rxn (2 main things)
  2. how can help prev renal damage from becoming irrev
A

Amphotericin B AEs: infusion + renal

  1. decr infusion rxn by slow infusion and premedicate (antipyretics, antihistamines, sodium loading)
  2. prev renal damage by limiting cumulative dose
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5
Q

Lipid formulations vs conventional Amphotericin B

  1. 2 major pros
  2. which has more severe immed infusion risk
  3. what is the major con
A

Lipid formulations vs conventional Amphotericin B

  1. 2 major pros
    - less renal toxicity
    - less severe immed infusion rxns
  2. Amphotec = more severe immed infusion risk
  3. major con
    - greater hepatotoxicity risk
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6
Q

Uses for Amphotericin B

  1. main use
  2. Preferred over which 2 drugs in preg?
A

Uses for Amphotericin B

  1. main use = serious life threatening mycotic infxns
  2. preferred in pregnancy over azoles and caspofungin
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7
Q

What do ALL azoles inhibit which leads to the decr syn of ergosterol

A

ALL azoles inhibit fungal cytochrome P450 enzyme –> decr syn of ergosterol

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8
Q

Comparing Azoles

  1. which of the azoles has the best CNS penetration and highest therapeutic index
  2. which of the azoles has poor CNS penetration
  3. which has broadest spectrum
A

Comparing Azoles

  1. Fluconazole = best CNS pentration and highest therapeutic index
  2. Itraconazole = poor CNS penetration
  3. Voriconazole = broadest spectrum
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9
Q

AEs of Fluconazole

  1. major skin SE
  2. major SE affecting preg women
  3. what does it inhibit that incr serum conc of phenytoin, warfarin and causes bleeding
A

AEs of Fluconazole

  1. major skin SE = SJS
  2. teratogenic
  3. it inhibits CYP2C9 –> incr serum conc of phenytoin, warfarin –> bleeding
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10
Q

Uses of Fluconazole

  1. what dz used for
  2. what types of pts is it used as ppx in (2 types)
A

Uses of Fluconazole

  1. what dz used for
  2. what types of pts is it used as ppx in
    - high risk neutropenic pts
    - HIV/AIDs pts w/recurrent candidiasis
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11
Q

Which azole has:

  • decr abs w/ PPIs and H2 antag
  • decr bioavail w/rifampin and rifamycins
A

Itraconazole

  • decr abs w/ PPIs and H2 antag
  • decr bioavail w/rifampin and rifamycins
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12
Q

Itraconazole

  1. major AE
  2. what is it a potent inhibitor of therefore
  3. what 3 drugs is it CI w/
A

Itraconazole

  1. major AE = CHF
  2. potent inhibitor of CYP34A soo…
  3. CI w/ some statins, midazolam, triazolam
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13
Q

Itraconazole

DoC for what 3 things

A

Itraconazole used for

  1. dimorphic fungi histoplasma
  2. blastomyces
  3. sporothrix
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14
Q

What drugs is a/w visual disturbances including blurring and changes in color vision or brightness that is reversible and usu only occurs in 1st 30 min

A

Voriconazole

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15
Q

Uses for Voriconazole

- main thing it Txs

A

Uses for Voriconazole

- main thing it Txs = invasive aspergillosis

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16
Q

drug prototype for class echinocandins

A

echinocandins class

- drug = Caspofungin

17
Q

Caspofungin (echinocandins)

  1. MOA
  2. how must it be admin
  3. major AE
  4. what 2 species can it only tx
A

Caspofungin

  1. MOA = cell wall synthesis inhibitor
  2. must it be admin IV (poorly abs if PO)
  3. major AE = hepatotoxicity
  4. only txs Candida or Aspergillus species
18
Q

Caspofungin AEs

  1. Hepatoxicity incr when given w/ what other med
  2. what 2 drugs does it interact w/
  3. risk in preg
A

Caspofungin AEs

  1. Hepatoxicity incr when given w/ cyclosporine
  2. 2 drug interactions = tacrolimus, rifampin
  3. embryotoxic in preg
19
Q

Caspofungin

- what is it a 2nd line Tx for

A

Caspofungin

  • 2nd line Tx for Invasive aspergillosis (if Voriconazole doesnt work)
20
Q

What antifungal is a mitotic inhibitor so it intereferes with microtubule assembly so the fungus cant divide

A

Griseofulvin

  • mitotic inhibitor so it intereferes with microtubule assembly so the fungus cant divide
21
Q

Griseofulvin AEs

  1. what 3 organ systems does it affect
  2. what type of inducer is it –> what 2 drugs does it incr the metab of
A

Griseofulvin AEs

  1. CNS, Liver, GI
  2. P450 inducer
    - incr metab of warfarin, phenobarbital
22
Q

Tx w/Griseofulvin

  1. what can it only be used for
  2. how long must tx last
A

Tx w/Griseofulvin

  1. only used for dermatophytosis
  2. tx until old infected tissue gone (months - 1 yr)
23
Q

Which 2 antifungals are keratophyliic and get deposited into newly growing keratin of skin/nails –> prevent fungal infxn of new nail

A

2 antifungals that are keratophyliic

  • Griseofulvin
  • Terbinafine/Lamisil

(get deposited into newly growing keratin of skin/nails –> prevent fungal infxn of new nail)

24
Q

Terbinafine/Lamisil

  1. what fungal enzyme does it inhibit –> causes ____
  2. drug interactions?
  3. what is it used for (and esp)?
  4. other MOA
A

Terbinafine/Lamisil

  1. inhibits fungal enzyme squalene epoxidase –> incr squalene levels (toxic)
  2. NO drug interactions
  3. used for dermatophytosis (esp onychomycosis)
  4. other MOA = decr ergosterol syn
25
Q

What type of drug is Flucytosine

- and precursor to?

A

Flucytosine = anti metabolite and precursor to 5-FU

26
Q

Flucytosine MOA

  1. in fungal cells what enzyme takes it up
  2. what does it then get converted to
  3. what then metab to
  4. ultimately stopping what in fungal cells
A

Flucytosine MOA

  1. in fungal cells taken up by cytosine permease–>
  2. converted to 5-FU –>
  3. metab to –> nucleotide –>
  4. ultimately stops RNA/DNA synth in fungal cells
27
Q

Flucytosine

  1. major AE (gen/spp)
    - what 2 groups of pts is it esp seen in
A

Flucytosine AEs

  1. hematotoxicity (pancytopenia)
    - seen esp in renal insuffic, AIDs pts
28
Q

Flucytosine Uses

- what is it only used in and why

A

Flucytosine Uses

- only used in combos b/c narrow spectrum of action

29
Q

Flucytosine: use in combos

  1. used w/ amph B for ______
  2. used w/ itraconazole for _____
A

Flucytosine: use in combos

  1. used w/ amph B for cryptococcus neoformans
  2. used w/ itraconazole for chromoblastomycosis

Spring 2018 Pharm Exam 4 (7 decks)

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