Fitz - Antifungal Drugs Flashcards

1
Q

MOA: Amphoterecin B

A

insert into yeast membrane, physical association w/ ergosterol to form hydrophilic pores in cell membrane > disruption of membrane integrity

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2
Q

AEs: Amphotericin B Deoxycholate

A

-at infusion: chills, fever, anemia, hypotension
-later onset: nephrotoxicity
(mostly ass’d with the deoxycholate)

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3
Q

polyene drug

A

amphotericin B

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4
Q

mechanism of nephrotoxicity caused by amphotercin B

A
  • direct damage to distal tubule
  • Na, Mg, K wasting > hypokalemia
  • decreased GFR> arteriole constriction
  • further concentration of drug in tubule > inc damage
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5
Q

pts at increased risk for nephrotoxicity caused by amphotericin B

A
  • transplant pt
  • HIV pts
  • pts with serious inf (gm(-), MRSA)
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6
Q

triazole drugs - 1st gen

A
  • fluconazole

- utraconazole

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7
Q

triazole drugs - 2nd gen

A
  • voriconazole

- posaconazole

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8
Q

MOA: fluconazole

A
  • inhibition of lanoserol > ergosterol synthesis

- disrupts sterol content in cell membrane

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9
Q

what yeast CYP450 enzyme does fluconazole target?

A

14-alpha-demethylase

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10
Q

Fluconazole indications

A
  • candida albicans

- cyptococcus (w/ AmpB)

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11
Q

Fluconazole limitations

A

aspergillus

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12
Q

Fluconazole clearance

A

75% renal

-good for candiduria

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13
Q

Itraconizole indications

A
  • candida albicans
  • other candida
  • histo*
  • coccidioides*
  • blastomycoses*
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14
Q

voriconisol indications

A
  • candida albicans
  • other candida
  • aspergillus
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15
Q

echinocandins

A
  • caspifungin
  • micafungin
  • anidulafungin
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16
Q

MOA: echinocandins

A

inhibition of beta-(1,3)-glucan synthase leading to osmotic fragility of the fungal cell wall

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17
Q

metabolism of caspofungin

A

hepatic - good for renal pts

18
Q

what type of pts do you worry about caspofungin drug interactions with?

A

immunocomp pts d/t cyclocporine or tacrolimus

19
Q

caspofungin indications

A

-serious opportunistic infections (candidiasis, aspergillosis)

20
Q

how long can it take to see results of antifungals?

A

up to 8 days!

21
Q

what would you use in an HIV pt with cadidiasis who failed fluconazole, amphotericin B, and itraconazole

A

caspofungin

22
Q

caspofungin limitations

A
  • histoplasmosis
  • coccidiomycosis
  • fusarium spp
23
Q

histoplasmosis has been ass’d with what type of therapy?

A

anti-TNFalpha therapy

24
Q

most common pulmonary and systemic mycosis in humans

A

histoplasmosis

25
Q

triazole opportunistic indications

A
  • aspergilllus
  • candida
  • rhizopus
  • cryptococcus
26
Q

triazole pathogenic indications

A
  • histoplasma
  • coccidioides
  • blastomyces
  • paracoccidiodies
27
Q

intraconizole is front line tx for

A
  • histoplasmosis
  • coccidioides
  • blastomycoses
28
Q

tx of oral candidiasis in HIV pts

A
  • oral fluconazole

- can also use itraconazole

29
Q

drug of choice for invasive aspergillosis

A

voriconazole

30
Q

what do you use for candidiasis resistant to fluconasole (C. krusi, c. galbrata)

A

voriconazole

31
Q

AEs: ketoconazole

A
  • inhibition of adrenal and gonadal steroid synthesis
  • gynecomastia
  • decreased libido
32
Q

2 triazoles with wide dist including the CSF

A
  • voriconazole

- fluconazole

33
Q

what would impair the absorption of itraconazole?

A

antacids - needs gastric acidity to dissolve

34
Q

2 triazoles that inhibit hepatic CYP450 and enhance renal toxicity

A
  • voriconazole

- itraconazole

35
Q

why do you avoid voriconazole in kids?

A

vision disturbances

36
Q

rare fungal infection ass’d with tornado-related wounds

A

zygomycosis

37
Q

tx of mucormycosis (zygomycosis)

A

amphotericin B

38
Q

drug of choic for crytoccal meningitis

A

amphotericin B + 5-FC

39
Q

MOA: 5-FC

A

inhibition of DNA & protein synthesis

40
Q

intrinsic resistance to 5-FC is caused by

A

mutated cytosine permease (can’t cross cell membrane)

41
Q

acquired resistance to 5-FC is caused by

A

mutated cytosine deaminase (can’t be converted to active form, 5-FU)

42
Q

role of amphotericin B in tx of cryptococcal meningitis

A

creates ergosterol pores for 5-FU to enter in the case of resistance