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Pharmacology - Final Exam > Antifungals > Flashcards

Antifungals Flashcards

1
Q

Define halo sign

A
  • CT finding of a fungal infx in the lung

- dense center with fuzzy outline

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2
Q

Define candidemia

A
  • fungal infx in the blood
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3
Q

What are the symptoms of fungal infx?

A
  • vague
  • inflam response (topical redness)
  • fever, cough
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4
Q

What are good indicators of a fungal infx?

A
  • presence of risk factors

- serologic testing, although not definitive

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5
Q

What are the levels of fingal infx tx?

A
  • empiric
  • targeted
  • prophylaxis
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6
Q

Define empiric therapy

A
  • tx of possible/probable fungal infx

- symptoms consistent, no positive culture data

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7
Q

Define targeted therapy

A
  • definitive positive culture data
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8
Q

Define prophylaxis

A
  • preventative tx in at-risk pt
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9
Q

Who are at risk for fungal infections?

A
  • immunosuppresed
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10
Q

What are the challenges of fungal infections?

A
  • difficult to dx
  • potential toxicity of available agents
  • need for targeted tx
  • resistance develops
  • limited formulations
  • aggressiveness of pathogens
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11
Q

What are the 3 main classes of antifungals?

A
  • azoles
  • polyenes/amphotericins
  • echinocandins
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12
Q

Define fungistatic

A
  • drugs that inhibit growth
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13
Q

Define fungicidal

A
  • drugs that kill fungal pathogens
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14
Q

What is the 1/2 life of amphotericin?

A
  • very long (15d)
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15
Q

T/F: Amphotericin does not require renal or hepatic adjustment.

A
  • true
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16
Q

What is the MOA of amphotericin?

A
  • binds to and disrupts ergosterol which creates pores
  • pores alter permeability of membrane increasing leaking of intracellular components
  • leads to fungal cell death
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17
Q

What is the coverage of amphotericin?

A
  • broad spec

- excellent coverage

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18
Q

What are the ADEs of amphotericin?

A
  • infusion related reactions

- renal + hepatic toxicity in chronic use

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19
Q

Labs = increased Scr & BUN, K & Mg wasting

What ADE is this?

A
  • renal toxicity
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20
Q

Labs = increased LFTs

What ADE is this?

A
  • hepatic toxicity
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21
Q

What is the purpose of lipid formulations of amphotericin?

A
  • improve tolerability

- reduce toxicity

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22
Q

When is amphotericin used?

A
  • life-threatening or refractory infx
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23
Q

What is a benefit of flucytosine?

A
  • large volume of distribution
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24
Q

What is the MOA of flucytosine?

A
  • prodrug that inhibits fungal DNA & RNA synthesis
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25
Q

What is the tx for Cryptococcus and Candida meningitis?

A
  • amphotericin + flucytosine
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26
Q

What are the ADEs of flucytosine?

A
  • GI tract (N/V)
  • myelosuppression (anemia, thrombocytopenia, leukopenia)
  • hepatotoxicity (increased LFTs)
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27
Q

When is flucytosine used?

A
  • cytprococal meningitis
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28
Q

What is a common use of flucytosine?

A
  • cytprococal meningitis
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29
Q

What are the 2 types of -azoles?

A
  • imidazoles

- triazoles

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30
Q

What is the MOA of azoles?

A
  • inhibit fungal CYP P450 dependent enzyme lanosterol = reduces formation of ergosterol
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31
Q

Are azoles fungistatic or fungicidal?

A
  • fungistatic
32
Q

What are the ADEs of azoles?

A
  • GI upset

- increased LFTs

33
Q

What are the DIs of azoles?

A
  • CYP450 3A4 is a major target results in enzyme inhibition

- decrease metabolism of other drugs metabolized by affected CYP450 enzymes

34
Q

Of the two types of azoles, which is more likely to have DIs?

A
  • imidazoles
35
Q

Is ketoconazole more or less selective for fungal CYP450 enzymes & what does that mean?

A
  • less

- more likely to cause DIs

36
Q

What is the use of ketoconazole?

A
  • topical fungal infections
37
Q

What is an unexpected use of ketoconazole?

A
  • prostate cancer
38
Q

T/F: Itraconazole is a good broad spectrum abx.

A
  • true
39
Q

How should itraconazole be taken?

A
  • with food (coca cola)

- NOT WITH ACID REDUCERS

40
Q

What does itraconazole cover?

A
  • candida

- aspergilllus

41
Q

What does itraconazole treat?

A
  • onychomycosis

histoplasmosis & blastomycosis is rare

42
Q

T/F: Fluconazole does not need to be dose adjusted for renal insufficiency.

A
  • false, decrease dose
43
Q

What is fluconazole used for?

A
  • tx & prophylaxis of coccidodial & cryptococcal meningitis
  • tx of candida
44
Q

What does fluconazole NOT have activity against?

A
  • Aspergillus
45
Q

What is resistant to fluconazole?

A
  • C. krusei & glabrata
46
Q

What is the bioavailability of oral voriconazole?

A
  • excellent, no issues with acid reducers
47
Q

What are the ADEs of voriconazole?

A
  • hepatic toxicity
  • rash
  • visual changes
48
Q

When does voriconazole require dose adjustments?

A
  • hepatic not renal insufficiency
49
Q

What does voriconazole cover?

A

broad spectrum

  • candida, including fluconaole resistant candida
  • aspergillis
  • Secedosporoium apiospermum
  • Fusarium
50
Q

When is voriconazole used?

A
  • tx or prophylaxis of invasive fungal infections
51
Q

What is the coverage of posaconazole?

A
  • broad spec
52
Q

What is approved for use a prophylaxis of fungl infx in immunosuppressed patients?

A
  • posaconazole
53
Q

What is posaconazole used to tx?

A
  • oropharyngeal candidiasis
54
Q

What does taking posaconazole after a full meal or with an acidic carbonated beverage do?

A
  • increases bioavailability
55
Q

What is isavuconazole’s MOA?

A
  • prodrug

- isavuvuconazonium sulfate –> isavuconazole

56
Q

When is isavuconazole used?

A
  • tx of invasive aspergillosis & mucormycosis
57
Q

How is isavuconazole administered?

A
  • IV with inline filter
58
Q

What is a risk of isavuconazole?

A
  • increased LFTs

- infusion related rxn

59
Q

What is eficonazole?

A
  • first topical azole approved to treat onychomycosis
60
Q

What is the class echinocandins active against?

A
  • candida

- aspergillus

61
Q

What is the MOA of the class echinocandins?

A
  • inhibit glucan synthase
  • inhibits creation of component of fungal cell wall
  • disrupts fungal cell integrity & leads to cell death
62
Q

T/F: Echinocandins are fungicidal against Candida & aspergillus.

A
  • false
  • fungicidal against candida
  • fungistatic against aspergillus
63
Q

What are the drugs in the class echinocandins?

A
  • suffix: - fungin
64
Q

What are the ADEs of echinocandins?

A
  • GI (N/V)
  • flushing rxn if infused too fast
  • increased LFTs
65
Q

T/F: In comparison to -azoles, echinocandins have greatly reduced DIs.

A
  • true
66
Q

When are echinocandins used?

A
  • refractory cases

- renal or hepatic impairment (no dose adj needed)

67
Q

What is terbinafine used to tx?

A
  • topical dermatophytoses
68
Q

What is the MOA of terbinafine?

A
  • interferes with ergosterol synthesis by inhibiting squalene peroxidase
69
Q

What is a risk of terbinafine?

A
  • hepatic toxicity (monitor LFTs)
70
Q

What is the use of tolnaftate?

A
  • tineas

- superficial fungal infx

71
Q

What does tolnaftate not work against?

A
  • candida

- onychomycosis

72
Q

What is a ADE of tolnaftate?

A
  • skin irritation
73
Q

What is nystatin & what is it active against?

A
  • same class as amphotericin, polyene macrolide antifungal

- candida

74
Q

How do you select antifungal therapy?

A
  • confirmed fungal infx or at risk
  • prophylaxis vs. empiric/targeted
  • based on organism
  • severity
75
Q

When in doubt of what to treat a fungal infx, what do you do?

A
  • look it up!

Pharmacology - Final Exam (4 decks)

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