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PHRM 865 > Antifungals (Kays) > Flashcards

Antifungals (Kays) Flashcards

1
Q

What is amphotericin B’s mechanism of action?

A

binds ergosterol and increases cell permeability, leading to leakage of Na/K/cellular constituents and ultimately cell death

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2
Q

What is flucytosine’s mechanism of action?

A

deaminates to 5-FU, when converts to 5-fluorodeoxyuridylic acid monophosphate and inhibits thymidylate synthetase, ultimately interfering with DNA synthesis

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3
Q

What is the azole drugs’ mechanism of action?

A

inhibits ergosterol synthesis via inhibition of lanosterol 14-α-demethylase (damages cell membrane, causes cytoplasmic leakage, and inhibits growth)

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4
Q

Are azole antifungals fungicidal or -static?

A

fungistatic

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5
Q

What is the echinocandins’ mechanism of action?

A

inhibits glucan synthesis, leading to noncompetitive inhibition of 1,3-β-D-glucan (nothing can bind to chitin to help provide cell wall structure)

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6
Q

Are the echinocandins fungicidal or -static?

A

fungicidal

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7
Q

What is ibrexafungerp’s mechanism of action?

A

inhibits glucan synthesis, leading to noncompetitive inhibition of 1,3-β-D-glucan (nothing can bind to chitin to help provide cell wall structure)

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8
Q

Which antifungal covers Pneumocystis jirovecii?

A

ibrexafungerp

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9
Q

What antifungal(s) cover Fusarium?

A

voriconazole and echinocandins (limited)

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10
Q

What antifungal covers Scedosporium apiospermum?

A

voriconazole

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11
Q

What antifungal covers Sporothrix schenckii?

A

itraconazole

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12
Q

What antifungal(s) cover Coccidioides immitis?

A
  • amphotericin B
  • itraconazole
  • fluconazole
  • posaconazole

“AND IT FUCKS PUSSIES” (cocc sounds like cock)

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13
Q

What antifungal(s) cover Blastomyces?

A
  • amphotericin B
  • itraconazole
  • fluconazole
  • voriconazole

“AWAY IT FLIES VERTICALLY” (blast=fireworks)

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14
Q

What antifungal(s) cover Histoplasma capsulatum?

A
  • amphotericin B
  • ketoconazole
  • itraconazole
  • fluconazole
  • voriconazole
  • posaconazole
  • echinocandins (limited)

“ANIMALS KEEP INTENTIONALLY FLYING VERY POOR ENVIRONMENTS” (bats spread histoplasma)

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15
Q

What antifungal(s) cover Mucor?

A
  • amphotericin B
  • posaconazole
  • isavuconazole
  • echinocandins (limited)

“ALLERGIES PROBABLY, IT’S EXHAUSTING” (Mucor = mucus)

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16
Q

What antifungal covers Absidia?

A

amphotericin B

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17
Q

What antifungal(s) cover Rhizopus?

A
  • amphotericin B
  • isavuconazole
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18
Q

What antifungal(s) cover Cryptococcus neoformans?

A
  • amphotericin B
  • flucytosine
  • ketoconazole
  • itraconazole
  • fluconazole
  • voriconazole
  • posaconazole
  • echinocandins (limited)

everything except for isavuconazole and ibrexafungerp

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19
Q

What antifungal(s) cover Aspergillus?

A
  • amphotericin B
  • itraconazole
  • voriconazole
  • posaconazole
  • isavuconazole
  • echinocandins
  • ibrexafungerp

“ASPARAGUS IS VERY POPULAR IN ENTREES INTERNATIONALLY” (Aspergillus = asparagus)

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20
Q

What antifungal(s) cover Candida?

A
  • amphotericin B
  • flucytosine
  • ketoconazole
  • itraconazole
  • fluconazole
  • voriconazole
  • posaconazole
  • echinocandins
  • ibrexafungerp

everything covers Candida on some level, except isavuconazole

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21
Q

What happens with amphotericin B in low concentrations?

A

K+ channel activity is increased

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22
Q

What happens with amphotericin B in higher concentrations?

A

pores are formed in the fungal cell membrane

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23
Q

Amphotericin B’s onset can be described as __________.

A

rapid

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24
Q

Through which two routes could resistance to amphotericin B develop?

A
  • decreased ergosterol biosynthesis
  • alternative sterol synthesis
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25
Q

What is the pharmacodynamic parameter for amphotericin B?

A

peak/MIC

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26
Q

Which Candida type is not covered by amphotericin B?

A

C. lusitaniae

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27
Q

Amphotericin B has reduced activity against which Aspergillus?

A

A. terreus

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28
Q

Describe amphotericin B deoxycholate’s oral absorption.

A

poor

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29
Q

Describe amphotericin B deoxycholate’s intramuscular absorption.

A

poor

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30
Q

Although amphotericin B deoxycholate widely distributes into tissues, where does it primary deposit?

A

reticuloendothelial tissues (liver, spleen, bone marrow)

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31
Q

Describe amphotericin B deoxycholate’s CSF penetration.

A

poor, even with inflamed meninges

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32
Q

Amphotericin B deoxycholate is highly protein-bound, mainly to _____________.

A

β-lipoproteins

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33
Q

Describe amphotericin B deoxycholate’s metabolism.

A

not appreciably metabolized (most of the drug is degraded in situ)

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34
Q

Amphotericin B deoxycholate’s elimination pattern can best be described as ______________.

A

tri-exponential

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35
Q

Amphotericin B deoxycholate can be detected in serum concentrations for at least ___________ after the end of therapy.

A

7 weeks

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36
Q

Does amphotericin B deoxycholate need to be renally/hepatically dose-adjusted?

A

no

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37
Q

True or false: all lipid-associated formulations of amphotericin B have similar PK patterns.

A

false

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38
Q

What are the clinical uses for amphotericin B?

A
  • disseminated candidiasis
  • cryptococcosis
  • aspergillosis
  • histoplasmosis
  • blastomycosis
  • coccidioidomycosis
  • mucormycosis
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39
Q

Should you pre-medicate when giving a test dose of amphotericin B deoxycholate?

A

no

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40
Q

What are the dosing rules for amphotericin B deoxycholate?

A
  • test dose of 0.1 mg/kg or 1 mg over 20-30 minutes
  • total daily dose of 0.3-1.0 mg/kg/day over 4-6 h (generally)
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41
Q

What can happen if amphotericin B deoxycholate is too rapidly infused in a patient with severely compromised renal function?

A
  • acute hyperkalemia
  • ventricular fibrillation
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42
Q

Data suggest that there are significantly fewer adverse events if amphotericin B deoxycholate is administered as a continuous infusion over ___________.

A

24 hours

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43
Q

How should you administer intrathecal/intraventricular amphotericin B deoxycholate?

A

start with 0.1 mg and gradually increase to max 0.5 mg q48-72 h

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44
Q

How should liposomal amphotericin B be dosed/administered?

A

1.5-6 mg/kg daily, infused over 2 h

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45
Q

What is the recommended daily dose for ABLC?

A

5 mg/kg

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46
Q

Which patient weight should be used for dosing amphotericin B?

A

ideal body weight (or adjusted body weight)

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47
Q

What infusion-related adverse reactions can occur with amphotericin B deoxycholate?

A
  • headache
  • fever/chills
  • arthralgias/myalgias
  • N/V
  • tachypnea
  • hypotension
  • thrombophlebitis
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48
Q

What should be used to pre-treat infusion-related reactions from amphotericin B deoxycholate?

A
  • APAP or aspirin
  • antihistamines
  • meperidine
  • phenothiazine
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49
Q

What can be used to combat thrombophlebitis reactions from amphotericin B deoxycholate?

A

add heparin 500-1000 units to infusion bag

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50
Q

What can be used to combat the non-thrombophlebitic infusion-related reactions from amphotericin B deoxycholate?

A

add hydrocortisone 25-50 mg to the infusion bag

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51
Q

What non-infusion-related adverse reactions are associated with amphotericin B deoxycholate?

A
  • nephrotoxicity (inreased SCr and BUN)
  • HYPOkalemia
  • HYPOmagnesemia
  • bicarbonate wasting
  • anemia
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52
Q

How can we attempt to prevent thrombophlebitis from amphotericin B deoxycholate?

A
  • infuse slowly (4-6 h)
  • rotate infusion sites
  • use in-line filters (>0.22 micron)
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53
Q

Through what mechanism does amphotericin B deoxycholate produce nephrotoxic effects?

A

direct vasocontriction of afferent renal arterioles resulting in cortical ischemia and decrease in GFR

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54
Q

Is amphotericin B deoxycholate nephrotoxicity reversible?

A

no; permanent loss of renal function related to total dose

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55
Q

How can we prevent/manage nephrotoxicity associated with amphotericin B deoxycholate?

A
  • sodium repletion (0.5-1 L NS 30 minutes before and after completion)
  • hydration
  • adjustment of daily dose
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56
Q

Is amophotericin B deoxycholate-associated anemia reversible?

A

yes

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57
Q

What adverse reactions can happen when amphotericin B deoxycholate is intrathecally administered?

A
  • peripheral nerve pain
  • headache
  • vomiting
  • paresthesias
  • paraplegia
  • seizures
  • difficulty voiding
  • impaired vision
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58
Q

True or false: lipid-associated amphotericin B formulations generally cause more nephrotoxicity and infusion-related toxicities.

A

false; less nephrotoxicity and infusion-related toxicities

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59
Q

High-dose liposomal amphotericin (7.5 mg/kg/d) is associated with high _______________ rates.

A

nephrotoxicity

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60
Q

How should we manage infusion-related reactions from liposomal amphotericin B?

A

diphenhydramine

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61
Q

Amphotericin B can interact with what drugs?

A
  • other nephrotoxic drugs
  • digoxin
  • skeletal muscle reactions
  • flucytosine (used together for cryptococcal meningitis)
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62
Q

Describe flucytosine’s oral absorption.

A

well-absorbed orally

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63
Q

Does flucytosine penetrate the CSF adequately?

A

yes

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64
Q

How is flucytosine affected by hemodialysis and peripheral dialysis?

A

removed by HD and PD

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65
Q

What is flucytosine’s primary clinical use?

A

in combination with amphotericin B for cryptococcal meningitis

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66
Q

What adverse reactions are associated with flucytosine?

A
  • Hematologic (bone marrow suppression)
  • GI (N/V/D, abdominal pain, enterocolitis)
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67
Q

What is the recommended dose range for flucytosine in patients with normal renal function?

A

25-37.5 mg/kg q6h

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68
Q

Should flucytosine be renally/hepatically dose adjusted?

A

yes for renal, no for hepatic

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69
Q

How should flucytosine be renally dose adjusted?

A

as ClCr worsens, continue to double the dosing interval

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70
Q

Which patient weight is used to dose flucytosine?

A

IBW if non-severe, AdjBW if severe

71
Q

What baseline parameters should be monitored in patients taking flucytosine?

A
  • CBC
  • platelets
  • SCr
  • BUN
72
Q

What is the goal peak concentration for flucytosine?

A

70-80 μg/mL (drawn 2 hours post-dose after 3-5 days)

73
Q

At what peak concentration is flucytosine associated with increased toxicity?

A

> 100 μg/mL

74
Q

What trough concentration range is recommended to prevent rapid selection of resistance in yeast for patients taking flucytosine?

A

20-40 μg/mL

75
Q

Describe ketoconazole’s oral absorption.

A

well-absorbed orally; inversely-related to gastric pH

76
Q

Does ketoconazole penetrate the CSF?

A

no; negligible CSF penetration

77
Q

Ketoconazole is extensively metabolized in the ________.

A

liver

78
Q

The major excretory route of ketoconazole is ____________.

A

enterohepatic

79
Q

Ketoconazole’s elimination pattern can best be described as _____________.

A

biphasic

80
Q

Does ketoconazole need to be renally/hepatically dose adjusted?

A

doesn’t need to be renally adjusted, contraindicated in acute/chronic liver disease

81
Q

When should ketoconazole be used 1st line for fungal infection?

A

NEVER! This is due to risk of hepatotoxicity and drug interactions.

82
Q

What are the clinical uses of ketoconazole?

A
  • chronic mucocutaneous candidiasis
  • histoplasmosis (in immunocompetent hosts)
83
Q

What adverse reactions are associated with ketoconazole?

A
  • GI (N/V/D, anorexia, abdominal pain)
  • hepatotoxicity
  • endocrine (gynecomastia, decreased libido, oligospermia, hair loss, menstrual irregularities)
84
Q

Ketoconazole is a VERY potent inhibitor of CYP____.

A

3A4

85
Q

What drugs may interact with ketoconazole?

A
  • drugs that affect gastric pH
  • anticoagulants
  • rifampin
  • cyclosporine/tacrolimus/sirolimus
  • phenytoin
86
Q

Describe itraconazole’s oral absorption.

A

good and dependent on gastric acidity

87
Q

Which formulation of itraconazole is better absorbed in a fasting state?

A

oral solution

88
Q

Which formulation of itraconazole is better absorbed when taken with a meal or acidic cola beverage?

A

capsules

89
Q

Which formulation of itraconazole is better absorbed: oral solution or capsules?

A

oral solution

90
Q

Is SUBA-itraconazole affected by gastric acidity?

A

no; may be given with or without food

91
Q

Describe itraconazole’s CSF penetration.

A

poor

92
Q

What is the active metabolite of itraconazole?

A

hydroxyitraconazole

93
Q

Does itraconazole need to be renally/hepatically dose adjusted?

A

no

94
Q

What are the clinical uses for itraconazole?

A
  • histoplasmosis (DOC)
  • aspergillosis
  • blastomycosis
  • life-threatening infections
  • onychomycosis
95
Q

What is the goal serum trough itraconazole concentration associated with efficacy?

A

> 0.5-1 μg/mL

96
Q

What itraconazole serum concentration is associated with increased adverse events?

A

> 3 μg/mL

97
Q

What adverse events are associated with itraconazole?

A
  • hepatotoxicity
  • CHF (boxed warning)
  • QTc prolongation
  • peripheral neuropathy
  • GI (nausea, abdominal discomfort)
  • rash
98
Q

In what groups is itraconazole contraindicated?

A
  • ventricular dysfunction (CHF)
  • history of CHF
  • pregnancy
  • nursing
99
Q

What is the drug of choice for histoplasmosis?

A

itraconazole 200 mg PO TID x 3 days, then 200 mg PO BID

100
Q

What drugs will interact with itraconazole capsules to decrease their absorption?

A
  • H2 antagonists
  • PPIs
  • antacids
101
Q

Itraconazole is a potent inhibitor of CYP___.

A

3A4

102
Q

What drugs’ concentrations will be increased in administered with itraconazole?

A
  • digoxin
  • quinidine
  • benzodiazepines
  • HMG-CoA reductase inhibitors (not pravastatin)
  • rifabutin
  • cyclosporin/tacrolimus/sirolimus
  • protease inhibitors (ritonavir, indinavir, saquinavir)
103
Q

What drugs’ concentrations will be decreased if given with itraconazole?

A
  • carbamazepine
  • phenytoin
  • phenobarbital
  • rifampin
  • rifabutin
  • nevirapine
104
Q

What drugs can increase the concentration of itraconazole?

A
  • clarithromycin
  • indinavir
  • ritonavir
105
Q

What Candida is fluconazole NOT active against?

A

C. krusei

106
Q

Describe fluconazole’s oral absorption.

A

well-absorbed orally; independent of gastric activity

107
Q

Describe fluconazole’s CSF penetration.

A

good

108
Q

Does fluconazole need to be renally/hepatically dose adjusted?

A

yes for renal, no for hepatic

109
Q

What are the clinical uses for fluconazole?

A
  • non-invasive candidiasis (OPC, EC, vaginal)
  • invasive candidiasis
  • bone marrow transplant prophylaxis
  • Candida UTI
  • cryptococcal meningitis (inferior for induction, okay for consolidation and maintenance)
110
Q

What patient weight should be used for fluconazole dosing?

A

TBW (total body weight)

111
Q

What adverse reactions are associated with fluconazole?

A
  • QTc prolongation
  • headache
  • nausea
  • anorexia
  • torsades de pointes
  • elevation of hepatic transaminases
112
Q

Fluconazole is a potent inhibitor of CYP____ and a moderate inhibitor of CYP____.

A

2C9; 3A4

113
Q

Describe voriconazole’s oral bioavailability.

A

good; NOT affected by H2 antagonists, PPIs, antacids

114
Q

What key counseling point should be included when telling patients about voriconazole administration?

A

tablets and PO suspensions should be taken 1 hour before or after meals

115
Q

Voriconazole is significantly metabolized by ________________.

A

CYP2C19, 2C9, 3A4

116
Q

Voriconazole’s metabolism is ______________ and its pharmacokinetics are _________________.

A

saturable; non-linear

117
Q

Does voriconazole need to be renally/hepatically dose adjusted?

A

for renal, avoid IV voriconazole in ClCr < 50 (PO is okay)

decrease PO maintenance dose in hepatic cirrhosis

118
Q

What are the clinical uses for voriconazole?

A
  • invasive aspergillosis
  • candidemia in nonneutropenic patients and other deep-tissue Candida infections
  • esophageal candidiasis
  • scedosporiosis and fusariosis
119
Q

Adults who weigh < 40 kg should receive _______ of the oral maintenance dose of voriconazole.

A

half

120
Q

What patient weight should be used when dosing voriconazole?

A

IBW or adjusted body weight

121
Q

What adverse reactions are associated with voriconazole?

A
  • visual disturbances
  • elevated LFTs
  • QTc prolongation
  • CNS (cognitive difficulties, memory loss)
  • peripheral neuropathy
  • phototoxic skin reactions
  • periostitis secondary to excess fluoride
122
Q

What voriconazole trough range is associated with clinical response?

A

> 1-1.5 μg/mL

123
Q

What voriconazole trough range is associated with a higher incidence of CNS adverse events?

A

> 5-6 μg/mL

124
Q

What drug class can decrease the oral absorption of posaconazole suspension?

A

PPIs (absorption affected by gastric pH)

125
Q

What is the preferred oral formulation of posaconazole?

A

DR tablets (absorption not affected by gastric pH)

126
Q

Most of posaconazole is recovered in ________.

A

feces

127
Q

At what CrCl should IV posaconazole be avoided?

A

< 50 mL/min (IV formulation contains cyclodextrin)

128
Q

What are the clinical uses of posaconazole?

A
  • invasive Candida or Aspergillus prophylaxis in immunocompromised patients
  • oropharyngeal candidiasis (+ refractory to fluconazole/itraconazole)
  • may be used as salvage therapy for aspergillosis or Mucor infections
129
Q

What posaconazole trough concentration is associated with higher incidence of breakthrough fungal infections during prophylaxis with suspension?

A

> 0.7 μg/mL

130
Q

What posaconazole trough concentration is associated with treatment response for invasive aspergillosis?

A

> 1 μg/mL

131
Q

Posaconazole is a strong inhibitor of CYP___.

A

3A4

132
Q

What drug is CONTRAINDICATED with posaconazole?

A

sirolimus

133
Q

What adverse events are associated with posaconazole?

A
  • QTc prolongation
  • elevated LFTs
  • hypokalemia
  • GI (N/V/D, abdominal pain)
  • rash
134
Q

Isavuconazole has __________ pharmacokinetics.

A

linear

135
Q

Describe isavuconazole’s oral absorption.

A

well-absorbed orally

136
Q

Does isavuconazole need to be renally/hepatically dose adjusted?

A

no

137
Q

Does the isavuconazole IV formulation contain cyclodextrin?

A

no

138
Q

What are the clinical uses for isavuconazole?

A
  • invasive aspergillosis in patients 18+
  • invasive mucormycosis in patients 18+
139
Q

What administration tip would you give to a patient taking isavuconazole oral capsules?

A

swallow whole; do not crush/chew/dissolve/open

140
Q

What adverse effects are associated with isavuconazole?

A
  • GI (N/V/D)
  • headache
  • increased LFTs
  • infusion-related reactions (hypotension, dyspnea, chills, dizziness, paresthesias, hypoesthesia); discontinue if these occur
  • HYPOkalemia
  • hypersensitivity and severe skin reactions (anaphylaxis, Stevens Johnson)
141
Q

Does isavuconazole cause QTc prolongation?

A

no

142
Q

Isavuconazole is a substrate for CYP___.

A

3A4

143
Q

Isavuconazole is a mild inhibitor of ___________.

A

P-glycoprotein

144
Q

When is isavuconazole contraindicated?

A
  • strong CYP3A4 inhibitors (e.g. ketoconazole, high-dose ritonavir)
  • strong CYP3A4 inducers (e.g. rifampin, carbamazepine, St. John’s wort, long-acting barbiturates)
  • familial short QT syndrome
145
Q

What genes encode for glucan synthase expression?

A

FKS1 and FKS2

146
Q

Describe the echinocandins’ oral bioavailability.

A

poor (administered IV)

147
Q

Caspofungin plasma concentration declines in a _________ manner.

A

polyphasic

148
Q

Caspofungin is slowly metabolized by __________ and __________.

A

hydrolysis; N-acetylation

149
Q

Does caspofungin need to be renally/hepatically dose adjusted?

A

no for renal, only dose-adjust for severe hepatic dysfunction

150
Q

What is caspofungin indicated for?

A
  • candidemia
  • esophageal candidiasis
  • empiric therapy of presumed fungal infections in febrile neutropenia
  • invasive aspergillosis in patients who are refractory to or intolerant to other therapies
151
Q

Does caspofungin induce or inhibit any CYP450s?

A

no

152
Q

What drug interactions can occur with caspofungin?

A
  • tacrolimus
  • cycosporine
  • inducers of drug clearance (efavirenz, nelfinavir, nevirapine, phenytoin, rifampin, carbamazepine)
153
Q

What adverse reactions are associated with caspofungin?

A
  • histamine-mediated symptoms (rash, face swelling, pruritus, flushing)
  • fever
  • phlebitis at infection site
  • N/V
  • headache
  • increased liver transaminases
  • decreased potassium
  • eosinophilia
  • increase in urine protein and RBCs
  • decreased hemoglobin/hematocrit
154
Q

Micafungin is metabolized by the _________.

A

liver

155
Q

Does micafungin need to be renally/hepatically dose adjusted?

A

no

156
Q

What are the clinical uses for micafungin?

A
  • EC and OPC
  • candidemia
  • aspergillosis
  • Candida prophylaxis in HSCT
157
Q

Is micafungin metabolized by any CYP450s?

A

no

158
Q

What adverse reactions are associated with micafungin?

A
  • hyperbilirubinemia
  • N/D
  • eosinophilia
  • rash, pruritus, urticaria (rare)
159
Q

How is anidulafungin eliminated?

A

through slow chemical degradation

160
Q

Should anidulafungin be renally/hepatically dose adjusted?

A

no

161
Q

What are the clinical uses for anidulafungin?

A
  • candidemia and other Candida infections (peritonitis, intra-abdominal abscess)
  • EC
162
Q

What drug interactions are of concern with anidulafungin?

A

none; not a substrate/inducer/inhibitor of CYP450

163
Q

What adverse reactions are associated with anidulafungin?

A
  • histamine-mediated symptoms (rash, urticaria, flushing, pruritus, hypotension)
  • diarrhea
  • increased LFTs
  • hypokalemia
164
Q

Describe ibrexafungerp’s oral absorption.

A

good; dependent on gastric acid and better absorbed with food

165
Q

How is ibrexafungerp’s CSF penetration?

A

poor

166
Q

91% of ibrexafungerp is recovered in _______.

A

feces

167
Q

What are the clinical uses for ibrexafungerp?

A

VVC in adults and post-menarchal pediatric females

168
Q

In what patient group is ibrexafungerp contraindicated?

A

pregnancy; use effective contraception during and for 4 days after treatment

169
Q

What adverse reactions are associated with ibrexafungerp?

A
  • GI (N/V/D, abdominal pain)
  • dizziness
170
Q

Does ibrexafungerp cause QTc prolongation?

A

no

171
Q

Ibrexafungerp is a weak inhibitor of CYP_____ and _____.

A

3A4; 2C8

172
Q

What drug type should be avoided with ibrexafungerp?

A

strong/moderate CYP3A4 inducers

173
Q

What adverse reactions are associated with anidulafungin?

A
  • histamine-mediated symptoms (rash, urticaria, flushing, pruritus, hypotension)
  • diarrhea
  • increased LFTs
  • hypokalemia

PHRM 865 (59 decks)

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