Fluconazole: Difference between revisions

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*Antifungal in the triazole family with excellent bioavadilability but limited efficacy outside of ''Candida''
  
*Antifungal in the triazole family with excellent bioavadilability but limited efficacy outside of ''Candida''
   
−
=== Pharmacokinetics and Pharmacodynamics ===
 +
===Pharmacokinetics and Pharmacodynamics===
   
−
* Good oral bioavailability
 +
*Good oral bioavailability
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* Good CNS penetration
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*Good CNS penetration
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* Fungistatic
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*Fungistatic
  +
*Efficacy predicted by AUC/MIC ratio
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* Susceptibility breakpoints for [[Candida albicans]] are:
  
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** Susceptible MIC ≤2
  
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** Susceptible dose-dependent MIC 4
  
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** Resistant MIC ≥8
  
   
  +
===Clinical Breakpoints===
−
==Monitoring==
  
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{| class="wikitable"
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! rowspan="2" |Species
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! rowspan="2" |ECV (μg/mL)
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! colspan="4" |Breakpoints (μg/mL)
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! colspan="4" |Breakpoints (mm)
  +
|-
  +
!S
  +
!SDD
  +
!I
  +
!R
  +
!S
  +
!SDD
  +
!I
  +
!R
  +
|-
  +
|[[Candida albicans]]
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|0.5
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|≤2
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|4
  +
|—
  +
|≥8
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|≥17
  +
|14-16
  +
|—
  +
|≤13
  +
|-
  +
|[[Candida dubliniensis]]
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|0.5
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|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|-
  +
|[[Candida glabrata]]
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|8
  +
|—
  +
|≤32
  +
|—
  +
|≥64
  +
|—
  +
|≥15
  +
|—
  +
|≤14
  +
|-
  +
|[[Candida guilliermondii]]
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|8
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|-
  +
|[[Candida krusei]]
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|
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| colspan="4" |intrinsically resistant
  +
| colspan="4" |intrinsically resistant
  +
|-
  +
|[[Candida lusitaniae]]
  +
|1
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|-
  +
|[[Candida parapsilosis]]
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|1
  +
|≤2
  +
|4
  +
|—
  +
|≥8
  +
|≥17
  +
|14-16
  +
|—
  +
|≤13
  +
|-
  +
|[[Candida tropicalis]]
  +
|1
  +
|≤2
  +
|4
  +
|—
  +
|≥8
  +
|≥17
  +
|14-16
  +
|—
  +
|≤13
  +
|-
  +
|[[Cryptococcus neoformans]]
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|8
  +
| colspan="8" rowspan="2" |
  +
|-
  +
|[[Cryptococcus gattii]]
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|16-32
  +
|}
  +
  +
== Dosing ==
  +
  +
* Invasive candidiasis: fluconazole 6 to 12 mg/kg PO/IV q24h
  +
*[[Candidemia]]: 12 mg/kg IV load followed by 6 mg/kg PO/IV daily
  +
**Can use 800 mg daily for isolates that show dose-dependent susceptibility
  +
*[[Vaginal candidiasis]]: 150 mg PO once, with or without intravaginal [[clotrimazole]]
  +
*[[Oral thrush]]: 100 mg po daily for 7 to 14 days
  +
*[[Esophageal candidiasis]]: 200 mg PO daily for 14 to 21 days
  +
*[[Urinary tract infection]]: 200 mg po daily for 7 to 14 days
  +
*[[Intra-abdominal infections|Intraabdominal infection]]: 400 mg PO daily
  +
  +
===Monitoring===
   
 
*ECG for QT prolongation
  
*ECG for QT prolongation
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*Beware [[Adverse drug reaction::drug-drug interactions]], especially with new DOACs
  
*Beware [[Adverse drug reaction::drug-drug interactions]], especially with new DOACs
   
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[[Category:Antifungals]]
 +
[[Category:Triazoles]]

Latest revision as of 19:25, 12 November 2021

Background

  • Antifungal in the triazole family with excellent bioavadilability but limited efficacy outside of Candida

Pharmacokinetics and Pharmacodynamics

  • Good oral bioavailability
  • Good CNS penetration
  • Fungistatic
  • Efficacy predicted by AUC/MIC ratio

Clinical Breakpoints

Species ECV (μg/mL) Breakpoints (μg/mL) Breakpoints (mm)
S SDD I R S SDD I R
Candida albicans 0.5 ≤2 4 — ≥8 ≥17 14-16 — ≤13
Candida dubliniensis 0.5
Candida glabrata 8 — ≤32 — ≥64 — ≥15 — ≤14
Candida guilliermondii 8
Candida krusei intrinsically resistant intrinsically resistant
Candida lusitaniae 1
Candida parapsilosis 1 ≤2 4 — ≥8 ≥17 14-16 — ≤13
Candida tropicalis 1 ≤2 4 — ≥8 ≥17 14-16 — ≤13
Cryptococcus neoformans 8
Cryptococcus gattii 16-32

Dosing

Monitoring

  • ECG for QT prolongation
  • Liver enzymes for hepatitis

Adverse Drug Reactions

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