Fluconazole: Difference between revisions

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==Background==
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== Classification ==
  
   
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* Antifungal in the triazole family with excellent bioavadilability but limited efficacy outside of ''Candida''
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*Antifungal in the triazole family with excellent bioavadilability but limited efficacy outside of ''Candida''
   
  +
===Pharmacokinetics and Pharmacodynamics===
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== Indications ==
  
   
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*Good oral bioavailability
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* Fungal infections
  
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*Good CNS penetration
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*Fungistatic
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*Efficacy predicted by AUC/MIC ratio
   
  +
===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)
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|-
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!S
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!SDD
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!I
  +
!R
  +
!S
  +
!SDD
  +
!I
  +
!R
  +
|-
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|[[Candida albicans]]
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|0.5
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|≤2
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|4
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|—
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|≥8
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|≥17
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|14-16
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|—
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|≤13
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|-
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|[[Candida dubliniensis]]
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|0.5
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|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|-
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|[[Candida glabrata]]
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|8
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|—
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|≤32
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|—
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|≥64
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|—
  +
|≥15
  +
|—
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|≤14
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|-
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|[[Candida guilliermondii]]
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|8
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|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|-
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|[[Candida krusei]]
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|
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| colspan="4" |intrinsically resistant
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| colspan="4" |intrinsically resistant
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|-
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|[[Candida lusitaniae]]
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|1
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|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|
  +
|-
  +
|[[Candida parapsilosis]]
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|1
  +
|≤2
  +
|4
  +
|—
  +
|≥8
  +
|≥17
  +
|14-16
  +
|—
  +
|≤13
  +
|-
  +
|[[Candida tropicalis]]
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|1
  +
|≤2
  +
|4
  +
|—
  +
|≥8
  +
|≥17
  +
|14-16
  +
|—
  +
|≤13
  +
|-
  +
|[[Cryptococcus neoformans]]
  +
|8
  +
| colspan="8" rowspan="2" |
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|-
  +
|[[Cryptococcus gattii]]
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|16-32
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|}
   
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== Dosing ==
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* ECG for QT prolongation
  
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* Liver enzymes for hepatitis
  
   
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* Invasive candidiasis: fluconazole 6 to 12 mg/kg PO/IV q24h
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== Pharmacokinetics ==
  
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*[[Candidemia]]: 12 mg/kg IV load followed by 6 mg/kg PO/IV daily
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**Can use 800 mg daily for isolates that show dose-dependent susceptibility
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*[[Vaginal candidiasis]]: 150 mg PO once, with or without intravaginal [[clotrimazole]]
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*[[Oral thrush]]: 100 mg po daily for 7 to 14 days
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*[[Esophageal candidiasis]]: 200 mg PO daily for 14 to 21 days
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*[[Urinary tract infection]]: 200 mg po daily for 7 to 14 days
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*[[Intra-abdominal infections|Intraabdominal infection]]: 400 mg PO daily
   
  +
===Monitoring===
−
* Good oral bioavailability
  
−
* CNS penetration
  
   
  +
*ECG for QT prolongation
−
== Adverse Drug Reactions ==
  
  +
*Liver enzymes for hepatitis
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* Best side effect profiles of the antifungals
  
−
* Before starting, check:
  
−
** Liver enzymes as baseline ([[Adverse drug reaction::hepatitis]])
  
−
** Creatinine (requires renal dosing)
  
−
** EKG ([[Adverse drug reaction::QTc prolongation]])
  
−
* Beware [[Adverse drug reaction::drug-drug interactions]], especially with new DOACs
  
   
  +
==Adverse Drug Reactions==
−
[[Category:Antifungals]]
  
  +
  +
*Best side effect profiles of the antifungals
  +
*Before starting, check:
  +
**Liver enzymes as baseline ([[Adverse drug reaction::hepatitis]])
  +
**Creatinine (requires renal dosing)
  +
**EKG ([[Adverse drug reaction::QTc prolongation]])
  +
*Beware [[Adverse drug reaction::drug-drug interactions]], especially with new DOACs
  +
  +
[[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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