Fluconazole
DIFLUCAN
What it isTriazole that inhibits fungal CYP51; candidiasis and cryptococcal disease.
Why this oneReliable oral absorption plus penetration into CSF and urine distinguishes it from many other azoles.
What limits itCYP2C9 and CYP3A4 inhibition raises warfarin and statin exposure; QT prolongation and hepatotoxicity also matter.
FDA-approved for
- fungal infections (1990)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Vaginal candidiasis | Adults | 150 mg single dose | 150 mg single dose | 150 mg single dose |
| Oropharyngeal candidiasis | Adults | 200 mg day 1 | 100 mg QD | 100 mg QD |
| Esophageal candidiasis | Adults | 200 mg day 1 | 100 mg QD | 400 mg/day |
| Systemic Candida infections | Adults | up to 400 mg QD | up to 400 mg QD | 400 mg QD |
| Cryptococcal meningitis (acute) | Adults | 400 mg day 1 | 200 mg QD | 400 mg QD |
| Cryptococcal meningitis relapse suppression (AIDS) | Adults | 200 mg QD | 200 mg QD | 200 mg QD |
| Candidiasis prophylaxis in bone marrow transplant | Adults | 400 mg QD | 400 mg QD | 400 mg QD |
| Oropharyngeal/esophageal candidiasis | Peds ≥6 months | 6 mg/kg day 1 | 3 mg/kg QD (esophageal up to 12 mg/kg/day) | 12 mg/kg/day |
| Systemic Candida infections | Peds ≥3 months | 25 mg/kg load day 1 (max 800 mg) | 12 mg/kg QD (max 400 mg) | 400 mg QD |
| Cryptococcal meningitis | Peds | 12 mg/kg day 1 | 6 mg/kg QD | 12 mg/kg QD |
Renal Multiple-dose: after loading dose, CrCl >50 = 100% dose, CrCl ≤50 (no dialysis) = 50%; hemodialysis = 100% after each session. No adjustment for single-dose vaginal candidiasis.
Hepatic Undefined
Instructions
- Take with or without food
- Give a loading dose of twice the daily dose on day 1 (multiple-dose indications)
Contraindications
- Coadministration with QT-prolonging CYP3A4 substrates (erythromycin, pimozide, quinidine)
Cautions
- Serious hepatic reactions (hepatitis, cholestasis, fulminant hepatic failure)
- QT prolongation / torsades de pointes
- Anaphylaxis / angioedema
- Serious skin reactions (SJS, TEN, DRESS, AGEP)
Adverse reactions
- Headache
- Nausea
- Abdominal pain
- Diarrhea
- Vomiting
- Rash
- Elevated transaminases
Pregnancy High-dose (400–800 mg/day) first-trimester exposure linked to a distinctive pattern of congenital anomalies; avoid except in severe/life-threatening infection. Single 150 mg dose may also pose risk.
Lactation Undefined
NO BOXED WARNINGS
Principal riskQT prolongation; a moderate CYP2C9 and CYP3A4 inhibitor
Cost, est. cash$10–$500/bag or supply
Generic entryBy 2023
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityUsually well tolerated at replacement doses; excessive dosing can cause agent-specific metabolic or organ toxicity.
Mechanism of action: Fluconazole ballicule
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Memory aids: mascots and interaction avatars
Fluffer inHibitor (fluoxetine, fluvoxamine, fluconazole)
