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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIMYCOTICS FOR SYSTEMIC USE › ANTIMYCOTICS FOR SYSTEMIC USE › Triazole and tetrazole derivatives
fluconazole
J02AC01
Forms & Strengths
- Tablet: 50 mg, 100 mg, 150 mg, 200 mg
- Oral Suspension: 10 mg/mL, 40 mg/mL
- Injection: 2 mg/mL in 100 mL, 200 mL
Adult Dosing
- Vaginal candidiasis: 150 mg oral single dose
- Oropharyngeal candidiasis: 200 mg on day 1, then 100 mg daily for at least 2 weeks
- Esophageal candidiasis: 200-400 mg on day 1, then 100-200 mg daily for at least 3 weeks
- Candidemia / Invasive candidiasis: 400-800 mg daily
- Cryptococcal meningitis: 400-800 mg daily for 10-12 weeks after induction, then 200 mg daily suppression
Pediatric Dosing
- Neonates < 2 weeks: 6-12 mg/kg every 72 hours
- Neonates 2-4 weeks: 6-12 mg/kg every 48 hours
- Candidiasis (infants > 14 days and children): 6-12 mg/kg daily
- Cryptococcal meningitis (children): 6-12 mg/kg daily (up to 12 mg/kg every 12 hours for severe infections)
Indications
- Vaginal candidiasis (treatment and prophylaxis)
- Oropharyngeal and esophageal candidiasis
- Candidemia, disseminated candidiasis, and candida peritonitis
- Cryptococcal meningitis
- Prevention of candidiasis in immunocompromised patients
Mechanism of Action
- Triazole antifungal agent
- Inhibits fungal cytochrome P450 14-alpha-demethylase (CYP51)
- Blocks conversion of lanosterol to ergosterol, disrupting fungal cell membrane formation
Contraindications
- Hypersensitivity to fluconazole or other azole antifungals
- Co-administration with drugs that prolong QT interval and are metabolized by CYP3A4 (e.g., cisapride, terfenadine, pimozide, quinidine, erythromycin)
Adverse Reactions
- Common: Headache, nausea, abdominal pain, diarrhea, dizziness, rash
- Serious: Hepatotoxicity, severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis), QT prolongation, torsades de pointes, anaphylaxis
Drug Interactions
- CYP3A4 and CYP2C9 inhibitor: Increases levels of warfarin, phenytoin, cyclosporine, tacrolimus, sulfonylureas, and statins
- CYP2C19 inhibitor: Increases concentrations of omeprazole and other proton pump inhibitors
- Rifampin: Induces fluconazole metabolism, decreasing its plasma concentrations
- QT-prolonging agents: Increased risk of ventricular arrhythmias when co-administered
Curated Content: Needs Vetting Before Put to Clinical Use