Distribution: Widely throughout the body with good penetration into CSF, eye, peritoneal fluid, sputum, skin, and urine; Vd: Adults: ~0.6 L/kg.
Protein binding, plasma: 11% to 12%.
Half-life elimination: Adults: ~30 hours (range: 20 to 50 hours).
Excretion: Urine (80% as unchanged drug).
禁忌症
Hypersensitivity to fluconazole or any component of the formulation (cross-reaction with other azole antifungal agents may occur, but has not been established; use caution); coadministration with CYP3A4 substrates, which may lead to QTc prolongation (eg, erythromycin, pimozide, quinidine).
懷孕分類
C; Should not be initiated during pregnancy for esophageal, oropharyngeal, or vaginal candidiasis; fluconazole should be discontinued if pregnancy occurs during therapy.
哺乳分類
Fluconazole is present in breast milk.
副作用
劑量和給藥方法
1. Candidiasis, treatment:
- Candidemia: Initial therapy (alternative agent): IV: Loading dose of 800 mg (or 12 mg/kg) on day 1, then 400 mg (or 6 mg/kg) once daily; if fluconazole-susceptible Candida glabrata isolated, transition to 800 mg (or 12 mg/kg) once daily; Duration: ≥14 days.
- Cardiac infection, native or prosthetic valve endocarditis, or device infection: Step-down therapy: IV: 400 to 800 mg (or 6 to 12 mg/kg) once daily; Duration: ≥ 4 weeks after device removal.
- Endophthalmitis, endogenous: IV: Loading dose of 800 mg (or 12 mg/kg) on day 1, then 400 to 800 mg (or 6 to 12 mg/kg) once daily for ≥4 to 6 weeks and until examination indicates resolution.
- Esophageal, treatment: IV: 400 mg (or 6 mg/kg) on day 1, then 200 to 400 mg (or 3 to 6 mg/kg) once daily for 14 to 21 days.
- Intra-abdominal infection, acute, including peritonitis and/or abscess (alternative agent): IV: 800 mg (or 12 mg/kg) on day 1, then 400 mg (or 6 mg/kg) once daily. Total antifungal duration is ≥14 days based on source control and clinical response.
- Oropharyngeal: IV: 200 mg on day 1, then 100 to 200 mg once daily for 7 to 14 days; some experts increase to 400 mg once daily for those who do not initially respond.
- Osteoarticular (osteomyelitis or septic arthritis): Initial or step-down therapy: IV: 400 mg (or 6 mg/kg) once daily. Duration for osteomyelitis is 6 to 12 months and for septic arthritis is 6 weeks.
- Peritonitis, associated with peritoneal dialysis: IV: 200 mg on day 1, then 100 to 200 mg once daily for 2 to 4 weeks.
- Thrombophlebitis, suppurative: IV: 400 to 800 mg (or 6 to 12 mg/kg) once daily for ≥2 weeks after candidemia (if present) has cleared.
2. Candidiasis, prophylaxis:
- High-risk patients in the ICU in units with a high rate (>5%) of invasive candidiasis: IV: Loading dose of 800 mg (or 12 mg/kg) once on day 1, then 400 mg (or 6 mg/kg) once daily.
- Solid organ transplant recipients: IV: 400 mg (or 6 mg/kg) given perioperatively and continued once daily postoperatively.
小兒調整劑量
1. Candida infections, prophylaxis:
- Oncology patients at high risk of invasive candidiasis: IV: 6 to 12 mg/kg/dose once daily; maximum dose: 400 mg/dose.
- Surgical prophylaxis , high-risk patients undergoing liver, pancreas, kidney, or pancreas-kidney transplantation: IV: 6 mg/kg as a single dose 60 minutes before procedure; maximum dose: 400 mg/dose.
2. Candidiasis, systemic (including Candidemia and invasive candidiasis), treatment: IV: 12 mg/kg/dose once daily; maximum dose: 800 mg/dose; continue treatment for ≥14 days.
3. Candidiasis, CNS candidiasis, step-down therapy: IV: 12 mg/kg/dose once daily following initial therapy with liposomal amphotericin B (with or without flucytosine); maximum dose: 800 mg/dose.
4. Candidiasis, endophthalmitis, treatment: IV: 12 mg/kg/dose once daily for at least 4 to 6 weeks until examination indicates resolution; maximum dose: 800 mg/dose.
5. Candidiasis, esophageal: IV: 6 to 12 mg/kg/dose once daily for 14 to 21 days; maximum dose: 600 mg/dose.
6. Candidiasis, peritoneal dialysis-related infections: Treatment: IV: 6 to 12 mg/kg/dose every 24 to 48 hours; maximum dose: 400 mg/dose; Prophylaxis for high-risk situations: IV: 3 to 6 mg/kg/dose every 24 to 48 hours; maximum dose: 200 mg/dose.
7. Coccidioidomycosis, HIV-exposed/-infected: IV: 6 to 12 mg/kg/dose once daily; maximum dose: 400 mg/dose.
8. Cryptococcal infection:
- Mild to moderate localized infection including pneumonia (not CNS), treatment, HIV-exposed/-infected: IV: 12 mg/kg on day 1, then 6 to 12 mg/kg/dose once daily; maximum dose: 600 mg/dose.
腎功能調整劑量
1. Altered kidney function:
CrCl >50 mL/minute: No dosage adjustment necessary.
CrCl ≤50 mL/minute: Reduce dose by 50%.
2. Peritoneal dialysis: reduce maintenance doses by 50%.