Antifungal Agent, Azole Derivative
Interferes with fungal cytochrome P450 activity (lanosterol 14-α-demethylase), decreasing ergosterol synthesis (principal sterol in fungal cell membrane) and inhibiting cell membrane formation
藥動學
Distribution:
1. Vd: (children age 5 to 15 years) 0.722 to 1.069 L/kg
2. Protein binding: 11% to 12% Excretion:
1. Renal: approximately 80% unchanged, 11% as metabolite
2. Dialyzable: yes (hemodialysis), 50% removed in 3 hours
禁忌症
1. Hypersensitivity to fluconazole or any component of the formulation (cross-reaction with other azole antifungal agents may occur; use caution)
2. Coadministration with CYP3A4 substrates, which may lead to QTc prolongation (eg, erythromycin, pimozide, quinidine)
懷孕分類
D [FDA.AUS]
哺乳分類
Infant risk is minimal
副作用
Nausea, vomiting, elevation in liver function tests, hypokalemia
劑量和給藥方法
Candidemia:
1. For initial therapy: 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
2. Duration: Continue for ≥14 days after first negative blood culture and resolution of signs/symptoms Cardiac device infection (eg, implantable cardiac defibrillator, pacemaker, ventricular assist device), CNS infection, endocarditis:
400 to 800 mg (or 6 to 12 mg/kg) once daily for 4 to 6 weeks Esophageal infection:
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:
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 Peritonitis:
200 mg on day 1, then 100 to 200 mg once daily for 2 to 4 weeks
小兒調整劑量
Not recommended in children <16 years of age.
腎功能調整劑量
1. ClCr >50ml/min: No dosage adjustment necessary
2. ClCr< 50ml/min: 50% of usual daily dose
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
安定性
Store glass bottles between 5 and 30 degrees C (41 and 86 degrees F). Protect from freezing.