黴菌感染 Treatment of susceptible fungal infections caused by Candida or Cryptococcus
藥理
Antifungal Agent
Penetrates fungal cells and is converted to fluorouracil which competes with uracil interfering with fungal RNA and protein synthesis
藥動學
Absorption:
1. Rapid; serum concentrations tended to be higher in children <12 years of age
2. Bioavailability: 78% to 89%; decreased in neonates
3. Time to peak, serum: ~1 to 2 hours Distribution:
1. Into CSF, aqueous humor, joints, peritoneal fluid
2. Vd: 0.6 L/kg
3. Protein binding: 3-4% Metabolism:
Minimally hepatic; deaminated both in yeasts and possibly via gut bacteria to 5-fluorouracil Excretion:
1. Urine (>90% as unchanged drug)
2. Half-life elimination:(Neonates) 4-34 hours; (Infants) 7.4 hours; (Adults) 2-5 hours; (Anuria) 85 hours; (ESRD) 75-200 hours
禁忌症
1. Hypersensitivity to flucytosine 2. Known complete dihydropyrimidine dehydrogenase enzyme deficiency <20220727>
懷孕分類
C [FDA]
哺乳分類
Excretion in breast milk unknown/ not recommended.
副作用
Nausea or vomiting in high dose, diarrhea, elevated LFTs, skin rashes, bone marrow suppression
劑量和給藥方法
Usual dosage range: 50-150 mg/kg/day in divided doses every 6 hours
小兒調整劑量
腎功能調整劑量
1. CrCl >40 mL/minute: No dosage adjustment necessary
2. CrCl 21-40 mL/minute: 25 mg/kg/dose every 12 hours
3. CrCl 10-20 mL/minute: 25 mg/kg/dose every 24 hours
4. CrCl <10 mL/minute: 25 mg/kg/dose every 48 hours
5. End-stage renal disease on intermittent hemodialysis: 25 to 50 mg/kg/dose every 48 to 72 hours; administer dose after hemodialysis
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.