Info

🌱 來自: Fluorouracil

5FU

• Dosing: Dose, schedule, & administration (IVB vs. IV continuous infusion) are based on malignancy. Common ranges, IVB: 400-600 mg/m2/dose; IV continuous infusion 200-1,500 mg/m2/d. No renal or hepatic dose adjustments recommended; use w/ caution
• PK/PD: Extensive tissue distribution; saturable catabolism; excretion via metabolism, lung, & urine; T1/2 8-20 min after IVB
• AEs: Dependent on dose & administration (IV bolus vs. IV continuous infusion), diarrhea (DLT), mucositis (DLT), N/V (low emetogenic potential), myelosuppression (bolus > continuous infusion), neurotoxicity, coronary artery vasospasm, conjunctivitis, hand-foot syndrome (continuous infusion > bolus), alopecia, nail changes
• DDI: CYP2C9 substrates (↓ substrate levels), cimetidine (↓ clearance of 5-FU), oral anticoagulants (↑ levels of anticoagulants), leucovorin (↑ tox of 5-FU)
• Clinical pearls: AEs w/ DPD deficiency (prolonged clearance, ↑ tox), radiosensitizer; leucovorin is given w/ bolus administration to ↑ intracellular half-life of 5-FU (↑ cytotoxicity). Uridine triacetate used as antidote in cases of overdose or DPD deficiency