Info

🌱 來自: Metastatic Colon Cancer

Fluorouracil

• 5-FU
• (5-FU, Adrucil)
• 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 󰒖: 💩👄🤮🩸🤞🫀👁️🖐️🦶😇🐌
• 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