Info

🌱 來自: Capecitabine

Xeloda

• Dosing: 1,000-1,250 mg/m2 PO twice daily × 2 wks every 21 d. Renal: CrCl 30-50 mL/min: 75% of dose; CrCl <30 mL/min: use contraindicated
• PK/PD: Oral prodrug of 5-FU, converted via 3-step activation process. Bioavailability ∼80%, protein binding <60%, hepatic & tissue metabolism (active metabolite: 5-FU), renal excretion (96%), T1/2 0.5-1 h
• AEs: Diarrhea, hand-foot syndrome, myelosuppression, mucositis, neurologic tox, coronary vasospasm
• DDI: Inhibits CYP2C9 weakly, warfarin (BBW), oral anticoagulants (↑ levels of anticoagulants), phenytoin (↑ levels of phenytoin), leucovorin (↑ tox of capecitabine)
• Clinical pearls: Increased risk of fatal/sev. AEs w/ DPD deficiency. Available as 150-mg & 500-mg tablets, take w/in 30 min after a meal, radiation sensitizer, uridine triacetate used as antidote in cases of overdose, accidental ingestion, & possible DPD deficiency