大腸直腸癌、解毒劑 Colorectal cancer, advanced: Palliative treatment of advanced colorectal cancer (in combination with fluorouracil) Megaloblastic anemia: Treatment of megaloblastic anemias due to folic acid deficiency (when oral therapy is not feasible) Methotrexate toxicity: Rescue agent after high-dose methotrexate treatment in osteosarcoma and to diminish the toxicity and counteract the effects of impaired methotrexate elimination and of inadvertent overdosage of folic acid antagonists
藥理
Antidote; Chemotherapy Modulating Agent
Leucovorin calcium is a reduced form of folic acid, leucovorin supplies the necessary cofactor blocked by methotrexate. Leucovorin actively competes with methotrexate for transport sites, displaces methotrexate from intracellular binding sites, and restores active folate stores required for DNA/RNA synthesis. Leucovorin stabilizes the binding of 5-dUMP and thymidylate synthetase, enhancing the activity of fluorouracil.
Colorectal cancer, advanced:
200 mg/m2/day over ≥3 minutes for 5 days every 4 weeks for 2 cycles, then every 4 to 5 weeks (in combination with fluorouracil) or 20 mg/m2/day for 5 days every 4 weeks for 2 cycles, then every 4 to 5 weeks (in combination with fluorouracil) Megaloblastic anemia, folate-deficient:
≤1 mg once daily Methotrexate-rescue (high-dose methotrexate):
Initial: 15 mg (~10 mg/m2); start 24 hours after beginning MTX infusion; continue every 6 hours for 10 doses, until MTX level is <0.05 mmoL Methotrexate overdose (inadvertent):
1. Begin as soon as possible after overdose; 10 mg/m2 Q6H until the MTX level is <0.01 mmoL
2. If serum creatinine is increased >50% above baseline 24 hours after MTX administration, if 24 hour MTX level is >5 mmoL, or if 48 hour MTX level is >0.9 mmol, increase leucovorin dose to 100 mg/m2 IV every 3 hours until the MTX level is <0.01 mmoL
小兒調整劑量
Refer to adult dosing
腎功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling.
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling.