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VARIOUS › ALL OTHER THERAPEUTIC PRODUCTS › ALL OTHER THERAPEUTIC PRODUCTS › Detoxifying agents for antineoplastic treatment
calcium levofolinate
V03AF04
Forms & Strengths
- Injection: 10 mg/mL, 50 mg/5 mL, 175 mg/17.5 mL, 250 mg/25 mL solution
- Lyophilized powder for injection: 50 mg, 175 mg, 250 mg per vial
Adult Dosing
- Leucovorin rescue after high-dose methotrexate: 7.5 mg (approx. 5 mg/m2) every 6 hours for 8 to 12 doses
- Megaloblastic anemia due to folate deficiency: 1 mg daily intramuscularly
- Combination with 5-fluorouracil in colorectal cancer: 100-200 mg/m2 intravenously prior to 5-FU
Pediatric Dosing
- Methotrexate rescue: 7.5 mg (5 mg/m2) every 6 hours for 8 to 12 doses starting 24 hours after methotrexate start
- Dosing adjusted based on methotrexate serum clearance levels
Indications
- Rescue from high-dose methotrexate therapy in osteosarcoma and acute lymphoblastic leukemia
- Diminishing toxicity and neutralizing action of folate antagonists (methotrexate)
- Treatment of megaloblastic anemias due to folate deficiency when oral therapy is not feasible
- Potentiation of 5-fluorouracil cytotoxicity in advanced colorectal cancer
Mechanism of Action
- Levotartrate isomer of folinic acid (5-formyltetrahydrofolate)
- Acts as a reduced form of folic acid bypassing dihydrofolate reductase inhibition
- Provides necessary reduced folate cofactor for purine and pyrimidine synthesis
- Protects normal tissues from high-dose methotrexate toxicity while enhancing 5-FU binding to thymidylate synthase
Contraindications
- Pernicious anemia and other megaloblastic anemias secondary to vitamin B12 deficiency
- Known hypersensitivity to levofolinate or calcium leucovorin products
Adverse Reactions
- Allergic reactions (urticaria, pruritus, rash, anaphylaxis)
- Injection site reactions
- Fever and chills (with high intravenous doses)
- Potentiation of 5-FU toxicities when used in combination regimens (diarrhea, nausea, stomatitis, myelosuppression)
Drug Interactions
- Folic acid antagonists (methotrexate): High doses may decrease the efficacy of methotrexate
- Antiepileptic drugs (phenytoin, phenobarbital, primidone): May decrease anticonvulsant efficacy leading to increased seizure frequency
- 5-Fluorouracil: Enhances toxicity and efficacy of 5-FU; requires careful dose reduction of cytotoxic agent
Curated Content: Needs Vetting Before Put to Clinical Use