Calcium Folinate Injection

Generic name: Calcium Folinate

Drug class: Antidote, Chemoprotective Agent

Dosage form: Injection

Root of administration: Intravenous, Intramuscular

Dose:

• For Methotrexate Toxicity: 15 mg/m² intramuscularly or intravenously every 6 hours for 4 doses, starting 24 hours after methotrexate administration.
• For Folate Deficiency: 1 mg intramuscularly or intravenously daily until response is observed.
• For High-Risk Colorectal Cancer Chemotherapy: 200 mg/m² intravenously over 2 hours, followed by 400 mg/m² orally daily for 10 days, starting 24 hours after fluorouracil administration.

Mechanism of action: Calcium Folinate is the calcium salt of folinic acid, a reduced form of folic acid. It acts as a cofactor in the synthesis of purines and thymidylate, essential for DNA synthesis and repair. By bypassing the inhibition of dihydrofolate reductase, it enhances the efficacy of fluorouracil in cancer therapy and mitigates the toxic effects of methotrexate by replenishing tetrahydrofolate levels.

Drug usage cases:

• Management of high-dose methotrexate toxicity
• Adjunctive therapy with fluorouracil in colorectal cancer treatment
• Correction of folate deficiency anemia
• Management of megaloblastic anemia due to folate deficiency
• Treatment of certain cases of hyperhomocysteinemia

Drug contra indications:

• Hypersensitivity to calcium folinate or any component of the formulation
• Untreated vitamin B12 deficiency anemia
• Leukemia (in patients with megaloblastic anemia due to vitamin B12 deficiency)

Side effects:

• Gastrointestinal disturbances: nausea, vomiting, diarrhea
• Allergic reactions: rash, pruritus, anaphylaxis
• Hematologic effects: leukopenia, thrombocytopenia
• Neurological effects: confusion, dizziness, headache
• Cardiovascular effects: hypertension, arrhythmias
• Injection site reactions: pain, redness, swelling

Warnings:

• Monitor blood counts regularly during therapy
• Use caution in patients with renal impairment
• Ensure adequate hydration to reduce the risk of nephrotoxicity
• Administer with caution in patients with a history of gastrointestinal ulcers or bleeding
• Discontinue if signs of severe hypersensitivity reactions occur
• Use with caution in pregnant or breastfeeding women; weigh potential benefits against risks

Use during pregnancy or breastfeeding:

Calcium Folinate is classified as a Category C drug for pregnancy, indicating that risk to the fetus cannot be ruled out. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. There are no adequate and well-controlled studies in pregnant women. Caution is advised when administering Calcium Folinate to breastfeeding women, as it is not known whether it is excreted in human milk. The decision to continue breastfeeding or discontinue the drug should be made based on the importance of the drug to the mother and the potential risks to the nursing infant.