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Medication Description: Calcium Folinate (Calcii folinas; Calcium-folinate)

CALCIUM FOLINAT (Calcii folinas; Calcium-folinate).

Calcium salt of folinic acid, or 5-formyl-5, 6, 7, 8-tetrahydrofolic acid, i.e. N- {4 '- [(2-amino-5-formyl-5, 6, 7, 8-tetrahydro -4-hydroxy-pteridyl) methyl] aminobenzoyl} -L-glutamic acid.

Available in the form of pentahydrate.

Synonyms of folinic acid: Leucovorin, Citrovorum factor (The name is associated with the fact that folinic acid is a growth factor for the bacteria Leuconostoc citrovorum), Chemifolin, Lederfoline, Rescufolin, Tonofolin, etc.

Yellowish white crystalline powder. Easily soluble in water. Unstable in the light.

The chemical structure and physiological activity is similar to folic acid.

Folinic acid is the product of folic acid conversion (see) in the body and plays the role of its active metabolite. The conversion of folic acid to folinic occurs with the participation of ascorbic acid.

Folinic acid, like folic acid, is effective for megaloblastic and other anemias, sprue, but it does not have advantages over folic acid. The main medicinal value of folinic acid lies in its antidote action in relation to medicinal (mainly antitumor) agents that are antagonists of folic acid. For this purpose, it is used in the form of a calcium salt.

The main use of calcium folinate has as an antagonist of the side effects of the antitumor drug methotrexate (see).

The antitumor effect of methotrexate (growth inhibition of actively proliferating tissues, growth retardation of malignant tissues) is associated with inhibition of dihydrofolate reductase and blocking the formation of tetrahydrofolate necessary for DNA biosynthesis. Simultaneously with the antitumor effect, however, the blood is suppressed. Calcium folinate helps to restore folate metabolism, prevents damage to bone marrow cells, protects hematopoiesis, and allows the use of methotrexate in high doses needed for chemotherapy of tumors.

Calcium folinate can be used as an antidote of methotrexate to prevent the possible toxic effects of elevated, high and ultra-high doses, as well as toxic manifestations developed from the use of usual doses of methotrexate (ulcerative-necrotic stomatitis, enteropathy, etc.).

Calcium folinate is applied intramuscularly or intravenously. Before use, the drug is dissolved in 1-2 ml of isotonic sodium chloride solution. The solution is suitable for use for 12 hours when stored in a cool place (not higher than +8 ° C).

During therapy with methotrexate in high doses (1 to 5 g), calcium folinate is administered in a single dose from 3 to 10 mg / m 2, with high doses of methotrexate (10 to 20 g) in a single dose from 10 to 20 mg / m 2. Begin injections at 6–18 hours, but no later than 24 hours after the infusion of methotrexate, then at 6-hour intervals for 48–72 hours. In total, the course of treatment is 10–12 doses (from 30 to 360 mg).