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Description of the medicine: Calcium folinate (Calcii folinas; Calcium-folinate)

CALCIUM FOLINATE (Calcii folinas; Calcium-folinate).

The 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 due to the fact that folinic acid is a growth factor for the bacteria Leuconostoc citrovorum), Chemifolin, Lederfoline, Rescufolin, Tonofolin, etc.

A yellowish white crystalline powder. Easily soluble in water. Unstable in the light.

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

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

Folic acid, like folic acid, is effective for megaloblastic and other anemia, spru, but has no advantages over folic acid. The main medicinal value of folinic acid lies in its antidote effect in relation to drugs (mainly antitumor), which are folic acid antagonists. For this purpose, it is used in the form of calcium salt.

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

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

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

Apply calcium folinate intramuscularly or intravenously. Before use, the drug is dissolved in 1 to 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 - 5 g), calcium folinate is administered in a single dose from 3 to 10 mg / m 2, at high doses of methotrexate (10 - 20 g) - in a single dose from 10 to 20 mg / m 2. Injections begin after 6 to 18, but no later than 24 hours after methotrexate infusion, then at 6-hour intervals for 48 to 72 hours. In total, 10 to 12 doses (from Z0 to 360 mg) per course of treatment.