Calcium фолинат

General characteristics. Structure:

Active ingredient: 50 mg or 100 mg of calcium of a folinat.

Pharmacological properties:

Pharmacodynamics. Calcium фолинат is got into condition folic acid and it is used as an antidote of medicines which work as antagonists of folic acid. This connection is known also as foliniyevy acid. Antagonists of folic acid, such as methotrexate. Inhibit a digidrofolatreduktaza and, thereby, interfere with education from folic acid of tetrahydrofolate which serves as an important cofactor of transfer of the one-carbon remains in biosynthesis of nucleic acids. Blocking of synthesis of nucleic acids and cellular division results. Calcium фолинат, unlike folic acid, does not demand recovery digidrofolatreduktazy for transformation into tetrahydrofolate that allows to recover the broken process of biosynthesis of DNA, RNA and proteins at its use.

Protective action of calcium of a folinat is shown only concerning healthy cells. Prevents toxic action of a methotrexate on cells of marrow and digestive tract, but does not influence significantly already rendered nephrotoxic effect of a methotrexate. Promotes completion of deficit in an organism of folic acid. Calcium фолинат can also strengthen antineoplastic action of a ftoruratsil. At interaction of these two drugs the stable complex containing thymidylate to a sintetaz that inhibits is formed or suppresses DNA synthesis. Beginning of effect of drug: at intramuscular introduction – in 10-20 minutes, at intravenous administration – less than in 5 minutes. Action duration — about 3-6 hours irrespective of a way of introduction.

Pharmacokinetics. The maximum concentration of the recovered folate in blood serum at intramuscular introduction is reached on average in 40 minutes, at intravenous administration — in 10 minutes. Gets through a blood-brain barrier in moderate quantities; more collects in a liver.

5 methyltetrahydrofolate are metabolized in a liver and a mucous membrane of intestines preferential in an active metabolite. An elimination half-life - 6,2 hours irrespective of a way of introduction. It is removed by kidneys of 80-90%, with a fecal masses - 5-8%.

Indications to use:

• Intoxication antagonists of folic acid (methotrexate, Trimethoprimum and Pyrimethaminum).

• Prevention of toxic action of a methotrexate at its use in the raised and high doses.

• A colorectal cancer (as a part of a combination therapy with ftoruratsily).

• Megaloblastny anemia against the background of deficit of folic acid (including against the background of a sprue, insufficiency of food, pregnancy, to a spr, at early children's age at inborn insufficiency of a digidrofolatreduktaza).

Route of administration and doses:

Solution is entered intramusculary or intravenously. Calcium фолинат cannot be entered intratekalno.

For preparation of solution for injections contents of a bottle weighing 50 mg or 100 mg are dissolved in 5 ml or 10 ml of sterile water for injections respectively, to concentration of 10 mg/ml. The prepared solution is suitable for the use within 12 hours at a temperature not above +25 °C. Before intravenous administration of drug in the form of infusions the prepared solution is dissolved by 5% with solution of a dextrose or 0,9% sodium chloride solution for injections. Infusion solution should be used right after preparation. If solution was not entered at once, it is stored in aseptic conditions within 12 hours at a temperature not above +25 °C.

As drug contains calcium in high concentration, speed in/in administrations of drug should not exceed 160 mg/min. or 16 ml of the prepared solution with concentration of 10 mg/ml. At the choice of a specific dose the doctor has to be guided by special medical literature. Usually at purpose of drug in combination with high doses of a methotrexate (12-15g/sq.m) introduction there begin in 24 hours after the end of treatment with a methotrexate in a dose of 10 mg/sq.m each 6 hours within 72 hours. At patients with acid reaction of urine, exudative exudates, a renal failure, impassability of intestines higher dose of calcium of a folinat and/or big duration of treatment as this group of patients can have a removal of a methotrexate in a slowed-up way can be required.

Use of calcium of a folinat in these cases is recommended to be based on obligatory definition of concentration of a methotrexate in a blood plasma. For prevention of development of a chronic renal failure carry out hydration (Zl / days) and enter Natrii hydrocarbonas for maintenance рН urine at the level of 7 or above. At accidental overdose of a methotrexate of calcium фолинат it is entered in a dose equal or exceeding a dose of the entered methotrexate no later than in 1 hour after a methotrexate injection, further the drug is administered each 3 hours on 10 mg/sq.m before disappearance of signs of toxicity. At a combination with 5-ftoruratsily calcium фолинат it is entered before introduction of a 5-ftoruratsil. At treatment of the megaloblastny anemia caused by deficit of folic acid, calcium фолинат appoint 1 mg intramusculary or intravenously once a day.

Features of use:

Use of calcium of a folinat at pernicious and other megaloblastny anemias caused by deficit of cyanocobalamine (B12 vitamin) can lead to hematologic remission with simultaneous progressing of neurologic frustration.

Can increase the frequency of epileptic seizures at the children predisposed to them owing to decrease in effect of antiepileptic drugs – derivative hydantoin and Primidonum (hexamidine).

Side effects:

Allergic reactions: skin rash, small tortoiseshell, itch, acute anaphylaxis.

At use of high doses of calcium of a folinat dispepsichesky disturbances are possible. Seldom – a sleep disorder, excitement.

Interaction with other medicines:

Calcium фолинат at simultaneous use reduces efficiency of antagonists of folic acid.

Reduces anticonvulsant activity of phenobarbital, Phenytoinum and Primidonum.

Can lead to strengthening of both therapeutic, and toxic action of a ftoruratsil in this connection, at combined use of a dose of a ftoruratsil have to be reduced.

Contraindications:

Hypersensitivity to calcium to the folinat or any other substance which is a part of drug.

The Megaloblastny anemia caused by deficit of cyanocobalamine (B12 vitamin).

With care: alcoholism, epilepsy, the chronic renal failure (CRF), children's age (up to 2 years – safety and efficiency for children is not established).

Overdose:

Calcium фолинат it is not toxic. Even at use of very high doses of signs of overdose it is not observed.

Issue conditions:

According to the recipe

Packaging:

The lyophilized powder for preparation of solution for injections of 50 mg or 100 mg in bottles in packaging No. 1 and No. 40.