Leucovorine-LANS, 50mg vials, 5pcs

Composition

Active ingredient: Calcium folinate (calcium leucovorin) anhydrous 0.054 g based on folinic acid 0.0500 gw Auxiliary substances: Methylparahydroxybenzoate (nipagin) 0.0008 g, Propylparahydroxybenzoate (nipazole) 0.0002 g

Pharmacological action

Calcium folinate is a reduced form of folic acid and is used as an antidote to drugs that act as folic acid antagonists. This compound is also known as folinic acid. Folic acid antagonists, such as methotrexate, inhibit dihydrofolate reductase and thus prevent the formation of tetrahydrofolate from folic acid, which serves as an important cofactor for the transfer of single-carbon residues in nucleic acid biosynthesis. As a result, the synthesis of nucleic acids and cell division is blocked. Calcium folinate, unlike folic acid, does not require reduction by dihydrofolate reductase for conversion to tetrahydrofolate, which allows its use to restore the disturbed biosynthesis of DNA, RNA and proteins. The protective effect of calcium folinate is shown only in relation to healthy cells. Prevents the toxic effect of methotrexate on bone marrow and gastrointestinal tract cells, but does not significantly affect the already exerted nephrotoxic effect of methotrexate. Helps to fill the deficiency of folic acid in the body. Calcium folinate may also enhance the antitumor effect of fluorouracil. When these two drugs interact, a stable complex containing thymidylate synthetase is formed, which inhibits or suppresses DNA synthesis. The onset of action of the drug: with intramuscular use-in 10-20 minutes, with intravenous use-in less than 5 minutes. The duration of action is about 3-6 hours, regardless of the method of use.

Indications

• Intoxication with folic acid antagonists (methotrexate, trimethoprim, and pyrimethamine).
• Prevention of toxic effects of methotrexate when used in high and high doses.
• Colorectal cancer (in combination therapy with fluorouracil).
• Megaloblastic anemia on the background of folic acid deficiency (including malabsorption syndrome, malnutrition, pregnancy, sprue, in early childhood with congenital dihydrofolate reductase deficiency)

Recommendations for use

The solution is administered intramuscularly or intravenously. Due to the fact that different regimens of Leucovorin-LANCE are used, when choosing a specific dose, the doctor should be guided by special medical literature. Usually, when the drug is prescribed in combination with high doses of methotrexate (12-15 g/m), use begins 24 hours after the end of treatment with methotrexate at a dose of 10 mg/m2 every 6 hours for 72 hours or until the concentration of methotrexate in blood plasma is less than 5×10 -8 M. In patients with an acidic urine reaction, exudative effusions, impaired renal function, intestinal obstruction, a higher dose of Leucovorin-LANCE® and/or a longer duration of treatment may be required, since Methotrexate may be delayed in this group of patients. The use of Leucovorin-LANCE® in these cases is recommended to be based on the mandatory determination of the concentration of methotrexate in blood plasma. To prevent the development of CRF, hydration is performed (3 liters/day) and sodium bicarbonate is administered to maintain the pH of urine at a level of 7 or higher. In case of accidental overdose of methotrexate, Leucovorin-LANCE® is administered at a dose equal to or exceeding the dose of methotrexate administered no later than 1 hour after the injection of methotrexate, then the drug is administered every 3 hours at 10 mg/m2 until the signs of toxicity disappear. When combined with fluorouracil, Leucovorin-LANCE® is administered: • at a dose of 200 mg / m2 intravenously slowly (at least 3 minutes) or intravenous drip followed by intravenous use of fluorouracil at a dose of 370 mg / m2 or * at a dose of 20 mg/m2 intravenously followed by intravenous use of fluorouracil at a dose of 425 mg/m2. The drugs are administered daily for 5 days with an interval of 4-5 weeks in repeated courses. In the treatment of megaloblastic anemia caused by folic acid deficiency, Leucovorin-LANCE®is prescribed 1 mg intramuscularly or intravenously per day.

Contraindications

• Hypersensitivity to calcium folinate or any other substance that is part of the drug.
• Megaloblastic anemia caused by cyanocobalamin (vitamin B12) deficiency.

With caution – alcoholism, epilepsy, chronic renal failure (CRF), children (under 2 years of age-safety and efficacy for children have not been established).

Side effects

Allergic reactions: skin rash, urticaria, pruritus, anaphylactic shock. When using high doses of calcium folinate, dyspeptic disorders are possible. Rare sleep disturbance, arousal

Interaction

of Calcium folinate with simultaneous use reduces the effectiveness of folic acid antagonists. Reduces the anticonvulsant activity of phenobarbital, phenytoin and pyrimidone. It can lead to an increase in both the therapeutic and toxic effects of fluorouracil, and therefore, when used together, the dose of fluorouracil should be reduced.

Overdose

of Calcium folinate is non-toxic. Even with very high doses, there are no signs of overdose.

Special instructions

The use of Leucovorin-LANCE®in pernicious and other megaloblastic anemia caused by cyanocobalamin (vitamin B12) deficiency may lead to hematological remission with simultaneous progression of neurological disorders. It may increase the frequency of epileptic seizures in children predisposed to them due to a decrease in the effect of antiepileptic drugs-derivatives of hydantoin and primidone (hexamidine).

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Shelf

life is 4 years. Do not use after the expiration date.

Active ingredient

Calcium Folinate

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection and infusion