Leucovorin Lahema (Leucovorin Lachema)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceCalcium folinateCalcium folinate
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    • Dosage form: & nbsplyophilizate for the preparation of solution for intravenous and intramuscular administration
    Composition:

    1 bottle contains:

    Active substance: calcium folinate pentahydrate 12.7 mg, which in terms of folinic acid is 10 mg and calcium folinate pentahydrate is 31.8 mg, which in folic acid is 25 mg.

    Excipients: sodium chloride, sodium hydroxide.

    1 ml of the solution contains:

    Active substance: calcium folinate pentahydrate 10.8 mg, which in terms of folinic acid is 10 mg.

    Excipients: sodium chloride, disodium edetate, sodium hydroxide, nitrogen, water for injection.

    Description:

    Lyophilized powder of light yellow color in the form of amorphous or compressed mass.

    The clear solution is from light yellow to yellow.

    Pharmacotherapeutic group:Vitamins
    ATX: & nbsp

    V.03.A.F   Drugs that reduce the toxicity of cytostatic therapy

    Pharmacodynamics:

    Leucovorin Lachema - a derivative of tetrafolic acid, is a restored form of folic acid and is used as an antidote for drugs that act as antagonists of folic acid. This compound is also known as folinic acid.

    Folate antagonists, such as methotrexate, inhibit dihydrofolate reductase and, thereby, prevent the formation of tetrahydrofolate from folic acid, which serves as an important cofactor for the transfer of single-carbon residues in the biosynthesis of nucleic acids. As a result, the synthesis of nucleic acids and cell division is blocked. Calcium folinate in contrast to folic acid does not require the reduction of dihydrofolate reductase for conversion into tetrahydrofolate, which allows its application to restore the broken process of biosynthesis of DNA, RNA and proteins.The protective action of calcium folinata is manifested only in relation to healthy cells. Prevents the toxic effect of methotrexate on the cells of the bone marrow and gastrointestinal tract, but does not significantly affect the already provided nephrotoxic effect of methotrexate.

    It helps to fill the deficiency of folic acid in the body.

    Calcium folinate can also enhance the antitumor effect of fluorouracil. When these two drugs interact, a stable complex containing thymidylate synthetase is formed, which inhibits and suppresses the synthesis of DNA.

    The beginning of the drug: with intramuscular injection - after 10-20 minutes, with intravenous administration - less than 5 minutes. The duration of the drug, regardless of the route of administration, is 3-6 hours.

    Pharmacokinetics:

    The maximum concentration for intramuscular injection of 15 mg of the drug is achieved after 1.72 hours and is 241 ng / ml. With intravenous administration of 25 mg, the maximum concentration (1259 ng / ml) is reached after 10 minutes.

    Penetrates through the blood-brain barrier in moderate amounts; more accumulates in the liver.Metabolized in the liver and intestinal mucosa mainly in the active metabolite of 5-methyl tetrahydrofolate. The maximum concentration of reduced folate in the blood serum is achieved with intramuscular injection of the preparation on average after 40 minutes. The elimination half-life is 6.2 hours, regardless of the route of administration.

    It is deduced, basically, by kidneys - 80-90%, with caloric masses - 5-8%.

    Indications:

    - Intoxication with folic acid antagonists (methotrexate, trimethoprim, pyrimethamine);

    - Prevention of toxic effects of methotrexate when used in high and high doses;

    - Colorectal cancer (as part of complex therapy with fluorouracil);

    - Megaloblastic anemia in the background of a deficiency of folic acid (including against the background of malabsorption syndrome, malnutrition, pregnancy, sprue, in early childhood with congenital insufficiency dihydrofolate reductase).

    Contraindications:

    Hypersensitivity to calcium folinate or any other substance included in the preparation;

    Megaloblastic anemia due to cyanocobalamin deficiency (vitamin A B12).

    Carefully:Alcoholism, epilepsy, chronic renal failure (CRF), children's age (up to 2 years - safety and efficacy for children not established).
    Pregnancy and lactation:

    Studies of folate calcium on reproductive function in animals and humans have not been carried out. It is not known whether calcium folinate harmful effects on the fetus when prescribing the drug to pregnant women and whether it can affect reproductive function. It is not known whether the calcium folinate in the mother's milk.

    The use of the drug during pregnancy and lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

    Dosing and Administration:

    It is administered intramuscularly or intravenously.

    In connection with the fact that different schemes of application of Leucovorin Lachem are used, the doctor should be guided by special medical literature when choosing a specific dose.

    All below given doses are calculated in accordance with the conversion to folinic acid.

    Usually when the drug is administered in combination with high doses of methotrexate (12-15 g / m2) the administration 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 methotrexate concentration in the blood plasma is less than 5 x 10-8 M.

    In patients with acid urine reaction, exudative effusions, impaired renal function, intestinal obstruction, a higher dose of Leucovorin Lachema and / or longer duration of treatment may be required, since the administration of methotrexate in this group of patients may be delayed. The use of leucovorin Lachem in these cases is recommended to be based on the mandatory determination of the concentration of methotrexate in the blood plasma. To prevent the development of chronic renal failure, hydration (3 L / day) is performed and administered sodium hydrogen carbonate to maintain the pH of urine at 7.0 or higher.

    At random overdose of methotrexate Leucovorin Lahema is administered at a dose equal to or greater than 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 disappearance of signs of toxicity.

    When combined with fluorouracil Leucovorin Lahema is introduced:

    - in a dose of 200 mg / m2 intravenously slowly (at least 3 minutes) or intravenously drip followed by intravenous fluorouracil at a dose of 370 mg / m2 or

    - in a dose of 20 mg / m2 intravenously followed by intravenous fluorouracil at a dose of 425 mg / m2.

    The drugs are administered daily for 5 days at intervals of 4-5 weeks between repeated courses.

    In the treatment megaloblastic anemia, caused by a deficiency of folic acid, Leucovorin Lahema is appointed by 1 mg intramuscularly or intravenously per day.

    For the preparation of solution for injection in the vial with lyophilizate for the preparation of solution for intravenous and intramuscular injection add 1 ml of water for injection.

    Before intravenous administration of the drug in the form of infusion, the solution for intravenous and intramuscular administration is diluted with 5% dextrose solution or 0.9% solution of sodium chloride for injection.

    Infusion solution should be used immediately after its preparation. In the event that the solution was not injected immediately, it is stored under aseptic conditions at a temperature of 2-8 ° C for not more than 24 hours.

    Side effects:

    Allergic reactions: skin rash, hives, itching, anaphylactic shock, fever is possible. When high doses are used, dyspeptic disorders are possible. Rarely is sleep disturbance, agitation.

    Overdose:

    Calcium folinate is not toxic.Even with very high doses of signs of overdose is not observed.

    Interaction:

    - Reduces the effectiveness of folic acid antagonists.

    - Reduces anticonvulsant activity of phenobarbital, phenytoin and primidone.

    - May lead to an increase in both the therapeutic and toxic effects of fluorouracil, and therefore, when combined, fluorouracil doses should be reduced.

    - Do not use the drug simultaneously with infusion solutions containing bicarbonate, due to the chemical instability of calcium folinate.

    - Direct mixing in one syringe of droperidol and calcium folinate can lead to precipitation.

    Special instructions:

    The use of calcium folinate in pernicious and other megaloblastic anemias caused by a deficiency of cyanocobalamin (vitamin B12) can lead to hematologic remission with a simultaneous progression of neurological disorders.

    It can increase the frequency of epileptic seizures in children predisposed to them due to a decrease in the effect of antiepileptic drugs - hydantoin derivatives and primidon (hexamidine).

    Form release / dosage:

    Lyophilizate for the preparation of a solution for intravenous and intramuscular administration.

    Solution for intravenous administration.

    Packaging:

    Lyophilizate for the preparation of a solution for intravenous and intramuscular administration in vials of 10 mg or 25 mg in terms of folinic acid.

    For 1 or 10 vials with instructions for use in a cardboard pack.

    Solution for intravenous administration of 10 mg / ml to 45 ml and 80 ml in colorless glass bottles (type I, Eur.Ph.), sealed with a rubber stopper (Eur.Ph.) and rolled with an aluminum cap with a plastic lid (Flip off).

    1 or 5 bottles of 45 ml and 1 80 ml bottle along with the instructions for use are placed in a cardboard box.

    Storage conditions:

    Lyophilizate - at a temperature of no higher than 25 ° C in a dark place. The prepared solution is stored for 12 hours.

    Solution - at a temperature of 2 - 8 ° C in the dark place.

    Keep out of the reach of children.

    Shelf life:

    Lyophilizate - 2 years.

    Mortar - 3 years

    Do not use after expiration of the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N016085 / 01
    Date of registration:17.11.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:Pliva-Lahema, AOPliva-Lahema, AO Czech Republic
    Manufacturer: & nbsp
    PLIVA-LACHEMA, a.s. Czech Republic
    Representation: & nbspPliva of Hvartska dooPliva of Hvartska doo
    Information update date: & nbsp06.03.2018
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