Leucovorin-Teva (Leucovorin-Teva)

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: & nbspsolution for intravenous and intramuscular administration
    Composition:In 1 ml of solution contains:
    active ingredient: calcium folinate pentahydrate 12.71 mg corresponds to calcium folinate anhydrous 10.8 mg (calculated as folinic acid 10.0 mg);
    auxiliary substances: sodium chloride 8.0 mg, sodium hydroxide 1% solution or hydrochloric acid 1 M solution to pH 8.2-8.5, water for injection up to 1 ml.
    Description:Transparent solution from colorless to yellow. Evaluation is carried out visually.
    Pharmacotherapeutic group:Vitamin - antidote of folic acid antagonists (modifier of biological action of fluorouracil)
    ATX: & nbsp

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

    Pharmacodynamics:

    Calcium folinate is a restored form of folic acid and is used as an antidote for medicines that act as antagonists of folic acid.

    Folate antagonists, such as methotrexate, inhibit dihydrofolate reductase and, thereby, prevent the formation of tetrahydrofolate from folic acid, which is a cofactor of the transfer of monocarbon 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. Due to the indicated properties calcium folinate prevents the toxic effect of methotrexate on the cells of the bone marrow and gastrointestinal tract, but does not significantly affect the already developed nephrotoxic effect of methotrexate.

    The drug helps to fill the deficit in the body of folic acid.

    Calcium folinate can also enhance the antitumor effect of fluorouracil. When these two drugs interact, a stable complex of components is formed, which contains thymidylate synthetase inhibiting and suppressing 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 action is about 3-6 hours, regardless of the route of administration.

    Pharmacokinetics:

    The maximum concentration of reduced folate in the blood serum with intramuscular injection is achieved on average in 40 minutes, with intravenous administration - after 10 minutes and with oral administration in 1 hour 40 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 half-life (T 1/2) - 6.2 hours regardless of the route of administration.

    It is excreted by the kidneys 80-90%, intestine - 5-8%.

    Indications:

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

    - Prevention of toxic effects of methotrexate, used in high doses;

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

    - Megaloblastic anemia, caused by 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 component included in the preparation;

    - Megaloblastic anemia, caused by a deficiency of cyanocobalamin (vitamin B12);

    - Pregnancy and lactation.

    Carefully:

    Carefully: is used for alcoholism, epilepsy, chronic renal failure (CRF), children under 2 years of age (safety and efficacy not established).

    Dosing and Administration:

    The solution is administered intramuscularly or intravenously.

    When choosing the doses and the mode of administration of the drug in each individual case, you should refer to the special literature.

    Usually when the drug is administered in combination with high doses of methotrexate (12-15 mg / m2) the administration begins 24 hours after the end of treatment with methotrexate in a dose of 10 mg / m2 every 6 hours for 72 hours or until the plasma methotrexate concentration is less than 5x10-8 M.

    In patients with acid urine reaction, exudative effusions, impaired renal function, intestinal obstruction, a higher dose of calcium folinate and / or longer duration of treatment may be required, since excretion of methotrexate in this group of patients may be delayed. The use of leucovorin-Teva 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 chronic renal failure, hydration (3 L / day) is performed and administered sodium hydrogen carbonate to maintain the pH of urine at 7 or higher.

    At random overdose of methotrexate Leucovorin-Teva 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 combination with fluorouracil Leucovorin-Teva 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.

    Drugs are administered daily for 5 days at intervals of 4-5 weeks for repeated courses.

    In the treatment megaloblastic anemia caused by a deficiency of folic acid Leucovorin-Teva is prescribed at 1 mg / day intramuscularly or intravenously.

    Preparation of injection solution

    The drug Leucovorin-Teva is bred in the Ringer Ringer; r-re Ringer with lactate; 10% of r-re dextrose in water; 5% of r-re dextrose in water; 0.9% of the sodium chloride solution to a concentration of 0.06 mg / ml to 1 mg / ml. The resulting solution remains stable for 24 hours. The solution remaining after the injection should not be used.

    Side effects:

    The following undesirable phenomena noted with the use of Leucovorin-Teva are distributed according to the frequency of occurrence according to the following gradation: very often (> 1/10), often (> 1/100 to <1/10) infrequently (from> 1/1000 to <1/100), rarely (from> 1/10000 to <1/1000), very rarely (<1/10000).

    From the immune system: very rarely - allergic reactions: skin rash, hives, itching, anaphylactic shock.

    From the nervous system: rarely - insomnia, agitation, depression, agitation, increased frequency of epileptic seizures.

    On the part of the digestive system: rarely - dyspeptic phenomena (with the use of high doses of calcium folinata).

    Other: infrequently, fever.

    Overdose:

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

    Interaction:

    - Calcium folinate with simultaneous application reduces the effectiveness of folic acid antagonists.

    - Reduces anticonvulsant activity phenobarbital, phenytoin and primidon.

    - Its use can lead to an increase in both therapeutic and toxic effects fluorouracil, in connection with which, when a dose is jointly administered fluorouracil should be reduced.

    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).

    Use with caution calcium folinate with acidic urine reaction, ascites, dehydration, exudative pleurisy, impaired renal function.

    Before and during the therapy should monitor the function of the kidneys, the pH of the urine. In case of an accidental overdose of methotrexate, calcium folinate should be taken as soon as possible.

    Form release / dosage:Solution for intravenous and intramuscular injection of 50 mg / 5 ml, 100 mg / 10 ml, 200 mg / 20 ml, 300 mg / 30 ml and 500 mg / 50 ml (10 mg / ml).
    Packaging:

    A solution for intravenous and intramuscular administration of 50 mg / 5 ml, 100 mg / 10 ml, 200 mg / 20 ml, 300 mg / 30 ml and 500 mg / 50 ml (10 mg / ml) in colorless glass bottles USP type 1, with a stopper made of rubber chlorobutyl, an aluminum cap provided with a protective cap-insert made of colored polypropylene.

    1 bottle with instructions for use in a cardboard pack

    Storage conditions:

    List B.

    At a temperature of 2 to 8 ° C, in a dark place.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012095 / 03
    Date of registration:04.09.2009
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp11.09.2015
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