Universal reference book for medicines
Product name: LEUKOVORIN LACHEMA (LEUCOVORIN LACHEMA)

Active substance: calcium folinate

Type: Antidote antagonists of folic acid

Manufacturer: PLIVA-LACHEMA (Czech Republic)
Composition, form of production and packaging
Lyophilizate for the preparation of a solution for intravenous and / or injections
in the form of an amorphous or compressed mass of light yellow color.

1 f.

calcium folinate pentahydrate 12.7 mg,

which corresponds to the content of folinic acid 10 mg

Excipients: sodium chloride, sodium hydroxide.

Vials (1) - packs of cardboard.

Vials (10) - packs of cardboard.

Lyophilizate for the preparation of a solution for intravenous and / or injections in the form of an amorphous or compressed mass of light yellow color.

1 f.

calcium folinate pentahydrate 31.8 mg,

which corresponds to the content of folinic acid 25 mg

Excipients: sodium chloride, sodium hydroxide.

Vials (1) - packs of cardboard.

Vials (10) - packs of cardboard.

The solution for intravenous administration is clear, from light yellow to yellow.

1 ml of 1 fl.

calcium folinate pentahydrate 10.8 mg 486 mg,

which corresponds to the content of folinic acid 10 mg 450 mg

Auxiliary substances: sodium chloride, disodium edetate, sodium hydroxide, nitrogen, water d / u.

45 ml - vials of colorless glass (1) - packs cardboard.

45 ml - bottles of colorless glass (5) - packs cardboard.

The solution for intravenous administration is clear, from light yellow to yellow.

1 ml of 1 fl.

calcium folinate pentahydrate 10.8 mg 864 mg,

which corresponds to the content of folinic acid 10 mg 800 mg

Auxiliary substances: sodium chloride, disodium edetate, sodium hydroxide, nitrogen, water d / u.

80 ml - vials of colorless glass (1) - packs cardboard.

INSTRUCTION FOR THE SPECIALIST.

The product description was approved by the manufacturer for the 2009 print edition.

PHARMACHOLOGIC EFFECT

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 thus 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, unlike folic acid, does not require the reduction of dihydrofolate reductase for conversion to tetrahydrofolate, which allows using it 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 bone marrow and gastrointestinal cells, 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 action of the drug with the / m introduction - after 10-20 minutes, with the / in the introduction - less than 5 minutes.
The duration of the drug, regardless of the mode of administration, is 3-6 hours.
PHARMACOKINETICS

C max with a / m administration of 15 mg of the drug is achieved after 1.72 hours and is 241 ng / ml.
With intravenous administration of 25 mg C max (1259 ng / ml) is reached after 10 minutes.
It penetrates through the BBB in moderate amounts;
more accumulates in the liver. Metabolized in the liver and intestinal mucosa mainly in the active metabolite of 5-methyl tetrahydrofolate. Cmax of reduced folate in the blood serum is achieved with an IV injection of the drug on average after 40 minutes. T 1/2 - 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 on the background of a deficiency of folic acid (including against the background of malabsorption syndrome, malnutrition, pregnancy, sprue, in early childhood with congenital insufficiency of dihydrofolate reductase).

DOSING MODE

It is entered in / m or / in.

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.

Administration of the drug in combination with high doses of methotrexate (12-15 g / m 2 ) usually starts at 24 hours after the end of methotrexate treatment at a dose of 10 mg / m 2 every 6 hours for 72 hours or until the plasma methotrexate concentration is reached 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 sodium bicarbonate is added to maintain urine pH at 7 or higher.
In case of an accidental overdose of methotrexate, Leucovorin Lachema is given 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 injected every 3 hours at 10 mg / m 2 until the signs of toxicity disappear.

When combined with fluorouracil, Leucovorin Lachema is administered at a dose of 200 mg / m 2 IV slowly (at least 3 minutes) or IV in the drip followed by IV fluorouracil at a dose of 370 mg / m 2 or at a dose of 20 mg / m 2 I / O followed by intravenous administration of fluorouracil in a dose of 425 mg / m 2 .

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

In the treatment of megaloblastic anemia caused by a deficiency of folic acid , Leucovorin Lachema is prescribed 1 mg IM or IV day.

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

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

Infusion solution should be used immediately after its preparation.
In this case, if 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 EFFECT

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.

CONTRAINDICATIONS

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

- hypersensitivity to calcium folinate or any other substance that is part of the drug.

With caution - alcoholism, epilepsy, chronic renal failure, children under 2 years of age (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 has a harmful effect on the fetus when the drug is administered to pregnant women and whether it can affect reproductive function. It is not known whether calcium folate penetrates the mother's milk.
The use of the drug during pregnancy and during lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

APPLICATION FOR FUNCTIONS OF THE LIVER

With caution , chronic renal failure.

SPECIAL INSTRUCTIONS

The use of calcium folinate in pernicious and other megaloblastic anemias caused by cyanocobalamin deficiency can lead to hematological remission with 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).

OVERDOSE

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

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The lyophilizate should be stored at a temperature of no higher than 25 ° C in a dark place.
The prepared solution is stored for 12 hours.
The solution for intravenous administration should be stored at a temperature of 2 ° -8 ° C in a dark place.
Keep out of the reach of children.
Shelf life of the lyophilizate is 2 years, the solution for intravenous administration is 3 years.

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