Folic acid antagonists such as methotrexate inhibit dihydrofolate reductase and thereby prevent the formation of folic acid, tetrahydrofolate, which serves as an important cofactor for transferring one-carbon residue in the biosynthesis of nucleic acids. The result is the blocking of the synthesis of nucleic acids and cell division. Calcium folinate Unlike folic oral primobolan acid does not require recovery for dihydrofolate reductase in the conversion of tetrahydrofolate, which allows its use to restore the disturbed process of biosynthesis of DNA, RNA and proteins. The protective effect of calcium folinate is shown only in respect of normal cells. It prevents the toxic effects of methotrexate on bone marrow cells and the gastrointestinal tract, but not significantly affect the already extended to nephrotoxic effect of methotrexate. Helps replenish folic acid deficiency in the body.Calcium folinate may enhance the antitumor effect of fluorouracil. The interaction of the two drugs produced a stable complex comprising a thymidylate synthetase, and inhibits that inhibits DNA synthesis. The onset of action of the drug: intramuscular injection – 10-20 min after intravenous injection – less than 5 minutes. The duration of action of the drug, regardless of the route of administration is 3-6 hrs.
- Intoxication folic acid antagonists (methotrexate, trimethoprim, pyrimethamine);
- Preventing toxic effect of MTX when administered in high doses and high;
- Colorectal cancer (in the complex therapy with fluorouracil);
- Megaloblastic anemia on background folate deficiency (including on the background of the syndrome of malabsorption, malnutrition, pregnancy, sprue, in early childhood with a congenital deficiency of dihydrofolate reductase).
- Hypersensitivity to calcium folinate, or to any other substance included in the composition of the drug;
- Megaloblastic anemia due to deficiency of cyanocobalamin (vitamin B12).
Be wary – alcoholism, epilepsy, chronic renal failure (CRF), children’s age (up to 2 years – the safety and effectiveness for children have not been established).
Pregnancy and lactation
Studies folinic acid on the reproductive function have not been conducted in animals and humans. It is not known whether he has whether calcium folinate harmful effects on the fetus when administering the drug to pregnant women and can affect reproductive function. It is not known whether calcium folinate in the mother’s milk.
Use of the drug during pregnancy and lactation is possible only when the intended benefits to the mother outweighs the potential risk to the fetus.
Dosing and Administration
is administered intramuscularly or intravenously.
Due to the fact that use different patterns of use of leucovorin Lachema, when choosing a particular dose of a doctor should be guided by the special medical literature.
Everything below the specified doses are calculated in accordance with conversion to folinic acid.
Typically, when administering the drug in combination with high doses of methotrexate (12-15 g / m 2 ) administration was initiated 24 hours after treatment with methotrexate at a dose of 10 mg / m 2 every 6 hours for 72 hours or until the methotrexate concentration in the blood plasma of less than 5 × 10 -8 M.
in patients with acidic urine reaction exudative effusions, renal impairment, intestinal obstruction may require a higher dose of leucovorin Lachema and / or longer duration of treatment as well as the introduction of methotrexate in oral primobolan this group of patients can be slow. The use of leucovorin Lachema in these cases it is recommended to establish mandatory definition of methotrexate concentration in plasma.To prevent the development of CKD conduct hydration (3 liters / day) and sodium hydrogen carbonate is introduced to maintain the urine pH at 7.0 or above.
When methotrexate Leucovorin accidental overdose Lachema administered at a dose equal to or greater than the dose of methotrexate administered not later than 1 hour after injection of methotrexate, then the drug is administered every 3 hours for 10 mg / m 2 until the disappearance of signs of toxicity.
In combination with fluorouracil, leucovorin Lachema introduces:
- 200 mg / m 2 by slow intravenous injection (at least 3 minutes) or intravenously followed by intravenous administration of fluorouracil at a dose of 370 mg / m 2 or
- 20 mg / m 2 intravenously followed by intravenous administration of fluorouracil at a dose of 425 mg / m 2 .
Drugs administered daily for 5 days with an interval of 4-5 weeks between repeated courses.
In the treatment of megaloblastic anemia due to folic acid deficiency, leucovorin Lachema appoint 1 mg intramuscularly or intravenously per day.
To prepare the solution for injection in a vial with lyophilisate for preparation solution for intravenous and intramuscular injection, add 1 ml of water for injection.
Before intravenous infusion of the drug as a solution for intravenous and intramuscular injection diluted 5% dextrose or 0.9% sodium chloride solution for injection.
The infusion solution should be used immediately after its preparation . In that case, if the solution was not introduced immediately, it is stored under aseptic conditions at 2 – 8 ° C for up to 24 hours.
Side effects: Allergic reactions: skin rash, urticaria, pruritus, anaphylactic shock, possible fever. When high doses are possible dyspeptic disorders. Rarely – sleep disturbance, agitation.
Calcium folinate is not toxic. Even when using very high doses overdosage symptoms are observed.
Interaction with other drugs
- Reduces the effectiveness of folic acid antagonists.
- It reduces the anticonvulsant activity of phenobarbital, phenytoin and primidone.
- It may lead to an increase both therapeutic and toxic effect of fluorouracil, in this connection, the joint application of fluorouracil dose should be reduced.
- Should not be used concurrently with a drug infusion solutions containing bicarbonate, in relation to the chemical instability of calcium folinate.
- Intimately mixing in the same syringe droperidol and calcium folinate can result in a precipitate.
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. Use of calcium oral primobolanfolinate with pernicious and other megaloblastic anemias caused by deficiency of cyanocobalamin (vitamin Bn), can lead to remission while the progression of neurological disorders
may increase the frequency of seizures in susceptible thereto children due to a reduction effect of antiepileptic drugs – derivatives of hydantoin and primidone (hexamidine). steroiden kaufen
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