Leucovorin Lachema
It is administered intramuscularly or intravenously.
Due to the fact that different regimens for the use of Leucovorin Lachem are used, when choosing a specific dose, the doctor should be guided by special medical literature.
All doses indicated below are calculated in accordance with the conversion to folinic acid.
Usually when the drug is prescribed in combination with high doses of methotrexate (12-15 g/m2)
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 concentration of methotrexate in the blood plasma is less than 5 x 10-8 M.
In patients with acidic urine, exudative effusions, impaired renal function, and intestinal obstruction, a higher dose of Leucovorin Lachem and/or a longer duration of treatment may be required, since the administration of methotrexate in this group of patients may be slower. 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 administered and sodium bicarbonate is administered to maintain urine pH at 7.0 or higher.
In case of accidental overdose of methotrexate
Leucovorin Lahema is administered at a dose equal to or greater than the dose of administered methotrexate no later than 1 hour after the injection of methotrexate, then the drug is administered every 3 hours at 10 mg/m2 until signs of toxicity disappear.
When combined with fluorouracil
Leucovorin Lachema is administered:
- at a dose of 200 mg/m2 intravenously slowly (at least 3 minutes) or intravenously drip followed by intravenous administration of fluorouracil at a dose of 370 mg/m2 or
— at a dose of 20 mg/m2 intravenously, followed by intravenous administration of fluorouracil at a dose of 425 mg/m2.
The drugs are administered daily for 5 days with an interval of 4-5 weeks between repeated courses.
In the treatment of megaloblastic anemia caused by folic acid deficiency,
Leucovorin Lachem is prescribed
1
mg intramuscularly or intravenously per day.
To prepare a solution for injection, add 1 ml of water for injection to a bottle with lyophilisate for preparing a solution for intravenous and intramuscular administration.
Before intravenous administration of the drug as an infusion, the solution for intravenous and intramuscular administration is diluted with 5% dextrose solution or 0.9% sodium chloride solution for injection.
The infusion solution should be used immediately after its preparation. If the solution was not administered immediately, it is stored under aseptic conditions at a temperature of 2 - 8 ° C for no more than 24 hours.
Leucovorin 50 mg 5 pcs. lyophilisate for the preparation of solution for injection
pharmachologic effect
Antidote for folic acid antagonists (folinic acid is an active derivative of folic acid). Reduces the therapeutic and toxic effects of folic acid antagonists (for example, methotrexate), helps restore the biosynthesis of nucleic acids and replenishes folic acid deficiency in the body.
Composition and release form Leucovorin 50 mg 5 pcs. lyophilisate for the preparation of solution for injection
Solution for intravenous and intramuscular administration 1 vial: calcium folinate - 50 mg.
Bottles (5) - cardboard boxes.
Directions for use and doses
The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed. The dosage regimen of calcium folinate after intravenous infusions of methotrexate in high doses (12-15 g/m2 after 4 hours) is set individually, taking into account the state of renal excretory function, subject to systematic (at least 1 time/day) monitoring of the concentration of creatinine and methotrexate in plasma.
If methotrexate is eliminated normally (methotrexate plasma level is approximately 10 μM 24 hours after administration, 1 μM after 48 hours, and less than 0.2 μM after 72 hours), calcium folinate is used at a dose of 15 mg (approximately 10 mg/m2) orally, i.v. or IM every 6 hours for 60 hours (10 doses, starting 24 hours after the start of methotrexate administration).
With delayed late elimination of methotrexate (methotrexate level above 0.2 μM after 72 hours and above 0.05 μM after 96 hours after administration), calcium folinate is continued to be administered at a dose of 15 mg orally, intravenously or intramuscularly every 6 hours until the level of methotrexate in plasma does not fall below 0.05 µM.
In case of delayed early elimination of methotrexate from the body (methotrexate level 50 µM and above after 24 hours, 5 µM and above after 48 hours or an increase in plasma creatinine level by 100% or more within 24 hours after methotrexate administration), calcium folinate is administered at a dose of 150 mg IV every 3 hours until the plasma methotrexate level is below 1 μM, then at a dose of 15 mg IV every 3 hours until the plasma methotrexate level is below 0.05 μM. Simultaneous hydration and administration of sodium bicarbonate are required (to prevent the development of renal failure).
In cases where severe toxic reactions are observed, treatment with calcium folinate should be continued for an additional 24 hours (a total of 14 consecutive doses over 84 hours).
For megaloblastic anemia caused by folic acid deficiency, calcium folinate is prescribed in a dose of up to 1 mg/day.
Pharmacokinetics
Penetrates through the BBB. Accumulates in the liver. Metabolized in the liver and in the intestinal mucosa to form an active metabolite, the extent and rate of metabolism is higher when taken orally than when administered parenterally. T1/2 averages 6 hours. It is excreted mainly by the kidneys.
Indications for use Leucovorin 50 mg 5 pcs. lyophilisate for the preparation of solution for injection
Prevention and treatment of the toxic effects of methotrexate, overdose of folic acid antagonists. Treatment of megaloblastic anemia caused by folic acid deficiency. Palliative therapy of colon and rectal cancer (in combination with fluorouracil).
Contraindications
Megaloblastic anemia caused by vitamin B12 deficiency, hypersensitivity to calcium folinate.
Application Leucovorin 50 mg 5 pcs. lyophilisate for the preparation of solution for injection during pregnancy and lactation
If it is necessary to use calcium folinate during pregnancy, the expected benefit of therapy for the mother and the potential risk to the fetus should be carefully assessed. If necessary, use during lactation should stop breastfeeding.
When used in children, it should be borne in mind that calcium folinate may increase the frequency of seizures in predisposed patients by reducing the effectiveness of anticonvulsants.
special instructions
When treating with methotrexate in cases where clinical signs of toxicity or any abnormalities in laboratory parameters are noted, the possibility of an increase in the concentration of methotrexate in plasma due to interaction with other drugs that interfere with the elimination of methotrexate or displace it from association with plasma albumin should be excluded.
Use calcium folinate with caution in case of acidic urine, ascites, dehydration, exudative pleurisy, and impaired renal function. It should be borne in mind that with nausea and vomiting, the absorption of calcium folinate may deteriorate (it is preferable to use parenteral administration).
Before starting and during therapy, kidney function and urine pH should be monitored.
In case of accidental overdose of methotrexate, calcium folinate should be started as soon as possible.
When used in children, it should be borne in mind that calcium folinate may increase the frequency of seizures in predisposed patients by reducing the effectiveness of anticonvulsants.
Side effects Leucovorin 50 mg 5 pcs. lyophilisate for the preparation of solution for injection
From the digestive system: when taken orally - nausea, vomiting (in this case parenteral use is indicated).
Allergic reactions: urticaria, anaphylactic shock.
Drug interactions
Calcium folinate reduces the therapeutic and toxic effects of folic acid antagonists.
When used in high doses of calcium, folinate reduces the anticonvulsant effect of phenobarbital, phenytoin, primidone and increases the incidence of seizures in predisposed patients.
Calcium folinate enhances the antitumor and toxic effects of fluorouracil, especially on the gastrointestinal tract.
