Leucovorin Lachema (The solution for the on / in the)

Active material: Calcium folinate
When ATH: V03AF03
CCF: Antidote to folic acid antagonists
When CSF: 22.11.01
Manufacturer: PLIVA-LACHEMA a.s. (Czech Republic)

DOSAGE FORM, STRUCTURE AND PACKAGING

The solution for the on / in the clear, from light yellow to yellow.

Excipients: sodium chloride, disodium эdetat, Sodium hydroxide, nitrogen, water d / and.

45 ml – colorless glass vials (1) – packs cardboard.
45 ml – colorless glass vials (5) – packs cardboard.

The solution for the on / in the clear, from light yellow to yellow.

Excipients: sodium chloride, disodium эdetat, Sodium hydroxide, nitrogen, water d / and.

80 ml – colorless glass vials (1) – packs cardboard.

DESCRIPTION OF ACTIVE SUBSTANCES

Pharmacological action

Antidote to folic acid antagonists (folinic acid is the active derivative of folic acid). It reduces the therapeutic and toxic effects of folic acid antagonists (eg, methotrexate), It helps restore the biosynthesis of nucleic acids and makes up for the deficit of folic acid in the body.

Pharmacokinetics

It penetrates through the BBB. It accumulates in the liver. It is metabolized in the liver and in the intestinal mucosa with the formation of the active metabolite, degree and rate of metabolism higher ingestion, than when parenterally administered. T_1/2 averages 6 no. Report mostly kidneys.

Testimony

Prevention and treatment of toxic action of methotrexate, overdose of folic acid antagonists. Treatment of megaloblastic anemia, caused by folic acid deficiency. Palliative treatment of cancer of the colon and rectum (in combination with fluorouracil).

Dosage regimen

The dosage regimen of calcium folinate after / in infusions of methotrexate in high doses (12-15 g / m² through 4 no) set individually, given the state of renal excretory function, provided systematic (minimum 1 time / day) monitoring the concentration of creatinine and methotrexate in plasma.

In the normal excretion of methotrexate (the level of methotrexate in plasma approximately 10 M through 24 hours after injection, 1 M through 48 hr or less 0.2 M through 72 no) calcium folinate was used in a dose 15 mg (about 10 mg / m²) inside, w / w or w / o each 6 h for 60 no (10 doses, commencing 24 hours after the start of methotrexate).

During slow excretion of methotrexate later (higher levels of methotrexate 0.2 M through 72 h or higher 0.05 M through 96 hours after injection) calcium folinate continue administered at a dose 15 mg orally, w / w or w / o every 6 h until, until the level of methotrexate in plasma is below 0.05 M.

In delayed early methotrexate excretion from the body (methotrexate level 50 uM and up through 24 no, 5 uM and up through 48 h or increasing creatinine level in plasma 100% and more over 24 hours after the administration of methotrexate) Calcium folinate is administered in a dose of 150 mg / in every 3 h until, until the level of methotrexate in plasma is below 1 M, then dose 15 mg / in every 3 no, until the level of methotrexate in plasma is below 0.05 M. Always simultaneous hydration and administering sodium bicarbonate (for prophylaxis of renal failure).

In cases, When the expressed toxic reactions, treatment of calcium folinate should continue further, for another 24 no (Total 14 successive doses of 84 no).

When megaloblastic anemia, caused by folic acid deficiency, calcium folinate administered at a dose of 1 mg / day.

Side effect

From the digestive system: ingestion – nausea, vomiting (in this case shown parenteral application).

Allergic reactions: hives, anaphylactic shock.

Contraindications

Megaloblastnaya anemia, caused by a deficiency of vitamin B₁₂, Hypersensitivity to calcium folinate.

Pregnancy and lactation

If necessary, use of calcium folinate in pregnancy should carefully evaluate the expected benefits of therapy for the mother and the potential risk to the fetus. If necessary, use during lactation should stop breastfeeding.

Cautions

In the treatment of methotrexate in cases, When marked clinical signs of toxicity or any laboratory abnormalities, It should eliminate the possibility of increasing the concentration of MTX in the plasma due to interactions with other drugs, violate the elimination of methotrexate, or wipe it out due to the plasma albumin.

With careful use of calcium folinate at acidic urine, asci, Dehydration, pleural effusion, impaired renal function. It should be taken into account, that nausea and vomiting absorption of calcium folinate may deteriorate (preferable to the parenteral administration).

Before and during the treatment should monitor renal function, urine pH.

In case of accidental overdose of methotrexate calcium folinate reception should begin as soon as possible.

When applied in children should be understood, that calcium folinate may increase the frequency of seizures in susceptible patients, by reducing the effectiveness of anticonvulsants.

Drug Interactions

Calcium folinate reduces the therapeutic and toxic effects of folic acid antagonists.

When used in high doses of calcium folinate reduces anticonvulsant effect phenobarbital, phenytoin, primidone, and increase the frequency of seizures in susceptible patients.

Calcium folinate enhances the antitumor and toxic effects of fluorouracil, particularly in the gastrointestinal tract.