Description
Release form
Solution for intravenous administration
Pharmacological action of
Pharmacodynamics
Antidote of folic acid antagonists (folinic acid is an active derivative of folic acid). It reduces the therapeutic and toxic effects of folic acid antagonists (for example, methotrexate), helps restore the biosynthesis of nucleic acids and makes up for folic acid deficiency in the body.
Pharmacokinetics
Penetrates through the BBB. Accumulates in the liver. It is metabolized in the liver and in the intestinal mucosa with the formation of an active metabolite, the degree and rate of metabolism is higher when taken orally than with parenteral administration. T1 / 2 averages 6 hours. It is excreted mainly by the kidneys.
Indications
Leucovorin is used: 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 for colon and rectal cancer (in combination with fluorouracil).
contraindications Megaloblastic anemia caused by vitamin deficiency mine B12
hypersensitivity to calcium folinate.
Use during pregnancy and lactation
If calcium folinate is required during pregnancy, the intended benefits of the therapy to the mother and the potential risk to the fetus should be carefully evaluated.
If necessary, use during lactation should stop breastfeeding.
Special instructions
When treating with methotrexate in cases where clinical signs of toxicity or any deviations in laboratory parameters are noted, the possibility of increasing the concentration of methotrexate in the plasma due to interaction with other drugs that disrupt the excretion of methotrexate or displacing it from the plasma albumin should be excluded .
Caution is taken with calcium folinate for acid urine, ascites, dehydration, exudative pleurisy, impaired renal function. Should be considered, that with nausea and vomiting, the absorption of calcium folinate may deteriorate (parenteral administration is preferred).
Before starting and during therapy, kidney function and urine pH should be monitored.
In case of an 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 can increase the frequency of seizures in predisposed patients, due to a decrease in the effectiveness of anticonvulsants.
Composition
1 bottle contains active substance: 5 mg calcium .
Solvent: sodium chloride solution 0.9% – 2 ml.
Dosing and Administration
Dosing regimen of calcium folinate after iv infusion 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 ) control the concentration of creatinine and methotrexate in plasma.
With normal excretion of methotrexate (plasma methotrexate level of approximately 10 ?M 24 hours after administration, 1 ?M after 48 hours and less than 0.2 ?M after 72 hours), calcium folinate is used at a dose of 15 mg (approximately 10 mg / m2) inside, in / in or in / m every 6 hours for 60 hours (10 doses, starting 24 hours after the start of methotrexate administration).
With delayed late excretion of methotrexate (methotrexate levels higher than 0.2 ?M after 72 hours and above 0.05 ?M after 96 hours), calcium folinate is continued to be administered at a dose of 15 mg orally, iv or IM every 6 hours until the plasma methotrexate level drops below 0.05 ?M.
In case of delayed early excretion of methotrexate from the body (methotrexate level 50 ?M or higher after 24 hours, 5 ?M or higher after 48 hours or an increase in plasma creatinine by 100% or more within 24 hours after administration of methotrexate), calcium folinate is administered at a dose 150 mg iv every 3 hours until the plasma methotrexate level drops below 1 ?M, then at a dose of 15 mg iv every 3 hours, until the plasma methotrexate level drops below 0.05 ?M. Be sure to simultaneously hydrate and administer sodium bicarbonate (to prevent the development of renal failure).
In cases where severe toxic reactions are observed, calcium folinate treatment should be continued for an additional 24 hours (a total of 14 consecutive doses over 84 hours).
In megaloblastic anemia caused by folic acid deficiency, calcium folinate is prescribed at a dose of up to 1 mg / day.
Side effects of the digestive system
: when taken orally – nausea, vomiting (in this case, parenteral use is indicated).
Allergic reactions: urticaria, anaphylactic shock.
Drug interaction
Calcium folate acid reduces toxicity.
When used in high doses of calcium, folinate reduces the anticonvulsant effect of phenobarbital, phenytoin, primidone and increases the incidence of seizures in susceptible patients.
Calcium folinate enhances the antitumor and toxic effects of fluorouracil, especially on the gastrointestinal tract.
Storage conditions
Store in a dark place at a temperature not exceeding 25 ° C.
Expiration
3 years. The reconstituted solution is stored for 12 hours.
Deystvuyuschee substances
calcium folynat
