Calcium folinate
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Clinical Pharmacology
Antidote to 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 to restore the biosynthesis of nucleic acids and compensates for the lack of folic acid in the body.
Pharmacokinetics
Gets through the BBB. Accumulates in the liver. 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 administered orally than when administered parenterally. T1/2 averages 6 hours. Excreted mainly by the kidneys.
Indications
- Prevention and treatment of the toxic effect of methotrexate, an overdose of folic acid antagonists.
- Treatment of megaloblastic anemia caused by a folic acid deficiency.
- Palliative treatment of colon and rectal cancer (in combination with fluorouracil).
Composition
1 bottle contains:
Active substances: calcium folinat 25 mg.
Solvent: rr sodium chloride 0.9% - 2 ml.
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Dosage and Administration
Dosing regimen of calcium folinate after intravenous infusion of methotrexate in high doses (12-15 g / m2 after 4 h) set individually, taking into account the state of renal excretory function, subject to the systematic (at least 1 time / day) control of plasma creatinine and methotrexate concentrations.
With normal removal of methotrexate (the level of methotrexate in plasma is approximately 10 μM after 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, intravenously or intramuscularly every 6 hours for 60 hours (10 doses, starting 24 hours after the start of methotrexate administration).
With delayed removal of methotrexate (the level of methotrexate is higher than 0.2 μM after 72 hours and higher than 0.05 μM after 96 hours after administration) calcium folinate is continued to be administered at a dose of 15 mg orally, IV or intramuscularly every 6 hours until the level plasma methotrexate will not fall below 0.05 μM.
With slow early clearance of methotrexate from the body (the level of methotrexate 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 administration of methotrexate) calcium folinate is administered at a dose of 150 mg IV every 3 h until plasma methotrexate level drops below 1 μM, then at a dose of 15 mg IV every 3 h until plasma methotrexate level drops below 0.05 μM. It is necessary to simultaneously conduct hydration and the introduction of sodium bicarbonate (for the prevention of the development of renal failure).
In cases where severe toxic reactions are observed, treatment with calcium folinate should be continued additionally, for another 24 hours (a total of 14 consecutive doses in 84 hours).
With megaloblastic anemia caused by folic acid deficiency, Calcium folinate is prescribed at a dose of up to 1 mg / day.
Adverse reactions
From the digestive system: ingestion - nausea, vomiting (in this case, parenteral administration 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 action 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 digestive tract.
Pregnancy and Lactation
If necessary, the use of calcium folinata during pregnancy should carefully assess the intended benefit of therapy for the mother and the potential risk to the fetus.
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 plasma due to interaction with other drugs that violate the removal of methotrexate or displacing it from plasma albumin should be excluded.
Calcium folinate is used with caution in acidic urine reactions, ascites, dehydration, exudative pleurisy, and impaired renal function. It should be borne in mind that with nausea and vomiting, absorption of calcium folinate may deteriorate (it is preferable to use parenteral administration).
Before and during the therapy, the kidney function, urine pH should be monitored.
In case of an accidental overdose of methotrexate, calcium folinate intake 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 susceptible patients, by reducing the effectiveness of anticonvulsants.
- Brand name: Leucovorin-LENS
- Active ingredient: Calcium folinate
- Dosage form: Lyophilisate for preparation of solution for IV and IM introductions.
- Manufacturer: Lance farm
- Country of Origin: Russia
Studies and clinical trials of Calcium folinate (Click to expand)
- LC–MS characterization of trace impurities contained in calcium folinate
- Two cases of severe liver injury possibly related to 5-fluorouracil and calcium folinate
- Pharmacokinetic and pharmacodynamic comparison of two doses of calcium folinate combined with continuous fluorouracil infusion in patients with advanced colorectal cancer
- Disposition of 5-formyl- and 5-methyltetrahydrofolic acid in serum after i.v. bolus of calcium folinate: pharmacokinetic drug interaction with preadministered interferon-alpha-2b
- Protective effect of calcium folinate against methotrexate-induced endosalpinx damage in rats
- Adjuvant intraperitoneal chemotherapy with cisplatinum, mitoxantrone, 5-fluorouracil and calcium folinate in stage II–III gastric cancer
- Tegafur/Uracil + Calcium Folinate in Colorectal Cancer
- Calcium folinate + fluorouracil in advanced colorectal cancer
- Simultaneous determination of methotrexate and calcium folinate with electrochemical method based on a poly-ABSA/functionalized MWNTs composite film modified electrode
- Vincristine overdose in a cat: clinical management, use of calcium folinate, and pathological lesions
- Anaphylactic Reaction During a Folfox Scheme Administration Secondary To Calcium Folinate: A Case Report
- Pharmacokinetics of folinic acid and 5-methyltetrahydrofolic metabolite after repeated oral administration of calcium folinate following methotrexate treatment
- Fluorouracil/calcium folinate
- Fluorouracil + calcium folinate enhances QOL in colorectal cancer
- The antineoplastic regimen etoposide, calcium folinate [leucovorin] and fluorouracil (ELF) is too costly
- Calcium folinate/fluorouracil
- Fluorouracil see Calcium folinate/fluorouracil
- QOL with vinorelbine vs fluorouracil/ calcium folinate in NSCLC
- Hypereosinophilia Caused by Calcium Folinate
- Calcium folinate see Fluorouracil/calcium folinate
- Fluorouracil/calcium folinate
- Calcium folinate see Fluorouracil/calcium folinate
- Fluorouracil/calcium folinate