2010/06/11

Calcium folinate

The international name:
Folinat Calcium (Calcium folinate)

Group Affiliation:
Vitamin

Description of the active substance (INN):
Calcium folinat

Dosage form:
capsule lyophilisates for solution for intravenous and intramuscular injection, solution for intravenous and intramuscular injection, tablets

Mode of action:
Folinievaya acid, which is a reduced form of folic acid is easily converted into other recovered derivatives of folic acid (dihydro-and then to tetrahydrofolic) required for synthesis of thymine and purines and, hence, DNA, RNA and proteins. Contributes to the shortfall in the body of folic acid. Has hematopoietic action, stimulates growth of tissues quickly updated (including the mucosa of the gastrointestinal tract). As an antidote to folic acid antagonist, prevents the damage of bone marrow hematopoiesis provides safety and allows the use of cytostatics, including methotrexate and 5-fluorouracil required for tumor chemotherapy with high doses. The initial effect develops in 20-30 minutes after ingestion, after 10-20 minutes - after i / m administration, less than 5 minutes - after i / v administration and lasts for 3 - 6 h regardless of route of administration.

Indications:
Oral and parenteral administration - intoxication folic acid antagonists (methotrexate, trimethoprim and pyrimethamine). Parenteral - megaloblastic anemia against a background of folic acid deficiency when oral therapy is ineffective (including against the background of malabsorption syndrome, malnutrition, pregnancy, sprue, in early childhood with congenital dihydrofolate reductase deficiency). Cancer of the large intestine, including the rectum (as adjuvant). Local - ulcer-necrotic stomatitis on a background of metotreksatae

Contraindications:
Hypersensitivity, megaloblastic anemia caused by vitamin A deficiency B12.C caution. Predisposition to the development of epileptic seizures in children with chronic renal failure.

Side effects:
Allergic reactions: skin rash, hives, itching and anaphylactic shock.

Dosage and administration:
V / m, in / in, inside (hereinafter all doses of calcium folinata given in terms of base). After i / v infusion of methotrexate in high doses (12-15 g / sq m) and multiple dose administration of calcium folinata determined by the state renal excretory function in a systematic (at least 1 time per day) control the concentration of creatinine and methotrexate in plasma. In the normal breeding (the concentration of methotrexate in plasma - approximately 10 mmol 24 h after injection, 1 mmol - 48 hours and less than 0.2 mmol - 72 hrs), calcium folinat prescribe a dose of 15 mg (approximately 10 mg / m) inside , in / or / m every 6 h for 60 h (starting 24 hours after methotrexate). In the case of reducing "late" removal (methotrexate concentration above 0.2 mmol - 72 hrs and 0.05 micromol - after 96 hours after introduction) - inside, in / m or i / c, 15 mg every 6 h up to as long as the concentration of methotrexate does not become lower than 0.05 mmol. In "early" decline excretion (concentration of methotrexate - 50 uM and above 24 h , 5 uM and above - 48 hours or increase the content of creatinine in plasma by 100% or more within 24 hours after methotrexate) - a / c, a dose of 150 mg every 3 h up to as long as the concentration of methotrexate to be below 1 uM, and then - I / O and 15 mg every 3 hours until the concentration of methotrexate in plasma becomes lower than 0.05 mmol. At the same time to prevent the development of CRF spend hydration (3 l / day) and injected sodium bicarbonate to maintain pH urine at a level 7 or higher. With the development of toxic reactions expressed by the introduction of methotrexate should be extended for an additional 24 h in subsequent courses (total number - 24 doses within 84 h). In case of accidental overdose of methotrexate calcium folinat injected immediately after an overdose (or slow breeding methotrexate - within 24 hours) in / in / m or oral (expressed in gastrointestinal events apply only to parenteral administration) to 10 mg / m every 6 hours until methotrexate level becomes less than 0.01 uM. Determination of the concentration of creatinine and methotrexate should be carried out every 24 h. When 24 h creatinine content in plasma increased by 50% or the concentration of methotrexate than 5 uM, or the concentration of methotrexate after 48 h more than 0.9 uM, calcium folinat injected into / in a dose of 100 -150 mg / m every 3 h up to as long as the concentration of methotrexate in plasma becomes lower than 0.01 mmol. When ulcer-necrotic stomatitis during treatment with methotrexate - locally, at the ulcerated surface of the oral mucosa (avoid swallowing the solution for injection). In megaloblastic anemia, deficiency of folic acid - inside the / m or i / v, 1 mg / day. In cancer, colon and rectum - in / slowly, for not less than 3 min, 200 mg / m, followed by a / in the introduction of fluorouracil at a dose of 370 mg / m or i / v, 20 mg / m, followed by a / in the injection of fluorouracil at a dose of 425 mg / sqm. The course of treatment - 1 times a day for 5 days. Repeated courses are held at intervals of 4 weeks for 2 courses, then - at intervals of 4-5 weeks, depending on the toxic effect of the previous year. When the manifestation of hematological or gastrointestinal toxicity of fluorouracil to reduce the dose (at a moderate toxicity in 20%, with severe - 30%). When tolerance to fluorouracil in the previous course of its dose should be increased. In the absence of toxicity from the previous year dose increased by 10%. The dose of calcium folinata depending on the toxicity does not change.

Cautions:
When using large doses dissolved with sterile water for injection (a solution not be stored). The prepared solution should be used within 12 hours Do not use the medication in pernicious and other megaloblastic anemia due to deficiency of cyanocobalamin, because during treatment, along with improved haematological parameters, neurological phenomena continue to progress. may increase the frequency of epileptic seizures in children prone to them due to reduce the effect of antiepileptic drugs (phenytoin and primidona). Doses above 25 mg should be given by injection, as ingestion doses are not absorbed.

Interactions:
Reduces the effect of folic acid antagonists. Reduces toxic effect of methotrexate, anticonvulsant activity of phenobarbital, phenytoin and primidona. Strengthens the toxicity of fluorouracil.