Calcium Folinate (Solution, Lyophilisate) Instructions for Use
ATC Code
V03AF03 (Calcium Folinate)
Active Substance
Calcium Folinate (Rec.INN registered by WHO)
Clinical-Pharmacological Group
Folic acid antagonists antidote
Pharmacotherapeutic Group
Vitamin, antidote to folic acid antagonists, biological response modifier of fluorouracil
Pharmacological Action
Calcium Folinate is an 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), promotes the restoration of nucleic acid biosynthesis and replenishes folic acid deficiency in the body.
Pharmacokinetics
It penetrates the blood-brain barrier. It 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 are higher with oral administration than with parenteral administration.
The average elimination half-life (T1/2) is 6 hours. It is excreted primarily by the kidneys.
Indications
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 cancer of the colon and rectum (in combination with fluorouracil).
ICD codes
| ICD-10 code | Indication |
| C18 | Malignant neoplasm of colon |
| C19 | Malignant neoplasm of rectosigmoid junction |
| C20 | Malignant neoplasm of rectum |
| D52 | Folate deficiency anemia |
| T45.1 | Poisoning by antineoplastic and immunosuppressive drugs |
| Y43.1 | Antineoplastic antimetabolites |
| Z51.5 | Palliative care |
| ICD-11 code | Indication |
| 2B90.Z | Malignant neoplasm of colon, unspecified |
| 2B91.Z | Malignant neoplasm of rectosigmoid junction, unspecified |
| 2B92.Z | Malignant neoplasm of rectum, unspecified |
| 3A02.Z | Folate deficiency anemia, unspecified |
| NE60 | Poisoning by drugs, medicaments or biological substances, not elsewhere classified |
| PL00 | Drugs, medicaments or biological substances causing injury or harm in therapeutic use |
| QB9B | Palliative care |
Dosage Regimen
| The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen. |
Solution, Lyophilisate
The dosage regimen of Calcium Folinate after high-dose intravenous infusions of methotrexate (12-15 g/m2 after 4 hours) is established individually, taking into account the state of renal excretory function, provided that the plasma concentrations of creatinine and methotrexate are systematically monitored (at least once a day).
With normal methotrexate elimination (plasma methotrexate level approximately 10 µM 24 hours after administration, 1 µM at 48 hours, and less than 0.2 µM at 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 late methotrexate elimination (methotrexate level above 0.2 µM at 72 hours and above 0.05 µM at 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 plasma methotrexate level falls below 0.05 µM.
With delayed early elimination of methotrexate from the body (methotrexate level of 50 µM and above at 24 hours, 5 µM and above at 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 intravenously every 3 hours until the plasma methotrexate level falls below 1 µM, then at a dose of 15 mg intravenously every 3 hours until the plasma methotrexate level falls below 0.05 µM. Simultaneous hydration and administration of sodium bicarbonate are mandatory (to prevent 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 over 84 hours).
For 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 with oral administration – nausea, vomiting (in this case, parenteral use is indicated).
Allergic reactions urticaria, anaphylactic shock.
Contraindications
Megaloblastic anemia caused by vitamin B12 deficiency, hypersensitivity to Calcium Folinate.
Use in Pregnancy and Lactation
If it is necessary to use Calcium Folinate during pregnancy, the intended benefit of therapy for the mother and the potential risk to the fetus should be carefully assessed.
If it is necessary to use during lactation, breastfeeding should be discontinued.
Use in Renal Impairment
Calcium Folinate should be used with caution in case of impaired renal function. Renal function and urine pH should be monitored before starting and during therapy.
Pediatric Use
When used in children, it should be borne in mind that Calcium Folinate may increase the frequency of seizures in predisposed patients, due to a decrease in the effectiveness of anticonvulsant drugs.
Special Precautions
During methotrexate treatment, in cases where clinical signs of toxicity or any abnormalities in laboratory parameters are noted, the possibility of an increase in plasma methotrexate concentration due to interaction with other drugs that impair methotrexate excretion or displace it from plasma albumin binding should be excluded.
Calcium Folinate should be used with caution in cases of acidic urine reaction, ascites, dehydration, exudative pleurisy, and impaired renal function. It should be taken into account that with nausea and vomiting, the absorption of Calcium Folinate may be impaired (parenteral administration is preferable).
Renal function and urine pH should be monitored before starting and during therapy.
In case of accidental methotrexate overdose, 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, due to a decrease in the effectiveness of anticonvulsant drugs.
Drug Interactions
Calcium Folinate reduces the therapeutic and toxic effects of folic acid antagonists.
When used in high doses, Calcium Folinate reduces the anticonvulsant effect of phenobarbital, phenytoin, primidone and increases the frequency of seizures in predisposed patients.
Calcium Folinate enhances the antitumor and toxic effects of fluorouracil, especially on the gastrointestinal tract.
Storage Conditions
Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.
Dispensing Status
Rx Only
Important Safety Information
This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.
Medical DisclaimerBrand (or Active Substance), Marketing Authorisation Holder, Dosage Form
Solution for intravenous and intramuscular administration 5 mg/ml
Solution for intravenous and intramuscular administration 10 mg/ml
Marketing Authorization Holder
PSK Pharma, LLC (Russia)
Dosage Forms
 |
Calcium Folinate PSK | Solution for intravenous and intramuscular administration 5 mg/ml |
| Solution for intravenous and intramuscular administration 10 mg/ml |
Dosage Form, Packaging, and Composition
Solution for intravenous and intramuscular administration
| 1 ml | |
| Calcium Folinate (calcium leucovorin) anhydrous | 5.4 mg, |
| In terms of folinic acid | 5 mg |
10 ml – vials – cardboard packs – Prescription only
10 ml – vials (10 pcs.) – cardboard packs – Prescription only
10 ml – vials (5 pcs.) – cardboard packs – Prescription only
3 ml – vials – cardboard packs – Prescription only
3 ml – vials (10 pcs.) – cardboard packs – Prescription only
3 ml – vials (5 pcs.) – cardboard packs – Prescription only
5 ml – vials – cardboard packs – Prescription only
5 ml – vials (10 pcs.) – cardboard packs – Prescription only
5 ml – vials (5 pcs.) – cardboard packs – Prescription only
Solution for intravenous and intramuscular administration
| 1 ml | |
| Calcium Folinate (calcium leucovorin) anhydrous | 10.8 mg, |
| In terms of folinic acid | 10 mg |
10 ml – vials – cardboard packs – Prescription only
10 ml – vials (10 pcs.) – cardboard packs – Prescription only
10 ml – vials (5 pcs.) – cardboard packs – Prescription only
3 ml – vials – cardboard packs – Prescription only
3 ml – vials (10 pcs.) – cardboard packs – Prescription only
3 ml – vials (5 pcs.) – cardboard packs – Prescription only
5 ml – vials – cardboard packs – Prescription only
5 ml – vials (10 pcs.) – cardboard packs – Prescription only
5 ml – vials (5 pcs.) – cardboard packs – Prescription only
Lyophilizate for the preparation of solution for intravenous and intramuscular injection 50 mg: fl. 1 or 5 pcs.
Marketing Authorization Holder
Belmedpreparaty RUP (Republic of Belarus)
Dosage Form
|
Calcium Folinate-Vial | Lyophilizate for the preparation of solution for intravenous and intramuscular injection 50 mg: fl. 1 or 5 pcs. |
Dosage Form, Packaging, and Composition
Lyophilizate for the preparation of solution for intravenous and intramuscular injection in the form of a porous mass from light yellow to yellow in color of heterogeneous color; hygroscopic.
| 1 vial | |
| Calcium folinate monohydrate | 55.9 mg, |
| Which corresponds to the content of folinic acid | 50 mg |
Excipients : methylparahydroxybenzoate.
Glass vials (1) – cardboard packs.
Glass vials (5) – cardboard packs.
Solution for intravenous and intramuscular administration 10 mg/1 ml: amp. 3 ml or 5 ml 5 or 10 pcs.
Marketing Authorization Holder
Lekpharm, SOOO (Republic of Belarus)
Dosage Form
|
Calcium Folinate-Lekpharm | Solution for intravenous and intramuscular administration 10 mg/1 ml: amp. 3 ml or 5 ml 5 or 10 pcs. |
Dosage Form, Packaging, and Composition
Solution for intravenous and intramuscular administration in the form of a transparent, colorless or light yellow liquid.
| 1 ml | |
| Calcium folinate hydrate (in terms of folinic acid) | 10 mg |
Excipients : sodium chloride, hydrochloric acid solution 1M/sodium hydroxide solution 1M, water for injection.
3 ml – dark glass ampoules (5) with a filling volume of 5 ml – contour cell packs (1) – cardboard packs.
3 ml – dark glass ampoules (5) with a filling volume of 5 ml – contour cell packs (2) – cardboard packs.
5 ml – dark glass ampoules (5) with a filling volume of 5 ml – contour cell packs (1) – cardboard packs.
5 ml – dark glass ampoules (5) with a filling volume of 5 ml – contour cell packs (2) – cardboard packs.
![Calcium Folinate [Solution, Lyophilisate] 1](https://www.medixlife.com/wp-content/uploads/Medixlife_favi_512.png "Calcium Folinate [Solution, Lyophilisate] 2")