Calcium folinate

Chemical properties

Light yellow to yellow solid

Originator

Leucovorin calcium,AstraZeneca

The Uses of Calcium folinate

Calcium folinate offsets the effects of folic acid antagonists that act by binding dihydrofolate reductase and blocking the conversion of folic acid to tetrahydrofolate. In medicine, calcium folinate is used after treatment with methotrexate to reduce the toxicity of the methotrexate. Calcium folinate is also used to enhance the cytotoxic effect of 5-fluorouracil in the treatment of cancer.

The Uses of Calcium folinate

antianemic, antidote to folic acid antagonists.
Calcium folinate (folinic acid, calcium leucovorin, tetrahydrofolate) can be used in the management of methotrexate overdose and to reduce the toxicity of high-dose methotrexate chemotherapy.Calcium folinate is a reduced form of folic acid, which bypasses the inhibition of dihydrofolate reductase by methotrexate.Calcium folinate also has a role in combination with fluorouracil in the treatment of bowel cancer, where its use enhances the effect of fluorouracil by inhibition of thymidilate synthase.

What are the applications of Application

Folinic acid calcium salt is a compound that reduces the effect of folic acid antagonists

Definition

ChEBI: Calcium folinate is a tetrahydrofolic acid.

Manufacturing Process

5,10-Methenyl-5,6,7,8-tetrahydrofolic acid, chloride hydrochloride dihydrate (20 g) was added in one portion to 100 ml water at 60°C followed by N,Ndiethylethanolamine (14.9 g) which adjusted the pH to 6. The mixture was maintained at reflux for 5 hours and the pH kept between 5.7 and 6.2 by addition of N,N-diethylethanolamine. The mixture was cooled, synthetic magnesium silicate (15 g) added and slurried, and filtered through celite and diluted with 40 ml SD3A (95% ethanol with 5% methanol). The filtrate was kept at -5°C for 16 hours, aqueous calcium chloride (4.0 g) was added dropwise to the cold filtrate, and the precipitate filtered, washed with SD3A (100 ml) and with ethyl acetate (100 ml) and dried under reduced pressure.

brand name

Wellcovorin (GlaxoSmithKline).

Therapeutic Function

Antidote (folic acid antagonists), Antianemic

General Description

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards.

Biochem/physiol Actions

Folinic acid serves as a cofactor and participates in one-carbon-transfer reactions. It helps in improving wound healing in rats. Folinic acid plays a major role in children with autism to enhance verbal communication.

Mechanism of action

The mechanism of action of Calcium folinate against cancer is to stabilise the complex between 5-FU and thymidylate synthase, thereby enhancing the cytotoxicity of 5-FU, a pyrimidine analogue and inhibitor of thymidylate synthase, which blocks DNA production. Thymidylate synthase converts deoxyuridine monophosphate to thymine monophosphate. Administration of 5-FU reduces deoxythymidine monophosphate, preventing DNA synthesis and leading to cell death.