Calcium folinate for injection

Folinic acid is a mixture of diastereoisomers of the 5-formyl derivative of tetrahydrofolate (THF), and its biologically active substance is the levorotatory isomer called levofolinic acid. Folinic acid does not need to be reduced by dihydrofolate reductase and directly participates in biological reactions that use folic acid as a carrier for transferring "one-carbon groups" in the body. L-folinic acid (L-5-formyltetrahydrofolate) is rapidly metabolized (in order to 5,10-methyltetrahydrofolate and 5,10-folinic tetrahydrofolate) to L-5-methyltetrahydrofolate. L-5-methyltetrahydrofolate can be metabolized to 5,10-methylenetetrahydrofolate through other pathways, and 5,10-methylenetetrahydrofolate is irreversibly converted to 5-methyltetrahydrofolate through catalytic reduction by PDAH2 and NADPH coenzymes. The use of folinic acid can counteract the therapeutic effects and toxicity of hydrochloride antagonists (such as methotrexate) that inhibit dihydrofolate reductase. Folinic acid can enhance the efficacy and toxicity of fluoropyrimidines (such as 5-fluorouracil) in tumor treatment. The simultaneous use of folinic acid does not seem to change the pharmacokinetic process of 5-fluorouracil in plasma. 5-Fluorouracil is metabolized into deoxyfluorouracil nucleotides in the body, which bind to and inhibit thymidylate synthase (an enzyme that is very important in DNA repair and replication). Folinic acid is easily converted into 5,10-methylenetetrahydrofolate in the body, which can stabilize the binding of deoxyfluorouracil nucleotides to thymidylate synthase, thereby enhancing the inhibitory effect on the enzyme. Toxicological studies Reproductive toxicity studies in rats and rabbits showed that calcium folinate was not embryotoxic at a dose of at least 50 times that of humans.

The main ingredient of this product is calcium folinate, and its chemical name is (-)-N-[4[[[(6S)-2-amino-5-formyl-1,4,5,6,7,8-hexahydro-4-oxo-6-pterydinyl]methyl]amino]benzoyl]-L-glutamic acid calcium salt pentahydrate. Its auxiliary material is mannitol.

Used in combination with 5-fluorouracil for the treatment of gastric cancer and colorectal cancer.

Calcium folinate 100 mg was added to 100 ml of 0.9% sodium chloride injection and intravenously dripped for 1 hour, followed by intravenous drip of 5-fluorouracil 375-425 mg/m2 for 4-6 hours.

In foreign clinical studies, 63 patients with gastric cancer and 47 patients with colorectal cancer used this product. The results showed that the adverse reactions of this product included nausea, vomiting (86.36%), sensory neurotoxicity (51.82%), diarrhea (22.73%), hair loss (10.00%), motor neurotoxicity (3.64%), oral mucositis (2.73%), and fever (1.82%). The above adverse reactions are mainly grade I and grade II. Grade III adverse reactions include nausea, vomiting, fever and sensory neurotoxic reactions. Laboratory abnormalities mainly include leukopenia, neutropenia, decreased hemoglobin, decreased platelets, increased total bilirubin, increased alanine aminotransferase, aspartate aminotransferase, and increased BUN and Cr. Foreign clinical trials have shown that this product

1. Patients with severe bone marrow suppression; 2. Patients with diarrhea; 3. Patients with severe infection; 4. Patients with pleural effusion and ascites; 5. Patients with severe heart disease or a history of it; 6. Patients with worsening systemic condition; 7. Patients with a history of severe allergy to the ingredients of this product or fluorouracil; 8. Patients who have been used in combination with tegafur or within 7 days after stopping use. Refer to the (drug interactions) item.

(1) Drugs that cannot be used in combination Drug name Clinical symptoms, treatment methods Mechanism, risk factors Tegafur may cause early severe hematological toxicity and gastrointestinal reactions such as diarrhea and oral endocarditis, so they cannot be used at the same time. They cannot be used at the same time for at least 7 days. It hinders the catabolism of fluorouracil, and the blood fluorouracil level is significantly increased. (2) Precautions for combined use Drug name Clinical symptoms, treatment methods Mechanism, risk factors Phenytoin sometimes causes language disorders, movement disorders, impaired consciousness and other symptoms of phenytoin poisoning. The mechanism is unknown. Fluorouracil can increase the blood concentration of phenytoin Potassium Benzylpropionate Coumarin Potassium Fluorouracil sometimes enhances the action of potassium Benzylpropionate Coumarin The mechanism is unknown Other chemotherapy and radiotherapy sometimes enhance hematological toxicity and gastrointestinal reactions Adverse reactions

Keep away from light, tightly closed and in a dry place.

0.15g (based on folinic acid)

Guangdong Lingnan Pharmaceutical Co., Ltd.

• Founded in:

  1991-04-12

• Address:

  No. 5, Muxi 8th Road, Xilian Town, Wujiang District, Shaoguan City

• Tax NO.:

  91440000190333956C

• Registered Funds:

  11.38 million yuan

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