Introduction | calcium levofolinate is the calcium salt of levofolinic acid, and levofolinic acid is 5-formyltetrahydrofolic acid (I. E. Another form of the isomer, folinic acid dl body, that is, dl-LV, in vivo dl body can not be used, just to delay the metabolism of LV in the body, so that its long-term survival, and reduce the L body in vivo metabolic pathway, and weaken the effect of L body. |
Application | calcium folinate is a new anti-tumor drug, mainly used for the treatment of osteosarcoma after high-dose methotrexate treatment and folic acid antagonism related symptoms. Calcium levofolinate can also be used to treat giant cell anemia caused by folic acid deficiency, and can also be used in combination with fluorouracil to prolong survival or relieve symptoms in patients with advanced colon cancer. |
pharmacological action | calcium levofolinate is a biologically active substance of calcium folinate, and calcium folinate is tetrahydrofolate (THF) diastereomeric mixtures of the 5-formyl derivatives. Calcium folinate does not need to undergo reduction by dihydrofolate reductase and is directly involved in biological reactions using folic acid as a carrier for the transfer of one-carbon groups in vivo. Rapid metabolism of L-folinic acid (L-5 leucovorin) (followed by 5,10-methyltetrahydrofolic acid, 5,10-leucovorin tetrahydrofolic acid) was L-5-methyltetrahydrofolic acid. L-5-methyltetrahydrofolic acid can be metabolized to 5, 10-methylenetetrahydrofolic acid through other pathways, and 5, 10-methylenetetrahydrofolic acid is catalytically reduced by PDAH2 and NADPH coenzymes, irreversibly converted to 5-methyltetrahydrofolic acid. The use of folinic acid can counteract the therapeutic effects and toxicity of hydrochloric acid antagonists that inhibit dihydrofolate reductase, such as methotrexate. Calcium folinate can also enhance the efficacy and toxicity of fluoropyrimidines (e. G., 5-fluorouracil) in cancer therapy. The simultaneous use of folinic acid does not change the pharmacokinetic processes of 5-fluorouracil in plasma. 5-fluorouracil is metabolized in vivo to deoxyfluorouracil nucleotides, which bind to and inhibit thymidylate synthase, an enzyme important in DNA repair and replication. Folinic acid is easily converted into 5, 10-methylenetetrahydrofolic acid in vivo, which can stabilize the combination of deoxyfluorouracil nucleotide and thymidylate synthase, thereby enhancing the inhibitory effect on the enzyme, play a very important auxiliary role, the pharmacological effects of calcium levofolinate and calcium folinate the same, at the same time side effects much less than calcium folinate, |
dosage | add calcium levofolinate 100mg to 0.9% ml sodium chloride injection for 1 hour, the patient was then given 5-fluorouracil 375-425mg/m2 IV drip for 4-6 hours. |
biological activity | Calcium Levofolinate (Calcium Folinate, levocovorin calcium) is a Calcium salt of Folinic acid, it is an adjuvant for cancer chemotherapy. |