Calcium folinate
English Synonyms: Folinic acid calcium salt; FOLINIC ACID, CALCIUM SALT UPS28; Calcium folinate, Leucovorine calcium; Folinic acid calcium salt> 97.5%; Calcium Folinate Hydrate; Calcium Leucoverin; 5-Formyl-5,6,7,8-tetrahydrofolic acid calcium salt, 5-HCO-H4PteGlu, Calcium folinate, Citrovorum factor calcium salt, Leucovorin calcium salt, 5-Formyl-5,6,7,8-tetrahydropteroyl-L-glutamic acid calcium salt; Folinic acid hydrate calcium salt
CAS number: 1492-18-8
Molecular formula: C20H21CaN7O7
Molecular weight: 511.5
EINECS No. 216-082-8
Related Categories: APIs; Antitumors for Research and Experimental Use; Biochemistry; API's; Research Reagents; Nutritional Studies; WELLCOVERIN; Antineoplastic Agents and Immunosuppressants; Plant Biochemical Extracts; Vitamins; Intermediates; APIs for APIs; Body; Small molecule inhibitors; Pharmaceutical raw materials
Mol file: 1492-18-8.mol
Leucovorin
Leucovorin properties
Form powder
CAS Database 1492-18-8 (CAS DataBase Reference)
Calcium folinate use and synthesis method
Folic acid antagonist antidote Calcium leucovorin folic acid antagonist drugs is also antidote, also known as Ca folium, melo folate, aldehyde folate calcium, acetic acid, calcium valerate, leucovorin, at room temperature Yellowish white to yellow crystalline or amorphous powder, odorless. Soluble in water, almost insoluble in ethanol or ether, soluble in sodium hydroxide solution. Calcium leucovorin is a folic acid-reduced formylated derivative that acts like folic acid and is the active form of folic acid in the body. Into the human body, through the tetrahydrofolate reductase into tetrahydrofolate, can effectively combat methotrexate-induced toxicity. Calcium leucovorin has the "rescue" toxic effects of folic acid antagonists in vivo, is conducive to thymine nucleotide, DNA, RNA and protein synthesis, can stimulate leukocyte growth and maturation. This product can limit the extent of damage methotrexate on normal cells, through mutual competition, and can reverse methotrexate on bone marrow and gastrointestinal mucosal response, but there is no effect on the methotrexate neurotoxicity . Mainly used as folic acid antagonists (such as methotrexate, methotrexate, phenytoin, phenobarbital, pyrimethamine or trimethoprim, etc.) antidote. When oral folic acid poor efficacy, for stomatitis, malnutrition, gestational or infancy-induced megaloblastic anemia and leucopenia. However, vitamin B12 deficiency anemia does not apply.
In recent years, the application of leucovorin as colon, rectal cancer adjuvant therapy, combined with the use of fluorouracil, prolong survival.
Intramuscular injection:
(1) moderate anti-folate metabolism drugs, 1 6 ~ 12mg, once every 6 hours, a total of 4 times.
(2) Megaloblastic anemia: 1mg on the 1st, 1st on the 1st.
(3) leukopenia: each 3 ~ 6mg, 1 day. Intravenous drip: Anti-folic acid metabolism drug poisoning: 75mg drip completed within 12 hours, then changed to intramuscular injection. Adverse reactions are rare, occasionally rash, hives or asthma and other allergic reactions. Aciduria (pH <7), ascites, dehydration, gastrointestinal obstruction, pleural effusion or renal dysfunction in patients with caution.
Calcium leucovorin oral absorption, 1.72h ± 0.8h serum reduced folic acid peak; intramuscular injection 0.71h ± 0.09h peak. Serum folic acid folic acid t1 / 2 after intramuscular injection of 3.5h. Whether oral or intramuscular injection can be maintained 3 ~ 6h. The role of the liver and intestinal mucosa metabolism of 5-methyltetrahydrofolate, oral more than intramuscular injection of metabolism. 80% to 90% of renal excretion, a small amount of discharge with the feces.