Leucovorin calcium is used for the rescue of the toxicity reaction caused by excessive amount of aminopterin and methotrexate as well as being used for the treatment of giant red blood cell anemia.
Calcium folinate is an antidote for folic acid antagonistic drugs, also known as calcium folate, calcium folate, calcium aldehyde hydrofolate, ferrous acetic acid, calcium aluronate, calcium formyltetrahydrofolate, yellowish white to yellow crystal or amorphous powder at room temperature, odorless. Easily soluble in water, almost insoluble in ethanol or ether, easily soluble in sodium hydroxide solution. Calcium folinate is a reduced formylated derivative of folic acid. Its effect is similar to that of folic acid. It is an activated form of folic acid in the body. After entering the human body, it is converted into tetrahydrofolate by tetrahydrofolate reductase, which can effectively resist the toxic reaction caused by methotrexate. Calcium folinate has the toxic reaction of "rescuing" excessive folic acid antagonists in the body, which is beneficial to the synthesis of thymine nucleotides, DNA, RNA and even protein, and can stimulate the growth and maturation of white blood cells. This product can limit the damage degree of methotrexate to normal cells, through mutual competition, and can reverse the reaction of methotrexate to bone marrow and gastrointestinal mucosa, but has no effect on the existing neurotoxicity of methotrexate. Mainly used as an antidote for folic acid antagonists (such as methotrexate, methotrexate, phenytoin, phenobarbital, pyrimethamine or trimethoprim, etc.). When oral folic acid is not effective, it is used for stomatitis diarrhea, malnutrition, megaloblastic anemia caused by pregnancy or infancy, and leukopenia. However, it is not applicable to vitamin B12 deficiency anemia.
In recent years, calcium folinate has been used as an adjuvant treatment for colon and rectal cancer. Combined with fluorouracil, it can prolong survival.
