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• Description

  Levomefolate calcium also called Calcium L-5-methyltetrahydrofolate belongs to the folic acid family of vitamins (vitamin B9, folic acid), which is a coenzyme form of folic acid. Calcium L-5-methyltetrahydrofolate (5-mthf) is a salt-forming methyl derivative form naturally produced by folic acid. 5-mthf is also known as L-methylfolate. It is the most biologically active and functional folic acid. In calcium salt form, it is easier to absorb than ordinary folic acid.
  
  Levomefolate calcium is a stable salt of the naturally occurring form of folates and is the predominant folate form in foods.
  Levomefolate is the calcium salt of 5-methyltetrahydrofolic acid, a biologically active form of folic acid that functions, in conjunction with Vitamin B12, as a methyl-group donor involved in the conversion of homocysteine to methionine.The availability of methyl groups is essential for a variety of methylation reactions including the synthesis of DNA and proper neural tube closure. Levomefolate is included in formulations of certain oral contraceptives to ensure adequate folic acid levels in women of child-bearing age to reduce the risk of neural tube defects. The combination of levomefolate and oral contraceptives increases folic acid levels.;

• Function

  Folic acid from Levomefolate calcium(Calcium L-5-Methyltetrahydrofolate) will reduce the ability of cells to synthesize and repair DNA. Supplementing folic acid may be a more advantageous way to increase folic acid to reduce homocysteine levels, and support normal cell proliferation, vascular endothelial function. Cardiovascular disease, nervous system function, Especially supplementing 5-MTHF(Calcium L-5-Methyltetrahydrofolate) during pregnancy has been shown to reduce the risk of neural tube malformations and recurrence.;

• Metabolic pathways

  Ordinary folic acid must be converted to L- methylfolate to participate in the two main metabolic pathways: methylation process and DNA synthesis. The only form of free folic acid that usually appears in human plasma and cells is 5-mthf. Lack of folic acid is usually due to lack of vitamins, which leads to insufficient intake. During pregnancy, breastfeeding, and children's growth, the need for folic acid is increased.;

• Mechanism of Action

  The  biochemical pathways of folic acid involves a series of enzymatic reactions and cofactors. The absorbed folic acid is reduced and methylated to 5-MTHF(Calcium L-5-Methyltetrahydrofolate) during the metabolism of intestinal mucosal cells. This transformation is limited and does not change the appearance of folic acid in the blood circulation. The heavy amino acid is then converted to s-adenosylmethionine (SAMe), and the methyl donor is involved in a number of biochemical processes. It can also be used as a donor to participate in the synthesis of nucleotides and support biosynthesis of DNA.;

• Pharmacokinetics

  Absorption:
  Orally administered levomefolate calcium is absorbed rapidly and is incorporated into the body folate pool. Peak plasma concentrations of about 50 nmol/l above baseline are reached within 0,5 to 1,5 hours after single oral administration of 0,451 mg levomefolate calcium.
  Distribution:
  Biphasic kinetics is reported for folates with a fast- and a slow-turnover pool. The fast-turnover pool probably reflecting newly absorbed folate is consistent with the terminal half-life of approximately 4 to 5 hours after single oral administration of 0,451 mg levomefolate calcium. The slow-turnover pool reflecting turnover of folate polyglutamate has a mean residence time of greater than or equal to 100 days. Exogenous folate and an enterohepatic folate cycle help to maintain a constant supply of L-5-methyl-THF.
  Elimination: L-5-methyl-THF is eliminated from the body by urinary excretion of intact folates and catabolic products as well as faecal excretion through a biphasic kinetics process. A rapid decline in urinary and faecal concentration of folates and their catabolites with a half-life of several hours is followed by a long decline with a half-life of about 100 to 360 days.
  Steady-state conditions: Steady-state conditions for L-5-methyl-THF in plasma after intake of 0,451 mg levomefolate calcium are reached after about 8 to 16 weeks depending on the baseline levels. In red blood cells achievement of steady-state is delayed due to the long life-span of red blood cells of about 120 days.
  https://www.bayer.com/sites/default/files/YASMIN_PLUS_EN_PI.pdf;

• Uses

  • Mainly for folic acid antagonists (such as methotrexate, pyrimethamine, benzyl cefalexin and trimethoprim) antidote, it's usually used for prevention of methotrexate dose or overdose treatment caused severe toxic effects.
  • Folic acid treatment of the following diseases, such as inflammatory diarrhea and protein-energy malnutrition (poor nutrition), pregnancy or infancy megaloblastic anemia caused by poor.
  • As adjuvant therapy for colon cancer, rectal cancer.
  • Combined with 5-FU and treatment of digestive tract tumors or other 5-FU-sensitive tumors. High-dose CF used in conjunction with 5-FU (LF), the basic programme is currently the treatment of colon and rectal cancer.
  • For children with leukemia, lymphoma, and osteosarcoma, such as high dose MTX treatment when rescued.  
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• Folic Acid Supplement

  Folic acid is the man-made form of folate. Folate is a B-vitamin naturally found in some foods. It is needed to form healthy cells, especially red blood cells. Folic acid supplements may come in different forms (such as L-methylfolate, levomefolate, methyltetrahydrofolate). They are used to treat or prevent low folate levels. Low folate levels can lead to certain types of anemia. Conditions that can cause low folate levels include poor diet, pregnancy, alcoholism, liver disease, certain stomach/intestinal problems, kidney dialysis, among others. Women of childbearing age should receive adequate amounts of folic acid either through their diet or supplements to prevent infant spinal cord birth defects. The calcium salt of Levomefolate calcium which belongs to the group of folate vitamins (Vitamin B9, Folacin). It is a coenzymated form of folic acid and a more bioavailable alternative in dietary supplements.

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