L-methylfolate
L-methylfolate Uses, Dosage, Side Effects, Food Interaction and all others data.
L-methylfolate (INN) is the metabolite of folic acid (Vitamin B9) and it is a predominant active form of folate found in foods and in the blood circulation, accounting for 98% of folates in human plasma . It is transported across the membranes including the blood-brain barrier into various tissues where it plays an essential role in the DNA synthesis, cysteine cycle and regulation of homocysteine, where it methylates homocysteine and forms methionine and tetrahydrofolate (THF). Levomefolate is approved as a food additive and is designated a GRAS (generally regarded as safe) compound . It is available commercially as a crystalline form of the calcium salt (Metafolin(R)), which has the stability required for use as a supplement . Supplementation of levomefolic acid is desired over folic acid due to reduced potential for masking vitamin B12 deficiency symptoms.
L-methylfolate is an active metabolite of folic acid and a methyl group donor in one-carbon metabolism reactions. It regulates important cellular functions such as DNA biosynthesis, gene expression regulation, amino acid synthesis and metabolism, and myelin synthesis and repair. As a only form of folate that can cross the blood-brain barrier, it acts as a cofactor in the production of monoamine neurotransmitters such as dopamine, serotonin and norepinephrine . L-methylfolate is also involved in red blood cell formation .
| Trade Name | L-methylfolate |
| Generic | Levomefolic acid |
| Levomefolic acid Other Names | L-methylfolate, Levomefolate, Levomefolic acid, LMSR |
| Weight | 15mg, 7.5mg, 15mg, 7.5mg, 30mg |
| Type | Oral capsule, oral tablet, oral tablet, extended release |
| Formula | C20H25N7O6 |
| Weight | Average: 459.4558 Monoisotopic: 459.186631567 |
| Protein binding | Approximately 56% bound to plasma proteins |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
L-methylfolate is a folate supplement used to prevent neural tube defects in pregnancy or folate deficiency.
For the treatment and prevention of folate deficiency and for use as an antidote against folic acid antagonists. Contained in oral contraceptives to reduce the risk of neural tube defects arising from folic acid deficiency for pregnant women who conceived during use or shortly after the discontinuation of the product. Being studied for use as a treatment for cardiovascular diseases and adjunct therapy for patients undergoing antidepressant pharmacotherapy .
L-methylfolate is also used to associated treatment for these conditions: Nutritional supplementation
How L-methylfolate works
L-methylfolate plays a critical role in methylating homocysteines into methionine by acting as a methyl donor in a reaction catalyzed by vitamine B12-dependent methionine synthase. Homocysteine must either be further metabolized via transulfuration to become cysteine, taurine, and glutathione via a B6-dependent process, or re-methylated to become methionine again. Methionine formed from remethylation of homocysteine by levomefolic acid forms the downstream metabolite S-adenosylmethionine (SAMe), which is involved in numerous biochemical methyl donation reactions, including reactions forming monoamine neurotransmitters . Studies suggest that high plasma levels of homocysteine is associated with increased incidences of arterial plaque formation .
Toxicity
Overdose of levomefolic acid is unlikely to cause clinically significant adverse events.
Food Interaction
- Take with or without food. Recommendations vary from product to product - consult individual product monographs for additional information.
Volume of Distribution
Circulates in its free form or loosely bound to plasma proteins
Elimination Route
Absorbed in the proximal small intestines via the active proton-coupled folate transporter (PCFT) that transports both oxidized and reduced folic acids. Passive diffusion also occurs at the proximal and distal portions of the small intestines . A single oral dose of 906nmol of levomefolic acid in healthy females resulted in the mean peak plasma concentration of 39.4nmol/L .
Half Life
The mean elimination half-life is approximately 3 hours after 5mg of oral L-methylfolate, administered daily for 7 days [775].
Elimination Route
Mainly eliminated through renal or fecal excretion. Small proportion of excreted levomefolic acid is in unchanged form as over 99% of tissue folate is in polyglutamate form. Some portions of levomefolic acid is secreted into bile.
Innovators Monograph
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