l-methyl folate

Action and Spectrum

Actions and spectrum: 

L-methylfolate is the active form of folate, which is a vitamin B that plays a crucial role in several metabolic pathways in the body. L-methyl folate is involved in the synthesis of DNA, RNA, and proteins, as well as in the production of neurotransmitters such as serotonin, dopamine, and norepinephrine. 

The main action of L-methyl folate is to provide the body with the necessary building blocks for the formation of new cells, especially in tissues with a high rate of turnover, such as bone marrow, skin, and the lining of the digestive tract. L-methyl folate also helps to maintain healthy levels of homocysteine, an amino acid that can be more harmful to CVS when present in high concentrations. 

L-methyl folate has been studied extensively in the treatment of depression, where it has been shown to be effective as an adjunct therapy for patients who do not respond well to traditional antidepressants. This is thought to be due to L-methyl folate’s role in the production of neurotransmitters, as well as its ability to reduce inflammation and oxidative stress in the brain. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Difficulty in concentrating 

Overactivity 

Confusion 

Anorexia 

Abdominal 

Flatulence 

Altered sleep patterns 

Irritability 

Excitement 

Impaired judgment 

Nausea 

Distention 

Bitter or bad taste 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Allergy or hypersensitivity: People who are allergic to L-methyl folate or any of its ingredients should not take this supplement. 
• Uncontrolled seizures: L-methyl folate may increase the risk of seizures in people with uncontrolled seizures or a history of seizures. 
• Vitamin B12 deficiency anemia: L-methyl folate may mask the symptoms of vitamin B12 deficiency anemia, which can lead to neurological damage if left untreated. 
• Methylmalonic acidemia: L-methyl folate may worsen symptoms of methylmalonic acidemia, a rare genetic disorder that affects the body’s ability to process certain proteins and fats. 
• Cobalamin hypersensitivity: Some people may have a rare hypersensitivity to cobalamin, which is a form of vitamin B12 that is sometimes used in combination with L-methyl folate. 
• Pregnancy and breast-feeding: While L-methyl folate is commonly used during pregnancy to reduce the risk of birth defects, it is important to consult with a doctor before taking any supplement during pregnancy or breastfeeding.

Caution: 

• Side effects: Common side effects of L-methyl folate include stomach upset, headache, and sleep disturbances. Rare but serious side effects include allergic reactions, breathing difficulty, and swelling of the face, tongue, lips, or throat. 
• Interactions: L-methyl folate may interact with certain medications, including those used to treat seizures, cancer, and depression. It may also interact with supplements such as vitamin B12 and SAMe. 
• Dosage: L-methyl folate is available in different strengths, and the appropriate dosage may vary depending on the individual’s age, health status, and reason for taking it. It is crucial to follow the dosage instructions carefully and not exceed the recommended dose without consulting a doctor. 
• Medical conditions: L-methyl folate may not be suitable for people with certain medical conditions, such as epilepsy, bipolar disorder, or kidney disease. People with these conditions should consult a doctor before taking L-methyl folate. 
• Pregnancy and breastfeeding: L-methyl folate is commonly used to reduce the risk of birth defects. However, it is essential to talk to a doctor before taking L-methyl folate during pregnancy or breastfeeding.

Comorbidities: 

• Epilepsy: L-methyl folate may increase the risk of seizures in people with epilepsy or a history of seizures. Therefore, people with epilepsy should consult with their doctor before taking L-methyl folate. 
• Bipolar disorder: L-methyl folate has been shown to improve depressive symptoms in people with bipolar disorder. However, there is a risk of inducing mania or hypomania, especially in people with a history of bipolar disorder or a family history of bipolar disorder. Therefore, people with bipolar disorder should be closely monitored by their doctor if they take L-methyl folate. 
• Cancer: L-methyl folate may interact with certain chemotherapy drugs used to treat cancer, which can reduce their effectiveness. Therefore, people with cancer should consult with their doctor before taking L-methyl folate. 
• Kidney disease: L-methyl folate is primarily excreted through the kidneys, and people with kidney disease may have reduced kidney function. Therefore, people with kidney disease should consult with their doctor before taking L-methyl folate and may require a lower dose. 
• Vitamin B12 deficiency: L-methyl folate may decrease the symptoms of vitamin B12 deficiency, which may lead to neurological damage if left untreated. Therefore, people with a history of vitamin B12 deficiency should consult with their doctor before taking L-methyl folate. 

Pregnancy / Lactation

Pregnancy consideration: US FDA pregnancy category: Not assigned 

Lactation: L-methylfolate is a naturally occurring form of folate that is found in breast milk.  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

L-methyl folate also plays a role in the methylation cycle, which is a biochemical pathway that regulates gene expression and other cellular processes. Methylation is the addition of methyl groups to a molecule, which can activate or deactivate certain genes. L-methyl folate is a donor of methyl groups and is involved in many methylation reactions throughout the body. 

L-methyl folate is often used as a supplement to treat depression, improve cognitive function, and reduce the risk of birth defects in pregnant women. It may also have benefits for other conditions, such as cardiovascular disease and peripheral neuropathy. However, the exact mechanisms by which L-methyl folate exerts its therapeutic effects are not fully understood and require further research.  

Pharmacodynamics: 

• Increases levels of neurotransmitters: L-methyl folate involves in the production of neurotransmitters, which are important for mood regulation, cognition, and other brain functions. By increasing levels of these neurotransmitters, L-methyl folate may have antidepressant and cognitive-enhancing effects. 
• Regulates gene expression: L-methyl folate is involved in the methylation cycle, which is a biochemical pathway that regulates gene expression and other cellular processes. By providing methyl groups, L-methyl folate can activate or deactivate certain genes, which may have a wide range of effects on the body. 
• Improves vascular function: L-methyl folate has been shown to improve vascular function by reducing oxidative stress and inflammation, increasing nitric oxide production, and enhancing endothelial cell function. These effects may be beneficial for conditions such as cardiovascular disease and peripheral neuropathy. 
• Reduces homocysteine levels: Homocysteine is an amino acid that is associated with an increased risk of cardiovascular disease and other conditions. L-methyl folate can reduce homocysteine levels by providing methyl groups for the conversion of homocysteine to methionine, which is a non-toxic amino acid. 
• Reduces risk of birth defects: L-methyl folate is commonly used during pregnancy to reduce the risk of birth defects such as neural tube defects. This is because L-methyl folate is involved in DNA synthesis and cell division, which are important for fetal development.

Pharmacokinetics: 

Absorption 

L-methyl folate is absorbed in the small intestine and enters the bloodstream. It is absorbed more efficiently than other forms of folate due to its active form. 

Distribution 

L-methyl folate is distributed throughout the body via the bloodstream and can cross the blood-brain barrier and enter the brain. 

Metabolism 

L-methyl folate is metabolized in the liver by a process called methylation, which involves the transfer of a methyl group to the folate molecule. The methylated form of L-methyl folate is then excreted in the urine. 

Elimination and excretion 

L-methyl folate is primarily excreted in the urine. The half-life of L-methyl folate is approximately 2.5 hours. 

Factors that can affect the ADME of L-methyl folate include age, gender, genetics, and the presence of certain medical conditions. 

Adminstartion

Administration: 

L-methyl folate is typically available as an oral tablet or capsule and can be taken with or without food. The recommended daily dosage varies on the specific condition being treated and the individual’s age, weight, and medical history. 

• Take with or without food: L-methyl folate can be taken with or without food, but it may be better absorbed when taken with a meal. 
• Swallow whole: Swallow the tablet or capsule whole with a glass of water. Do not crush or chew the tablet or capsule. 
• Store properly: Store L-methyl folate at room temperature, away from moisture and heat. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: L-methyl folate 

Pronounced: [ L-METH-il-FOE-late ]  

Why do we use L-methyl folate? 

• Depression: L-methyl folate is used as an add-on treatment for major depressive disorder in people who have a genetic variation that impairs their ability to convert folic acid to L-methyl folate. 
• Cardiovascular disease: L-methyl folate has been shown to reduce homocysteine levels, a risk factor for cardiovascular disease, in people with elevated levels. 
• Pregnancy: L-methyl folate is important for preventing birth defects in the developing fetus, and supplementation is recommended for women who are planning to conceive or who are pregnant. 
• Cognitive function: Some research suggests that L-methyl folate may improve cognitive function in patients with the mild cognitive impairment and Alzheimer’s disease. 
• Polycystic ovary syndrome (PCOS): L-methyl folate may improve insulin sensitivity and reduce oxidative stress in women with PCOS, a condition that affects hormonal balance and can lead to infertility.