Usage
- L-Methylfolate Calcium is prescribed as a medical food for the distinct nutritional requirements of individuals with conditions like major depressive disorder (MDD) and schizophrenia, particularly those experiencing negative symptoms or cognitive impairment. It’s also used to address hyperhomocysteinemia (high homocysteine levels). It is often used adjunctively with antidepressants in MDD and with antipsychotics in schizophrenia.
- Pharmacological Classification: Metabolic Agent, Medical Food.
- Mechanism of Action: L-Methylfolate is the biologically active form of folate (vitamin B9). It plays a crucial role in various metabolic processes, including DNA synthesis, cell division, and neurotransmitter synthesis. It’s essential for the conversion of homocysteine to methionine, thereby reducing homocysteine levels. It is readily utilized by the body, bypassing the metabolic steps required for folic acid conversion.
Alternate Names
- Levomefolate Calcium
- (6S)-5-methyltetrahydrofolate calcium salt
- (6S)-5-MTHF-Ca
- Metafolin® (a common, but not universal, brand name for L-methylfolate, not specific to the calcium salt form. The calcium salt form is less common than other forms of L-methylfolate such as the glucosamine salt.)
How It Works
- Pharmacodynamics: L-Methylfolate participates in one-carbon metabolism, essential for DNA synthesis, repair, and methylation. It facilitates the synthesis of purines and pyrimidines (building blocks of DNA and RNA). It aids in neurotransmitter synthesis by acting as a cofactor for enzymes involved in these processes.
- Pharmacokinetics: Administered orally, L-Methylfolate is absorbed from the gastrointestinal tract. Being the active form of folate, it doesn’t require metabolic conversion. It crosses the blood-brain barrier, making it effective in addressing neurological conditions. Elimination pathways are primarily renal.
- Mode of Action: As a substrate for various enzymes including dihydrofolate reductase (DHFR) and thymidylate synthase (TS), L-Methylfolate is involved in cellular pathways producing DNA and RNA.
- Receptor Binding, Enzyme Inhibition or Neurotransmitter Modulation: L-Methylfolate does not directly bind to receptors. It acts as a cofactor for enzymes involved in amino acid metabolism and neurotransmitter synthesis, thereby indirectly modulating neurotransmitter activity.
Dosage
Standard Dosage
Adults:
- 7.5 mg to 15 mg orally once daily, with or without food. The dosage is often determined by the underlying condition and response to therapy.
Children:
- Safety and efficacy not established in pediatric population below 18 years.
Special Cases:
- Elderly Patients: No specific dosage adjustments are generally required.
- Patients with Renal Impairment: Dose adjustments may be needed, but specific guidelines are limited.
- Patients with Hepatic Dysfunction: Dose adjustments may be needed, but specific guidelines are limited.
- Patients with Comorbid Conditions: Use with caution in bipolar disorder. Screen for B12 deficiency.
Clinical Use Cases
- L-Methylfolate is a dietary supplement. The provided sources did not mention dosing recommendations for procedures such as intubation, surgery, or mechanical ventilation in the context of L-methylfolate use.
Dosage Adjustments
- Dose modifications should be individualized based on the patient’s clinical condition, response to therapy, and the presence of renal or hepatic impairment. Genetic testing for MTHFR polymorphism may inform dosage decisions in specific cases.
Side Effects
Common Side Effects
- Allergic reactions (rash, hives, itching, swelling, difficulty breathing)
- Nausea
- Abdominal distension
- Flatulence
- Sleep disturbances
- Irritability
- Anxiety
- Confusion
- Impaired Judgement
Rare but Serious Side Effects
- Severe allergic reactions (anaphylaxis)
Long-Term Effects
- No specific long-term adverse effects reported in current sources.
Adverse Drug Reactions (ADR)
- No specific ADRs were found in the provided sources.
Contraindications
- Hypersensitivity to L-Methylfolate Calcium or any of its components.
Drug Interactions
- Antiepileptic drugs (e.g., phenytoin, carbamazepine, primidone, valproic acid)
- Capecitabine
- Dihydrofolate Reductase Inhibitors (DHFRIs)
- Methotrexate
Pregnancy and Breastfeeding
- Pregnancy: Generally considered safe when used as directed. However, high doses should only be used under the supervision of a healthcare professional.
- Breastfeeding: Generally considered safe when used as directed.
Drug Profile Summary
- Mechanism of Action: Active form of folate, involved in one-carbon metabolism, DNA synthesis, neurotransmitter synthesis, and homocysteine reduction.
- Side Effects: Allergic reactions, gastrointestinal issues, sleep disturbances, mood changes.
- Contraindications: Hypersensitivity.
- Drug Interactions: Antiepileptics, capecitabine, DHFRIs, Methotrexate.
- Pregnancy & Breastfeeding: Generally safe when used as directed.
- Dosage: Adults: 7.5mg - 15 mg/day, with/without food; Children: Not established.
- Monitoring Parameters: Homocysteine levels, B12 levels, mood changes.
Popular Combinations
- Often combined with antidepressants in MDD.
- Used adjunctively with antipsychotics in schizophrenia.
- May be combined with other B vitamins.
Precautions
- Screen for B12 deficiency before and during treatment.
- Use with caution in patients with a history of bipolar disorder.
- Monitor for mood changes, particularly mood elevation.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for L-Methyl Folate Calcium?
A: The usual adult dose is 7.5mg - 15mg once daily, taken with or without food.
Q2: Is L-Methylfolate Calcium different from folic acid?
A: Yes. While folic acid is the synthetic form of folate, L-Methylfolate is the biologically active form, requiring no metabolic conversion.
Q3: Can L-Methylfolate Calcium mask a B12 deficiency?
A: Yes, similar to folic acid, high doses of L-Methylfolate Calcium can mask the hematological symptoms of B12 deficiency, while the neurological manifestations may progress.
Q4: How does L-Methylfolate Calcium impact patients with schizophrenia?
A: It helps reduce homocysteine levels and may improve negative symptoms and cognitive function when used as an adjunct to antipsychotic medications.
Q5: Are there specific precautions for pregnant or breastfeeding women using L-Methylfolate Calcium?
A: While generally considered safe, consulting a doctor before use is always recommended. The appropriate dosage should be determined and overseen by a healthcare professional.
Q6: What are the signs of an allergic reaction to L-Methylfolate Calcium?
A: Signs may include rash, hives, itching, swelling (especially of the face, tongue, or throat), dizziness, and difficulty breathing. Seek immediate medical attention if these symptoms occur.
Q7: Can L-Methylfolate Calcium be used in children?
A: Safety and efficacy in children below 18 years have not been established.
Q8: How does L-Methylfolate calcium interact with other medications?
A: L-Methylfolate calcium has been documented to interact with some medications, particularly anti-epileptics, dihydrofolate reductase inhibitors (DHFRIs), and certain chemotherapy agents. Consult a medical professional for a full list of drug interactions.
Q9: What are the key monitoring parameters for patients on L-Methylfolate Calcium?
A: Monitoring homocysteine levels and vitamin B12 levels is essential, as well as monitoring changes in mood and behavior. Regular medical checkups are recommended.
