Usage
L-Methyltetrahydrofolate Calcium, the calcium salt of the biologically active form of folate (vitamin B9), is prescribed for the clinical dietary management of metabolic imbalances associated with conditions like depression and schizophrenia. It’s also used to treat folate deficiency, which can lead to anemia. It’s classified as a medical food and sometimes as a dietary supplement, meaning it’s intended to be used under medical supervision to address specific nutritional deficiencies.
L-Methylfolate is crucial for numerous bodily functions, including DNA synthesis, cell division, and red blood cell formation. Unlike folic acid, which must be converted to L-methylfolate before the body can use it, L-methylfolate is readily available for use, making it particularly beneficial for individuals with certain genetic variations who may have difficulty converting folic acid efficiently.
Alternate Names
- Levomefolate calcium
- L-5-MTHF-Ca
- (6S)-5-methyltetrahydrofolic acid, calcium salt
- Metafolin (brand name)
- Deplin (brand name)
How It Works
Pharmacodynamics: L-Methyltetrahydrofolate is involved in single-carbon transfer reactions necessary for a variety of metabolic processes, including nucleotide biosynthesis, amino acid metabolism, and methylation reactions. It supports the synthesis of DNA, RNA, and neurotransmitters, thereby playing a role in cell growth and function, as well as nerve health.
Pharmacokinetics:
- Absorption: L-Methylfolate is absorbed in the small intestine and is not dependent on the enzyme dihydrofolate reductase for its activity, unlike folic acid.
- Metabolism: It’s the active form of folate and doesn’t require metabolic conversion for utilization.
- Elimination: L-Methylfolate is primarily excreted in the urine, with a smaller fraction in the bile.
Mode of Action: L-Methylfolate acts as a cofactor in several enzymatic reactions crucial for cell function and growth. Its role is in transferring single carbon units, essential for DNA synthesis and other metabolic processes. It can modulate neurotransmitter synthesis, affecting levels of serotonin, dopamine, and norepinephrine, which may be relevant to its use in depression.
Dosage
Standard Dosage
Adults: The typical dosage is 7.5mg to 15mg daily, taken with or without food, as directed by a physician.
Children: Pediatric dosing should be determined by a doctor, considering the child’s age, weight, and medical condition.
Special Cases:
- Elderly Patients: Dosage adjustments may be based on renal function and overall health status.
- Patients with Renal Impairment: Dose reductions might be necessary depending on the degree of impairment.
- Patients with Hepatic Dysfunction: Dosage adjustments may be needed.
- Patients with Comorbid Conditions: Individualized dosing considerations for patients with diabetes, cardiovascular disease, or other health conditions.
Clinical Use Cases
Dosages for specific clinical use cases like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations should be determined by the attending physician based on individual patient needs and condition. There is no standard dosage recommendation for these specific situations.
Dosage Adjustments
Dose modifications should be made based on patient-specific factors, including renal/hepatic dysfunction, metabolic disorders, or genetic polymorphisms that may affect drug metabolism.
Side Effects
Common Side Effects
Nausea, stomach upset, confusion, and sleeplessness have been reported. These often resolve without intervention.
Rare but Serious Side Effects
Allergic reactions such as rash, hives, itching, swelling, and difficulty breathing require immediate medical attention.
Long-Term Effects
Long-term effects are not well established, but it’s important to monitor B12 levels as L-methylfolate can mask vitamin B12 deficiency.
Adverse Drug Reactions (ADR)
Severe allergic reactions can occur and necessitate immediate medical intervention.
Contraindications
Known hypersensitivity to L-Methyltetrahydrofolate Calcium or its components is a contraindication.
Drug Interactions
L-Methylfolate Calcium can interact with certain medications, including:
- Antiepileptic drugs (AEDs): These can reduce folate absorption and vice-versa.
- Capecitabine: Concomitant use with folinic acid may increase the toxicity of capecitabine.
- Methotrexate: L-methylfolate can interfere with the efficacy of methotrexate.
It’s essential to disclose all medications, including OTC drugs and supplements, to the prescribing physician to avoid potential interactions. Alcohol should be limited or avoided as it can interfere with nutrient absorption.
Pregnancy and Breastfeeding
L-Methylfolate Calcium is generally considered safe during pregnancy and breastfeeding, though it should be used under the guidance of a physician. It’s crucial for fetal development, particularly neural tube closure, and adequate folate levels are important during lactation.
Drug Profile Summary
- Mechanism of Action: Participates in single-carbon transfer reactions for nucleotide biosynthesis, amino acid metabolism, methylation, and neurotransmitter synthesis.
- Side Effects: Generally well-tolerated, with some potential for nausea, stomach upset, confusion, sleeplessness, and allergic reactions.
- Contraindications: Hypersensitivity to the drug.
- Drug Interactions: AEDs, capecitabine, methotrexate.
- Pregnancy & Breastfeeding: Generally safe when used as directed by a physician.
- Dosage: 7.5mg to 15mg daily for adults. Pediatric and adjusted dosages should be determined by a physician.
- Monitoring Parameters: Monitor for allergic reactions and periodically check B12 levels.
Popular Combinations
L-Methylfolate is sometimes combined with other B vitamins, especially B12 (methylcobalamin) and B6 (pyridoxal-5-phosphate), for synergistic effects in supporting nerve health and addressing certain types of anemia.
Precautions
- Pre-existing conditions like bipolar disorder warrant careful monitoring.
- Screen for B12 deficiency before and during treatment.
- Pregnant or breastfeeding women should consult their doctor before use.
- No specific driving restrictions, but individual responses should be observed.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for L-Methyltetrahydrofolate Calcium?
A: The usual adult dose is 7.5mg to 15mg daily, as directed by a physician. Pediatric doses are determined based on the individual child’s needs.
Q2: Can L-methylfolate be taken with other medications?
A: It can interact with certain medications like AEDs, capecitabine, and methotrexate. Always inform your doctor about all other medications you are taking.
Q3: Is L-methylfolate safe during pregnancy?
A: Generally considered safe, but consult a doctor before use, especially if there’s a history of bipolar disorder.
Q4: What are the signs of an allergic reaction to L-methylfolate?
A: Rash, hives, itching, swelling, difficulty breathing, and tightness in the chest or throat are potential signs and require immediate medical attention.
Q5: Does L-methylfolate interact with food?
A: Alcohol should be avoided or limited.
Q6: How is L-methylfolate different from folic acid?
A: L-methylfolate is the active form of folate, readily usable by the body, whereas folic acid needs to be converted.
Q7: Can L-methylfolate mask a B12 deficiency?
A: Yes, it can improve the hematological symptoms of B12 deficiency without addressing the underlying neurological issues. B12 levels should be checked regularly.
Q8: Can L-methylfolate cause mood changes?
A: Some individuals may experience changes in mood, including irritability or increased anxiety. It’s important to monitor for any mood shifts and report them to your doctor.
Q9: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. If it’s close to the time for your next dose, skip the missed dose and continue your regular schedule. Do not double the dose.
