L-Methylfolate 15mg Tablets
It is used to aid diet needs.
Drug Class
Nutritional Supplement; Antidepressant Augmentation; Neuropathic Pain Adjunct
Pharmacologic Class
Folate Derivative; Methyl Donor
Pregnancy Category
Category A/B (Folate is essential during pregnancy)
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
L-Methylfolate is the active form of a B vitamin called folate (or folic acid). It's crucial for many body functions, including brain health, nerve function, and the production of important brain chemicals. Some people have a genetic variation that makes it harder for their body to convert regular folic acid into its active form. Taking L-methylfolate helps bypass this step, ensuring your body gets the folate it needs directly.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding bathrooms and areas where children and pets can access it. Keep all medications in a safe location and out of reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on proper disposal or participate in a drug take-back program in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. Continue taking it even if you feel well, unless your doctor or healthcare provider advises you to stop.
Storing and Disposing of Your Medication
Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding bathrooms and areas where children and pets can access it. Keep all medications in a safe location and out of reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on proper disposal or participate in a drug take-back program in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Take as directed by your healthcare provider, usually once daily with or without food.
- Continue other prescribed medications unless advised otherwise by your doctor.
- Maintain a balanced diet and healthy lifestyle.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
15 mg orally once daily
Dose Range:
7.5 - 15 mg
Condition-Specific Dosing:
Major Depressive Disorder (adjunctive therapy):
7.5 mg to 15 mg orally once daily
Diabetic Peripheral Neuropathy:
15 mg orally once daily
Folate Deficiency (due to impaired metabolism):
15 mg orally once daily
Pediatric Dosing
Neonatal:
Not established for these indications; specific folate supplementation may be used for deficiency.
Infant:
Not established for these indications; specific folate supplementation may be used for deficiency.
Child:
Not established for these indications; specific folate supplementation may be used for deficiency.
Adolescent:
Not established for these indications; specific folate supplementation may be used for deficiency.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed
Moderate:
No specific adjustment needed
Severe:
No specific adjustment needed
Dialysis:
No specific adjustment needed; generally considered safe.
Hepatic Impairment:
Mild:
No specific adjustment needed
Moderate:
No specific adjustment needed
Severe:
No specific adjustment needed
Pharmacology
Mechanism of Action
L-methylfolate is the primary biologically active form of folate. It is essential for the synthesis of monoamine neurotransmitters (serotonin, dopamine, norepinephrine) by acting as a methyl donor in the tetrahydrobiopterin (BH4) synthesis pathway. It also plays a critical role in the methylation cycle, including the conversion of homocysteine to methionine, and in DNA synthesis and repair. It bypasses the MTHFR enzyme step, which is crucial for individuals with MTHFR polymorphisms who have reduced ability to convert folic acid to its active form.
Pharmacokinetics
Absorption:
Bioavailability:
High (nearly 100% for the active form)
Tmax:
Approximately 1-3 hours
FoodEffect:
Minimal or no significant food effect
Distribution:
Vd:
Widely distributed throughout body tissues
ProteinBinding:
Not extensively protein bound
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 3 hours (for the active form)
Clearance:
Primarily renal
ExcretionRoute:
Urine
Unchanged:
Significant portion
Pharmacodynamics
OnsetOfAction:
Clinical effects (e.g., mood improvement) may take several weeks to manifest.
PeakEffect:
Weeks to months of consistent use.
DurationOfAction:
Sustained with daily dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
- Signs of an allergic reaction, such as:
- Rash
- Hives
- Itching
- Red, swollen, blistered, or peeling skin with or without fever
- Wheezing
- Tightness in the chest or throat
- Trouble breathing, swallowing, or talking
- Unusual hoarseness
- Swelling of the mouth, face, lips, tongue, or throat
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you have side effects that bother you or do not go away, contact your doctor for advice.
Reporting Side Effects
This list does not include all possible side effects. If you have questions or concerns about side effects, discuss them with your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
- Signs of an allergic reaction, such as:
- Rash
- Hives
- Itching
- Red, swollen, blistered, or peeling skin with or without fever
- Wheezing
- Tightness in the chest or throat
- Trouble breathing, swallowing, or talking
- Unusual hoarseness
- Swelling of the mouth, face, lips, tongue, or throat
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you have side effects that bother you or do not go away, contact your doctor for advice.
Reporting Side Effects
This list does not include all possible side effects. If you have questions or concerns about side effects, discuss them with your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of allergic reaction (rare): rash, itching, swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing. Seek immediate medical attention if these occur.
- Unusual or severe mood changes (though it's often used to improve mood, report any concerning changes).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to ensure safe use and avoid potential interactions.
* Any existing health problems, as this medication may interact with other medical conditions or drugs.
To guarantee your safety, it is vital to verify that this medication can be taken in conjunction with all your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor. Always consult with your doctor and pharmacist to confirm the safe use of this medication with your other medications and health problems.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to ensure safe use and avoid potential interactions.
* Any existing health problems, as this medication may interact with other medical conditions or drugs.
To guarantee your safety, it is vital to verify that this medication can be taken in conjunction with all your other medications and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor. Always consult with your doctor and pharmacist to confirm the safe use of this medication with your other medications and health problems.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. If you have any concerns or questions, be sure to discuss them with your doctor.
If you are allergic to tartrazine, also known as FD&C Yellow No. 5, consult your doctor before taking this medication, as some products may contain this ingredient.
When taking cholestyramine or colestipol, it is crucial to consult with your pharmacist to determine the best way to take these medications in conjunction with this drug to ensure safe and effective use.
If you are pregnant, planning to become pregnant, or are breast-feeding, it is vital to discuss the potential benefits and risks of this medication with your doctor to make an informed decision about your treatment.
If you are allergic to tartrazine, also known as FD&C Yellow No. 5, consult your doctor before taking this medication, as some products may contain this ingredient.
When taking cholestyramine or colestipol, it is crucial to consult with your pharmacist to determine the best way to take these medications in conjunction with this drug to ensure safe and effective use.
If you are pregnant, planning to become pregnant, or are breast-feeding, it is vital to discuss the potential benefits and risks of this medication with your doctor to make an informed decision about your treatment.
Overdose Information
Overdose Symptoms:
- L-methylfolate is generally considered non-toxic even at high doses. No specific overdose symptoms are well-documented.
- Very high doses might rarely cause mild gastrointestinal upset or sleep disturbances.
What to Do:
Discontinue use. Contact a healthcare professional or poison control center (1-800-222-1222) if any unusual or concerning symptoms occur, though severe toxicity is highly unlikely.
Drug Interactions
Moderate Interactions
- Folate antagonists (e.g., methotrexate, pyrimethamine, trimethoprim): May reduce the efficacy of L-methylfolate or increase the need for it.
- Anticonvulsants (e.g., phenytoin, carbamazepine, valproate): May interfere with folate metabolism, potentially increasing folate requirements.
Monitoring
Baseline Monitoring
Folate levels (serum or red blood cell)
Rationale: To assess baseline folate status and identify deficiency.
Timing: Prior to initiation
Homocysteine levels
Rationale: To assess methylation pathway function, especially if elevated.
Timing: Prior to initiation
Routine Monitoring
Clinical response (e.g., mood, neuropathic pain symptoms)
Frequency: Periodically, as clinically indicated
Target: Improvement in target symptoms
Action Threshold: Lack of improvement or worsening symptoms after adequate trial
Homocysteine levels (if elevated at baseline)
Frequency: 3-6 months initially, then annually or as clinically indicated
Target: Normalization of homocysteine levels
Action Threshold: Persistent elevation
Symptom Monitoring
- Mood changes (improvement or worsening)
- Energy levels
- Neuropathic pain symptoms (e.g., burning, tingling, numbness)
- General well-being
- Any signs of allergic reaction (rare: rash, itching, swelling)
Special Patient Groups
Pregnancy
Folate is essential during pregnancy to prevent neural tube defects. L-methylfolate is generally considered safe and beneficial, especially for individuals with MTHFR polymorphisms who may have difficulty metabolizing folic acid.
Trimester-Specific Risks:
First Trimester:
Crucial for neural tube development; L-methylfolate is highly beneficial.
Second Trimester:
Continued importance for fetal growth and development.
Third Trimester:
Continued importance for fetal growth and development.
Lactation
Folate is excreted in breast milk and is essential for infant development. L-methylfolate is considered safe and compatible with breastfeeding.
Infant Risk:
Low risk; beneficial for infant development.
Pediatric Use
Generally safe, but specific dosing for conditions like depression or neuropathy is not well-established. Folate supplementation is common in pediatrics for diagnosed deficiencies.
Geriatric Use
Generally safe. No specific dose adjustments are typically needed. May be beneficial for age-related cognitive decline or depression, particularly if folate deficiency or impaired metabolism is present.
Clinical Information
Clinical Pearls
- L-methylfolate is the active, bioavailable form of folate, bypassing the need for the MTHFR enzyme, which is often deficient or less efficient in a significant portion of the population.
- It is commonly used as an adjunctive therapy in major depressive disorder, especially in patients who have not responded adequately to standard antidepressants or those with known MTHFR polymorphisms.
- Also utilized in the management of neuropathic pain, particularly diabetic peripheral neuropathy, due to its role in nerve health and repair.
- Generally well-tolerated with a very low side effect profile, making it a favorable addition to treatment regimens.
- It is important to differentiate L-methylfolate from folic acid, as folic acid requires enzymatic conversion to become active, which can be impaired in some individuals.
Alternative Therapies
- For depression: Other antidepressant medications, psychotherapy, electroconvulsive therapy (ECT), transcranial magnetic stimulation (TMS).
- For neuropathy: Gabapentin, pregabalin, duloxetine, tricyclic antidepressants.
- For general folate deficiency: Folic acid supplementation.
Cost & Coverage
Average Cost:
Varies widely, typically $30-$100+ per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Often not covered by insurance, or covered as Tier 3/4 if classified as a medical food and prescribed for specific conditions with prior authorization.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.