L-Methylfolate Ca Me-Cblnac Tabs
It is used to help with nutrition needs in certain people.
Drug Class
Nutritional supplement; Medical food; Homocysteine management; Antioxidant
Pharmacologic Class
Folate derivative; Vitamin B12 analog; Mucolytic/Antioxidant
Pregnancy Category
Category A/B (Methylfolate/Methylcobalamin are A, Acetylcysteine is B)
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
This medication is a combination of three important nutrients: L-Methylfolate, Methylcobalamin (a form of Vitamin B12), and Acetylcysteine (NAC). It's often used to help your body process certain substances, support nerve health, and provide antioxidant benefits. It can be helpful for conditions where your body needs extra support for these processes, such as managing high homocysteine levels or supporting brain and nerve function.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. If it causes stomach upset, taking it with food may help.
Storing and Disposing of Your Medication
Keep your medication at room temperature, away from light and moisture. Avoid storing it in the bathroom. Ensure all medications are kept in a safe location, out of the 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 the best disposal method. Many areas have drug take-back programs that can help.
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 continue with 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. You can take this medication with or without food. If it causes stomach upset, taking it with food may help.
Storing and Disposing of Your Medication
Keep your medication at room temperature, away from light and moisture. Avoid storing it in the bathroom. Ensure all medications are kept in a safe location, out of the 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 the best disposal method. Many areas have drug take-back programs that can help.
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 continue with 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 exactly as prescribed by your doctor or as directed on the label.
- Do not exceed the recommended dose.
- Maintain a balanced diet rich in fruits, vegetables, and whole grains.
- Inform your healthcare provider about all other medications, supplements, and herbal products you are taking.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Typically 1 tablet orally once daily, or as directed by a healthcare professional. Doses vary based on specific product formulation and intended use.
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
General Nutritional Support:
1 tablet daily
Hyperhomocysteinemia:
May require higher doses based on individual needs and homocysteine levels.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established, use with caution and under medical supervision if considered.
Adolescent:
Not established, use with caution and under medical supervision if considered.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment generally required for Methylfolate or Methylcobalamin. Acetylcysteine generally safe.
Moderate:
No specific adjustment generally required for Methylfolate or Methylcobalamin. Acetylcysteine generally safe.
Severe:
No specific adjustment generally required for Methylfolate or Methylcobalamin. Acetylcysteine generally safe, but caution with fluid overload in anuric patients.
Dialysis:
Considerations: Water-soluble vitamins are dialyzable. Supplementation may be beneficial, but specific dosing for this combination is not established.
Hepatic Impairment:
Mild:
No specific adjustment generally required.
Moderate:
No specific adjustment generally required.
Severe:
No specific adjustment generally required.
Pharmacology
Mechanism of Action
L-Methylfolate is the primary biologically active form of folate, essential for DNA synthesis, repair, and methylation processes, including the conversion of homocysteine to methionine. Methylcobalamin is an active coenzyme form of Vitamin B12, crucial for methionine synthase activity (homocysteine metabolism) and nerve tissue health. Acetylcysteine (NAC) is a precursor to glutathione, a potent antioxidant, and plays a role in detoxification and reducing oxidative stress.
Pharmacokinetics
Absorption:
Bioavailability:
Methylfolate: High (nearly 100% for L-methylfolate); Methylcobalamin: Variable (oral ~1-5% at high doses); Acetylcysteine: Low oral bioavailability (~4-10%) due to first-pass metabolism.
Tmax:
Methylfolate: ~1-3 hours; Methylcobalamin: ~8-12 hours; Acetylcysteine: ~1-2 hours.
FoodEffect:
Generally minimal impact on absorption for Methylfolate and Methylcobalamin. Acetylcysteine absorption may be slightly delayed by food.
Distribution:
Vd:
Methylfolate: ~17 L; Methylcobalamin: Distributed widely, stored in liver; Acetylcysteine: ~0.47 L/kg.
ProteinBinding:
Methylfolate: High (~60-90%); Methylcobalamin: High (to transcobalamins); Acetylcysteine: ~66-83%.
CnssPenetration:
Methylfolate: Yes (crosses BBB); Methylcobalamin: Yes (crosses BBB); Acetylcysteine: Yes (crosses BBB).
Elimination:
HalfLife:
Methylfolate: ~3 hours (terminal); Methylcobalamin: ~6 days (tissue retention); Acetylcysteine: ~2 hours (oral).
Clearance:
Not readily available for combination; individual component clearance varies.
ExcretionRoute:
Methylfolate: Primarily renal; Methylcobalamin: Primarily renal (excess); Acetylcysteine: Primarily renal.
Unchanged:
Methylfolate: Minimal; Methylcobalamin: Minimal; Acetylcysteine: Minimal.
Pharmacodynamics
OnsetOfAction:
Nutritional effects: Days to weeks for sustained changes in homocysteine or vitamin levels. Antioxidant effects of NAC: Hours.
PeakEffect:
Nutritional effects: Weeks to months for optimal homocysteine reduction or neurological improvement. Antioxidant effects of NAC: Hours.
DurationOfAction:
Nutritional effects: Sustained with continued daily dosing. Antioxidant effects of NAC: Hours, requiring regular dosing for sustained effect.
Safety & Warnings
Side Effects
Serious 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
Back pain, belly pain, or blood in the urine, which may be signs of a kidney stone
Swelling
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor or seek medical help:
Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Flushing
Headache
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact your doctor for medical advice. 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
Back pain, belly pain, or blood in the urine, which may be signs of a kidney stone
Swelling
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor or seek medical help:
Constipation
Diarrhea
Stomach pain
Upset stomach
Vomiting
Flushing
Headache
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, contact your doctor for medical advice. 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 an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
- Severe or persistent gastrointestinal upset (nausea, vomiting, diarrhea)
- Unusual fatigue or weakness
- New or worsening neurological symptoms (e.g., numbness, tingling, difficulty walking)
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 conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reactions you have experienced.
A history of kidney stones, as this may affect your treatment.
If you are taking levodopa, as this may interact with the medication.
If you are breastfeeding, as you should not breastfeed while taking this medication.
For Children:
If the patient is under 12 years of age, consult with your doctor, as some products are not suitable for children of this age group. Additionally, some products are not approved for use in children.
Other Important Considerations:
This medication may interact with other drugs or health conditions. Therefore, it is crucial to inform your doctor and pharmacist about:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your overall health, including any existing medical conditions
Do not start, stop, or change the dose of any medication without consulting your doctor to ensure safe treatment and minimize potential interactions.
It is essential to inform your doctor about the following conditions to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Describe the allergic reactions you have experienced.
A history of kidney stones, as this may affect your treatment.
If you are taking levodopa, as this may interact with the medication.
If you are breastfeeding, as you should not breastfeed while taking this medication.
For Children:
If the patient is under 12 years of age, consult with your doctor, as some products are not suitable for children of this age group. Additionally, some products are not approved for use in children.
Other Important Considerations:
This medication may interact with other drugs or health conditions. Therefore, it is crucial to inform your doctor and pharmacist about:
All prescription and over-the-counter medications you are taking
Any natural products or vitamins you are using
* Your overall health, including any existing medical conditions
Do not start, stop, or change the dose of any medication without consulting your doctor to ensure safe treatment and minimize potential interactions.
Precautions & Cautions
It is essential to inform all of your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This drug may interfere with certain laboratory tests, so it is crucial to notify all of your healthcare providers and laboratory personnel that you are taking this medication. If you are pregnant or planning to become pregnant, you must discuss the potential benefits and risks of using this drug during pregnancy with your doctor.
Overdose Information
Overdose Symptoms:
- Generally considered to have low toxicity. High doses of L-Methylfolate and Methylcobalamin are usually well-tolerated.
- Very high doses of Acetylcysteine may cause nausea, vomiting, diarrhea, or rarely, more severe gastrointestinal distress.
What to Do:
If you suspect an overdose, contact your local poison control center (1-800-222-1222) or seek emergency medical attention immediately.
Drug Interactions
Major Interactions
- Folate antagonists (e.g., Methotrexate, Trimethoprim, Pyrimethamine): L-Methylfolate may reduce the efficacy of these drugs by bypassing the dihydrofolate reductase enzyme. Close monitoring is required.
- Anticonvulsants (e.g., Phenytoin, Phenobarbital, Primidone): Folate supplementation may decrease serum levels of these drugs, potentially increasing seizure frequency. Monitor anticonvulsant levels.
Moderate Interactions
- Metformin: May decrease Vitamin B12 absorption.
- Proton Pump Inhibitors (PPIs) and H2-receptor antagonists: May decrease Vitamin B12 absorption.
- Colchicine: May decrease Vitamin B12 absorption.
- Chloramphenicol: May decrease hematopoietic response to Vitamin B12.
- Nitroglycerin: Acetylcysteine may potentiate the vasodilatory and antiplatelet effects of nitroglycerin, leading to hypotension and headache.
- Activated Charcoal: If used for overdose, activated charcoal can adsorb oral acetylcysteine, reducing its efficacy.
Monitoring
Baseline Monitoring
Homocysteine levels
Rationale: To assess baseline cardiovascular risk and guide therapy for hyperhomocysteinemia.
Timing: Prior to initiation of therapy.
Serum Folate and Vitamin B12 levels
Rationale: To assess baseline nutritional status and identify deficiencies.
Timing: Prior to initiation of therapy.
Renal and Hepatic Function Tests
Rationale: To establish baseline organ function, especially if co-morbidities exist.
Timing: Prior to initiation, if clinically indicated.
Routine Monitoring
Homocysteine levels
Frequency: Every 3-6 months initially, then annually once stable.
Target: < 10-12 µmol/L
Action Threshold: If levels remain elevated despite therapy, consider dose adjustment or investigate other contributing factors.
Clinical symptoms (e.g., fatigue, neurological symptoms, mood changes)
Frequency: Ongoing, at each follow-up visit.
Target: Improvement or resolution of symptoms.
Action Threshold: Worsening or new symptoms may indicate inadequate dosing or alternative diagnoses.
Symptom Monitoring
- Gastrointestinal upset (nausea, diarrhea, abdominal pain)
- Skin rash or itching (signs of allergic reaction)
- Headache
- Fatigue or weakness (if underlying deficiency is not adequately addressed)
- Neurological symptoms (e.g., tingling, numbness, gait instability - if B12 deficiency persists)
Special Patient Groups
Pregnancy
L-Methylfolate and Methylcobalamin are essential nutrients during pregnancy and are often included in prenatal vitamins (Category A). Acetylcysteine is Category B. This combination is generally considered safe and potentially beneficial during pregnancy, especially for folate and B12 supplementation.
Trimester-Specific Risks:
First Trimester:
Folate and B12 are crucial for neural tube development and early fetal growth. Acetylcysteine is Category B.
Second Trimester:
Generally considered safe and beneficial.
Third Trimester:
Generally considered safe and beneficial.
Lactation
L-Methylfolate, Methylcobalamin, and Acetylcysteine are generally considered safe during lactation (L1 risk category). They are naturally present in breast milk and are important for infant development.
Infant Risk:
Low risk to the infant. Benefits of maternal supplementation likely outweigh any theoretical risks.
Pediatric Use
Specific dosing for this combination product in pediatric populations is not well-established. Use should be under the strict guidance of a healthcare professional, considering individual component needs.
Geriatric Use
Generally safe. Older adults may have impaired absorption of Vitamin B12, making supplementation beneficial. No specific dose adjustments are typically required, but monitoring for interactions with polypharmacy is important.
Clinical Information
Clinical Pearls
- This product is often classified as a 'medical food' or 'dietary supplement' rather than a traditional drug, which impacts its regulatory oversight and insurance coverage.
- L-Methylfolate is the active form of folate, which can be beneficial for individuals with genetic polymorphisms (e.g., MTHFR) that impair the conversion of folic acid to its active form.
- The combination of L-Methylfolate and Methylcobalamin is synergistic in reducing homocysteine levels, a risk factor for cardiovascular disease and cognitive decline.
- Acetylcysteine (NAC) provides antioxidant support and may have neuroprotective benefits, complementing the roles of folate and B12.
- Patients should be advised that while these are 'nutrients,' they should still be taken under medical guidance, especially if they have underlying medical conditions or are taking other medications.
Alternative Therapies
- Individual supplementation with L-Methylfolate, Methylcobalamin, and Acetylcysteine.
- Other B vitamins (e.g., Pyridoxal 5'-phosphate for B6).
- S-Adenosylmethionine (SAMe) for methylation support.
- Dietary modifications to increase folate and B12 intake.
Cost & Coverage
Average Cost:
$30 - $100+ per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Often not covered by insurance as a prescription drug, may be covered under medical food or supplement benefits if prescribed for a specific medical condition and deemed medically necessary. Coverage varies by plan.
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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.