Methylcobalamin – Dosage and Uses

What is Methylcobalamin?

Methylcobalamin is the activated form of Vitamin B12, available as an oral medicine. It is prescribed for people suffering from a deficiency of vitamin B12. The aim of this vitamin is to help with the proper functioning of the brain and nerves as well as the production of red blood cells.

Methylcobalamin helps treat the deficiency of vitamin B12 by producing a substance known as “myelin”. This substance is responsible for covering nerve fibres and protecting them. Without inadequate amounts of methylcobalamin in the body, the myelin sheath cannot develop well or stay healthy.

Properties and Characteristics of Methylcobalamin

Drug class Vitamins
Brand Names   Neurobion, Cobalin-M, Mecobalamin, Methyl-12, Metanerv-M, Methylcobal, Mecovit, Nurokind, Mecovon, Neurocetam, Mecozine, Cobamex, Neurodoron, Cobadex, Methycobal

Cobolin, Myoden, Cobaplex, Neurogard, Neurodex

Synonyms Methyl-B12, Methyl vitamin B12, Mecobalamin, Methyl-5,6-dimethylbenzimidazolylcobalamin, Methylcobalamin hydrochloride, Mecobalamine, Methylcobamide, Mecobal, Methylated B12, Methyl-Cbl, Methylcyano-B12, 5-Methyltetrahydrofolate-cobalamin-carrying cobamide coenzyme, Vitamin B12 Methylated Form
Molecular Formula C63H91CoN13O14P
Molecular Weight 1,344.4 g/mol
IUPAC Name carbanide;cobalt(2+);[(2R,3S,4R,5S)-5-(5,6-dimethylbenzimidazol-1-yl)-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl] 1-[3-[(1R,2R,3R,5Z,7S,10Z,12S,13S,15Z,17S,18S,19R)-2,13,18-tris(2-amino-2-oxoethyl)-7,12,17-tris(3-amino-3-oxopropyl)-3,5,8,8,13,15,18,19-octamethyl-2,7,12,17-tetrahydro-1H-corrin-24-id-3-yl]propanoylamino]propan-2-yl hydrogen phosphate
Structural formula of main components
Pure active ingredient        Active form of vitamin B12
Appearance Dark red crystals
Melting point   >190° C
Solubility         Soluble in alcohol; insoluble in acetone, chloroform, ether.
Excretion Excreted through urine
Storage At room temperature between 20°C and 25°C
Available Forms            Oral capsule, tablet, Oral Liquid or Drops, Nasal Spray, Intramuscular Injections, Topical Creams or Gels
Prescription     Doctor prescription is required

What are the uses of Methylcobalamin?

Some of the uses of methylcobalamin are

  • Methylcobalamin is prescribed for treating certain nerve problems and anaemia by restoring the levels of vitamin B12 in the body.
  • Replenishment of the vitamin helps in the regeneration and improvement of damaged and irritated nerves, which can be caused by medical conditions like pernicious anaemia, neuropathy, and neuralgia.
  • It is also prescribed for people who experience back pain, anaemia, or other problems related to the nervous system that can be caused by a deficiency of vitamin B12.
  • Methylcobalamin also works as a painkiller for people with diabetes.

What are the side effects of  Vitamin B12?

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Common side effects may include:

  • Nausea, vomiting, diarrhea;
  • Loss of appetite; or
  • Headache.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

Mechanism of action

Methylcobalamin, a biologically active form of vitamin B12, exerts its mechanisms of action primarily within the body’s cells, particularly nerve cells. Its vital role in various biochemical processes is due to its ability to act as a coenzyme in several key reactions. Here’s a simplified explanation of its mechanism of action:

  1. Methionine Synthesis: Methylcobalamin participates in a process called methylation, where it helps convert homocysteine (an amino acid) into methionine. Methionine is essential for the synthesis of proteins and DNA, and it’s involved in various metabolic reactions.
  2. Myelin Maintenance: Methylcobalamin is crucial for the maintenance and repair of the myelin sheath, the protective covering around nerve cells. This ensures proper nerve conduction and function. Without adequate methylcobalamin, nerve signals can be disrupted, leading to neurological symptoms.
  3. Neurotransmitter Regulation: Methylcobalamin plays a role in the production of certain neurotransmitters, such as serotonin and dopamine, which are important for mood regulation and overall brain function.
  4. DNA Synthesis: Vitamin B12, including methylcobalamin, is involved in the synthesis of DNA, the genetic material in cells. This is important for cell growth, repair, and overall health.

In summary, methylcobalamin’s primary mechanism of action is to facilitate methylation reactions, support myelin sheath integrity, regulate neurotransmitter production, and contribute to DNA synthesis. These functions are critical for neurological health, overall cellular function, and the maintenance of various physiological processes in the body.

What are the interactions of Methylcobalamin?

Whenever you take more than one medicine, or mix it with certain foods or beverages, you’re at risk of a drug interaction.

Interaction with Alcohol: It decreases the effectiveness of medication.

Interaction with Medicine: Some medication that have a serious interaction with Methylcobalamin are Leukeran (chlorambucil), Prilosec (omeprazole), colcrys and Mitigare and the herbal supplement goldenseal.

Interaction with Food: Since it’s derived from food sources there is no severe reaction with food.

Interaction with Disease: Vitamin B12 does not interact with diseases.

Dosage of Methylcobalamin

The recommended dosage of methylcobalamin, like any supplement or medication, can vary depending on individual factors and the specific medical condition being treated or the purpose of supplementation. It’s important to consult with a healthcare professional for personalized guidance on the appropriate dosage. However, here are some general dosage guidelines for methylcobalamin:

  • For Vitamin B12 Deficiency: The standard treatment for vitamin B12 deficiency typically involves an initial phase of higher-dose supplementation, followed by a maintenance phase. For example, an initial dose of 1,000 to 2,000 micrograms (mcg) of methylcobalamin given daily or weekly may be used, followed by a maintenance dose of 100 to 1,000 mcg per month.
  • For Neurological Conditions: In cases of neurological conditions, such as peripheral neuropathy or diabetic neuropathy, higher doses of methylcobalamin, often in the range of 1,500 to 6,000 mcg per day, may be recommended. Again, the specific dosage will depend on the severity of the condition and individual factors.
  • As a Dietary Supplement: Methylcobalamin is also available as a dietary supplement, commonly in the form of tablets, capsules, or sublingual (under the tongue) formulations. Typical over-the-counter dosages for general health and well-being range from 500 to 5,000 mcg per day.

Always follow the advice of your healthcare provider when determining the appropriate dosage of methylcobalamin for your specific needs. They will consider your medical history, existing health conditions, and any potential interactions with other medications or supplements you may be taking. Additionally, periodic monitoring of vitamin B12 levels through blood tests may be necessary to ensure that the chosen dosage is effective in addressing any deficiency. Self-administration of high doses of methylcobalamin without medical supervision is not recommended.

Overdosage of Methylcobalamin

Vitamin B12, including methylcobalamin, is generally considered safe, even at relatively high doses, as it is a water-soluble vitamin. This means that excess amounts are usually excreted in the urine rather than stored in the body, reducing the risk of overdose. However, extremely high doses of methylcobalamin can still lead to potential adverse effects.

Symptoms of a potential overdose of methylcobalamin or vitamin B12 are rare but may include:

  • Skin Rashes: High doses of vitamin B12 can sometimes cause skin reactions, such as itching, redness, or hives.
  • Gastrointestinal Issues: Excessive vitamin B12 intake can lead to digestive problems, including diarrhea and upset stomach.
  • Nervous System Symptoms: In rare cases, very high doses may lead to nervous system symptoms, such as anxiety, restlessness, or even neuropathy (nerve damage). This is more likely to occur in individuals with preexisting neurological conditions.

It’s important to note that the body usually excretes excess vitamin B12 through urine, and it is considered to have a low potential for toxicity. However, if you suspect an overdose or experience any unusual or severe symptoms after taking methylcobalamin supplements, it’s essential to seek medical attention promptly.

The best approach to using methylcobalamin or any vitamin supplement is to follow the recommended dosage guidelines provided by your healthcare provider or the product label. Avoid self-prescribing or taking excessive doses without professional guidance, especially if you do not have a diagnosed deficiency.

Precautions and warning

Methylcobalamin is generally considered safe when used as directed, especially in the context of treating vitamin B12 deficiency and certain neurological conditions. However, there are some precautions and considerations to keep in mind:

Allergies or Sensitivities: Some individuals may be allergic or sensitive to methylcobalamin or other components of vitamin B12 supplements. If you experience symptoms of an allergic reaction, such as rash, itching, swelling, dizziness, or difficulty breathing, seek medical attention immediately.

Interactions with Medications: Methylcobalamin supplements can interact with certain medications, such as certain antibiotics, anticonvulsants, and medications that reduce stomach acid (proton pump inhibitors). Inform your healthcare provider about all medications and supplements you are taking to assess potential interactions.

Kidney Disease: People with severe kidney disease may need to be cautious when taking methylcobalamin supplements because excess vitamin B12 may not be effectively cleared from the body, potentially leading to elevated levels.

Folic Acid Interaction: High doses of vitamin B12, including methylcobalamin, can mask the symptoms of a vitamin B9 (folic acid) deficiency. If you are taking vitamin B12 supplements for an extended period, it’s important to also ensure an adequate intake of folic acid.

Cyanide Sensitivity: Some people have a genetic condition called Leber’s hereditary optic neuropathy (LHON) that can be exacerbated by high doses of cyanocobalamin, another form of vitamin B12. Methylcobalamin is often preferred in such cases as it does not contain cyanide, but consultation with a healthcare provider is essential.

Pregnancy and Breastfeeding: Methylcobalamin is generally considered safe for pregnant and breastfeeding women when used at recommended doses. However, it’s crucial to consult with a healthcare provider for appropriate guidance during pregnancy and lactation.

Individual Tolerance: High doses of methylcobalamin may cause side effects in some individuals, such as diarrhea, itching, anxiety, or skin rash. Adjusting the dosage or trying a different form of vitamin B12 may help alleviate these symptoms.

Always consult with a healthcare professional before starting or altering the dosage of methylcobalamin supplements, especially if you have underlying health conditions, are pregnant or breastfeeding, or are taking other medications. They can provide personalized guidance and monitor your progress to ensure safe and effective use.

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