Vitamins are organic substances that naturally occur in food. Out of the 13 known, 8 make up the B-group of vitamins. 

The vitamin B-complex comprises vitamin B1 (thiamin), B2 (riboflavin), B3 (niacin), B5 (pantothenic acid), B6 (pyridoxine), B7 (biotin), B9 (folate), and B12 (cobalamin). 

Vitamin B12 is naturally found in animal foods. It is a key player in the function and development of nerve and red blood cells.

Methylcobalamin is the active form of Vitamin B12 and is the most abundant form in the circulation.

In this article, let us learn more about the potential health benefits, uses, and side effects of Methylcobalamin.

What is Methylcobalamin?

Vitamin B12, or cobalamin, is an essential water-soluble vitamin and medication used to manage and treat anemia, nerve problems, such as numbness and pain, and other similar conditions. 

Cobalamin consists of four compounds with different biological functions; cyanocobalamin and hydroxocobalamin are the synthetic forms, whereas adenosylcobalamin and methylcobalamin are both involved in DNA synthesis and myelin and fatty acids formation.

Methylcobalamin is one of the two coenzyme forms of vitamin B12. It is also the principal form of circulating vitamin B12, hence the form that is transported to the peripheral tissues. It has many functions, but its greatest impact is on new blood cell regeneration and neurological function.

The main dietary sources of methylcobalamin are animal products, such as red meat, dairy, and egg, because animals obtain vitamin B through their gut microbes.

Vitamin B12 is essential for cell metabolism and function, so a deficiency may cause many serious health problems. The most affected are organ systems with high cell turnover and metabolism, such as bone marrow, the gastrointestinal tract, the brain, and the nervous system. [1][2][3]

How does Methylcobalamin work?

methylcobalamin
Source: Canva

The intestine absorbs the oral formulation methylcobalamin through a specific mechanism that uses the intrinsic factor. Intrinsic factor is a protein produced by the stomach cells necessary for the absorption of B12 in the intestine.

However, it is worth mentioning that approximately 1.2% of vitamin B12 still can be absorbed passively in the absence of the intrinsic factor.

Upon reaching the circulation, methylcobalamin binds with a transporter protein called transcobalamin II. The transporter protein acts as a vehicle that carries the methylcobalamin in the bloodstream.

Methylcobalamin then enters the target tissue with the help of a transcobalamin II receptor representing the transporter protein’s docking site. 

Inside the cell, methylcobalamin plays an important cofactor role in an enzymatic reaction involving a key enzyme called methionine synthase. Methionine synthase helps to convert homocysteine to methionine. 

In this biochemical reaction, folate is a byproduct that is essential in DNA synthesis. If there is insufficient methylcobalamin available to participate in the process, anemia occurs as a result of inhibited DNA synthesis. [4][5]

Methylcobalamin Benefits

methylcobalamin
Source: Canva

Because of the various effects of methylcobalamin as a cofactor in many biochemical reactions, eating vitamin B12-enriched foods or taking supplements offers significant benefits. [1][6]

  1. Anti-anemic – Methylcobalamin can reverse and prevent anemia by sustaining the continuous production of tetrahydrofolate, an active form of folate, essential in red blood cell formation.
  2. Neuroprotection and repair – Methylcobalamin rejuvenates the damaged nerves by producing a compound called myelin, which covers and protects nerve fibers. It also helps synthesize neuronal lipids, which promote neurons to function properly and thus improve symptoms of Alzheimer’s disease, Parkinsonism, and Dementia.
  3. Analgesic – Methylcobalamin reduces the intensity of perceived pain by increasing the availability and effectiveness of the chemicals noradrenaline and 5- hydroxytryptamine, which inhibit pain sensation.

Methylcobalamin Uses

Methylcobalamin is an FDA-approved supplement indicated for individuals suffering from chronic anemia, neuropathy secondary to nerve or spine disorders, intestinal parasitism that competes with vitamin B12 absorption, and dietary deficiency of vitamin B12 due to vegetarian or vegan practices. [1][7]

Methylcobalamin Side Effects

methylcobalamin
Source: Canva

When ingested at a very high dose, methylcobalamin may cause side effects that can range from mild to severe. [1][7]

  • Nausea
  • Vomiting
  • Allergic reaction
  • Fever
  • Itching or rash
  • Tingling or numbness of joint
  • Shortness of breath
  • Rapid weight gain
  • Polycythemia
  • Hypokalemia

Bottomline

Methylcobalamin is a potent and active form of vitamin B12 which plays a key role in maintaining overall good health.

It can be obtained from consuming animal products, and once absorbed from the digestive system, methylcobalamin is used as a cofactor for enzymes that are involved in the synthesis of DNA, fatty acids, and myelin. As a result, methylcobalamin deficiency can lead to symptoms of blood disorders and nerve problems.

FAQs

Currently, methylcobalamin can only be administered orally or intramuscularly. The factors to consider which route to choose depend on the cause, presentation, and demands of the patients.

For severe vitamin B12 deficiency, 1mg daily, then weekly via intramuscular route, is preferred. For the recommended dose of those without any hematologic or neurologic symptoms, 500 mcg daily is advised.
The only group of people who are absolutely contraindicated from taking methylcobalamin is those with an allergy to cobalamin molecules.

Other individuals who should take precautions before consuming vitamin B12 include those with renal insufficiency, diabetes mellitus, the elderly, using bone marrow suppressants, having an ongoing infection, and iron or folate deficiency.
Alcoholic beverages irritate the lining of the stomach, reducing the absorption of vitamin B12. Medicines such as antibiotics, metformin, nitrous oxide, colchicines, and NSAIDs decrease the absorption and induce reversible malabsorption of methylcobalamin by altering the function of intestinal cells.

Disclaimer: This article is only a guide. It does not substitute the advice given by your healthcare professional. Before making any health-related decision, consult your healthcare professional.

Editorial References And Fact-Checking

  1. Al Amin ASM, Gupta V. Vitamin B12 (Cobalamin) [Updated 2023 Jan 9]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK559132/
  2. Methylcobalamin. (1998). Alternative medicine review : a journal of clinical therapeutic, 3(6), 461–463.
  3. Ankar A, Kumar A. Vitamin B12 Deficiency. [Updated 2022 Oct 22]. In: StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing; 2023 Jan-. Available from: https://www.ncbi.nlm.nih.gov/books/NBK441923/
  4. Methylcobalamin. (2023)Inxight drugs. National Center for Advancing Translational Sciences. National Institutes of Health.
  5. Wong, C. W. (2017). Vitamin B12 Deficiency in the Elderly. Nutrition and Functional Foods for Healthy Aging, 159–166. doi:10.1016/b978-0-12-805376-8.00016-2
  6. Zhang, M., Han, W., Hu, S., & Xu, H. (2013). Methylcobalamin: a potential vitamin of pain killer. Neural plasticity, 2013, 424651. https://doi.org/10.1155/2013/424651
  7. Gupta JK and Sana QS. Potential Benefits of Methylcobalamin: A Review. Austin J Pharmacol Ther. 2015; 3(3).1076. ISSN: 2373-6208.

Author

  • Dr. Kara Marcella Barro, M.D.

    Dr. Kara Marcella Barro is a licensed physician who has been serving as a General Practitioner at her local health center. She has devoted her skills and knowledge as a public health doctor to serve the poor and marginalized. At the same time, she is also an educator who passionately promotes preventive medicine through her lectures and writing in the hopes of a better health outcome for everyone. LinkedIn

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Dr. Kara Marcella Barro is a licensed physician who has been serving as a General Practitioner at her local health center. She has devoted her skills and knowledge as a public health doctor to serve the poor and marginalized. At the same time, she is also an educator who passionately promotes preventive medicine through her lectures and writing in the hopes of a better health outcome for everyone. LinkedIn