Potential Benefits of Methylcobalamin: A Review

Review Article

Austin J Pharmacol Ther. 2015; 3(3).1076.

Potential Benefits of Methylcobalamin: A Review

Gupta JK* and Qureshi Shaiba Sana

Department of Pharmacology, GLA University Mathura, India

*Corresponding author: : Jeetendra Kumar Gupta, Department of Pharmacology, Institute of Pharmaceutical Research, GLA University Mathura, India

Received: August 17, 2015; Accepted: September 30, 2015; Published: October 08, 2015


Methylcobalamin is an active form of vitamin B12 that helps in synthesis of methionine and S-adenosylmethionine. It is required for integrity of myelin, neuronal function, proper red blood cell formation and DNA synthesis. The largest group of vitamin B12 deficiency is found in typical vegetarians all over the world, which can be alleviated with its analogue Methylcobalamin. It is a beneficial drug to most of the common disorders like cardiovascular disorders, diabetes, anemia, hyperhomocysteinemia and degenerative disorders. Methylcobalamin helps in the synthesis of neuronal lipids, regeneration of axonal nerves and has neuroprotective activity, which promote neurons to function in proper way and thus improves Alzheimer disease, Parkinsonism, Dementia and neuropathic syndromes. It is an approved treatment for peripheral neuropathy.

Keywords: Mecobalamin; Neuropathy; Anemia; Nootropic; Dietary supplement


SAMe: S-Adenosyl Methionine; ERK: Extracellular Signal- Regulated Kinases; PKB: Protein Kinase B; B-globulin: Beta Globulin; ENFD: Epidermal Nerve Fiber Density; DPN: Diabetic Peripheral Neuropathy; NSAIDs: Non Steroidal Anti Inflammatory Drugs; THF: Tetrahydrofolate; BHMT: Betaine Homocysteine Methyltransferase.


Methylcobalamin is a potent and active form of vitamin cyanocobalamin. It plays a key role in maintaining good health. Dietary cobalamin deficiency causes many serious health problems. The commonest are blood deficiency, depression, irritability and psychosis. The long term deficiency of vitamin B12 substance can lead to hyperhomocysteinemia and finally cardiovascular disorder. In today’s world, healthcare plays an important role in our personal lives. This merges a huge responsibility for improving and saving thousand lives on earth. Despite having incredible improvements in health since 1950, there are number of challenges which have to be solved. Each year 36 million deaths are caused by non communicable diseases such as hyperhomocysteinemia, cancer, chronic lung disease, anemia, diabetes and almost 17.5 millions died from cardiovascular disease in 2005 [1].

Folate and vitamin B12 are essential nutrients which are not synthesized in humans and whose deficiency is considered as heath problem worldwide such as anemia and neuronal dysfunction. Vitamin B12 deficiency is observed more in elderly and pregnant women. Methylcobalamin (commonly known as mecobalamin or methyl B12) is an analog of vitamin B12 which treats or prevents the pathology arising from the deficiency of vitamin B12. It contains methyl alkyl bonds and is different from cyanocobalamin because it contains cynide [2]. It has an octahedral cobalt (III) center and is produced in laboratory by reducing cyanocobalamin with sodium borohydride in alkaline solution which is followed by the addition of methyl iodide. Methylcobalamin (5 mg, 60 mg vegetarian lozenges) is active in the central nervous system outside the mitochondrion and is essential for cell growth and replication. Sometimes the liver cannot convert cyanocobalamin into adequate amount of methylcobalamin needed for proper neuronal functioning. Through enhanced methylation, it exerts its nerve cell protective effect and accelerates its growth. A lot of energy is required for cyanocobalamin to remove its cyanide and replaces it with methyl group [3]. Methylcobalamin is the only form of vitamin B12 that can cross the blood brain barrier without biotransformation. Its methyl group stimulates serotonin creation, a neurotransmitter which is responsible for mood enhancement and protects the brain from damage against excitotoxins. High homocysteine level is the main culprit for brain, vascular diseases, stokes risk and causes sclerosis in the arteries. Methlcobalamine converts homocysteine to methionine and reduces the potential to damage. It also forms adenosylcobalamine, the other form of vitamin B12 for mitochondrial energy production. Along with methylcobalamin, 5 methyltetrahydrofolate is also an important element to eliminate homocysteine. Vitamin supplements reduce the chances of building homocysteine associated with stress. Sublingual absorption of methylcobalamin has become very popular because it can be easily absorbed with better bioavailability. It also increases the available amount of SAMe (S- adenosylmethionine), which acts as a mood enhancer and works as an effective alternative to tricyclic antidepressant [4].

Therapeutic use of Methylcobalamine

Methylcobalamin is used in the treatment of diabetic neuropathy, degenerative disorders and in the preliminary treatment of amyotropic lateral sclerosis. It has been used to treat some nutrition based disease such as dementia, rheumatoid arthritis and exerts neuronal protection by promoting regeneration to injured nerves. It antagonizes the glutamate induced neurotoxicity and also manifests analgesic effects. It alleviates pain behavior in diabetic neuropathy, low back pain, neuralgia and promotes nerve conduction. It helps the body to use fats and carbohydrates for energy.

Oral administration of 500 mcg three times daily for four weeks results in improvement of peripheral neuropathy and it produces very significant effect after 12 weeks of treatment [5]. An improvement in vibration sense, lower motor neuron weakness and sensitivity to pain is also observed. It also improves visual function in Bell’s palsy, sleep wake rhythm disorder [6].

Citation: Gupta JK and Sana QS. Potential Benefits of Methylcobalamin: A Review. Austin J Pharmacol Ther. 2015; 3(3).1076. ISSN: 2373-6208.