B12

B12

Methylcobalamin

1000 mcg

60 Sublingual Tablets ( SKU: 9420, NPN: 80026765 )

Benefits

  • Methylcobalamin is the active form of vitamin B12 for maximum benefit 

  • Superior bioavailability to the more common form, cyanocobalamin, which does not convert to enough methylcobalamin to correct some forms of anemia, neurological defects and aging1    

  • Lowers homocysteine levels for protective cardiovascular benefits
  • Sublingual tablets allow for fast acting delivery system directly into blood stream

Feature Summary

Vitamin B12 is the cofactor in enzymatic reactions with diverse physiological functions. It is required for the conversion of methylmalonyl CoA to succinyl CoA, as well as for the conversion of homocysteine to methionine by methionine synthase, which is then converted into S-adenosylmethionine.2 A B12 deficiency causes impairments in both of these pathways, disrupting neurological function, including poor formation of myelin nerve sheaths, production of toxic levels of homocysteine, and inefficient energy production in all cells.3,4 Methylcobalamin, the principal circulating form of B12 and the one transported into peripheral tissues, has been shown to not only reduce homocysteine, but also to reduce inflammatory factors and the volume of carotid artery plaques among stroke patients, as well as pain, and neuropathy among diabetics.5–8

Cobalamin is also required to remove the methyl group from methyltetrahydrofolate and generate tetrahydrofolate, a necessary step in DNA synthesis. As a consequence, B12 deficiency affects the growth, function, and repair of all cells, the most apparent sign of which is megaloblastic anemia, caused by inhibited mitosis of red blood cells.9 Some individuals, especially those with malabsorption or low dietary intake, are at higher risks for a B12 deficiency. B12 in sublingual form, at a dose of 1000 mcg per day bypasses active absorption routes, and can restore normal B12 levels even in those with gastric bypass, pernicious anemia and/or impaired absorptive capacity, with greater effectiveness than even intramuscular injection.10–13

Medicinal Ingredients

Each Tablet Contains:
Vitamin B12 (Methylcobalamin) 1000 mcg

Non-Medicinal Ingredients

Lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, vegetable grade magnesium stearate (lubricant).

Dosage:

Recommended Adult Dose: 1 tablet per day or as directed by a health care professional. Dissolve under the tongue. 

Warnings:

Keep out of reach of children.

Allergens:

Contains no artificial colours, preservatives, or sweeteners; no starch, sugar, wheat, gluten, yeast soy, corn, egg, fish, shellfish, salt, tree nuts, or GMOs. Suitable for vegetarians. Sealed for your protection. Do not use if seal is broken. For freshness, store in a cool, dry place.

Contraindications

Supplemental folic acid may mask a B12 deficiency, which should be ruled out. Folic acid, as well as increased potassium intake, is recommended with B12 therapy. B12 at this dosage is considered safe in pregnant and lactating women, and may be indicated in children with a low dietary intake.

Drug Interactions

Although several classes of drugs, such as aminoglycosides, anticonvulsants, bile acid sequestrants, and proton pump inhibitors, antihyperglycemic medications (Metformin), acne therapy (isotretinoin) are known to interfere with B12 absorption or function, there are no known negative interactions caused by B12 supplementation with any medications.15–21

  1. [No authors listed]. (1998). Methylcobalamin. Altern Med Rev, 3(6), 461-3.
  2. Guéant, J.L.1, Caillerez-Fofou, M., Battaglia-Hsu, S., et al. (2013). Molecular and cellular effects of vitamin B12 in brain, myocardium and liver through its role as co-factor of methionine synthase. Biochimie, 95(5), 1033-40.
  3. Calderón-Ospina, C.A., Nava-Mesa, M.O. (2020). B Vitamins in the nervous system: Current knowledge of the biochemical modes of action and synergies of thiamine, pyridoxine, and cobalamin. CNS Neurosci Ther, 26(1), 5-13.
  4. Austin, R.C., Lentz, S.R., Werstuck, G.H. (2004). Role of hyperhomocysteinemia in endothelial dysfunction and atherothrombotic disease. Cell Death Differ, 11(Suppl 1), S56-64.
  5. Miranda-Massari, J.R., Gonzalez, M.J., Jimenez, F.J., et al. (2011). Metabolic correction in the management of diabetic peripheral neuropathy: improving clinical results beyond symptom control. Curr Clin Pharmacol, 6(4), 260-73.
  6. Yuan, M., Wang, B., Tan, S. (2018). Methylcobalamin and early functional outcomes of ischemic stroke patients with H-type hypertension. Rev Assoc Med Bras (1992), 64(5), 428-432.
  7. Jiang, D.Q., Zhao, S.H., Li, M.X., et al. (2018). Prostaglandin E1 plus methylcobalamin combination therapy versus prostaglandin E1 monotherapy for patients with diabetic peripheral neuropathy: A meta-analysis of randomized controlled trials. Medicine (Baltimore), 97(44), e13020.
  8. Buesing, S., Costa, M., Schilling, J.M., et al. (2019). Vitamin B12 as a Treatment for Pain. Pain Physician, 22(1), E45-E52.
  9. Parry, T.E. (1987). Megaloblastic anaemia in the elderly. Baillieres Clin Haematol, 1(2), 315-53.
  10. Kim, H.I., Hyung, W.J., Song, K.J., et al. (2011). Oral vitamin B12 replacement: an effective treatment for vitamin B12 deficiency after total gastrectomy in gastric cancer patients. Ann Surg Oncol, 18(13), 3711-7.
  11. Schijns, W., Homan, J., van der Meer, L., et al. (2018). Efficacy of oral compared with intramuscular vitamin B-12 supplementation after Roux-en-Y gastric bypass: a randomized controlled trial. Am J Clin Nutr, 108(1, :6-12.
  12. Bolaman, Z., Kadikoylu, G., Yukselen, V., et al. (2003). Oral versus intramuscular cobalamin treatment in megaloblastic anemia: a single-center, prospective, randomized, open-label study. Clin Ther, 25(12), 3124-34.
  13. Bensky, M.J., Ayalon-Dangur, I., Ayalon-Dangur, R., et al. (2019). Comparison of sublingual vs. intramuscular administration of vitamin B12 for the treatment of patients with vitamin B12 deficiency. Drug Deliv Transl Res, 9(3), 625-630
  14. Paul, C., Brady, D.M. (2017). Comparative Bioavailability and Utilization of Particular Forms of B12 Supplements With Potential to Mitigate B12-related Genetic Polymorphisms. Integr Med (Encinitas), 16(1), 42-49.
  15. McColl, K.E. (2009). Effect of proton pump inhibitors on vitamins and iron. Am J Gastroenterol, 104(Suppl 2), S5-9.
  16. Aslan, K., Bozdemir, H., Unsal, C., et al. (2008). The effect of antiepileptic drugs on vitamin B12 metabolism. Int J Lab Hematol, 30(1), 26-35.
  17. de Jager, J., Kooy, A., Lehert, P., et al. (2010). Long term treatment with metformin in patients with type 2 diabetes and risk of vitamin B-12 deficiency: randomised placebo controlled trial. BMJ, 340, c2181.
  18. Aroda, V.R., Edelstein, S.L., Goldberg, R.B., et al. (2016). Long-term Metformin Use and Vitamin B12 Deficiency in the Diabetes Prevention Program Outcomes Study. J Clin Endocrinol Metab, 101(4), 1754-1761.
  19. Markkanen, T., Salmi, H.A., Sotaniemi, E. (1965). Effect of neomycin treatment on the vitamin B12 content of human serum and urine. Z Vitam Horm Fermentforsch, 14(1), 66-71.
  20. Karadag, A.S., Tutal, E., Ertugrul, D.T., et al. (2011). Effect of isotretinoin treatment on plasma holotranscobalamin, vitamin B12, folic acid, and homocysteine levels: non-controlled study. Int J Dermatol, 50(12), 1564-9.
  21. Dierkes, J., Westphal, S., Kunstmann, S., et al. (2001). Vitamin supplementation can markedly reduce the homocysteine elevation induced by fenofibrate. Atherosclerosis, 158(1), 161-4.