Hydroxocobalamin Injection

Overview of Hydroxocobalamin Injection

Dosage Strength

2 mg/mL 10 mL Vial

General Information

Cobalamins, or vitamin B12, are exclusively produced by bacteria and can only be obtained from a diet high in animal products. Megaloblastic anemia can be brought on by a cobalamin deficiency and may be associated with, among other things, a poor diet low in vitamin B12 or intrinsic factor. Pernicious anemia is the kind of anemia caused by a deficiency in an intrinsic factor. 1

A commercially available natural form of vitamin B12 is hydroxycobalamin (OHCbl). It is administered intravenously or intramuscularly by parenteral administration. The B12 forms found in human physiology and this type of cobalamin are bioidentical. 2 The commercial cyanocobalamin (marketed as Cytamen) originally contained 3 hydroxocobalamin as a manufacturing contaminant and byproduct of photolysis, but it was later discovered to be superior for many clinical situations.

OHCbl dosages work well to cure Leber’s optic atrophy, tobacco amblyopia, and cyanide poisoning as well as to prevent and treat pernicious anemia. They also work well as an antidote in situations of cyanide poisoning. A deadly illness called pernicious anemia is caused by a vitamin B12 shortage that impairs the production of healthy red blood cells and the appropriate operation of the neurological system. 4 Some people have auto-immune responses that prevent the generation of an intrinsic factor protein, which is a component of healthy gastric secretion. It is necessary for the absorption of vitamin B12, and its absence will result in clinical symptoms of a deficit. Loss of B12 absorption could also result from stomach surgeries that damage cells that produce intrinsic factor. In addition, a number of illnesses, including HIV, Crohn’s disease, and celiac disease, might impair the absorption of vitamin B12. Other causes include the improper kinds of bacteria in the small intestine, some medications, and tapeworms that feed on vitamin B12. 5

OHCbl is listed as an anti-anemic in the list of important medications for children issued by the W.H.O. because it is safe, cost-effective, and effective against pernicious anemia.

The hydroxocobalamin antidote for cyanide poisoning has demonstrated significant advantages over other antidotes. It responds very quickly, its byproducts are non-toxic and rapidly expelled from the body, it may be used safely even with patients who are not poisoned, and it has no effect on the blood’s ability to carry oxygen. It’s been used safely as an antidote to cyanide poisoning for a very long time. 7 The only drawback is that a hospital setting may be required and that it must be delivered intravenously for a considerable amount of time.

Hydroxocobalamin can be used to treat tobacco amblyopia, which is brought on by smoking. When OHCbl was administered intramuscularly (IM) to individuals with it, a noticeable improvement in visual acuity and color vision was noted, and the performance was superior than cyanocobalamin. 8


1.L. D. Smith and U. Garg, “Disorders of vitamins and cofactors,” in Biomarkers in Inborn Errors of Metabolism, Elsevier, 2017, pp. 361–397.
2.C. Paul and D. M. Brady, “Comparative Bioavailability and Utilization of Particular Forms of B12 Supplements With Potential to Mitigate B12-related Genetic Polymorphisms.,” Integr. Med. (Encinitas)., vol. 16, no. 1, pp. 42–49, Feb. 2017.
3.A. G. Freeman, “Optic Neuropathy and Chronic Cyanide Intoxication: A Review,” J. R. Soc. Med., vol. 81, no. 2, pp. 103–106, Feb. 1988.
4.“Pernicious Anemia,” National Heart, Lung, and Blood Institute; National Institutes of Health; U.S. Department of Health and Human Services. [Online]. Available: https://www.nhlbi.nih.gov/health-topics/pernicious-anemia. [Accessed: 16-Aug-2020].
5.P. A. McINTYRE, “Pathogenesis and Treatment of Macrocytic Anemia,” AMA. Arch. Intern. Med., vol. 98, no. 5, p. 541, Nov. 1956.
6.“WHO Model List of Essential Medicines for Children,” World Health Organization Model List of Essential Medicines for Children, 7th List, 2019.
7.M. Dobss, “Cyanide,” in Clinical Neurotoxicology, Elsevier, 2009, pp. 515–522.
8.I. Chisholm, J. Bronte-Stewart, and W. Foulds, “HYDROXOCOBALAMIN VERSUS CYANOCOBALAMIN IN THE TREATMENT OF TOBACCO AMBLYOPIA,” Lancet, vol. 290, no. 7513, pp. 450–451, Aug. 1967.
9.K. Thakkar and G. Billa, “Treatment of vitamin B12 deficiency–Methylcobalamine? Cyancobalamine? Hydroxocobalamin?—clearing the confusion,” Eur. J. Clin. Nutr., vol. 69, no. 1, pp. 1–2, Jan. 2015.
10.E. R. Ahangar and P. Annamaraju, Hydroxocobalamin. Treasure Island (FL): StatPearls Publishing, 2020.
11.G. B. J. GLASS, H. R. SKEGGS, and D. H. LEE, “Hydroxocobalamin,” Blood, vol. 27, no. 2, pp. 234–241, Feb. 1966.
12.C. P. Holstege, “Poisoning Emergencies in Humans,” Encyclopedia of Toxicology, 2nd Edition. 2005.
13.J. Hamel, “A Review of Acute Cyanide Poisoning With a Treatment Update,” Crit. Care Nurse, vol. 31, no. 1, pp. 72–82, Feb. 2011.
14.A. D. Shapeton, F. Mahmood, and J. P. Ortoleva, “Hydroxocobalamin for the Treatment of Vasoplegia: A Review of Current Literature and Considerations for Use,” J. Cardiothorac. Vasc. Anesth., vol. 33, no. 4, pp. 894–901, Apr. 2019.
15.S. N. Fedosov, L. Berglund, N. U. Fedosova, E. Nexø, and T. E. Petersen, “Comparative Analysis of Cobalamin Binding Kinetics and Ligand Protection for Intrinsic Factor, Transcobalamin, and Haptocorrin,” J. Biol. Chem., vol. 277, no. 12, pp. 9989–9996, Mar. 2002.
16.C. Gherasim, M. Lofgren, and R. Banerjee, “Navigating the B 12 Road: Assimilation, Delivery, and Disorders of Cobalamin,” J. Biol. Chem., vol. 288, no. 19, pp. 13186–13193, May 2013.
17.G. Marcoullis and S. Rothenberg, “Macromolecules in the assimilation and transport of cobalamin,” Contemp. Issues Clin. Nutr., vol. V, pp. 59–119, 1983.
18.“Hydroxocobalamin injection package insert.” Parsippany, NJ, Actavis Pharma, Inc.
19.J. A. Begley, P. D. Colligan, and R. C. Chu, “Transcobalamin II Mediated Delivery of Albumin-Bound Hydroxocobalamin to Human Liver Cells,” Exp. Biol. Med., vol. 204, no. 2, pp. 206–210, Nov. 1993.
20.C. Hall, J. Begley, and P. Green-Colligan, “The availability of therapeutic hydroxocobalamin to cells,” Blood, vol. 63, no. 2, pp. 335–341, Feb. 1984.
21.“CYANOKIT.” Product label: CYANOKIT (hydroxocobalamin) injection, powder, lyophilized, for solution [Meridian Medical Technologies, Inc.] Last revised: Dec 2019 [DailyMed].
22.E. R. Ahangar and P. Annamaraju, Hydroxocobalamin. Treasure Island (FL): StatPearls Publishing, 2020.
23.S. Dally and M. Gaultier, “[Anaphylactic shock caused by hydroxocobalamin].,” Nouv. Presse Med., vol. 5, no. 30, p. 1917, Sep. 1976.
24.G. Hovding, “Anaphylactic reaction after injection of vitamin B12.,” BMJ, vol. 3, no. 5610, pp. 102–102, Jul. 1968.
25.“CYANOKIT.” Product label: CYANOKIT (hydroxocobalamin) injection, powder, lyophilized, for solution [Meridian Medical Technologies, Inc.] Last revised: Dec 2019 [DailyMed].
26.O. J. Ayodele, “Megaloblastic Anemia,” in Current Topics in Anemia, InTech, 2018.
27.R. Hesp, I. Chanarin, and C. E. Tait, “Potassium Changes in Megaloblastic Anaemia,” Clin. Sci., vol. 49, no. 1, pp. 77–79, Jul. 1975.
28.J. Chandra et al., “Tremors and thrombocytosis during treatment of megaloblastic anaemia,” Ann. Trop. Paediatr., vol. 26, no. 2, pp. 101–105, Jun. 2006.
29.M. Sutter, N. Tereshchenko, R. Rafii, and G. P. Daubert, “Hemodialysis Complications of Hydroxocobalamin: A Case Report,” J. Med. Toxicol., vol. 6, no. 2, pp. 165–167, Jun. 2010.
30.K. R. Jones, “Hydroxocobalamin (Cyanokit),” Adv. Emerg. Nurs. J., vol. 30, no. 2, pp. 112–121, Apr. 2008.
31.E. J. D. Roderique, A. A. Gebre-Giorgis, D. H. Stewart, M. J. Feldman, and A. L. Pozez, “Smoke Inhalation Injury in a Pregnant Patient,” J. Burn Care Res., vol. 33, no. 5, pp. 624–633, 2012.
32.“BREASTFEEDING AND MATERNAL MEDICATION Recommendations for Drugs in the Eleventh WHO Model List of Essential Drugs.”
33.“BCG live – Drug Summary,” PDR, LLC. .
34.“Natural Medicines Comprehensive Database.” [Online]. Available: https://naturalmedicines.therapeuticresearch.com/. [Accessed: 29-Aug-2020].
35.H. F. Pierson, J. M. Fisher, and M. Rabinovitz, “Depletion of Extracellular Cysteine with Hydroxocobalamin and Ascorbate in Experimental Murine Cancer Chemotherapy,” Cancer Res., vol. 45, no. 10, pp. 4727 LP – 4731, Oct. 1985.
36.D. R. Buvat, “Use of metformin is a cause of vitamin B12 deficiency.,” Am. Fam. Physician, vol. 69, no. 2, pp. 264; author reply 264, 266, Jan. 2004.
37.W. A. Bauman, S. Shaw, E. Jayatilleke, A. M. Spungen, and V. Herbert, “Increased intake of calcium reverses vitamin B12 malabsorption induced by metformin.,” Diabetes Care, vol. 23, no. 9, pp. 1227–31, Sep. 2000.
38.“Vitamin B12 Fact Sheet for Health Professionals.” [Online]. Available: https://ods.od.nih.gov/factsheets/vitamin B12-HealthProfessional/#en86. [Accessed: 29-Aug-2020].
39.“Nursing Central,” Unbound Medicine, Inc. [Online]. Available: https://nursing.unboundmedicine.com/nursingcentral/view/Davis-Drug-Guide/109246/13/hydroxocobalamin. [Accessed: 08-Feb-2020].
40.J. E. Dimmel, A. Patel, J. F. Clark, V. S. Bhave, E. Samuel, and V. Mody, “Vitamins, amino acids, and drugs and formulations used in nutrition,” 2019, pp. 387–400.
41.W. Uhl, A. Nolting, G. Golor, K. Ludwig Rost, and A. Kovar, “Safety of Hydroxocobalamin in Healthy Volunteers in a Randomized, Placebo-Controlled Study,” Clin. Toxicol., vol. 44, no. sup1, pp. 17–28, Jan. 2006.

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