Hydroxocobalamin
intravenous | |
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Pharmacokinetic data | |
Protein binding | Very high (90%) |
Metabolism | Primarily liver, cobalamins are absorbed in the ileum and stored in the liver. |
Elimination half-life | ~6 days |
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Hydroxocobalamin, also known as vitamin B12a and hydroxycobalamin, is a
Side effects are generally few.
Hydroxocobalamin was first isolated in 1949.
Medical uses
Vitamin B12 deficiency
Standard therapy for treatment of vitamin B12 deficiency has been intramuscular (IM) or intravenous (IV) injections of hydroxocobalamin (OHCbl), since the majority of cases are due to malabsorption by the enteral route (gut).
In a newly diagnosed vitamin B12-deficient patient, normally defined as when serum levels are less than 200 pg/ml, daily IM injections of hydroxocobalamin up to 1,000 μg (1 mg) per day are given to replenish the body's depleted cobalamin stores. In the presence of neurological symptoms, following daily treatment, injections up to weekly or biweekly are indicated for six months before initiating monthly IM injections. Once clinical improvement is confirmed, maintenance supplementation of B12 will generally be needed for life.[citation needed]
Cyanide poisoning
Hydroxocobalamin is first line therapy for people with cyanide poisoning.[2] Hydroxocobalamin converts cyanide to the much less toxic cyanocobalamin. Cyanocobalamin is renally cleared. The use of hydroxocobalamin became first line due to its low adverse risk profile, rapid onset of action, and ease of use in the prehospital setting.[14]
Injectable hydroxocobalamin
Injection of hydroxocobalamin is used to rectify the following causes of vitamin B12 deficiency (list taken from the drug prescription label published by the
- Dietary deficiency of vitamin B12 occurring in strict vegetarians and in their breastfedinfants (isolated vitamin B12 deficiency is very rare)
- Malabsorption of vitamin B12 resulting from damage to the stomach, where nontropical sprue(celiac disease).
- Inadequate secretion of intrinsic factor, resulting from lesions that destroy the iron deficiency, and subtotal gastrectomy)
- Structural lesions leading to vitamin B12 deficiency, including regional ileitis, ileal reactions, and malignancies
- Competition for vitamin B12 by Diphyllobothrium latum) absorbs huge quantities of vitamin B12, and infested patients often have associated gastric atrophy. The blind loop syndrome may produce deficiency of vitamin B12 or folate.
- Inadequate use of vitamin B12, which may occur if neoplasia
Pernicious anemia is the most common cause of vitamin B12 deficiency.[15] While it technically refers to anemia caused specifically by autoimmune deficiency of intrinsic factor, it is commonly used to refer to B12-deficient anemia as a whole, regardless of cause.
Side effects
The literature data on the acute toxicity profile of hydroxocobalamin show it is generally regarded as safe with local and systemic exposure. The ability of hydroxocobalamin to rapidly scavenge and detoxify cyanide by chelation has resulted in several acute animal and human studies using systemic hydroxocobalamin doses at suprapharmacological doses as high as 140 mg/kg to support its use as an
The US FDA at the end of 2006 approved the use hydroxocobalamin as an injection for the treatment of cyanide poisoning.The drug causes a reddish discoloration of the urine (chromaturia), which can look like blood in the urine.[18]
Properties
Hydroxocobalamin acetate occurs as odorless, dark-red
Mechanism of action
Vitamin B12 refers to a group of compounds called cobalamins that are available in the human body in a variety of mostly interconvertible forms. Together with
- the mitochondrial succinate, which links lipid and carbohydrate metabolism, and
- the activation of 5-methyltetrahydrofolate.[19]
Cobalamins are characterized by a
References
- ^ ISBN 9789241547659.
- ^ a b c d e f g "Vitamin B12". The American Society of Health-System Pharmacists. Archived from the original on 30 December 2016. Retrieved 8 December 2016.
- PMID 24994676.
- ^ "Hydroxocobalamin 1mg in 1ml solution for injection - Summary of Product Characteristics (SPC) - (eMC)". www.medicines.org.uk. Archived from the original on 30 December 2016. Retrieved 30 December 2016.
- ^ "Hydroxocobalamin Use During Pregnancy". Drugs.com. Archived from the original on 1 January 2017. Retrieved 30 December 2016.
- ISBN 9781442564411. Archivedfrom the original on 31 December 2016.
- ^ a b "Office of Dietary Supplements - Dietary Supplement Fact Sheet: Vitamin B12". ods.od.nih.gov. 11 February 2016. Archived from the original on 31 December 2016. Retrieved 30 December 2016.
- PMID 24361556.
- ISBN 9781420050165. Archivedfrom the original on 31 December 2016.
- hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ISBN 9783527303854.
- PMID 25117994.
- PMID 3277892.
- S2CID 24097516. Archived from the original(PDF) on 7 November 2022. Retrieved 23 July 2021.
- PMID 32644742.
- PMID 8492341.
- S2CID 19462753.
- PMID 29881591.
- ^ ISBN 978-0-8385-1301-9.
- ISBN 978-0-07-135469-1.
- PMID 8154512.