Hydroxocobalamin (Vitamin B12a)

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Cyanokit, Erycytol, Hepavit; Belgium: Cyanokit; Czech Republic: Cyanokit; Denmark: Cyanokit, Vibeden; Estonia: Cyanokit; Finland: Cohemin Depot, Cyanokit; France: Cyanokit, Dodécavit; Germany: B~12~ Depot, Cyanokit, Depogamma, Vitamin B~12~-Depot; Greece: Articlox, Cyanokit; Hungary: Cyanokit; Ireland: Cyanokit; Italy: Cyanokit, Idroxoc, Neocytamen, OH B~12~; Latvia: Cyanokit; Luxembourg: Forta B~12~, Hydroxo 5.000, Novobedouze; Malta: Hydroxocobalamin; Netherlands: Hydrocobamine, Hydroxocobalamine, Cyanokit; Poland: Cyanokit; Portugal: Cyanokit, OHB~12~; Romania: Cyanokit; Slovakia: Cyanokit; Slovenia: Cyanokit; Spain: Cyanokit, Hidroxicobalamina, Megamilbedoce; Sweden: Behepan, Cyanokit; UK: Cobalin-H, Hydroxocobalamin, Neo-Cytamen.

North America

Canada: Acti-B~12~, Hydro Cobex, Hydroxy Cobal; USA: Cyanokit, Hydroxocobalamin.

Latin America

Brazil: Rubranova; Mexico: Axofor, Duradoce, Nebal.

Asia

Japan: Cobalamin-H, Colsamine S, Docelan, Foliron-H, Fresmin-S, Masblon H, V~12~.

Drug combinations

Hydroxocobalamin, Carisoprodol, Dexamethasone, Piroxicam, and Pyridoxine (Vitamin B~6~)

Other Hydroxocobalamin combinations: Betamethasone; Folic Acid (Vitamin B~9~); Iron Dextran; Phosphate; Procaine; Thiamine (Vitamin B~1~)

Chemistry

Hydroxocobalamin: C~62~H~89~CoN~13~O~15~P. Mw: 1346.36 (1) Cobinamide, dihydroxide, dihydrogen phosphate (ester), mono(inner salt), 3′-ester with 5,6-dimethyl-1-α-D-ribofuranosyl-1H-benzimidazole; (2) Cobinamide dihydroxide dihydrogen phosphate (ester), mono(inner salt), 3′-ester with 5,6-dimethyl-1-α-D-ribofuranosylbenzimidazole. CAS-13422-51-0 (1962).

Pharmacologic Category

Vitamins; Vitamin B Complex. Antidotes. Nutritional Supplement. (ATC-Code: B03BA03; V03AB33).

Mechanism of action

Hydroxocobalamin (vitamin B~12a~) is a precursor to cyanocobalamin (vitamin B~12~). Cyanocobalamin acts as coenzyme for various metabolic functions, including fat and carbohydrate metabolism and protein synthesis, used in cell replication and hematopoiesis. In the presence of cyanide, each hydroxocobalamin molecule can bind one cyanide ion by displacing it for the hydroxo ligand linked to the trivalent cobalt ion, forming cyanocobalamin.

Therapeutic use

Treatment of pernicious anemia and other vitamin B~12~ deficiency states. Dietary supplement particularly in conditions of increased requirements (e.g. pregnancy, thyrotoxicosis, hemorrhage, malignancy, liver or kidney disease). Diagnostic agent for Schilling test. Treatment of cyanide poisoning.

Pregnancy and lactiation implications

There are as yet no adequate, well-controlled studies in pregnant women. Use with caution during pregnancy or lactation.

Unlabeled use

Treatment of neuropathies, multiple sclerosis.

Contraindications

Hypersensitivity to hydroxocobalamin, cyanocobalamin, cobalt, or any component of the formulation.

Warnings and precautions

May cause photosensitivity. Vitamin B~12~ deficiency masks signs of polycythemia vera; vitamin B~12~ administration may unmask this condition. Treatment of severe vitamin B~12~ megaloblastic anemia may result in thrombocytosis and severe hypokalemia, sometimes fatal. Use caution in folic acid-deficient megaloblastic anemia. Blunted therapeutic response to vitamin B~12~ may occur in certain conditions (e.g. infection, uremia, concurrent iron or folic acid deficiency) or in patients on medications with bone marrow-suppressant properties (e.g. chloramphenicol). Approved for use as I.M. injection only.

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