Acti-B12 - General Information
Injectable form of vitamin B 12 that has been used therapeutically to treat vitamin B 12 deficiency.
Pharmacology of Acti-B12
Acti-B12 is a synthetic, injectable form of Vitamin B12. Acti-B12 is actually a precursor of two cofactors or vitamins (Vitamin B12 and Methylcobalamin) which are involved in various biological systems in man. Vitamin B12 is required for the conversion of methylmalonate to succinate. Deficiency of this enzyme could therefore interfere with the production of lipoprotein in myelin sheath tissue and so give rise to neurological lesions. The second cofactor, Methylcobalamin, is necessary for the conversion of homocysteine to methionine which is essential for the metabolism of folic acid. Deficiency of tetrahydrafolate leads to reduced synthesis of thymidylate resulting in reduced synthesis of DNA which is essential for cell maturation. Vitamin B12 is also concerned in the maintenance of sulphydryl groups in reduced form, deficiency leading to decreased amounts of reduced SH content of erythrocytes and liver cells. Overall, vitamin B12 acts as a coenzyme for various metabolic functions, including fat and carbohydrate metabolism and protein synthesis. It is necessary for growth, cell replication, hematopoiesis, and nucleoprotein as well as myelin synthesis. This is largely due to its effects on metabolism of methionine folic acid, and malonic acid.
Acti-B12 for patients
Cyanokit (hydroxocobalamin for injection) 5 g for intravenous use
Treatment for known or suspected cyanide poisoning
What is Cyanokit?
Cyanokit is an emergency treatment (antidote) used in patients with known or suspected cyanide poisoning. Cyanide is a chemical poison. Cyanide poisoning can happen from:
- breathing smoke from household and industrial fires
- breathing or swallowing cyanide
- having your skin exposed to cyanide
Cyanide poisoning is a life-threatening condition because cyanide stops your body from being able to use oxygen. You can die if your body does not have enough oxygen.
Cyanokit was approved for the treatment of known or suspected cyanide poisoning based on testing:
- how well it worked in animals (It is not ethical to poison people with cyanide in order to test a treatment.)
- its safety in people with cyanide poisoning
How is Cyanokit used?
Cyanokit is given through a vein (intravenous or IV) over 15 minutes by an emergency care provider or doctor. A second dose may be given to you if needed.
What are possible side effects with Cyanokit?
Serious side effects may include:
- allergic reactions Signs of a serious allergic reaction include chest tightness, trouble breathing, swelling, hives, itching, and a rash.
- increased blood pressure
Other side effects may include:
- red colored urine
- red colored skin and mucous membranes, acne-like rash
- nausea, vomiting, diarrhea, bloody stools, trouble swallowing, stomach pain
- throat tightness, dry throat
- headache, dizziness, memory problems, restlessness
- infusion site reaction
- eye swelling, irritation, or redness
- swelling of feet and ankles
- irregular heart heat, increased heart rate
- fluid in lungs
These are not all the side effects with Cyanokit.
After treatment with Cyanokit:
- Skin and urine redness. Skin redness may last up to 2 weeks. Avoid sun exposure while your skin is red. Urine redness may last up to 5 weeks.
- Acne-like rash. An acne-like rash may appear 7 to 28 days after treatment with Cyanokit. This rash usually goes away without any treatment.
- Breastfeeding. Talk to your doctor if you breastfeed. The ingredient in Cyanokit may pass into your breast milk. You and your doctor can decide when and if you can breastfeed your baby again
Talk to your doctor about any side effect that bothers you or that does not go away.
No formal drug interaction studies have been conducted with Cyanokit.
Additional information about Acti-B12
Acti-B12 Indication: For treatment of pernicious anemia and the prevention and treatment of vitamin B12 deficiency arising from alcoholism, malabsorption, tapeworm infestation, celiac, hyperthyroidism, hepatic-biliary tract disease, persistent diarrhea, ileal resection, pancreatic cancer, renal disease, prolonged stress, vegan diets, macrobiotic diets or other restrictive diets. Also for the treatment of known or suspected cyanide poisoning.
Mechanism Of Action: Vitamin B12 exists in four major forms referred to collectively as cobalamins; deoxyadenosylcobalamin, methylcobalamin, hydroxocobalamin, and cyanocobalamin. Two of these, methylcobalamin and 5-deoxyadenosyl cobalamin, are primarily used by the body. Methionine synthase needs methylcobalamin as a cofactor. This enzyme is involved in the conversion of the amino acid homocysteine into methionine. Methionine in turn is required for DNA methylation. 5-Deoxyadenosyl cobalamin is a cofactor needed by the enzyme that converts L-methylmalonyl-CoA to succinyl-CoA. This conversion is an important step in the extraction of energy from proteins and fats. Furthermore, succinyl CoA is necessary for the production of hemoglobin, the substances that carries oxygen in red blood cells.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Hydroxocobalamin
Synonyms: Hydroxocobalamin acetate; Hydroxocobalamin monohydrochloride; Hydroxocobalamin Vitamin B12; Hydroxocobalaminacetat; Hydroxomin; Vitamin B12a
Drug Category: Anti-anemic Agents; Nutritional Supplement
Drug Type: Small Molecule; Approved
Other Brand Names containing Hydroxocobalamin: Alpharedisol; Acti-B12; Cyanokit; Hydro Cobex; Hydroxy Cobal;
Absorption: Readily absorbed from the gastrointestinal tract, except in malabsorption syndromes. Vitamin B12 is absorbed in the lower half of the ileum.
Toxicity (Overdose): Not Available
Protein Binding: Very high (90%). Cobalamins are extensively bound to two specific plasma proteins called transcobalamin 1 and 2; 70% to transcobalamin 1, 5% to transcobalamin 2.
Biotransformation: Primarily hepatic. Cobalamins are absorbed in the ileum and stored in the liver. They continuously undergo enterohepatic recycling via secretion in the bile. Part of a dose is excreted in the urine, most of it in the first 8 hours.
Half Life: Approximately 6 days (peak plasma concentration after 8-12 hours from oral administration)
Dosage Forms of Acti-B12: Solution Oral
Chemical IUPAC Name: Hydroxocobalamin
Chemical Formula: C62H90CoN13O15P-2
Hydroxocobalamin on Wikipedia: http://en.wikipedia.org/wiki/Hydroxocobalamin
Organisms Affected: Humans and other mammals