Cyanocobalamin which is famously known as vitamin B-12 is a water-soluble vitamin which is found in foods like shellfish, fish, dairy products and meat. Even though the terms cyanocobalamin and vitamin B-12 are often used interchangeably, another drug substance that is known as hydroxocobalamin also contains the vitamin B-12. Cyanocobalamin can be used to treat a number of conditions which include; vitamin B-12 deficiency and pernicious anaemia. It can also be used to determine vitamin B-12 in a schilling test. In healthy individuals, vitamin B-12 deficiency is very rare. The people that are at risk of this disorder are patients with malabsorption, the elderly and strict vegetarians. If vitamin B-12 deficiency is not treated early in individuals using vitamin B-12 supplements, they may be at risk of developing intestinal problems, anaemia and even an irreversible damage to the nerves. Parenteral and nasal therapies are more efficient administration techniques for this therapy than oral administration because some individuals lack the Intrinsic Factor which is an endogenous substance produced in the stomach to facilitate the absorption of vitamin B-12. Some patients may not be able to absorb Vitamin B-12 due to a dysfunction or surgical removal of some parts of the intestine where vitamin B-12 should be absorbed.
The FDA approved cyanocobalamin in 1944, its intranasal gel solution from Nascobar was later approved in November 1996 for treating the deficiency of vitamin B-12. Later in 2002, it was approved in for treating this condition in patients infected with HIV/AIDs and Crohn’s disease. In January 2005, a nasal spray also named ‘Nascobar’ was approved by the FDA and the final spray ‘Calomist’ approved in 2007.
THE MODE OF ACTION OF CYANOCOBALAMIN.
Vitamin B-12 is very important in facilitating cell reproduction, growth, hematopoiesis and the synthesis of nucleoproteins and myelin. Epithelial cells, myeloid cells and the cells of the bone marrow have a higher requirement for vitamin B-12 because they undergo great and rapid cell division. In tissues, vitamin B-12 is converted into a co-enzyme which facilitates the metabolism of fats and carbohydrates. Some conditions that may arise as a result of vitamin B-12 deficiency include Gi lesions, neurological damages and megaloblastic anaemia. The lack of the intrinsic factor which facilitates an active transport of vitamin B-12 during its absorption can also lead to pernicious anaemia.
THE PHARMACOKINETICS OF CYANOCOBALAMIN, VITAMIN B-12
Vitamin B-12 in form of hydroxocobalamin can only be administered through injections while cyanocobalamin can be administered orally, intranasally and parenterally or intramuscularly using injections. After its absorption into the body, Vitamin B-12 binds to transcobalamin which is a carrier protein. It is then transported and distributed to the sites where it is required by the body. It is usually partially stored in the liver as a coenzyme B-12 and some significant amounts stored in the bone marrow. This vitamin can cross over through the placenta to a foetus and it can also be distributed in breast milk. Vitamin B-12 has a lifetime of about 400 days in the liver. It is eliminated through the bile and the excess comes out untransformed through the urine.
ROUTE SPECIFIC PHARMACOKINETICS.
Oral administration. When vitamin B-12 is taken into the body orally, it is transported in the digestive tract but for it to be absorbed and assimilated, it depends on an important component, the Intrinsic Factor. The Intrinsic Factor is produced in the stomach and it is responsible for dissociating cobalamin from its dietary sources in food. The intrinsic factor passes on to the small intestines attaches to the receptor sites on the ileum then facilitates the active transport of vitamin B-12 into the system. For the effective attachment of the Intrinsic factor to the receptor sites, the pH and calcium levels should be above 6. After the receptor sites become saturated with the Vitamin B-12, absorption occurs through normal diffusion. An oral administration of Vitamin B-12 together with the Intrinsic Factor has proven to greatly increase the levels of cobalamin in patients. However, a substantial number of patients can develop intestinal antibodies to the Intrinsic Factor. Proton Pump Inhibiting drugs like lansoprazole and omeprazole can interfere with the oral absorption of vitamin B-12 because they impair the secretion of pepsin and gastric acid which are presumed to be necessary for releasing vitamin B-12 from its protein binding sites in food.
When administered intranasally or intramuscularly, vitamin B-12 is absorbed straight into the bloodstream where it performs its functions.
The Following Contraindications and Precautions should be considered during the administration of this medication.
There are numerous situations when you should completely avoid this medication or have it administered under strict monitoring and evaluation from a qualified physician because it can lead to very serious and adverse effects.
You should never take the vitamin B-12 medication if you have a hypersensitive reaction to cyanocobalamin, cobalt and any other medical components present in the medication.
You should avoid cyanocobalamin if you suffer from Leber’s disease, a hereditary optic nerve atrophy, because this condition can worsen if you heighten your cyanocobalamin levels.
Cyanocobalamin contains benzyl alcohol so you should be cautious in case you react hypersensitively to ethanol.
You should never use Folic acid, vitamin B-9 as a substitute for cyanocobalamin, even though it has proven to improve the condition of vitamin B-12 megaloblastic anaemia, exclusive use of Vitamin B-9 for the treatment of this condition can result in an irreversible and progressive damage to your neurones.
Certain conditions like renal failure, concurrent renal and hepatic diseases, serious medical infections and the use of drugs that suppress the activities of the bone marrow can interfere with the response of the body to the cyanocobalamin treatment. If you suffer from these conditions, you might require higher doses during your treatment so that you can attain the normal effects but this is not recommended.
Representative studies have not been conducted on the effects of this treatment on pregnant and lactating women. No maternal or foetal complications have been reported so far. Cyanocobalamin is distributed in breast milk in similar amounts to that of the plasma in the mother’s blood. This allows breastfeeding infants to take in adequate amounts of this vitamin into their blood stream. This has its advantages since the requirements of vitamin B-12 increases substantially during lactation in mothers. This benefits the infants too.
There are numerous factors known to impede the effective absorption of cyanocobalamin. Before you decide to start on this treatment, you should inform your physician of all the drugs, herbs, herbs, hereditary supplements and any other substances that you use including illegal drugs, alcohol and cigarettes. Some substances that might not interact well with cyanocobalamin are.
– Drugs like para-aminosalicylic acid, colchicine, omeprazole and other proton pump inhibitors, chloramphenicol, antiinfective agents like pyrimethamine and any other medication that is known to suppress bone marrow activities, e.g. myelosuppressive antineoplastic agents.
– You should avoid heavy consumption of ethanol since it can limit the absorption of cyanocobalamin.
Some Adverse Reactions And Side Effects of this medication.
In a majority of cases, cyanocobalamin is not toxic in nature even in large doses. Some adverse side effects that have been reported from the use of this drug include; nausea or vomiting, headaches, paresthesias and rhinitis. The reactions due to an intramuscular injection can include; anxiety, mild diarrhoea, nervousness, ataxia, pruritus and a feeling of swelling of parts on your whole body.
Congestive heart failure and pulmonary oedema are some conditions that have been reported in early treatment periods using parenteral cyanocobalamin. This may be as a result of the high volume of blood that is produced by the action of cyanocobalamin. This can also cause peripheral vascular thrombosis and angioedema or angioedema related conditions.
Adverse reactions that are related to intranasal administration of this treatment can include; dizziness, headaches, rhinorrhoea, bronchitis, nasal pains, rashes, nasal discomfort, back pains, asthma, cough, hypersomnia, epistaxis, malaise, post nasal drips, procedural pains and tooth abseil.
You should always remember to contact your physician immediately in any case you develop some signs of hypersensitive reactions to this medication. These can include; skin rashes, swelling of body parts, wheezing, chest tightness, difficulty in breathing and passing out.
What is the best method for the administration of this medication?
The most effective way to administer this medication is through injections deep into the skin. You can do this by yourself but it is best to seek medical help and assistance from a qualified physician. If you ever happen to miss a dose. reschedule your appointment as soon as possible. If you take it personally, administer the treatment as soon as you can.
Cyanocobalamin (Vitamin B12) is usually prescribed for:helping in the growth of healthy nerve cells, blood cells and proteins in the body. It also helps with metabolism of fats and carbohydrates and it is a treatment for patients who cannot naturally absorb vitamin B12.
The available Dosage strengths of Cyanocobalamin are:
5-mL vial. 2000-mcg / mL 30 mL vial. 2,000 mcg / mL
The form available for Cyanocobalamin is an Injection Solution.
Our Pharmacy’s solutions are compounded under very stringent USP 797 guidelines. We practise sterile compounding, and endotoxin, potency and pH testing are performed on every batch before release. Our quality assurance procedure ensures consistency and uniformity in all compounds we dispense. Contact us today for more information.