Cyanocobalamin

Cyanocobalamin
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gloria Picoy [2]

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Overview

Cyanocobalamin is a vitamin B combination that is FDA approved for the treatment of cobalamin deficiency, malabsorption of cyanocobalamin and pernicious anemia, prophylaxis cobalamin deficiency, and diagnosis for Schilling test. Common adverse reactions include injection site pain, arthralgia, dizziness, headache and nasopharyngitis..

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

• Pernicious anemia

• 100 mcg daily for 6 or 7 days intramuscular
• Same amount on alternate days for 7 days
• Then every 3 to 4 days for another 2 to 3 weeks

This regimen should be followed by 100 mcg monthly for life. Folic acid should be administered concomitantly if needed.

• Patients with Normal Intestinal Absorption

• Where the oral route is not deemed adequate, initial treatment similar to that for patients with pernicious anemia may be indicated depending on the severity of the deficiency.
• Chronic treatment should be with an oral B12 preparation.
• If other vitamin deficiencies are present, they should be treated.

• Schilling Test

• The flushing dose is 1000 mcg.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Cyanocobalamin in adult patients.

Non–Guideline-Supported Use

• AIDS virus infection associated with pregnancy

• As part of a daily multivitamin supplement
• Dosage: 40ug

• Hyperhomocysteinemia

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

• Pernicious anemia

• 30 to 50 mcg IM daily for 2 or more weeks
• Then 100 mcg monthly to sustain remission

• Cobalamin deficiency

• 1000 mcg/day orally or 30 to 50 mcg intramuscular daily for 2 or more weeks
• Then 100 mcg monthly to sustain remission

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Cyanocobalamin in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Cyanocobalamin in pediatric patients.

Contraindications

Sensitivity to cobalt and/or vitamin B12

Warnings

• Patients with early Leber's disease (hereditary optic nerve atrophy) who were treated with cyanocobalamin suffered severe and swift optic atrophy.

• Hypokalemia and sudden death may occur in severe megaloblastic anemia which is treated intensely.

• Anaphylactic shock and death have been reported after parenteral vitamin B12 administration. An intradermal test dose is recommended before Cyanocobalamin Injection, USP is administered to patients suspected of being sensitive to this drug.

• This product contains Benzyl Alcohol, this has been reported to be associated with a fatal "Gasping Syndrome" in premature infants.

• This product contains aluminum that may be toxic. Aluminum may reach toxic levels with prolonged parenteral administration if kidney function is impaired. Premature neonates are particularly at risk because their kidneys are immature, and they require large amounts of calcium and phosphate solutions, which contain aluminum. Research indicates that patients with impaired kidney function, including premature neonates, who receive parenteral levels of aluminum at greater than 4 to 5 mcg/kg/day accumulate aluminum at levels associated with central nervous system and bone toxicity. Tissue loading may occur at even lower rates of administration.

Adverse Reactions

Clinical Trials Experience

Generalized

• Anaphylactic shock and death have been reported with administration of parenteral vitamin B12.
• Feeling of swelling of entire body

Cardiovascular

• Pulmonary edema and congestive heart failure early in treatment
• Peripheral vascular thrombosis.

Hematological

• Polycythemia vera

Gastrointestinal

• Mild transient diarrhea

Dermatological

• Itching
• Transitory exanthema

Postmarketing Experience

There is limited information regarding Cyanocobalamin Postmarketing Experience in the drug label.

Drug Interactions

• Persons taking most antibiotics, methotrexate and pyrimethamine invalidate folic acid and vitamin B12 diagnostic blood assays.

• Colchicine para-aminosalicylic acid and heavy alcohol intake for longer than 2 weeks may produce malabsorption of vitamin B12.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): C Adequate and well-controlled studies have not been done in pregnant women. However, vitamin B12 is an essential vitamin and requirements are increased during pregnancy. Amounts of vitamin B12 that are recommended by the Food and Nutrition Board, National Academy of Science-National Research Council for pregnant women (4 mcg daily) should be consumed during pregnancy.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Cyanocobalamin in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Cyanocobalamin during labor and delivery.

Nursing Mothers

Vitamin B12 is known to be excreted in human milk. Amounts of vitamin B12 that are recommended by the Food and Nutrition Board, National Academy of Science-National Research Council for lactating women (4 mcg daily) should be consumed during lactation.

Pediatric Use

Intake in children should be in the amount (0.5 to 3 mcg daily) recommended by the Food and Nutrition Board, National Academy of Science-National Research Council.

Geriatic Use

There is no FDA guidance on the use of Cyanocobalamin in geriatric settings.

Gender

There is no FDA guidance on the use of Cyanocobalamin with respect to specific gender populations.

Race

There is no FDA guidance on the use of Cyanocobalamin with respect to specific racial populations.

Renal Impairment

This product contains aluminum that may be toxic. Research indicates that patients with impaired kidney function, including premature neonates, who receive parenteral levels of aluminum at greater than 4 to 5 mcg/kg/day accumulate aluminum at levels associated with central nervous system and bone toxicity. Tissue loading may occur at even lower rates of administration.

Hepatic Impairment

There is no FDA guidance on the use of Cyanocobalamin in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Cyanocobalamin in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Cyanocobalamin in patients who are immunocompromised.

Administration and Monitoring

Administration

• Intramuscular

Monitoring

There is limited information regarding Cyanocobalamin Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Cyanocobalamin and IV administrations.

Overdosage

No overdosage has been reported with this drug.

Pharmacology

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Mechanism of Action

Cyanocobalamin exhibits a hematopoietic activity similar to the anti-anemia factor found in purified extract of the liver. Vitamin B12 is essential to growth, cell reproduction, hematopoiesis, and nucleoprotein and myelin synthesis.

Structure

The chemical name is 5,6-dimethyl-benzimidazolyl cyanocobamide; the molecular formula is C63H88CoN14O14P. The cobalt content is 4.34%. The molecular weight is 1355.39.

The structural formula is represented below.

Pharmacodynamics

There is limited information regarding Cyanocobalamin Pharmacodynamics in the drug label.

Pharmacokinetics

Cyanocobalamin is quantitatively and rapidly absorbed from intramuscular and subcutaneous sites of injection; the plasma level of the compound reaches its peak within 1 hour after intramuscular injection. Absorbed vitamin B12 is transported via specific B12 binding proteins, transcobalamin I and II to the various tissues. The liver is the main organ for vitamin B12 storage.

Within 48 hours after injection of 100 or 1000 mcg of vitamin B12, 50 to 98% of the injected dose may appear in the urine. The major portion is excreted within the first eight hours. Intravenous administration results in even more rapid excretion with little opportunity for liver storage.

Gastrointestinal absorption of vitamin B12 depends on the presence of sufficient intrinsic factor and calcium ions. Intrinsic factor deficiency causes pernicious anemia, which may be associated with subacute combined degeneration of the spinal cord. Prompt parenteral administration of vitamin B12 prevents progression of neurologic damage.

The average diet supplies about 5 to 15 mcg/day of vitamin B12 in a protein-bound form that is available for absorption after normal digestion. Vitamin B12 is not present in foods of plant origin, but is abundant in foods of animal origin. In people with normal absorption, deficiencies have been reported only in strict vegetarians who consume no products of animal origin (including no milk products or eggs).

Vitamin B12 is bound to intrinsic factor during transit through the stomach; separation occurs in the terminal ileum in the presence of calcium, and vitamin B12 enters the mucosal cell for absorption. It is then transported by the transcobalamin binding proteins. A small amount (approximately 1% of the total amount ingested) is absorbed by simple diffusion, but this mechanism is adequate only with very large doses. Oral absorption is considered too undependable to rely on in patients with pernicious anemia or other conditions resulting in malabsorption of vitamin B12.

Nonclinical Toxicology

Long term studies in animals to evaluate carcinogenic potential have not been done. There is no evidence from long-term use in patients with pernicious anemia that cyanocobalamin is carcinogenic. Pernicious anemia is associated with an increased incidence of carcinoma of the stomach, but this is believed to be related to the underlying pathology and not to treatment with cyanocobalamin.

Clinical Studies

During the initial treatment of patients with pernicious anemia, serum potassium must be observed closely the first 48 hours and potassium replaced if necessary.

Hematocrit, reticulocyte count, vitamin B12, folate and iron levels should be obtained prior to treatment. Hematocrit and reticulocyte counts should be repeated daily from the fifth to seventh days of therapy and then frequently until the hematocrit is normal. If folate levels are low, folic acid should also be administered. If reticulocytes have not increased after treatment or if reticulocyte counts do not continue at least twice normal as long as the hematocrit is less than 35%, diagnosis or treatment should be reevaluated. Repeat determinations of iron and folic acid may reveal a complicating illness that might inhibit the response of the marrow.

Patients with pernicious anemia have about 3 times the incidence of carcinoma of the stomach as the general population, so appropriate tests for this condition should be carried out when indicated.

How Supplied

Cyanocobalamin Injection, USP 1000 mcg/mL:

• 1 mL Fill in a 2 mL Vial

• NDC 0517-0031-25
• Boxes of 25

• 10 mL Multiple Dose Vial

• NDC 0517-0032-25
• Boxes of 25

• 30 mL Multiple Dose Vial

• NDC 0517-0130-05
• Boxes of 5

Storage

Store at 20°-25°C (68°-77°F)

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

Patients with pernicious anemia should be informed that they will require monthly injections of vitamin B12 for the remainder of their lives. Failure to do so will result in return of the anemia and in development of incapacitating and irreversible damage to the nerves of the spinal cord. Also, patients should be warned about the danger of taking folic acid in place of vitamin B12, because the former may prevent anemia but allow progression of subacute combined degeneration.

A vegetarian diet which contains no animal products (including milk products or eggs) does not supply any vitamin B12. Patients following such a diet, should be advised to take oral vitamin B12 regularly. The need for vitamin B12 is increased by pregnancy and lactation. Deficiency has been recognized in infants of vegetarian mothers who were breast fed, even though the mothers had no symptoms of deficiency at the time.

Precautions with Alcohol

Colchicine para-aminosalicylic acid and heavy alcohol intake for longer than 2 weeks may produce malabsorption of cyanocobalamin.

Brand Names

• Cobal
• Cobolin-M
• Depo-Cobolin
• LA-12
• Nascobal
• Neuroforte-R
• Twelve Resin-K
• Vita #12

Look-Alike Drug Names

There is limited information regarding Cyanocobalamin Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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