B12 Ankermann

Round, biconvex, white coated tablet.
1 coated tablet contains Cyanocobalamin (Vitamin B12) 1000 µg.
Excipients with known effect: Lactose, sucrose.
Excipients/Inactive Ingredients: Povidon K 30, stearic acid, montan glycol wax, lactose monohydrate, sucrose, acacia, dried dispersion, talc, calcium carbonate, titanium dioxide, kaolin, heavy, macrogol 6000, macrogolglycerol hydroxystearate, sodium laurilsulfate, croscarmellose sodium, hypromellose, hydroxypropylcellulose, triglycerides, medium-chain.
Gluten-free, contains lactose.

Pharmacotherapeutic group: Anti-anaemic, vitamin B12. ATC code: B03BA01.
Pharmacology: Pharmacodynamics: As a member of the prosthetic groups of methylmalonyl CoA isomerase, vitamin B12 is needed to convert propionic acid into succinic acid. Furthermore, alongside folic acid, vitamin B12 is involved in the formation of labile methyl groups which are transmitted to other methyl acceptors via transmethylation processes. The vitamin also influences the synthesis of nucleic acids, in particular during haematopoiesis and other cell maturation processes.
Availability and requirement: The human body is unable to synthesize vitamin B12, and it is absorbed from food. Foods which contain vitamin B12 are liver, kidneys, heart, fish, oysters, milk, egg yolk and meat. Vitamin B12 is administered for therapeutic purposes in the form of cyanocobalamin and/or hydroxocobalamin. Both are pro-drugs that the body converts into the active forms methylcobalamin and 5-adenosylcobalamin. The daily requirement of B12 amounts to around 1 μg.
Signs of deficiency: An impairment or lack of vitamin B12 absorption will eventually result in clinical symptoms if plasma levels fall below 200 pg/ml. The consequences are megaloblastic anaemia and neurological deficits in the peripheral and central nervous system. Polyneuropathy may be present in combination with lesions in the dorsal columns of the spinal cord and psychological disorders. Early signs of deficiency may include fatigue and paleness, tingling in hands and feet, an unsteady gait and reduced physical strength.
Symptoms caused by a vitamin B12 deficiency can only be corrected by the intake of Vitamin B12.
Causes of deficiency: Pernicious anaemia; atrophic gastritis; celiac disease; malabsorption, following partial ventricle resection; as a result of blind-loop syndrome; long-term treatments using active substances which can lead to a reduction in vitamin B12 levels (e.g. gastric acid reducing drugs, aminosalicylates and metformin).
Pharmacokinetics: Vitamin B12 is absorbed via two different routes: Active absorption in the small intestine involving intrinsic factor. The transportation of vitamin B12 into the tissues involves attachment to transcobalamins which are substances from the plasma-beta globulins group.
Independently of intrinsic factor, the vitamin can also pass into the bloodstream by means of passive diffusion via the gastrointestinal tract or the mucous membranes. Approximately 1-3% of orally administered quantities enter the blood in a dose-linear fashion. Thus, for high oral doses (~ 1000 µg/day), adequate absorption is provided even in patients with a lack of intrinsic factor.
Up to 90% of body stores are in the liver, where the vitamin is stored as the active coenzyme with a turnover rate of 0.5 to 0.8 μg daily. In healthy omnivorous adult humans, the total body content of vitamin B12 is about 3 to 5 mg. It will generally take 3-5 years for clinical signs of vitamin B12 deficiency to occur.
Vitamin B12 is excreted mainly by the gall bladder and up to 1 μg is reabsorbed via the enterohepatic circulation. If the body's storage capacity is exceeded due to high doses, in particular subsequent to parenteral administration, the non-retained portion is excreted in the urine.
Toxicology: Preclinical safety data: No toxicity was shown in animal studies even at very high doses. There are no reports of any adverse effects relating to the administration of cyanocobalamin on male and female pre- and postnatal development and no reports of supplement-associated teratogenic, mutagenic or carcinogenic effects.

For the treatment of haemotological and neurological symptoms resulting from vitamin B12 deficiencies.

Posology: Adults: daily dosage is 1 coated tablet cyanocobalamin 1000 µg for the treatment of clinical vitamin B12 deficiency. In severe cases an initial treatment with 2 coated tablets cyanocobalamin 1000 µg is recommended. In case of severe neurological symptoms, initial parenteral application is recommended.
Children and adolescents: In children and adolescents, oral cyanocobalamin in daily doses of up to 1000 µg are recommended as an alternative to parenteral therapy of vitamin B12 deficiency.
Elderly: Normal dosage regimens are recommended in the elderly.
Patients with hepatic impairment: Pharmacokinetic data and clinical experience on patients with hepatic impairment are not available. Safety and efficacy in patients with hepatic impairment have not been established.
Method of administration: The coated tablet should be swallowed whole with some fluid, preferably in the morning on an empty stomach. The treatment duration is determined by the therapeutic response.
A targeted diagnostics and therapy control should adjust the patient to an optimal dose of cyanocobalamin.

Vitamin B12 has a large therapeutical range. Poisonings or overdose symptoms are not known. Cases of accidental overdose should be treated symptomatically, if necessary.

Hypersensitivity to the active substance or to any of the excipients listed in Description.
Cyanocobalamin 1000 µg coated tablets must not be used in patients who are in need of cyanide detoxification (e.g. patients with tobacco amblyopia or retrobulbar neuritis in pernicious anaemia). In this situation, other cobalamin derivatives should be administered.
B12-deficient individuals who are at risk for Leber's optic atrophy should not be given cyanocobalamin to treat the B12 deficiency.

The following should be noted in the case of blood-formation disorders and/or neurological disorders: Due to the serious nature of the disease and the possible sequelae in the event of an inadequate response or lack of patient compliance with the treatment plan, the success of oral treatment should generally be strictly monitored. It is recommended that seven days after the start of treatment, the symptoms, reticulocyte count, a blood count (including haemoglobin -H_b and haematocrit -H_k levels) are checked, as well as the mean corpuscular volume (MCV).
Then the symptoms, blood count and MCV should be monitored at 4-weekly intervals for the first three months of treatment and if patient compliance is good, again at six-monthly/annual intervals.
If a lack of patient compliance is suspected, more frequent controls may be necessary. Caution is advised in patients with folic acid deficiency. Folate deficiency may blunt therapeutic response. In these patients the use of Cyanocobalamin 1000 µg coated tablets is not indicated.
Patients with rare hereditary galactose intolerance, lactase deficiency, glucose-galactose malabsorption, rare hereditary fructose intolerance or sucrase-isomaltase deficiency should not take Cyanocobalamin 1000 µg coated tablets.
Effects on ability to drive and use machines: None.

Evidence suggests that vitamin B12 supplementation during pregnancy and lactation poses minimal risk to the mother and infant.
However, Cyanocobalamin 1000 µg should not be used to treat megaloblastic anaemia of pregnancy that is caused by folate deficiency.

Skin and subcutaneous tissue disorders: Uncommon (0.1-1%): Severe hypersensitivity reactions which can manifest as hives, skin rash or itching of large areas of the body.
Not known: Acneiform skin reactions.
General disorders and administration site conditions: Not known: Fever.

The absorption of vitamin B12 may be impaired by proton pump inhibitors (e.g. omeprazol), histamine H2-antagonists (e.g. cimetidine), colchicine, neomycin, and aminosalicylic acid.
Serum levels may also be lowered by oral contraceptives, but this interaction is unlikely to have clinical significance.
Chloramphenicol may attenuate the effect of vitamin B12 in anaemia.
Steroid drugs, such as prednisone, have been reported to increase the absorption of vitamin B12 in patients with pernicious anaemia.
Nitrous oxide (N₂O) induces a functional vitamin B12 deficiency.
Metformin may lower the serum levels of vitamin B12.

Special precautions for disposal and other handling: None.
Incompatibilities: None previously known for oral use.

Do not store above 30°C.
Shelf-life: 2 years.

Vitamins & Minerals (Pre & Post Natal) / Antianemics

B03BA01 - cyanocobalamin ; Belongs to the class of vitamin B12 (cyanocobalamin and analogues). Used in the treatment of anemia.

NDD