Cyanocobalamin - instructions for use, dose, side effects, contraindications

Vitamin B12. In the body (mainly in the liver) is converted to methylcobalamin and 5-deoxyadenosylcobalamin. Methylcobalamin participates in the homocysteine conversion reaction in methionine and S-adenosylmethionine are key reactions of the metabolism of pyrimidine and purine bases (and, consequently, DNA and RNA). If the vitamin is deficient in this reaction, it can be replaced by methyltetrahydrofolic acid, with folic acid reactions of metabolism being disturbed. 5-deoxyadenosylcobalamin serves as a cofactor in the isomerization of L-methylmalonyl-CoA in succinyl-CoA, an important carbohydrate and lipid metabolism reaction.

Deficiency of vitamin-B 12- leads to disruption of the proliferation, rapidly dividing cells of the hematopoietic tissue and the epithelium, and also to the violation of the formation of the myelin sheath of neurons.

Pharmacokinetics:

In blood cyanocobalamin binds to the trans-balanamines I and II, which

transport it into tissues. It is deposited mainly in the liver. Communication with plasma proteins is 90%. The maximum concentration after subcutaneous and intramuscular injection is achieved after 1 hour.

From the liver is excreted with bile into the intestine and again absorbed into the blood. Half-life is 500 days.It is excreted at normal kidney function - 7-10% by kidneys, about 50% - by the intestine; with a decrease in kidney function - 0-7% in kidneys, 70-100% in the bowels. Penetrates through the placental barrier, into breast milk.

Indications:

Conditions accompanied by a deficiency of vitamin B12: B12-deficiency anemia; in the complex therapy of anemia (including iron deficiency, posthemorrhagic, aplastic, anemia, caused by toxic substances and / or drugs). In complex therapy:

In neurology: neuralgia (including trigeminal neuralgia), polyneuropathy (including alcoholic).

With the preventive purpose - with the appointment of biguanides, PASK, ascorbic acid in high doses, abnormalities of the stomach and intestines with a violation of absorption of vitamin B12 (resection of part of the stomach, small intestine, Crohn's disease, malabsorption syndrome, sprue), radiation sickness.

Contraindications:Hypersensitivity to the drug components, thromboembolism, erythremia, erythrocytosis, pregnancy (there are separate indications of possible teratogenic effects of B vitamins in high doses), lactation period.

Carefully:Angina pectoris, benign and malignant neoplasms, accompanied by megaloblastic anemia and vitamin B12 deficiency, propensity to form blood clots.

Dosing and Administration:

The drug is administered subcutaneously, intramuscularly, intravenously.

Subcutaneously, with B12-deficiency anemia - 100-200 mcg / day every other day; with B12-deficiency anemia with addition of disorders of the nervous system function - 400-500 mcg / day in the first week - daily, then with intervals between administrations up to 5-7 days (concomitantly prescribe folic acid); during the remission, the maintenance dose is 100 mcg / day 2 times a month, in the presence of neurologic symptoms - 200-400 mcg 2-4 times a month.

In acute posthemorrhagic and iron deficiency anemia - 30-100 mcg 2-3 times a week; at aplastic anemia, anemia caused by toxic substances and / or drugs - 100 μg before the onset of clinical and hematological improvement. With violations of the nervous system - 200-400 mcg 2-4 times a month.

In neurology: neuralgia (including trigeminal neuralgia), polyneuropathy (including alcoholic) - 200-500 mcg every other day for 2 weeks.

With the preventive purpose - 60-100 mcg daily for 20-30 days.

To eliminate the deficiency of vitamin B12 is administered intramuscularly (in / m) or intravenously (iv) 1 mg daily for 1-2 weeks.

Young children with alimentary anemia and premature infants undercut 30 mcg daily for 15 days.

Side effects:

Allergic reactions, mental agitation, cardialgia, tachycardia, diarrhea, headache, dizziness, hypercoagulation, violation of purine metabolism.

Overdose:No data available.

Interaction:

Pharmaceutically incompatible with ascorbic acid, heavy metal salts (inactivation of cyanocobalamin), thiamine, pyridoxine, riboflavin (because the cobalt ion contained in the cyanoballamine molecule destroys other vitamins). You can not combine with drugs that increase blood coagulability. The risk of developing allergic reactions increases when combined with thiamine.

Chloramphenicol reduces the hematopoietic response of cyanocobalamin. Do not combine with drugs that increase blood coagulability.

Special instructions:The deficiency of cyanocobalamin should be confirmed diagnostically prior to the prescription of the drug, since it can mask a deficiency of folic acid.During the period of treatment, it is necessary to monitor the parameters of peripheral blood: on the 5th-8th day of treatment, the content of reticulocytes, the concentration of iron is determined. The number of erythrocytes, hemoglobin and color index should be monitored for 1 month. 1-2 times a week, and then - 2-4 times a month. Remission is achieved with an increase in the number of red blood cells to 4-4.5 million / μl, when normal erythrocyte sizes reach, aniso-and poikilocytosis disappear, normalizing the content of reticulocytes after a reticulocytic crisis. After reaching hematological remission, control of peripheral blood is carried out at least once in 4-6 months.

Observe caution in individuals prone to thrombosis, with angina (in smaller doses up to 100 μg per injection). Take a long time with pernicious anemia, the upcoming operations on the gastrointestinal tract.

Effect on the ability to drive transp. cf. and fur:The adverse effect of the drug on the ability to drive vehicles and engage in other activities that require concentration and speed of psychomotor reactions have not been reported.However, given that the drug can cause dizziness, care should be taken when implementing these activities.

Form release / dosage:

Solution for injection 0.2 mg / ml, 0.5 mg / ml.

Packaging:

Solution for injection 0.2 mg / ml, 0.5 mg / ml.

1 ml per ampoule type B neutral glass grade HC-1 or HC-3 or ampoule syringe filling.

For 10 ampoules together with instructions for use and a knife for opening ampoules or a scarifier ampoule in a box of cardboard.

5 ampoules per contour cell pack.

2 contoured cell packs together with instructions for use and a knife for opening ampoules or a scarifier ampullum in a pack of cardboard.

When using ampoules with notches, rings and dots, the ampoule opener or scarifier is not inserted.

Storage conditions:In the dark place at a temperature of 5 to 25 ° C. Keep out of reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000077

Date of registration:12.01.2010

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp01.12.2015

Illustrated instructions

Instructions

Cyanocobalamin (Cyanocobalamin)