Pharmacological properties

Pharmacodynamics. vitamin v12 (cyanocobalamine) has metabolic, hemopoietic effect. in an organism (mainly in a liver) turns into a coenzymatical form — adenozilkobalamin, or Cobamamidum which is an active form of vitamin v12. Cobamamidum is a part of numerous enzymes, including composition of the reductase restoring folic acid in tetrahydrofolic. has high biological activity. Cobamamidum participates in transfer of methyl and other one-carbon fragments therefore it is necessary for formation of desoxyribose and DNA, creatine, methionine — the donor of methyl groups, in synthesis of a lipotropic factor — sincaline, for transformation of methyl-malonic acid into amber, being a part of a myelin, for utilization of propionic acid. Cobamamidum is necessary for a normal hemopoiesis as it promotes maturing of erythrocytes. participates in synthesis and accumulation in erythrocytes of the connections containing sulfhydryl groups that increases their tolerance to hemolysis. activates the system of fibrillation, in high doses causes increase in thromboplastic activity and activity of a prothrombin. reduces level hs in blood. positively influences function of a liver and nervous system. increases ability of fabrics to regeneration.

Pharmacokinetics. At parenteral use _{12 vitamin B} quickly comes to a system blood stream. In blood contacts transcobalamine I and II which transports it in fabric. It is deposited in a liver. Communication with proteins of blood plasma — 90%. Time of achievement of the maximum concentration (T _max ) after p / to or introductions in oil is about 1 h. From a liver it is allocated with bile in intestines and again soaked up in blood. T _½ from a liver — 500 days. It is removed at normal function of kidneys: 7–10% — kidneys, about 50% — with a stake; at reduced function of kidneys: 0–7% — kidneys, 70–100% — with a stake. Gets through a placental barrier.

Indication

Treatment of malignant, posthemorrhagic and iron deficiency anemias, aplastic anemias at children, the anemias of alimentary character caused by toxic substances and medicines, connected with deficiency of b12 vitamin irrespective of the deficit reason (a stomach resection, helminthic invasions, disturbance of process of absorption in intestines, pregnancy). polyneurites, epileptiform neuralgias, sciatica, kauzalgiya, migraine, diabetic neuritis, side amyotrophic sclerosis, cerebral palsy, Down syndrome, tremens. to apply in dystrophy at children, after the postponed infectious diseases, at a spra (together with folic acid), liver diseases (hepatitis, cirrhosis, an infectious disease), radiation sickness, psoriasis, herpetiform dermatitis, neurodermatitises, photodermatoses.

Use

to use Drug p / to, in oil, in/in, and in a side funicular myelosis and an amyotrophic sclerosis also intralyumbalno.

Adult

At In ₁₂ - scarce anemias medicament to apply in doses 100–200 mkg (0.1-0.2 mg) every other day before achievement of remission.

At emergence of symptoms of a funicular myelosis and in macrocytic anemias with injury of nervous system cyanocobalamine to apply in a single dose 400–500 mkg (0.4-0.5 mg) and more. Within 1 week to enter daily, and then with intervals of 5-7 days (at the same time to appoint folic acid). In hard cases to enter into the spinal canal, since a single dose of 15-30 mkg, at each subsequent injection to raise a dose (50; 100; 150; 200 mkg). To do Intralyumbalny injections each 3 days, all on a course 8–10 injections are necessary. During remission in the absence of the phenomena of a funicular myelosis for maintenance therapy to appoint 100 mkg 2 times a month, in the presence of neurologic symptoms — on 200–400 mkg 2–4 times within a month.

At a side amyotrophic sclerosis, encephalomyelitis, neurologic diseases with a pain syndrome to administer the medicament in the increasing doses from 200 to 500 mkg on an injection (at improvement — 100 mkg/days). A course of treatment — 14 days.

In injuries of peripheral nerves 200–400 mkg of 1 times in 2 days within 40–45 days.

In hepatitis and cirrhosis on 15–30 mkg/days or on 100 mkg every other day within 25–40 days.

In diabetic neuropathy, to a spr, radiation sickness to enter 60–100 mkg daily within 20–30 days.

At deficiency of _{12 vitamin B} for treatment — in oil and in/in on 1 mg every day during 1–2 weeks, a maintenance dose — 1–2 mg in oil or in/in from 1 time a week up to 1 time a month. Treatment duration cyanocobalamine and carrying out repeated courses depend on a course of the disease and efficiency of treatment.

to Enter

only p / to.

In posthemorrhagic and iron deficiency anemias on 30–100 mkg 2–3 times a week.

In aplastic anemia at children on 100 mkg before kliniko-hematologic improvement.

In anemias of alimentary character at children's age on 30 mkg within 15 days.

In dystrophies at children of early age, a Down syndrome on 15–30 mkg every other day.

In hepatitis and cirrhosis on 15–30 mkg/days or on 100 mkg every other day within 25–40 days.

Contraindication

Hypersensitivity to medicament components. erythremias, hyperglobulia. new growths, except for the cases which are followed by megaloblastny anemia and deficiency of b12 vitamin. acute thromboembolic diseases. angina of exertion of a high functional class.

Side effects

from blood: hypercoagulation.

from a cardiovascular system: tachycardia, pain in heart.

from nervous system: headache, dizziness, nervous excitement.

from a metabolism: an acne, bullous rash, nausea, the increased sweating, disturbance of purine exchange.

from the immune system: allergic reactions, including skin manifestations, including hyperaemia, urticaria, rash, itching, dermatitis, hypostases, in particular a Quincke's edema; breath disturbance, including suffocation attack, acute anaphylaxis, anaphylactoid reactions.

from a GIT: softening of stool.

General disturbances: indisposition, fever.

Local reactions, including hyperaemia, an itching, pain, hypostasis, consolidation and necrosis in the place of an injection.

Special instructions

during treatment needs to control indicators of peripheral blood: for the 5-8th day of therapy to define the maintenance of reticulocytes, concentration of iron. it is necessary to control quantity of erythrocytes, hemoglobin and a color indicator within 1 month 1–2 times a week, and further — 2–4 times a month. remission is reached at increase in quantity of erythrocytes up to 4 000 000–4 500 000/mkl, at achievement of the normal sizes of erythrocytes, disappearance anizo- and a poikilocytosis, normalization of maintenance of reticulocytes after reticulocytic crisis. after achievement of hematologic remission to carry out control of peripheral blood at least 1 time in 4–6 months

At a trend of development leucio- and a hyperglobulia the dose of medicament needs to be lowered or to temporarily suspend treatment.

Cannot apply cyanocobalamine with the medicaments increasing blood clotting.

At persons with tendency to a thrombogenesis and patients with stenocardia in the course of treatment needs to be careful and control blood clotting.

Use during pregnancy and feeding by a breast. With care, under observation of the doctor to apply during pregnancy (there are separate data on teratogenic effect of _{12 vitamin B} in high doses) and feeding by a breast, considering a ratio advantage/risk.

Children. Not to apply a dosage form in a dosage of 0.5 mg/ml at children under 3 years.

only p / to.

Ability to influence speed of response at control of vehicles or work with other mechanisms. During treatment it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity requiring special attention and speed of psychomotor reactions.

Interaction

Aminoglycosides, salicylates, antiepileptic drugs, colchicine, medicaments of potassium reduce medicament absorption, influence its kinetics.

At simultaneous use with Kanamycinum, Neomycinum, polymyxins, tetracyclines the absorption of cyanocobalamine decreases.

Pharmaceutical it is incompatible with ascorbic acid, salts of heavy metals (cyanocobalamine inactivation), Thiamini bromidum, a pyridoxine, Riboflavinum (the cobalt ion which is contained in a cyanocobalamine molecule destroys other vitamins).

Thiamine — raises risk of development of the allergic reactions caused by thiamine.

Chloramphenicol — reduces the hemopoietic answer to drug.

Cytamenum — at simultaneous use decreases effect of Cytamenum.

Oral contraceptives — reduce concentration of cyanocobalamine in blood.

Overdose

Symptoms: fluid lungs, stagnant heart failure, thrombosis of peripheral vessels.

symptomatic treatment.

Storage conditions

In original packing at a temperature not above 25 °C. not to freeze.