Instructions for use Cyanocobalamin-Darnitsa (Vitamin B12-Darnitsa) solution for injection 0.05% ampoule 1 ml No. 10
Composition
active ingredient: cyanocobalamin;
1 ml of solution contains 0.5 mg of cyanocobalamin;
Excipients: sodium chloride, sodium acetate trihydrate, acetic acid, water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: transparent red liquid.
Pharmacotherapeutic group
Vitamin B12 (cyanocobalamin and its analogues). Cyanocobalamin. ATX code B03B A01.
Pharmacological properties
Pharmacodynamics
Vitamin B12 (cyanocobalamin) has a metabolic and hematopoietic effect. In the body (mainly in the liver), it is converted into a coenzyme form - adenosylcobalamin, or cobamamide, which is the active form of vitamin B12. Cobamamide is a component of numerous enzymes, including reductase, which reduces folic acid to tetrahydrofolic acid. It has high biological activity. Cobamamide is involved in the transfer of methyl and other one-carbon fragments, therefore it is necessary for the formation of deoxyribose and DNA, creatine, methionine - a donor of methyl groups, in the synthesis of lipotropic factor - choline, for the conversion of methylmalonic acid into succinic acid, which is part of myelin, for the utilization of propionic acid. Cobamamide is necessary for normal hematopoiesis, because it promotes the maturation of erythrocytes. Participates in the synthesis and accumulation of compounds containing sulfhydryl groups in erythrocytes, which increases their tolerance to hemolysis. Activates the blood coagulation system, in high doses causes an increase in thromboplastic activity and prothrombin activity. Reduces blood cholesterol levels. Has a positive effect on liver and nervous system function. Increases the ability of tissues to regenerate.
Pharmacokinetics
When administered parenterally, vitamin B12 quickly enters the systemic bloodstream. In the blood, it binds to transcobalamins I and II, which transport it to the tissues. It is deposited mainly in the liver. Plasma protein binding is 90%. The time to reach maximum concentration (TCmax) after subcutaneous or intramuscular administration is about 1 hour. It is excreted from the liver with bile into the intestines and is reabsorbed into the blood. The half-life (T1/2) from the liver is 500 days. With normal kidney function, 7−10% is excreted by the kidneys, about 50% with feces; with reduced kidney function, 0−7% by the kidneys, 70−100% with feces. Penetrates the placental barrier.
Indication
Treatment of malignant, posthemorrhagic and iron deficiency anemias, aplastic anemias in children, nutritional anemias caused by toxic substances and drugs associated with vitamin B12 deficiency, regardless of the cause of the deficiency (gastric resection, helminthic invasions, impaired intestinal absorption, pregnancy). Polyneuritis, trigeminal neuralgia, radiculitis, causalgia, migraine, diabetic neuritis, amyotrophic lateral sclerosis, cerebral palsy, Down's disease, alcoholic delirium. Use for dystrophy in children, after infectious diseases, for sprue (together with folic acid), for liver diseases (hepatitis, cirrhosis, Botkin's disease), radiation sickness, psoriasis, herpetimorphic dermatitis, neurodermatitis, photodermatoses.
Contraindication
Hypersensitivity to the components of the drug. Erythremia, erythrocytosis. Neoplasms, except for cases accompanied by megaloblastic anemia and vitamin B12 deficiency. Acute thromboembolic diseases. Angina pectoris of high functional class.
Interaction with other medicinal products and other types of interactions
Aminoglycosides, salicylates, antiepileptic drugs, colchicine, potassium preparations reduce the absorption of the drug and affect its kinetics.
When used simultaneously with kanamycin, neomycin, polymyxins, tetracyclines, the absorption of cyanocobalamin decreases.
Pharmaceutically incompatible with ascorbic acid, heavy metal salts (inactivation of cyanocobalamin); thiamine bromide, pyridoxine, riboflavin (the cobalt ion contained in the cyanocobalamin molecule destroys other vitamins).
Thiamine – the risk of developing allergic reactions caused by thiamine increases.
Chloramphenicol – reduces the hematopoietic response to the drug.
Oral contraceptives – reduce the concentration of cyanocobalamin in the blood.
Application features
If there is a tendency to develop leukocytosis and erythrocytosis, the dose of the drug should be reduced or treatment temporarily suspended.
Cyanocobalamin should not be used with drugs that increase blood clotting.
During treatment, caution should be exercised and blood clotting should be monitored in individuals with a tendency to thrombosis and patients with angina pectoris.
Important information about excipients.
This medicinal product contains less than 1 mmol (23 mg) sodium/dose, i.e. essentially 'sodium-free'.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, it is necessary to refrain from driving vehicles and potentially dangerous activities that require increased attention and speed of psychomotor reactions.
Use during pregnancy or breastfeeding
Use with caution, under the supervision of a physician, during pregnancy (there is some evidence of the teratogenic effect of vitamin B12 in high doses) or breastfeeding, taking into account the benefit/risk ratio.
Method of administration and doses
The drug should be administered subcutaneously, intramuscularly, intravenously, and in the case of lateral funicular myelosis and amyotrophic sclerosis, also intralumbarly.
Adults
In case of B12 deficiency anemia, the drug should be used in doses of 100−200 mcg (0.1−0.2 mg) every other day until remission is achieved.
When symptoms of funicular myelosis appear and in macrocytic anemias with damage to the nervous system, cyanocobalamin is used in a single dose of 400−500 μg (0.4−0.5 mg) and more. During the first week, administer daily, and then at intervals of 5−7 days (at the same time prescribe folic acid). In severe cases, inject into the spinal canal, starting with a single dose of 15−30 μg, with each subsequent injection, increase the dose (50, 100, 150, 200 μg). Intralumbar injections are given every 3 days, a total of 8−10 injections are required per course. During the period of remission, in the absence of funicular myelosis, for maintenance therapy, 100 μg is prescribed twice a month, in the presence of neurological symptoms - 200−400 μg 2−4 times a month.
In amyotrophic lateral sclerosis, encephalomyelitis, neurological diseases with pain syndrome, the drug is administered in increasing doses from 200 to 500 mcg per injection (with improvement - 100 mcg per day). The course of treatment is 14 days.
For peripheral nerve injuries, prescribe 200−400 mcg once every 2 days for 40−45 days.
For hepatitis and cirrhosis, prescribe 15-30 mcg per day or 100 mcg every other day for 25-40 days.
For diabetic neuropathy, sprue, and radiation sickness, administer 60-100 mcg daily for 20-30 days.
In case of vitamin B12 deficiency, treatment is intramuscularly and intravenously 1 mg every day for 1−2 weeks, maintenance dose is 1−2 mg intramuscularly or intravenously from 1 time per week to 1 time per month. The duration of treatment with cyanocobalamin and repeated courses depend on the course of the disease and the effectiveness of treatment.
Children
Administer subcutaneously only.
For post-hemorrhagic and iron deficiency anemia, prescribe 30−100 mcg 2−3 times a week.
For aplastic anemia in children, administer 100 mcg until clinical and hematological improvement occurs.
For nutritional anemia in children, prescribe 30 mcg for 15 days.
For dystrophies in young children, Down syndrome, and cerebral palsy, prescribe 15−30 mcg every other day.
For hepatitis and cirrhosis of the liver, children should be prescribed 15-30 mcg per day or 100 mcg every other day for 25-40 days.
Children
The 0.5 mg/ml dosage form should not be used in children under 3 years of age.
Administer subcutaneously only.
Overdose
Symptoms: pulmonary edema, congestive heart failure, peripheral vascular thrombosis.
Treatment: symptomatic.
Adverse reactions
Gastrointestinal: loose stools.
Metabolism: acne, bullous rashes, nausea, sweating, purine metabolism disorders, hypokalemia.
From the nervous system: headache, dizziness, nervous excitement, drowsiness, muscle paralysis, loss of consciousness.
Cardiovascular system: tachycardia, pain in the heart area, congestive heart failure, peripheral vascular thrombosis, low blood pressure, cardiac arrest.
On the part of the blood: hypercoagulation.
On the part of the immune system: allergic reactions, including skin manifestations, including hyperemia, urticaria, rash, itching, dermatitis, edema, including angioedema; respiratory disorders, including suffocation, anaphylactic shock, anaphylactoid reactions.
General disorders and administration site conditions: malaise, fever; injection site: hyperemia, itching, pain, swelling, induration, and necrosis.
Reporting of suspected adverse reactions.
Reporting suspected adverse reactions after the marketing authorisation of a medicinal product is an important procedure. It allows for continued monitoring of the benefit-risk balance of the medicinal product in question. Healthcare professionals should report any suspected adverse reactions via the national reporting system.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ° C. Do not freeze.
Keep out of reach of children.
Packaging
1 ml in an ampoule; 5 ampoules in a contour blister pack; 2 contour blister packs in a pack.
Vacation category
According to the recipe.
Producer
PrJSC "Pharmaceutical Company "Darnitsa".
Location of the manufacturer and its business address
Ukraine, 02093, Kyiv, Boryspilska St., 13.
