Cocarnit lyophilisate for preparation of injection solution, 2ml No. 3

Symptomatic treatment of diabetic polyneuropathy.

V / m (in the gluteus muscle). The drug is injected deeply.

In cases of severe pain syndrome, it is advisable to start treatment with an intramuscular injection of 1 amp. (2 ml / day) until acute symptoms are relieved. Duration of application is 9 days.

After improvement of symptoms or in cases of moderate symptoms of polyneuropathy: 1 amp. 2-3 times a week for 2-3 weeks. The recommended course of treatment is 3Ц9 injections, depending on the severity of the disease. The duration of treatment and repeated courses are determined by the doctor, depending on the nature and severity of the disease.

Children. There are no data on the efficacy and safety of using Cocarnit in children.

hypersensitivity to any component of the drug or solvent;

cardiovascular diseases: acute myocardial infarction, uncontrolled arterial hypertension, arterial hypotension, severe forms of bradyarrhythmias, AV block II Ц III degrees, chronic heart failure (III Ц IV degrees according to NYHA), cardiogenic shock and other types of shocks, QT prolongation syndrome, thromboembolism, hemorrhagic stroke;

inflammatory lung diseases, chronic obstructive pulmonary diseases, bronchial asthma;

hypercoagulation (including in acute thrombosis), erythremia, erythrocytosis;

peptic ulcer of the stomach or duodenum in the acute stage;

gout;

hepatitis, liver cirrhosis;

pregnancy;

breastfeeding period;

children under 18 years of age.

With care: angina pectoris.

Trade name of the drug:

Cocarnit

International non-proprietary name:

Dosage form:

lyophilisate for the preparation of a solution for intramuscular administration

Composition

Each ampoule of the drug contains:
Active ingredient - triphosadenine disodium trihydrate - 10.0 mg, cocarboxylase - 50.0 mg, cyanocobalamin - 0.5 mg, nicotinamide - 20.0 mg;
Excipients glycine - 105.875 mg, methyl parahydroxybenzoate - 0.6 mg, propyl parahydroxybenzoate - 0.15 mg.
Each ampoule of solvent contains:
Lidocaine hydrochloride - 10 mg, water for injection - up to 2 ml.

Description

The lyophilized mass is pink. The reconstituted solution is transparent, pink in color.

Pharmacotherapeutic group

Vitamins and metabolic agents.

ATX code: ј11DA

Pharmacological properties

The drug is a rationally selected complex of metabolic substances and vitamins.
Triphosadenine is a derivative of adenosine that stimulates metabolic processes. Has a vasodilating effect, including on the coronary and cerebral arteries. Improves metabolism and energy supply to tissues. It has hypotensive and antiarrhythmic effects. After parenteral administration, it penetrates into the cells of organs, where it is split into adenosine and inorganic phosphate with the release of energy. Subsequently, cleavage products are included in the synthesis of ATP. Under the influence of ATP, there is a decrease in blood pressure, relaxation of smooth muscles, and improved conduction of nerve impulses.
Cocarboxylase- a coenzyme formed in the body from thiamine (vitamin B1) coming from outside. It is a part of the enzyme carboxylase, which catalyzes the carboxylation and decarboxylation of ?-keto acids. Indirectly promotes the synthesis of nucleic acids, proteins and lipids. Reduces the concentration of lactic and pyruvic acids in the body, promotes the absorption of glucose. Improves trophism of nervous tissue.
Cyanocobalamin (vitamin B12)in the body is converted into methylcobalamin and 5-deoxyadenosylcobalamin. Methylcobalamin is involved in the conversion of homocysteine ??to methionine and S-adenosylmethionine, the key metabolic reactions of pyrimidine and purine bases (and, consequently, DNA and RNA). In case of vitamin deficiency in this reaction, methyltetrahydrofolic acid can replace it, while folate-demanding metabolic reactions are disturbed.
5-deoxyadenosylcobalamin serves as a cofactor in the isomerization of L-methylmalonyl-CoA to succinyl-CoA, an important metabolic reaction of carbohydrates and lipids.
Deficiency of vitamin B12 leads to impaired proliferation of rapidly dividing cells of hematopoietic tissue and epithelium, as well as to impaired formation of the myelin sheath of neurons.
Nicotinamide- one of the forms of vitamin PP, participates in redox processes in the cell, improves carbohydrate and nitrogen metabolism, and regulates tissue respiration.

Pharmacodynamics
Triphosadenin
After parenteral administration, it penetrates into the cells of organs, where it is split into adenosine and inorganic phosphate with the release of energy. Subsequently, the decomposition products are included in the resynthesis of ATP.
Cocarboxylase is
rapidly absorbed after intramuscular administration. Penetrates into most body tissues. Undergoes metabolic decomposition. Metabolic products are excreted mainly by the kidneys.
Cyanocobalamin
In the blood, cyanocobalamin binds to transcobalamins I and II, which transport it to tissues. It is deposited mainly in the liver. Communication with plasma proteins 0 90%. It is rapidly and completely absorbed after intramuscular and subcutaneous administration. The maximum concentration after intramuscular administration is reached after 1 hour.
From the liver, it is excreted by bile into the intestines and again absorbed into the blood. The half-life is 500 days. It is excreted with normal renal function - 7-10% by the kidneys, about 50% by the intestines. With reduced kidney function - 0-7% by the kidneys, 70-100% by the intestines. Penetrates through the placental barrier into breast milk.
Nicotinamide is
rapidly distributed into all tissues. Penetrates through the placental barrier and into breast milk. It is metabolized in the liver to form nicotinamide-N-methylnicotinamide. It is excreted by the kidneys.
The plasma half-life is about 1.3 hours, the stationary volume of distribution is about 60 liters, the total clearance is about 0.6 l / min.

Indications for use

Symptomatic treatment of diabetic polyneuropathy.

Contraindications

• Hypersensitivity to any component of the drug or solvent;

• cardiovascular diseases: acute myocardial infarction, uncontrolled arterial hypertension, arterial hypotension, severe forms of bradyarrhythmias, AV block II-III degree, chronic heart failure (III-IV grade NYHA), cardiogenic shock and other types of shocks, QT prolongation syndrome, thromboembolism, hemorrhagic stroke;

• inflammatory lung diseases, chronic obstructive pulmonary diseases, bronchial asthma;

• pregnancy, breastfeeding period;

• children under 18 years of age;

• hypercoagulation (including in acute thrombosis), erythremia, erythrocytosis;

• peptic ulcer of the stomach or duodenum in the acute stage;

• gout;

• hepatitis, cirrhosis of the liver.

Carefully

The drug should be used for angina pectoris.

Application during pregnancy and during breastfeeding

It is not recommended to use the drug COCARNIT during pregnancy.
It is recommended that breastfeeding be discontinued during drug treatment.

Method of administration and dosage

The drug is injected deeply intramuscularly (into the gluteus muscle).
In cases of severe pain syndrome, it is advisable to start treatment with intramuscular injection of 1 ampoule (2 ml) per day until acute symptoms are relieved.
Duration of application is 9 days.
After improvement of symptoms or in cases of moderate symptoms of polyneuropathy: 1 ampoule 2-3 times a week for 2-3 weeks.
The recommended course of treatment is 3-9 injections, depending on the severity of the disease.
The duration of treatment and repeated courses are determined by the doctor depending on the nature and severity of the disease.
Application in children

There are no data on the efficacy and safety of using the drug Cocarnitum in children.

Side effect
The frequency of manifestation of adverse side effects is given in accordance with the WHO classification: very often (more than 1/10); often (less than 1/10, but more than 1/100); infrequently (less than 1/100, but more than 1/1000); rarely (less than 1/1000, but more than 1/10000); very rarely (less than 1/10000), including isolated cases; the frequency is unknown.
From the immune system : rarely - allergic reactions (skin rash, shortness of breath, anaphylactic shock, Quincke's edema).
From the side of the nervous system : in some cases - dizziness, headache, agitation, confusion.
From the side of the heart : very rarely - tachycardia; in some cases bradycardia, arrhythmia; frequency unknown - pain in the region of the heart
From the side of the vessels: frequency unknown - redness of the skin of the face and upper half of the body with a tingling and burning sensation, 'hot flashes'.
From the side of the gastrointestinal tract : in some cases - vomiting, diarrhea.
From the side of the skin and subcutaneous tissues : very rarely - increased sweating, acne, itching, urticaria.
On the part of the musculoskeletal and connective tissue : very rarely - convulsions.
General disorders and disorders at the injection site : very rarely - irritation, pain and burning at the injection site, weakness may occur.
If any of these adverse reactions worsened or any other adverse reactions that are not indicated in the instructions appear, you must inform your doctor about it.
With the development of severe adverse reactions, the drug is canceled.

Overdose

The components of the COCARNIT preparation have a wide therapeutic range.
Symptoms of an overdose of
Triphosadenine : exceeding the maximum daily dose (about 600 mg for an adult) can lead to the development of the following symptoms: dizziness, decreased blood pressure, short-term loss of consciousness, arrhythmia, atrioventricular block II and III degrees, asystole, bronchospasm, ventricular disturbances, sinus bradycardia and tachycardia.
Cocarboxylase: the following symptoms have been reported after more than 100 times the recommended dose: headache, muscle spasm, muscle weakness, paralysis, arrhythmia.
Cyanocobalamin: After parenteral administration of a high dose, eczematous skin disorders and benign acne have been observed. When used in high doses, it is possible to develop hypercoagulability, impaired purine metabolism.
Nicotinamide : when using large doses, hyperpigmentation, jaundice, amblyopia, weakness, exacerbation of gastric ulcer and duodenal ulcer were observed. With prolonged use, the development of steatohepatosis, an increase in the concentration of uric acid in the blood, and impaired glucose tolerance were noted.
Treatment . The administration of the drug is stopped immediately, symptomatic therapy is prescribed, including desensitizing therapy.

Interaction with other medicinal products

In patients using hypoglycemic agents of the biguanide group (metformin), due to impaired absorption of cyanocobalamin from the gastrointestinal tract, a decrease in the concentration of cyanocobalamin in the blood may be observed. No drug interactions have been described with other hypoglycemic agents.
Cyanocobalamin is not compatible with ascorbic acid, heavy metal salts, thiamine bromide, pyridoxine, riboflavin, folic acid.
Do not use cyanocobalamin at the same time with drugs that increase blood clotting. In addition, the simultaneous use of cyanocobalamin with chloramphenicol should be avoided.
Aminoglycosides, salicylates, antiepileptic drugs, colchicine, potassium preparations reduce the absorption of cyanocobalamin.
With the combined use of drugs containing triphosadenine with dipyridamole, the effect of dipyridamole is enhanced, in particular the vasodilating effect.
Dipyridamole enhances the effect of triphosadenine.
Some antagonism appears when the drug is used together with purine derivatives (caffeine, theophylline).
It is impossible to enter simultaneously with cardiac glycosides in large doses, since the risk of developing adverse reactions from the cardiovascular system increases.
With simultaneous use of nicotinate with xanthinol, the effect of the drug decreases.
Nicotinamide potentiates the effect of sedatives, tranquilizers, and antihypertensive drugs.

Special instructions (warnings)

If the symptoms of the disease worsen or there is no effect after 9 days, it is necessary to correct the course of treatment.
When using the drug COCARNIT, proper selection of the dose of the hypoglycemic drug and adequate control of the course of diabetes mellitus are necessary.
The color of the prepared solution should be pink.
Do not use the drug if the color of the solution has changed.
The solution must be applied immediately after its preparation!

Influence on driving a car and working with mechanisms

In the event of side effects from the central nervous system (dizziness, confusion), it is recommended to refrain from driving and other mechanisms.

Release form

Lyophilisate for the preparation of a solution for intramuscular administration / complete with a solvent.
187.125 mg of the drug in dark glass ampoules with one or two break rings with a volume of 3 ml.
2 ml of solvent (0.5% lidocaine hydrochloride solution) in dark glass ampoules with a break ring with a volume of 2 ml.
3 ampoules with the drug complete with 3 ampoules of solvent in a blister strip packaging.
One blister strip with instructions for use is placed in a cardboard box.

Shelf life

Drug: 3 years.
Solvent: 4 years.
Do not use after the expiration date printed on the package.

Storage conditions

In the dark place at a temperature of 15 to 25 ? C.
Keep out of the reach of children.

Conditions of dispensing from pharmacies

On prescription.