Cocarnit, lyophilizate 187.125 mg+2 ml p-val 2 ml 3 pcs

Pharmacodynamics

The drug is a rationally selected complex of metabolic substances and vitamins. Triphosadenine is a derivative of adenosine and stimulates metabolic processes. It has a vasodilatory effect, including on coronary and cerebral arteries.

It improves metabolism and energy supply of tissues. It has hypotensive and antiarrhythmic action. Under the influence of ATP the blood pressure decreases, smooth muscles relax, and the conduction of nerve impulses improves. Cocarboxylase is a coenzyme formed in the body from ingested thiamine (vitamin B1).

It is part of the enzyme carboxylase, which catalyzes the carboxylation and decarboxylation of α-keto acids. Indirectly promotes the synthesis of nucleic acids, proteins and lipids. Reduces the concentration of lactic and pyruvic acids in the body, promotes glucose absorption. Improves the trophism of nervous tissue.

The body converts cyanocobalamin (vitamin B12) into methylcobalamin and 5-deoxyadenosylcobalamin. Methylcobalamin is involved in the conversion of homocysteine to methionine and S-adenosylmethionine, key reactions in the metabolism of pyrimidine and purine bases (and therefore of DNA and RNA). If the vitamin is deficient in this reaction, it can be replaced by methyltetrahydrofolic acid, with impaired folic metabolic reactions.

5-deoxyadenosylcobalamin serves as a cofactor in the isomerization of L-methylmalonyl-CoA into succinyl-CoA, an important reaction in carbohydrate and lipid metabolism. Vitamin B12 deficiency 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, a form of vitamin PP, is involved in redox processes in the cell, improves carbohydrate and nitrogen metabolism, regulates tissue respiration.

Pharmacokinetics

Trifosadenin After parenteral administration penetrates the cells of organs where it splits into adenosine and inorganic phosphate with release of energy. Subsequently, the breakdown products are included in ATP resynthesis. Cocarboxylase Quickly absorbed after intramuscular administration. It penetrates into most body tissues. It undergoes metabolic degradation. Products of metabolism are excreted mainly by the kidneys.

Cyanocobalamin

In the blood cyanocobalamin binds to transcobalamin I and II, which transport it to the tissues. It is deposited mainly in the liver. The binding to plasma proteins is 0 90%. It is quickly and completely absorbed after intramuscular and subcutaneous administration. Maximum concentration after intramuscular administration is reached after 1 hour. It is excreted from the liver by bile into the intestine and is absorbed back into the blood. Period of semiejection is 500 days. Withdrawal in normal renal function is 7-10% by the kidneys and about 50% by the intestines. With reduced renal function 0-7% by kidneys and 70-100% by intestines. Passes through the placental barrier, in breast milk.4

Nicotinamide

Fastly distributed to all tissues. Passes 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 elimination half-life is about 1.3 h, steady-state volume of distribution is about 60 liters, total clearance is about 0.6 l/min.

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Indications

Symptomatic treatment of diabetic polyneuropathy.

Composition

Each ampule of the drug contains:

active ingredients:

Trifosadenine dinatrium trihydrate – 10.0 mg,

cocarboxylase – 50.0 mg,

p> cyanocobalamin – 0.5 mg,

nicotinamide – 20.0 mg;

excipients:

Glycine – 105.875 mg,

methylparahydroxybenzoate – 0.6 mg,

propylparahydroxybenzoate – 0.15 mg.

Each ampoule of solvent contains:

Lidocaine hydrochloride – 10 mg,

water for injection – up to 2 ml

How to take, the dosage

The drug is injected deeply intramuscularly (into the gluteal muscle). In cases of severe pain syndrome it is reasonable to start treatment with intramuscular injection of 1 ampoule (2 ml) per day until relief of acute symptoms.

The duration of use is 9 days.

After improvement of symptoms or in cases of moderately expressed 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 the drug Kokarnit in children.

Interaction

In patients using hypoglycemic agents of biguanide group (metformin), due to impaired absorption of cyanocobalamin from the gastrointestinal tract, decreased concentration of cyanocobalamin in blood may be observed. No drug interactions have been described with other hypoglycemic agents.

Cyanocobalamin is not compatible with ascorbic acid, salts of heavy metals, thiamine bromide, pyridoxine, riboflavin, folic acid. Cyanocobalamin should not be used simultaneously with drugs that increase blood clotting. In addition, concomitant use of cyanocobalamin with chloramphenicol should be avoided.

The aminoglycosides, salicylates, antiepileptic drugs, colchicine, and potassium preparations reduce absorption of cyanocobalamin.

When co-administration of drugs containing trifosadenine with dipyridamole the effects of dipyridamole are enhanced, particularly the vasodilatory effect. Dipyridamole increases the effect of trifosadenine.

There is some antagonism in co-administration of the drug with purine derivatives (caffeine, theophylline).

The drug should not be administered simultaneously with cardiac glycosides in high doses because of an increased risk of adverse cardiovascular reactions.

Concomitant use with xanthinol nicotinate decreases the effect of the drug.

Nicotinamide potentiates the effects of sedatives, tranquilizers and hypotensive drugs.

Special Instructions

If symptoms worsen or if there is no effect after 9 days, the course of treatment should be corrected.

When using KOCARNIT, proper selection of the dose of the hypoglycemic drug and adequate monitoring of the course of diabetes mellitus is necessary.

The color of the prepared solution should be pink.

The drug should not be used if the color of the solution has changed.

The solution must be used immediately after it has been prepared!

Effect on the ability to drive, operate machinery

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

Contraindications

The drug should be used with caution in angina pectoris.

Overdose

The components of COCARNIT have a wide therapeutic range.

Symptoms of overdose

Triphosadenine: exceeding the maximum daily dose (about 600 mg for an adult) may lead to the development of the following symptoms: Dizziness, decreased blood pressure, transient loss of consciousness, arrhythmias, grade II and III atrioventricular block, asystole,7 bronchospasm, ventricular disturbances, sinus bradycardia and tachycardia.

Cocarboxylase: The following symptoms have been reported after administering more than 100 times the recommended dose: headache, muscle spasm, muscle weakness, paralysis, arrhythmia.

Cyanocobalamin: eczematous skin disorders and a benign form of acne have been observed after parenteral administration of a high dose. When used in high doses, hypercoagulability and disorders of purine metabolism are possible.

Nicotinamide: in high doses hyperpigmentation, jaundice, amblyopia, weakness, exacerbation of gastric and duodenal ulcers were observed. With prolonged use the development of steatohepatosis, increased concentration of uric acid in the blood, impaired glucose tolerance was noted.

Treatment. Administration of the drug shall be stopped immediately; symptomatic therapy, including desensitizing therapy, shall be prescribed.