TRIKARNIT-K [Complex of metabolic substances and vitamins] Powder for solution for intramuscular injection

TRIKARNIT-K

instructions for medical use of the medicinal product

Tradename:

Trikarnit-K, Трикарнит-К

International non-proprietary name: -

Compound

Each lyophilized powder ampoule contains:

Adenosine triphosphate 10 mg

Cocarboxylase 50 mg

Cyanocobalamin 0.5 mg

Nicotinamide 20 mg

Each solvent ampoule contains Lidocaine hydrochloride 10 mg

Dosage form

Lyophilized powder for solution for injection.

Pharmacotherapeutic group

Vitamins and Metabolic Agents .

Pharmacological properties

Pharmacodynamics

The drug is a rationally selected complex of metabolic substances and vitamins.

Adenosine triphosphate (ATP) is a universal source of energy for all biochemical processes. Improves metabolism and energy supply of tissues. It has a vasodilatory effect, incl. to the coronary and cerebral arteries. It has hypotensive and antiarrhythmic action. Under the influence of ATP, there is a decrease in blood pressure, relaxation of smooth muscles, and the conduction of nerve impulses improves.

Cocarboxylase is a coenzyme formed in the body from thiamine (vitamin B ₁ ) supplied from outside. It is part of the carboxylase enzyme, 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 the absorption of glucose. Improves the trophism of the nervous tissue.

Cyanocobalamin (vitamin B ₁₂ ) in the body turns 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 (hence, DNA and RNA). If the vitamin is deficient in this reaction, it can be replaced by methyltetrahydrofolic acid, while the folic reactions of metabolism are disturbed.

5-deoxyadenosylcobalamin serves as a cofactor in the isomerization of L-methylmalonyl-CoA to succinyl-CoA, an important reaction in carbohydrate and lipid metabolism. Deficiency of vitamin B ₁₂ leads to a violation of the proliferation of rapidly dividing cells of the hematopoietic tissue and epithelium, as well as to a violation of the formation of the myelin sheath of neurons.

Nicotinamide - one of the forms of vitamin PP, is involved in redox processes in the cell, improves carbohydrate and nitrogen metabolism, regulates tissue respiration.

Pharmacokinetics

Adenosine triphosphate (ATP). After parenteral administration, it penetrates into the cells of organs, where it is cleaved into adenosine and inorganic phosphate with the release of energy. In the future, the decay products are included in the resynthesis of ATP.

Cocarboxylase. Rapidly absorbed after i / m administration. Penetrates into most tissues of the body. undergoes metabolic degradation. 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 - 90%. Rapidly and completely absorbed after i / m and s / c administration. _Cmax after i / m administration is achieved after 1 hour.

It is excreted from the liver by bile into the intestines and reabsorbed into the blood. T _1/2 - 500 days. It is excreted with normal kidney 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. Rapidly distributed to all tissues. Penetrates through the placental barrier and into breast milk. Metabolized in the liver to form nicotinamide-N-methylnicotinamide. Excreted by the kidneys. T _1/2 from plasma is about 1.3 h, stationary V _d is about 60 l, the total clearance is about 0.6 l / min.

Indications for use

Neuritis, neuropathy (including diabetes mellitus, pernicious anemia), neuralgia of various origins, myalgia, sciatica, lumbago, sciatica, bursitis, tendonitis, coronary artery disease, myocarditis, myocardiopathies.

Contraindications

Hypersensitivity to any component of the drug or solvent.

Cardiovascular diseases: acute myocardial infarction, uncontrolled arterial hypertension, arterial hypotension, severe forms of bradyarrhythmias, II-III degree AV blockade, chronic heart failure (III-IV degree according to NYHA), cardiogenic shock and other types of shocks, QT prolongation syndrome , thromboembolism, hemorrhagic stroke.

Inflammatory lung disease, chronic obstructive pulmonary disease, bronchial asthma.

Hypercoagulability (including with acute thrombosis), erythremia, erythrocytosis.

Peptic ulcer of the stomach or duodenum in the acute stage.

Gout, hepatitis, cirrhosis of the liver. Children's age up to 18 years.

With caution: angina pectoris.

Use during pregnancy or lactation

It is not recommended to use the drug during pregnancy and breastfeeding.

Interaction with other drugs

With the combined use of preparations containing triphosadenine with dipyridamole, the effect of dipyridamole, in particular vasodilating, is enhanced. Dipyridamole enhances the effect of triphosadenine.

Some antagonism appears when the drug is used together with purine derivatives (caffeine, theophylline).

You can not enter simultaneously with cardiac glycosides in large doses, since the risk of developing adverse reactions from the CCC increases.

Cyanocobalamin is incompatible with ascorbic acid, salts of heavy metals, thiamine bromide, pyridoxine, riboflavin, folic acid. Do not use cyanocobalamin simultaneously 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.

Nicotinamide potentiates the action of sedative drugs, tranquilizers, and antihypertensive drugs.

Special instructions and precautions

The solution must be applied immediately after its preparation. The color of the prepared solution should be red. Do not apply the solution if the color has changed.
As a solvent, a solution of lidocaine hydrochloride is used, which is included in the kit.

When using the drug, proper selection of the dose of the hypoglycemic drug and adequate control of the course of diabetes mellitus are necessary.

Use with caution in angina pectoris, bradycardia, atrioventricular blockade of the 1st degree, incomplete AV blockade, intraventricular conduction disorders, a tendency to arterial hypotension, with moderate heart failure, impaired liver and kidney function of a moderate degree, impaired respiratory function, with a tendency to bronchospasm, weakened sick and elderly patients, with gastritis, peptic ulcer of the stomach and duodenum (outside the stage of exacerbation).

Influence on the ability to drive vehicles and mechanisms.

If side effects from the central nervous system (dizziness, confusion) occur, it is recommended to refrain from driving vehicles and other mechanisms.

Dosage and administration

Intramuscularly (into the gluteal muscle). The drug is injected deeply. To prepare the solution, dilute the vial with lyophilized powder with a solvent.

In cases of severe pain syndrome, it is advisable to start treatment with an intramuscular injection of 1 amp. (2 ml / day) until the acute symptoms are relieved. After improvement of symptoms or in cases of mild symptoms of polyneuropathy: 1 amp. 2-3 times a week.

The duration of treatment and repeated courses are determined by the doctor depending on the nature and severity of the disease.

Side effect

When using the drug, the following adverse reactions may occur: facial hyperemia, itching, rash, urticaria, acne, tinnitus, weakness, headache, dizziness, short-term loss of consciousness, muscle spasm, muscle weakness, paralysis, arrhythmia, lowering blood pressure, arrhythmia, atrioventricular block II and III degree, asystole, bronchospasm, sinus bradycardia and tachycardia, hypercoagulability, purine metabolism disorders, exacerbation of gastric and duodenal ulcers, increased uric acid concentration in the blood, impaired glucose tolerance.

Local reactions: changes at the injection site, including pain, flushing, itching, swelling.

Treatment. The introduction of the drug is immediately stopped, symptomatic therapy is prescribed, including desensitizing.

Overdose

The components of the drug Tricarnit-K have a wide therapeutic range.

Symptoms

Adenosine triphosphate (ATP). 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, AV block II and III degree, asystole, bronchospasm, ventricular disturbances, sinus bradycardia and tachycardia.

Cocarboxylase. The following symptoms have been reported after administration of a dose greater than 100 times the recommended dose: headache, muscle spasm, muscle weakness, paralysis, arrhythmia.

Cyanocobalamin. After parenteral administration at a high dose, eczematous skin disorders and a benign form of acne were observed. When used in high doses, it is possible to develop hypercoagulability, a violation of purine metabolism.

Nicotinamide. When used in large doses, hyperpigmentation, jaundice, amblyopia, weakness, exacerbation of peptic ulcer of the stomach and duodenum 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 introduction of the drug is immediately stopped, symptomatic therapy is prescribed, incl. desensitizing.

Storage conditions

Store in a place protected from light, at a temperature of 15-25 ⁰ C. Keep out of the reach of children.

Best before date

3 years. Do not use after the expiry date stated on the package.

Holiday conditions

Released by prescription.

Release form

3 ampoules with lyophilized powder and 3 ampoules with a solvent, each containing lidocaine hydrochloride 0.5% - 2 ml with instructions for medical use in a cardboard box.