Instructions for use: Cocarnit lyophilized powder for solution for injection, ampoule with solvent in ampoules 2 ml No. 3
Composition
active ingredients: for the drug – nicotinamide, cocarboxylase, cyanocobalamin, disodium adenosine triphosphate trihydrate; for the solvent – lidocaine hydrochloride.
1 ampoule of the drug contains nicotinamide 20 mg, cocarboxylase 50 mg, cyanocobalamin 0.5 mg, disodium adenosine triphosphate trihydrate 10 mg;
excipients: glycine, methyl parahydroxybenzoate (E 218), propyl parahydroxybenzoate (E 216);
1 ampoule of solvent (2 ml of 0.5% solution) contains 10 mg of lidocaine hydrochloride;
excipient: water for injections.
Dosage form
The drug is a lyophilisate for solution for injection.
Solvent – solution for injection.
Main physicochemical properties:
The medicinal product is a pink lyophilisate;
solvent – a clear, colorless solution.
Pharmacotherapeutic group
Vitamins in combination with various substances. ATX code A11J C.
Pharmacological properties
Pharmacodynamics
The drug is a complex of metabolic substances and vitamins.
Nicotinamide is one of the forms of vitamin PP, participates in redox processes in the cell, improves carbohydrate and nitrogen metabolism, normalizes lipid metabolism, and reduces the level of atherogenic lipoproteins in the blood.
Cocarboxylase is a coenzyme formed in the body from thiamine (vitamin B1), which comes from the outside. It plays an important role in carbohydrate metabolism, is part of the carboxylase enzyme, which catalyzes the carboxylation and decarboxylation of a-keto acids. Indirectly promotes the synthesis of nucleic acids, proteins and lipids. Reduces the level of lactic and pyruvic acids in the body, promotes glucose absorption. Improves the trophism of nervous tissue.
Cyanocobalamin (vitamin B12) in the body is converted into an active form - adenosylcobalamin or cobamide, which has high biological activity. Increases protein synthesis in the body and promotes its accumulation. Activates the metabolism of carbohydrates and lipids. Reduces cholesterol levels in the blood, prevents fatty infiltration of the liver. Necessary for the normal functioning of hematopoietic organs, promotes the accumulation of compounds containing sulfhydryl groups in erythrocytes, increasing their resistance to hemolysis. Increases the ability of tissues to regenerate. Has a positive effect on the function of the liver and nervous system.
Disodium adenosine triphosphate trihydrate is a derivative of adenosine. Stimulates metabolic processes. Has hypotensive and antiarrhythmic, vasodilating effects, including on the coronary arteries.
Pharmacokinetics
The pharmacokinetics of the drug have not been studied.
Indication
As part of the complex treatment:
neuritis, neuropathy (including diabetes); neuralgia of various origins; myalgia, sciatica; lumbago, radiculitis; bursitis, tendinitis; ischemic heart disease (NYHA functional class I–II); myocarditis; myocardiopathy.
Contraindication
Hypersensitivity to the active substances or to other components of the drug; cardiogenic shock and other types of shock; decompensated heart failure; QT interval prolongation syndrome; severe forms of bradyarrhythmias; atrioventricular block (AV block) II-III degree; acute myocardial infarction; arterial hypotension; severe forms of arterial hypertension; hemorrhagic stroke; sudden decrease in peripheral vascular resistance in history, hypercoagulation (including in acute thrombosis); inflammatory lung diseases; obstructive diseases of the bronchopulmonary system; severe forms of bronchial asthma; hyperkalemia, hypermagnesemia; erythremia, erythrocytosis; neoplasms, except for cases accompanied by megaloblastic anemia and vitamin B12 deficiency; gastric ulcer and duodenal ulcer in the acute stage; gout; hyperuricemia; decompensated diabetes mellitus; severe liver failure (including cirrhosis).
Additionally for the solvent – 0.5% lidocaine hydrochloride solution:
Hypersensitivity to other amide-type local anesthetics; sick sinus syndrome; Wolff-Parkinson-White syndrome; Adams-Stokes syndrome; angina pectoris of high functional class (NYHA functional class III-IV); history of epileptiform seizures associated with the administration of lidocaine hydrochloride; myasthenia gravis; hypovolemia; porphyria; severe renal failure.
Interaction with other medicinal products and other types of interactions
Nicotinamide
Anticoagulants, acetylsalicylic acid - increased risk of hemorrhage. Caution should be exercised in case of simultaneous use.
Antihypertensives – increased hypotensive effect. Caution should be exercised in case of simultaneous use.
Antibiotics – possible increase in hyperemia caused by nicotinamide.
Neomycin, barbiturates, anti-tuberculosis drugs, sulfonamides – reducing the toxicity of the latter and preventing neomycin-induced reduction in cholesterol and high-density lipoprotein concentrations.
Oral contraceptives, isoniazid - possible increased need for nicotinamide (due to slowing the conversion of tryptophan to nicotinic acid).
Probenecid – weakens the effect of the latter.
Ciprofibrate – simultaneous use with nicotinamide is not recommended.
Fibrinolytic agents, antispasmodics, cardiac glycosides - enhancing the action of the latter.
Nicotinamide enhances the toxic effects of alcohol on the liver.
Cocarboxylase
Cardiac glycosides – increased cardiotonic effect of cardiac glycosides.
Cyanocobalamin
Agents that increase blood clotting - simultaneous use with nicotinamide is not recommended.
Oral contraceptives – decrease in cyanocobalamin concentration in blood plasma.
Thiamine – increased risk of allergic reactions caused by thiamine.
Chloramphenicol – decreased hematopoietic response to the drug.
Antimetabolites and most antibiotics alter the results of microbiological studies of cyanocobalamin.
Disodium adenosine triphosphate trihydrate
β-adrenergic blockers, nitrates – increased antianginal effect.
Dipyridamole – enhances the action of the latter, in particular its vasodilator effect.
Potassium-sparing diuretics, potassium supplements, ACE inhibitors – increased risk of hyperkalemia.
Carbamazepine – enhances the effect of adenosine (including to the development of blockade).
Xanthinol nicotinate – weakening the effect of adenosine.
Purine derivatives (caffeine and theophylline) – some antagonism with adenosine is found.
Magnesium preparations – increased risk of hypermagnesemia.
Cardiac glycosides - increased risk of adverse reactions from the cardiovascular system. The drug should not be administered in high doses simultaneously with cardiac glycosides.
Lidocaine hydrochloride
Amitriptyline, bupivacaine, disopyramide, imipramine, nortriptyline, pethidine, quinidine, chlorpromazine - decrease in the concentration of lidocaine in blood plasma.
Antiarrhythmics (including amiodarone, verapamil, quinidine, disopyramide, ajmalin) - increased cardiodepressive effect (due to prolongation of the QT interval) and in very rare cases the development of atrioventricular block or ventricular fibrillation is possible. Simultaneous use with amiodarone may also lead to the development of seizures.
Anticoagulants (including ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) - increased risk of bleeding.
Acetazolamide, thiazide and loop diuretics – weakening of the effect of lidocaine (due to hypokalemia).
Barbiturates (phenobarbital), anticonvulsants – increased metabolism and decreased plasma lidocaine concentration, as well as increased cardiodepressive effect.
β-Adrenergic blockers – slowing down the metabolism and enhancing the effects (including toxic) of lidocaine, in particular increasing the risk of bradycardia and arterial hypotension. When using these agents simultaneously, the dose of lidocaine should be reduced.
Vasoconstrictors (epinephrine, methoxamine, phenylephrine) - possible slowing of absorption and prolongation of the effect of lidocaine.
Glucagon, isadrin – increase in lidocaine clearance.
Guanadrel, guanethidine, mecamylamine, trimetaphan - during spinal and epidural anesthesia, the risk of severe hypotension and bradycardia increases.
Anesthetics (hexobarbital, thiopental sodium intravenously), ethanol - increased respiratory depression.
Agents that cause blockade of neuromuscular transmission – enhancing the effect of such agents (due to a decrease in the conductivity of nerve impulses).
Monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) - increased risk of arterial hypotension. Lidocaine should not be used parenterally during treatment with MAO inhibitors.
Curare-like agents – deepening of myorelaxation (up to paralysis of respiratory muscles).
Mexiletine, norepinephrine – increased toxicity of lidocaine (due to decreased clearance and hepatic blood flow).
Midazolam – increases the concentration of lidocaine in blood plasma.
Narcotic analgesics (morphine) – the analgesic effect of such drugs is enhanced, but respiratory depression is also increased.
Novocaine, novocainamide, procainamide – central nervous system (CNS) excitation, delirium, hallucinations.
Polymyxin B – in case of simultaneous use, respiratory function should be monitored.
Prenylamine – increased risk of torsades de pointes.
Propafenone – increased duration and severity of CNS side effects.
Rifampicin – decreased plasma concentration of the latter.
Sedatives and hypnotics – increased depressant effect on the CNS.
Cardiac glycosides – weakening of the cardiotonic effect of cardiac glycosides. Against the background of digitalis glycoside intoxication, lidocaine may increase the severity of AV block.
Cimetidine – decreased metabolism (decreased hepatic clearance due to inhibition of microsomal oxidation) and increased plasma concentrations of lidocaine, as well as increased toxic effects.
Application features
The drug should be used with caution in patients with bradycardia, first-degree atrioventricular block, incomplete AV block, intraventricular conduction disorders, a tendency to arterial hypotension, moderate heart failure, moderate liver and kidney dysfunction, respiratory dysfunction, a tendency to bronchospasm, a genetic predisposition to malignant hyperthermia, hyperacid gastritis, gastric and duodenal ulcer (outside the exacerbation stage), glaucoma, epilepsy, after heart surgery, with alcohol abuse, patients taking nitrates, calcium channel antagonists, β-adrenoceptor blockers, debilitated patients and elderly patients.
Caution should be exercised and blood coagulation parameters should be monitored when using the drug in patients with a tendency to thrombosis and with angina pectoris.
Intramuscular administration of lidocaine may increase creatinine concentration, which may lead to an error in the diagnosis of acute myocardial infarction.
Before using the drug, patients with heart disease should normalize the level of potassium in the blood plasma, since hypokalemia reduces the effectiveness of lidocaine.
The use of the drug may lead to an increase in the need for insulin in patients with diabetes mellitus. The drug is not advisable to use for the correction of dyslipidemia in patients with diabetes mellitus.
During use of the drug, peripheral blood parameters, liver function, glucose and uric acid levels in blood plasma should be monitored; with prolonged use, potassium and magnesium levels in blood plasma should be monitored.
ECG monitoring is necessary during the use of the drug. In case of development of sinus dysfunction, prolongation of the PQ interval, widening of the QRS complex or arrhythmia, the dose of the drug should be reduced or its use should be discontinued.
If there is a tendency to develop leukocytosis and erythrocytosis, the dose of the drug should be reduced or its use temporarily suspended.
While using the drug, you should limit the consumption of products containing caffeine (coffee, tea and other drinks).
Since prolonged use of the drug can lead to fatty liver disease, to prevent it, patients should include foods rich in methionine in their diet or prescribe methionine and other lipotropic agents.
The medicine contains methyl parahydroxybenzoate (E 218) and propyl parahydroxybenzoate (E 216), which may cause allergic reactions (possibly delayed), and in some cases - bronchospasm.
Ability to influence reaction speed when driving vehicles or other mechanisms
If dizziness or low blood pressure occurs while using the medicine, you should refrain from driving or operating other machinery.
Use during pregnancy or breastfeeding
The drug should not be used during pregnancy. Breastfeeding should be stopped while using the drug.
Method of administration and doses
The drug is intended for intramuscular administration.
After dilution with a solvent, the medicinal product is administered intramuscularly in 1–2 ampoules once a day. As a solvent, a solution of lidocaine hydrochloride included in the kit is used. When the injection site is treated with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.
Administration of lidocaine hydrochloride solution should be carried out only by medical personnel.
The solution should be used immediately after its preparation. The color of the prepared solution should be red. Do not use the solution if the color has changed.
The duration of drug treatment and repeated courses depend on the course and severity of the disease.
Children
There is no experience with the use of the drug in children, therefore it is not recommended for use in this category of patients.
Overdose
Treatment: discontinuation of the drug, oxygen therapy, anticonvulsants, vasoconstrictors (noradrenaline, mezaton), anticholinergics, symptomatic therapy, adenosine antagonists are xanthines (euphylline, theophylline). The patient should be in a horizontal position; it is necessary to ensure access to fresh air, oxygen supply and/or artificial respiration. CNS symptoms are corrected by the use of short-acting benzodiazepines/barbiturates. To correct bradycardia and conduction disorders, use atropine (0.5–1 mg intravenously), with arterial hypotension - sympathomimetics in combination with β-adrenoceptor agonists. In case of cardiac arrest, immediate resuscitation measures are indicated. Intubation and artificial ventilation of the lungs are possible. In the acute phase of overdose, dialysis is ineffective. There is no specific antidote.
Adverse reactions
Blood and lymphatic system disorders: hypercoagulation.
Immune system disorders: hypersensitivity reactions, including anaphylactic shock and anaphylactoid reactions, edema, including Quincke's edema.
From the nervous system: headache, dizziness, short-term loss of consciousness, inhibition, feeling of compression in the head, phobias, nervous excitement, paresthesias.
From the organs of vision: blurred vision, macular edema.
Cardiac: tachycardia, pain in the heart area, arrhythmia, bradycardia, chest discomfort, palpitations, AV conduction disturbances (AV block), asystole.
Vascular disorders: hypertension, hypotension, hot flashes.
Respiratory, thoracic and mediastinal disorders: shortness of breath, bronchospasm.
On the part of the digestive tract: nausea, metallic taste in the mouth, increased motility of the digestive tract, weakening of bowel movements.
Skin and subcutaneous tissue disorders: facial flushing, acrocyanosis, itching, skin rashes, urticaria, acne, bullous rashes, allergic dermatitis, exfoliative dermatitis, dry skin and mucous membranes of the eyes, acanthosis.
On the part of the kidneys and urinary system: increased diuresis.
General disorders and administration site conditions: changes at the injection site, including pain, hyperemia, itching, edema, induration and necrosis at the injection site; weakness, malaise, chills, fever, feeling of heat, increased sweating, pain in the arms, back, neck, disorders of purine metabolism.
Additionally, the following adverse reactions are possible for the solvent (0.5% lidocaine hydrochloride solution).
From the nervous system: motor restlessness, euphoria, drowsiness, sleep disturbances, tremor, trismus, convulsions (the risk of their development increases with hypercapnia and acidosis), motor block, sensory disturbances, anxiety, confusion, coma.
From the organs of vision: nystagmus, diplopia, photophobia, reversible blindness, conjunctivitis, flashing "flies" before the eyes.
From the auditory system: hearing impairment, tinnitus, hyperacusis.
From the respiratory system, chest organs and mediastinum: rhinitis, paralysis of respiratory muscles, respiratory paralysis.
On the part of the digestive tract: vomiting, unpleasant sensations in the epigastrium.
General disorders: weakness, malignant hyperthermia, feeling hot, cold or numb in the extremities.
With prolonged and uncontrolled use - hyperkalemia, hypermagnesemia.
Reporting of suspected adverse reactions
Reporting suspected adverse reactions that occur after the registration of a medicinal product is very important. This allows for continuous monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions through the national pharmacovigilance system.
Expiration date
Ready medicine - 3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in a place protected from light and out of the reach of children.
Packaging
3 brown glass ampoules with the drug (lyophilisate) and 3 brown glass ampoules with the solvent in a contour blister pack; 1 contour blister pack in a cardboard box.
Vacation category
According to the recipe.
Producer
E.I.P.I.Co., Egypt.
Location of the manufacturer and its business address
Tens of Ramadan City, First Industrial Zone, B1, P.O. Box 149 Tens, Egypt.
