Pharmacological properties

Pharmacodynamics. medicine is a complex of metabolic substances and vitamins.

Niacinamide — one of RR vitamin forms, takes part in oxidation-reduction processes in a cell, improves carbohydrate and nitric metabolism, normalizes lipidic exchange, reduces the level of atherogenous lipoproteins in blood.

Cocarboxylase — a coenzyme which is formed in an organism of thiamine ( _{1 vitamin B} ), arriving from the outside. Plays an important role in carbohydrate metabolism, is a part of enzyme carboxymanholes which catalyzes carboxylation and decarboxylation of α-ketonic acids. Indirectly promotes synthesis of nucleic acids, proteins and lipids. Reduces the level of milk and pyroracemic acids in an organism, promotes digestion of glucose. Improves a trophicity of nervous tissue.

Cyanocobalamine ( _{12 vitamin B} ) in an organism turns into an active form — adenozilkobalamin or kobamid which has high biological activity. Increases synthesis of protein in an organism and promotes its accumulation. Activates exchange of carbohydrates and lipids. Reduces level XC in blood, prevents fat infiltration of a liver. It is necessary for normal functioning of the haematogenic bodies, promotes accumulation in erythrocytes of connections which contain sulfhydryl groups, increasing their resistance to hemolysis. Increases ability of fabrics to regeneration. Has positive impact on function of a liver and nervous system.

Dinatrium adenosine triphosphate trihydrate is derivative adenosine, stimulates metabolic processes. Has hypotensive and antiarrhytmic, vasodilating effect, including on coronary arteries.

Pharmacokinetics of medicine was not investigated by

.

Indication

Neuritis, neuropathy (including at diabetes, pernicious anemia); neuralgia of various origin; myalgia, ischialgia; lumbago, sciatica; bursitis, tendinites; ibs; myocardites; myocardiopathies.

Use

Due to the existence in composition of medicine of lidocaine before use of medicine needs to take skin samples on hypersensitivity. existence of hypersensitivity is demonstrated by hypostasis and reddening in the place of an injection.

Kokarnit solvent to enter

After cultivation medicine of 1 times, in oil on 1–2 ampoules, in day.

Duration of treatment and carrying out repeated courses depend on the disease course and severity.

For medicine kokarnit

Contraindication

: hypersensitivity to medicine components; cardiogenic shock and other types of shock; dekompensirovanny heart failure, syndrome of prolongation of an interval of q-t, severe forms of bradyarrhythmia, av-blockade of ii-iii of degree, sharp myocardial infarction, arterial hypotension, severe forms ag; hemorrhagic stroke; obstructive diseases of a bronchopulmonary system; hyperpotassemia, gipermagniyemiya, severe forms oh; an erythremia, a hyperglobulia, new growths, except for the cases which are followed by megaloblastny anemia and deficiency of b12 vitamin; ulcer of stomach and duodenum in an aggravation stage; gout; hyperuricemia; heavy liver failure (including cirrhosis); dekompensirovanny diabetes, sudden decrease in peripheric vascular resistance in the anamnesis, hypercoagulation (including at sharp fibrinferments); inflammatory diseases of lungs.

In addition for solvent — 0.5% of solution of lidocaine of a hydrochloride: hypersensitivity to other local anesthetics of amide type; sick sinus syndrome; Wolf's syndrome — Parkinson — Whyte; Adams's syndrome — Stokes; angina of exertion of a high functional class; existence in the anamnesis of the epileptiform spasms connected with hydrochloride lidocaine introduction; myasthenia; hypovolemia; porphyria; heavy renal failure.

Side effects

At use of medicine kokarnit

following manifestations of side reactions are possible.

Neurologic violations: a headache, dizziness, a short-term loss of consciousness, feeling of compression in the head, a phobia, nervous excitement, paresthesias.

from an organ of sight: illegibility of sight.

Cardial violations: tachycardia, pain in heart, arrhythmia, bradycardia, unpleasant feelings in breasts, heartbeat, violation of AV conductivity (blockade), an asystolia.

from vessels: decrease in the ABP, hypercoagulation.

from a respiratory system: short wind, bronchospasm.

from digestive system: nausea, metal smack in a mouth, strengthening of motility of a GIT.

General violations: feeling of heat, an indisposition, fever, the increased sweating, hand, back, neck pain, violation of purine exchange.

from skin and hypodermic cellulose: hyperaemia of the person, itch, rash, urticaria, acne, bullous rash, allergic dermatitis, exfoliative dermatitis.

from the immune system: reactions of hypersensitivity, including an acute anaphylaxis, a Quincke's edema.

from kidneys and an urinary system: strengthening of a diuresis.

Local reactions: changes in the injection site, including pain, hyperaemia, an itch, hypostasis.

In addition for solvent (0.5% of solution of lidocaine of a hydrochloride) the following manifestations of side reactions are possible

.

Neurologic violations: motive concern, euphoria, drowsiness, a sleep disorder, a tremor, a lockjaw, spasms (the risk of their development increases at a hypercapnia and acidosis), the motor block, violation of sensitivity.

from an organ of sight: nystagmus, diplopia, photophobia, reverse blindness, conjunctivitis.

from an organ of hearing: hearing disorder, sonitus, hyperacusia.

from a respiratory system: rhinitis, paralysis of respiratory muscles, respiratory paralysis.

from digestive system: vomiting, unpleasant feelings in epigastriums.

General violations: weakness, feeling of heat, cold or numbness of extremities.

At long and uncontrollable reception — a hyperpotassemia, a gipermagniyemiya.

Special instructions

Solution needs to be applied right after its preparation. color of the prepared solution has to be red. not to apply solution if color changed.

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as solvent uses solution of lidocaine of a hydrochloride which goes in a set. Administration of solution of lidocaine of a hydrochloride is carried out only by health workers. When processing the place of an injection the disinfecting solutions containing heavy metals risk of development of local reaction in the form of morbidity and hypostasis increases.

Before use of lidocaine of a hydrochloride at heart diseases (the hypopotassemia reduces efficiency of lidocaine) needs to normalize potassium level in blood plasma.

to apply

With care at bradycardia, AV blockade of the I degree, incomplete AV blockade, violation of intra ventricular conductivity, tendency to arterial hypotension, with heart failure of moderate degree, abnormal liver functions and kidneys of average degree, breath dysfunction, at tendency to bronchospasms, after heart surgeries, at genetic predisposition to a malignant hyperthermia, the weakened patients and patients of advanced age, at hyperacid gastritis, ulcer of stomach and duodenum (out of an aggravation stage), glaucoma, at an alcohol abuse, to the patients accepting nitrates, antagonists of calcium channels, blockers of β-adrenoceptors.

As prolonged use of medicine can lead

to fat dystrophy of a liver, for its prevention it is necessary to include products rich with methionine in a diet of patients or to appoint methionine and other lipotropic means.

Use of medicine can lead

to increase in need for insulin for patients with diabetes, is inexpedient to apply to correction of a dislipidemiya sick diabetes.

during treatment needs to control indicators of peripheral blood, function of a liver, level of glucose and uric acid in blood, at prolonged use it is necessary to control the level of potassium and magnesium in blood.

during treatment the ECG monitoring is necessary for

. In sinus dysfunction, lengthening of an interval of P-Q, the QRS expansion or appearance of arrhythmia it is necessary to lower a dose of medicine or to stop treatment.

during treatment by MAO inhibitors should not apply lidocaine a hydrochloride parenterally.

At introduction of lidocaine of a hydrochloride the concentration of creatinine can increase that can lead to a mistake at establishment of the diagnosis of a sharp myocardial infarction.

to Limit to

use of products which part caffeine is (coffee, tea and other drinks).

not to apply

with medicines which increase blood clotting. It is necessary to be careful in the course of treatment of persons with tendency to a thrombogenesis and at patients with stenocardia and to control fibrillation indicators. At a tendency to development leucio- and a hyperglobulia the dose of medicine needs to be reduced or to temporarily suspend treatment.

Use during pregnancy and feeding by a breast. Not to appoint medicament during pregnancy. For the period of medicament treatment the feeding by a breast needs to be stopped.

Children. Experience of use of medicine for children is absent therefore its application for this category of patients is not recommended.

Influence on ability to steer vehicles or to work with difficult mechanisms. In cases if during treatment the dizziness, decrease in the ABP is observed, it is necessary to refrain from control of vehicles or work with other mechanisms.

Interaction

Dinatrium of adenosine of triphosphate trihydrate. at a concomitant use with kaliysberegayushchy diuretics, medicines of potassium and inhibitors apf risk of development of a hyperpotassemia, with magnesium medicines — gipermagniyemiya increases.

Drug can strengthen anti-anginal action of blockers of β-adrenoceptors, nitrates.

At simultaneous application with Dipiridamolum the effect of Dipiridamolum, in particular vasodilating effect amplifies.

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shows some antagonism at simultaneous application with purine derivatives (caffeine and theophylline).

Cannot be entered along with cardiac glycosides in high doses as risk of development of side reactions from a cardiovascular system increases.

At simultaneous application with Xantinoli nicotinas the effect of sodium of adenosine triphosphate decreases.

Karbamazepin can enhance effects of adenosine, lead to blockade development.

Cyanocobalamine. Aminoglycosides, salicylates, antiepileptic medicines, colchicine, medicines of potassium reduce cyanocobalamine absorption, influence its kinetics. At simultaneous application with Kanamycinum, Neomycinum, polymyxin, tetracycline the absorption of cyanocobalamine decreases.

cyanocobalamine Pharmaceutical is incompatible

with ascorbic acid, salts of heavy metals (cyanocobalamine inactivation), Thiamini bromidum, a pyridoxine, Riboflavinum (the cobalt ion which is contained in a cyanocobalamine molecule destroys other vitamins). In interaction of cyanocobalamine with thiamine the risk of development of the allergic reactions caused by thiamine with chloramphenicol amplifies — the hemopoietic answer to medicine decreases, with Cytamenum — the effect of Cytamenum decreases, with oral contraceptives — concentration of cyanocobalamine in blood decreases. Antimetabolites and the majority of antibiotics change results of microbiological researches of cyanocobalamine.

Lidokain. At the combined use of lidocaine with such medicines as Chlorpromazinum, pethidine, bupivacaine, quinidine, Disopyramidum, amitriptyline, Imipraminum, nortriptilin, concentration of lidocaine in blood plasma decreases.

Antiarrhytmic medicines (including Amiodaronum, verapamil, quinidine, Disopyramidum, Ajmalinum) — cardiodepressive action amplifies (there is a lengthening of an interval of Q-T and development of AV blockade or fibrillation of ventricles is seldom or never possible); simultaneous application with Amiodaronum can lead to development of spasms.

Novocaine, novokainamid, procaineamide — excitement of central nervous system, nonsense, hallucinations is possible.

Kurarepodobny medicines — muscle relaxation amplifies (paralysis of respiratory muscles is possible).

Ethanol strengthens the oppressing effect of lidocaine on breath.

Cimetidinum reduces hepatic clearance of lidocaine (decrease in metabolism owing to inhibition of microsomal oxidation), increases its concentration and risk of development of toxic effects.

Blockers of β-adrenoceptors slow down metabolism of lidocaine in a liver, enhance effects of lidocaine (including toxic) and increase risk of developing bradycardia and arterial hypotension. At simultaneous application of blockers of β-adrenoceptors and lidocaine it is necessary to lower a dose of the last.

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Cardiac glycosides — weakens cardiotonic effect of cardiac glycosides. Foxglove glycosides — against the background of intoxication lidocaine can increase weight of AV blockade.

Sleeping or sedative medicines — strengthening of the oppressing action on central nervous system of somnolent and sedative medicines is possible.

Narcotic analgetics (morphine) — analgeziruyushchy effect of narcotic analgetics, respiratory depression amplifies.

MAO Inhibitors (furasolidone, Procarbazinum, selegilin) — risk of developing arterial hypotension increases.

Anticoagulants (including ardeparin, dalteparin, danaparoidy, enoksaparin, heparin, warfarin) increase risk of developing bleedings.

Anesthetic — the oppressing action on a respiratory center of anesthetics amplifies (hexobarbital, sodium thiopental in / c).

Polymyxin B — is necessary for

breath function control.

Rifampitsin — decrease in concentration of the last in blood is possible.

Propafenon — increase in duration and a complication of side effects from central nervous system is possible.

Prenylaminum — raises risk of developing ventricular arrhythmia like pirouette.

Anticonvulsants, barbiturates (phenobarbital) — acceleration of metabolism of lidocaine in a liver, decrease in concentration in blood, strengthening of cardiodepressive effect is possible.

Isadrinum, a glucagon — raises clearance of lidocaine.

Norepinephrinum, meksiletin — decreases clearance of lidocaine (the toxicity amplifies), the hepatic blood-groove decreases.

Acetazoleamide, thiazide and loopback diuretics reduce effect of lidocaine as a result of a hypopotassemia.

Midazolam — raises concentration of lidocaine in blood plasma.

Drugs causing neuromuscular transmission blockade — effect of these medicines as they reduce conductivity of nervous impulses amplifies.

Niacin/niacinamide. Exponentiates action of fibrinolytic means, spasmolysants and cardiac glycosides, strengthens toxic impact of alcohol on a liver.

Should be careful at simultaneous application with antihypertensives (possibly strengthening of hypotensive action), anticoagulants, acetylsalicylic acid (in connection with risk of development of hemorrhages).

is Reduced by action of a probenetsin, toxicity of Neomycinum and prevents the decrease in concentration of XC induced by the last and LPVP. Weakens toxic action of barbiturates, antituberculous remedies, streptocides.

Oral contraceptives and an isoniazid slow down transformation of tryptophane to niacin and thus can increase the need for niacin. Antibiotics can strengthen hyperaemia caused by niacin. It was reported about rhabdomyolysis cases at use of niacin with lovastatiny.

Overdose

Symptoms: dizziness, weakness, tremor, ventricular violations; disorders of vision; toniko-clonic spasms; psychomotor excitement, the syncopal state connected with sudden decrease hell; collapse; stagnant heart failure, fluid lungs; hypercoagulation, thrombosis of peripheral vessels; coma, asphyxia; apnoea or strengthening of manifestations of side reactions.

Treatment: the termination of administration of medicine, oxygenotherapy, anticonvulsants, vasoconstrictors (Norepinephrinum, a phenylephine hydrochloride), cholinolytics, symptomatic therapy, antagonists of adenosine are xanthines (Euphyllinum, theophylline). The patient has to be in horizontal position; it is necessary to provide access of fresh air, supply of oxygen and/or performing artificial respiration. Symptoms from central nervous system are adjusted by application of benzodiazepines/barbiturates of short-term action. To apply atropine (0.5-1 mg) to correction of bradycardia and violations of conductivity, at arterial hypotension — sympathomimetics in a combination with agonists of β-adrenoceptors. In cardiac arrest immediate holding resuscitation actions is shown. Carrying out an intubation, IVL is possible. In a sharp phase of overdose dialysis is inefficient. There is no specific antidote.

Storage conditions

At a temperature not above 25 °C.