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Composition:


active ingredients: thiamine hydrochloride, pyridoxine hydrochloride, vitamin B12 crystalline (cyanocobalamin);


1 ml of the solution contains thiamine hydrochloride (in terms of 100% Substance) 50 mg, pyridoxine hydrochloride (in terms of 100% Substance) 50 mg, vitamin B12 crystalline (cyanocobalamin) (in terms of 100% Substance) 0.5 mg;


excipients: lidocaine hydrochloride, benzyl alcohol, sodium polyphosphate, potassium ferricyanide, sodium hydroxide, water for injection.


Dosage form. Solution for injection.


Basic physical and chemical properties: clear red liquid.


Pharmacotherapeutic group. Vitamin B1 preparations in combination with vitamin B6 and/or vitamin B12. ATX code A11D B.


Pharmacological properties.


Pharmacodynamics.


Neurotropic B vitamins have a beneficial effect on inflammatory and degenerative diseases of the nerves and motor system. Use to eliminate deficient conditions. In large doses, they have analgesic properties, improve blood circulation and normalize the nervous system and the process of hematopoiesis.


Vitamin B1 is a very important active substance. In the body, vitamin B1 is phosphorylated to form biologically active thiamine diphosphate (cocarboxylase) and thiamine triphosphate (TTR).


Thiamine diphosphate as a coenzyme is involved in important functions of carbohydrate metabolism, which are crucial in the metabolic processes of nervous tissue, affect the conduction of nerve impulses in synapses. When vitamin B1 is insufficient, metabolites accumulate in the tissues, primarily lactic and pyruvic acid, which leads to various pathological conditions and disorders of the nervous system.


Vitamin B6 in its phosphorylated form (pyridoxal-5’-phosphate, PALP) is a coenzyme of a number of enzymes that interact in the general non-oxidative metabolism of amino acids. Through decarboxylation, they are involved in the formation of physiologically active amines (epinephrine, histamine, serotonin, dopamine, tyramine), through transamination – to anabolic and catabolic metabolic processes (for example, glutamate-oxaloacetate transaminase, glutamate pyruvate transaminase, γ-aminobutyric acid, α-ketoglutarattransaminase), as well as to various processes of breakdown and synthesis of amino acids. Vitamin B6 acts on four different sites of tryptophan metabolism. In the processes of hemoglobin synthesis, vitamin B6 catalyzes the formation of α-amino-β-ketoadinic acid.


Vitamin B12 is essential for cellular metabolism. It affects the function of hematopoiesis (external anti-anemic factor), participates in the formation of choline, methionine, creatinine, nucleic acids, and has an analgesic effect.


Pharmacokinetics.


After parenteral administration, thiamine is distributed in the body. Approximately 1 mg of thiamine is broken down daily. Metabolites are excreted in the urine. Dephosphorylation occurs in the kidneys. The biological half-life of thiamine is 21 minutes. The accumulation of thiamine in the body does not occur due to its limited dissolution in fats.


Vitamin B6 is phosphorylated and oxidized to pyridoxal-5-phosphate. In blood plasma, pyridoxal-5-phosphate and pyridoxal bind to albumin. The form that is transported is pyridoxal. To pass through the cell membrane, pyridoxal - 5-phosphate bound to Albumin is hydrolyzed by alkaline phosphatase to pyridoxal.


Vitamin B12 after parenteral administration forms transport protein complexes that are rapidly absorbed by the liver, bone marrow, and other proliferative organs. Vitamin B12 enters the bile and participates in the intestinal-hepatic circulation. Vitamin B12 passes through the placenta.


Clinical characteristics.


Indications.


Neurological diseases of various origins: neuritis, neuralgia, polyneuropathies (diabetic, alcoholic), radicular syndrome, retrobulbar neuritis, facial nerve damage.


Contraindications.


Hypersensitivity to the components of the drug; acute violation of cardiac conduction; acute form of decompensated heart failure.


Vitamin B1 is contraindicated in allergic reactions.


Vitamin B6 is contraindicated for peptic ulcer of the stomach and duodenum in the acute stage (since it is possible to increase the acidity of gastric juice).


Vitamin B12 is contraindicated for use in erythremia, erythrocytosis, and thromboembolism.


Lidocaine. Hypersensitivity to lidocaine or other amide local anesthetics, a history of epileptiform seizures on lidocaine, severe bradycardia, severe hypotension, cardiogenic shock, severe forms of chronic heart failure (II–III degrees), sinus node weakness syndrome, Wolf-Parkinson-White syndrome, Adams-Stokes syndrome, atrioventricular block (AV) II and III degrees, hypovolemia, severe liver/kidney dysfunction, porphyria, myasthenia gravis.


Interactions with other drugs and other types of interactions.


The action of thiamine is inactivated by 5-fluorouracil, since the latter competitively inhibits the phosphorylation of thiamine to thiamine pyrophosphate. Loop diuretics, such as furosemide, which inhibit tubular reabsorption, can cause increased thiamine excretion during long-term therapy and thus reduce thiamine levels.


Concomitant use with levodopa is contraindicated, as vitamin B6 may reduce the antiparkinsonian effect of levodopa. Concomitant use with pyridoxine antagonists (for example, isoniazid, hydralazine, penicillamine or cycloserine), oral contraceptives may increase the need for vitamin B6.


Drinking beverages containing sulfites (such as wine) increases the degradation of thiamine.


Lidocaine enhances the depressing effect on the respiratory center of anesthesia agents (hexobarbital, sodium thiopental intravenously), sleeping pills and sedatives; weakens the cardiotonic effect of digitoxin. When used concomitantly with sleeping pills and sedatives, it is possible to increase the depressing effect on the central nervous system. Ethanol enhances the depressing effect of lidocaine on respiratory function.


Adrenoblockers (including propranolol, Nadolol) – slow down the metabolism of lidocaine in the liver, enhance the effects of lidocaine (including toxic ones) and increase the risk of bradycardia and hypotension. 


Curare-like drugs - possible deepening of muscle relaxation (up to paralysis of the respiratory muscles).


Norepinephrine, mexiletin - increases the toxicity of lidocaine (decreases the clearance of lidocaine).


Isadrin and glucagon – increases lidocaine clearance.


Cimetidine, midazolam - increases the concentration of lidocaine in plasma. Cimetidine displaces protein binding and slows down lidocaine inactivation in the liver, which leads to an increased risk of increased lidocaine side effects. Midazolam moderately increases the concentration of lidocaine in the blood.


Anticonvulsants, barbiturates – including phenobarbital) - it is possible to accelerate the metabolism of lidocaine in the liver, reduce the concentration in the blood.


Antiarrhythmic drugs (amiodarone, verapamil, quinidine, aimalin, disopyramide), anticonvulsants (hydantoin derivatives) – increases the cardiodepressive effect; simultaneous use with Amiodarone can lead to the development of seizures.


Novocaine, novocainamide-when combined with lidocaine, it is possible to excite the central nervous system, hallucinations.


Monoamine oxidase inhibitors, aminazine, bupivacaine, amitriptyline, nortriptyline, imipramine – when combined with Lidocaine, the risk of hypotension increases and the local anesthetic effect of the latter is prolonged.


Narcotic analgesics – when combined with Lidocaine, the analgesic effect of narcotic analgesics increases, but respiratory depression also increases.


Prenylamine-increases the risk of developing ventricular arrhythmia of the "pirouette"type.


Propafenone-it is possible to increase the duration and severity of side effects from the central nervous system.


Rifampicin-a possible decrease in the concentration of lidocaine in the blood.


Polymyxin B-respiratory function should be monitored.


Procainamide - possible hallucinations.


Cardiac glycosides-when combined with Lidocaine, the cardiotonic effect of cardiac glycosides is weakened.


Digitalis glycosides-lidocaine may increase the severity of AV block during intoxication.


Vasoconstrictors (epinephrine, methoxamine, phenylephrine) – when combined with lidocaine, they help slow down the absorption of lidocaine and prolong the effect of the latter.


Guanadrel, guanethidine, mecamylamine, trimetafan – combined use for spinal and epidural anesthesia increases the risk of severe hypotension and bradycardia.


beta – blockers-when used in combination, they slow down the metabolism of lidocaine in the liver, increase the effects of lidocaine (including toxic ones), and increase the risk of bradycardia and hypotension.  With simultaneous use of beta-blockers and lidocaine, it is necessary to reduce the dose of the latter.


Acetazolamide, thiazide and loop diuretics – when combined with lidocaine, as a result of creating hypokalemia, reduce the effect of the latter.


Anticoagulants (including ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) – when combined with lidocaine, increase the risk of bleeding.


Anticonvulsants, barbiturates – phenytoin) - when combined with lidocaine, it is possible to accelerate the metabolism of lidocaine in the liver, reduce the concentration in the blood, and increase the cardiodepressive effect.


Drugs that cause neuromuscular transmission blockade – when combined with Lidocaine, the effect of drugs that cause neuromuscular transmission blockade increases, since the latter reduce the conduction of nerve impulses.

Application features.


The drug should not be administered intravenously.


Parenteral administration of vitamin B12 may temporarily affect the diagnosis of funicular myelosis or pernicious anemia.


Long-term use of vitamin B6 (more than 6-12 months) in doses of more than 50 mg daily or in doses of more than 1000 mg per day (more than 2 months) can lead to reversible peripheral sensory neuropathy. If symptoms of peripheral sensory neuropathy (paresthesia) occur, the dose of the drug should be adjusted and, if necessary, treatment should be discontinued.


The drug contains sodium compounds. This should be taken into account in patients who are on a salt-free diet. Each ampoule may contain potassium residues.


Since the drug contains vitamin B6, the drug should be used with caution in patients with a history of peptic ulcer of the stomach and duodenum, with severe renal and hepatic impairment.


Patients with neoplasms, except in cases accompanied by megaloblastic anemia and vitamin B12 deficiency, should not use the drug.


The drug should not be used for severe decompensation of cardiac activity and angina pectoris.


Since the drug contains lidocaine, it should be noted that when treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of soreness and swelling increases.


Since lidocaine has a pronounced antiarrhythmic effect and can itself act as an arrhythmogenic factor that can cause the development of arrhythmia, the drug should be used with caution in people with complaints of arrhythmia in the past.


Use with caution in patients with moderate heart failure, moderate hypotension, incomplete AV block, impaired intraventricular conduction, moderate liver and kidney function disorders (creatinine clearance 10 mL/min), respiratory disorders, epilepsy, after heart surgery, with a genetic predisposition to hyperthermia, weakened patients and elderly patients.


During the use of lidocaine, ECG monitoring is mandatory. In case of sinus node disorders, prolongation of the PQ interval, expansion of QRS, or the development of a new arrhythmia, the dose should be reduced or the drug should be discontinued.


Before using lidocaine for heart diseases (hypokalemia reduces the effectiveness of lidocaine), it is necessary to normalize the level of potassium in the blood.


When administered intramuscularly, the concentration of creatinine may increase, which may lead to an error in the diagnosis of acute myocardial infarction.


Use during pregnancy or lactation.


The daily requirement for vitamin B6 during pregnancy and/or lactation is up to 25 mg.


The drug contains 100 mg of vitamin B6 in an ampoule, so it should not be used during pregnancy and/or lactation.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


The drug does not affect the ability to drive vehicles or work with complex mechanisms.


If dizziness is observed during treatment with the drug, you should refrain from driving vehicles or working with other mechanisms.


Dosage and administration.


For intramuscular administration.


Before using a drug containing lidocaine, it is mandatory to conduct a skin test for increased individual sensitivity to the drug, which is indicated by swelling and redness of the injection site.


In severe (acute) cases, treatment should begin with 2 ml of the solution intramuscularly 1 time a day until acute symptoms are relieved. To continue treatment, prescribe 2 ml (1 injection) 2-3 times a week. The course of treatment lasts at least 1 month.


Intramuscular injection should be performed in the upper outer quadrant of the gluteal muscle.


To maintain or continue the therapeutic course of injections or to prevent relapse, it is recommended to use oral medications of a similar pharmacotherapeutic group.


Children.


The drug should not be used in children.


Overdose.


In case of overdose, the symptoms of side effects of the drug increase.


Vitamin B1 has a wide therapeutic range. Very high doses (more than 10 g) show a curare-like effect, suppressing the conduction of nerve impulses.


Vitamin B6 has very low toxicity.


Excessive use of vitamin B6 in doses of more than 1 g per day for several months can lead to neurotoxic effects.


Neuropathies with ataxia and sensitivity disorders, cerebral convulsions with changes in the EEG, as well as in rare cases hypochromic anemia and seborrheic dermatitis were described after administration of more than 2 g per day.


Vitamin B12: after parenteral administration (in rare cases – after oral administration) of doses of the drug higher than recommended, allergic reactions, eczematous skin disorders and a benign form of acne were observed.


With prolonged use in high doses, there may be a violation of the activity of liver enzymes, pain in the heart, hypercoagulation.


Treatment: symptomatic therapy.


Lidocaine. Symptoms: psychomotor agitation, dizziness, general weakness, decreased blood pressure, tremor, visual impairment, tonic-clonic seizures, coma, collapse, possible atrioventricular block, central nervous system depression, respiratory arrest. The first symptoms of overdose in healthy people occur when the concentration of lidocaine in the blood is more than 0.006 mg/kg, convulsions – at 0.01 mg/kg.


Treatment: discontinuation of the drug, oxygen therapy, anticonvulsants, vasoconstrictors (norepinephrine, mezaton), with bradycardia – cholinolytics (0.5-1 mg of atropine). Intubation, artificial ventilation, and resuscitation measures are possible. Dialysis is ineffective.


Adverse reactions.


Long-term use (more than 6-12 months) in doses of more than 50 mg of vitamin B6 daily can lead to peripheral sensory neuropathy, nervous excitement, malaise, dizziness, headache.


From the digestive tract: gastrointestinal disorders, including nausea, vomiting, diarrhea, abdominal pain, increased acidity of gastric juice.


Immune system disorders: hypersensitivity reactions, including rash, respiratory disorders, anaphylactic shock, angioedema; increased sweating.


From the skin: pruritus, urticaria, acne, generalized exfoliative dermatitis, angioedema.


From the cardiovascular system: tachycardia, arrhythmias, bradycardia, slowing of heart conduction, transverse heart block, cardiac arrest, peripheral vasodilation, collapse, tachycardia, increased/decreased blood pressure, heart pain.


From the nervous system: agitation of the central nervous system (CNS) (when used in high doses), anxiety, headache, dizziness, sleep disorders, confusion, drowsiness, loss of consciousness, coma; in patients with hypersensitivity – euphoria, tremor, trismus, motor restlessness, paresthesia, convulsions.


From the side of the visual organs: nystagmus, reversible blindness, diplopia, flickering of "flies" in front of the eyes, photophobia, conjunctivitis.


From the side of the hearing organs: auditory disorders, tinnitus, hyperacusia.


From the respiratory system: shortness of breath, rhinitis, depression or respiratory arrest.


Others: a feeling of heat, cold or numbness of the extremities, swelling, weakness, malignant hyperthermia, impaired sensitivity, motor block.


General disorders: injection site reactions.


In the case of very rapid parenteral administration, systemic reactions in the form of seizures may develop.

Tags: Diagram [Thiamine Hydrochloride, Cyanocobalamin]