Borivit

General characteristics. Structure:

Active ingredients: 100 mg of thiamin of a hydrochloride, 100 mg of a pyridoxine of a hydrochloride, 1 mg of cyanocobalamine, 20 mg of lidocaine of a hydrochloride in 2 ml of solution.

Excipients: benzyl alcohol, sodium hexametaphosphate, potassium hexacyanoferrate, sodium hydroxide, water for injections.

Pharmacological properties:

Pharmacodynamics. Complex of vitamins of group B. Neurotropic vitamins of group B make favorable impact on inflammatory and degenerative diseases of nerves and the motive device, in high doses have analgetic properties, promote strengthening of a blood-groove and normalize work of a nervous system and process of a hemopoiesis (B12 vitamin - cyanocobalamine).

Thiamin (B1 vitamin) plays a key role in metabolism of carbohydrates, and also in a tricarbonic acid cycle with the subsequent participation in synthesis of TPF (thiamin a pyrophosphate) and ATP (adenosine triphosphate).

The pyridoxine (B6 vitamin) participates in metabolism of protein and, partially, in metabolism of carbohydrates and fats.

Physiological function of thiamin and pyridoxine is the potentiation of action of each other which is shown in positive influence on nervous and cardiovascular systems. At deficit of B6 vitamin eurysynusic conditions of deficit are quickly stopped after administration of these vitamins.

Cyanocobalamine (B12 vitamin) participates in synthesis of a myelin cover, stimulates a hemogenesis, reduces the pain connected with defeat of a peripheral nervous system, stimulates nucleinic exchange through activation of folic acid.

Lidocaine - the mestnoanesteziruyushchy means causing all types of local anesthesia (terminal, infiltration, conduction).

Pharmacokinetics. Absorption. After intramuscular introduction (in oil) thiamin is quickly absorbed and comes to blood. Concentration of thiamin makes 484 ng/ml in 15 min. after administration of drug in a dose of 50 mg (in the 1st day of introduction).

After introduction in oil the pyridoxine is quickly absorbed in a system blood stream and distributed in an organism, carrying out a coenzyme role after phosphorylation of the CH2OH group in the 5th situation.

Distribution. Thiamin is distributed in an organism unevenly. Content of thiamin in leukocytes makes 15%, in erythrocytes – 75% and in plasma – 10%. Due to the lack of considerable reserves of vitamin B an organism it has to come to an organism daily. Thiamin passes through a blood-brain barrier and a placental barrier and it is found in maternal milk.

The pyridoxine is distributed in all organism, passes through a placenta and it is found in maternal milk. The organism contains 40-150 mg of B6 vitamin, its daily speed of elimination makes about 1,7-3,6 mg at a speed of completion of 2,2 - 2,4%.

Metabolism and removal. The main metabolites of thiamin are tiaminkarbonovy acid, pyramine and some unknown metabolites. From all vitamins thiamin remains in an organism in the smallest quantities. The organism of the adult contains about 30 mg of thiamin in the form of 80% of thiamin of a pyrophosphate, 10% of thiamin of triphosphate and other quantity in the form of monophosphate thiamin. Thiamin is removed with urine, α-phase T1/2 - 0.15 h, β-phases - 1 h and a terminal phase - within 2 days.

The pyridoxine is deposited in a liver and is oxidized to 4-pyridoxynew acid which is removed with urine, at most in 2-5 h after absorption.

Indications to use:

The neurologic frustration of various origin caused by a group B vitamin deficiency which cannot be eliminated by correction of food.

Route of administration and doses:

In hard cases and at acute pains appoint intramusculary (deeply) 1 time a day in a dose 2 ml. After there will pass the aggravation, and at easy forms of a disease 1 injection 2-3 times a week is necessary. Further for continuation of treatment pass to reception of a dosage form for intake.

Weekly control of treatment by the doctor is recommended. Whenever possible it is necessary to aim at early transfer of the patient into treatment by a peroral form of Borivit.

Medicine is entered exclusively intramusculary. At accidental introduction observation of the doctor is intravenously necessary. In breaks between injections and after a course of parenteral therapy, and also at insignificant expressiveness of process transfer of the patient into reception of the tableted medicines containing group B vitamins is recommended.

Before use of lidocaine conducting skin test on the increased individual sensitivity to medicine which confirms is obligatory swelled also reddening of the place of an injection.

Features of use:

Children and elderly patients. Medicine should not be applied at children 12 years owing to availability in structure of an injection of benzyl alcohol and high doses of vitamins are younger. For elderly patients correction of a dose usually is not required.

Medicine is entered exclusively intramusculary. At accidental introduction observation of the doctor is intravenously necessary. Long reception of medicine (over 6 months) can cause development of neuropathy.

Renal failure: with an impaired renal function correction of a drug dose is not required from patients.

Abnormal liver function: with the broken function of a liver correction of a drug dose is not required from patients.

Before use of lidocaine conducting skin test on individual sensitivity to medicine which confirms is obligatory swelled also reddening of the place of an injection. At introduction to vaskulyarizirovany fabrics it is recommended to carry out aspiration test and to enter carefully for prevention of hit of lidocaine into a blood channel. Before administration of lidocaine in high doses purpose of barbiturates is recommended.

When processing the place of an injection the disinfecting solutions containing heavy metals the risk of development of local reaction in the form of morbidity and hypostasis increases.

At use of lidocaine ECG control is obligatory. In case of disturbances of activity of a sinus node, lengthening of an interval of PQ, the QRS expansion or at development of new arrhythmia it is necessary to reduce a dose or to cancel medicine.

With care and in smaller doses apply to patients with heart failure, arterial hypertension, an incomplete atrioventricular block, disturbances of intra ventricular conductivity, abnormal liver functions and kidneys, epilepsy, after heart operations, at genetic predisposition to a hyperthermia, the weakened patients.

To apply with care to patients of advanced age, and also persons with arrhythmia in the anamnesis.

Side effects:

Allergic reactions: very seldom - an itch, urticaria, the complicated breath, a Quincke's edema, an acute anaphylaxis;

Others: seldom - the increased sweating, tachycardia, acne rash.

Development of system reactions in the form of dizziness, nausea, arrhythmia, bradycardia, spasms is possible in case of very bystry parenteral administration or overdose.

Interaction with other medicines:

Thiamin completely collapses in the solutions containing sulfites.

Other vitamins are inactivated in the presence of decomposition products of vitamins of group B.

The pyridoxine reduces effect of a levodopa.

At parenteral use of lidocaine in case of additional use of Norepinephrinum and Epinephrinum strengthening of side effect on heart is possible. In case of overdose of mestnoanesteziruyushchy medicines it is impossible to apply Epinephrinum and Norepinephrinum in addition.

Interaction of medicine with Cycloserinum,   D-Penicillaminum, Epinephrinum, Norepinephrinum, sulfonamides which leads to decrease in effect of a pyridoxine is possible.

Thiamin is incompatible with the oxidizing substances, mercury chloride, iodide, a carbonate, acetate, tannin acid, iron-ammonium-citrate, and also phenobarbital, Riboflavinum, benzylpenicillin, a dextrose and metabisulphite.

Copper accelerates thiamin destruction.

Thiamin loses the action at increase in values рН (more than 3).

B12 vitamin is incompatible with salts of heavy metals.

The interactions caused by the content of lidocaine of a hydrochloride: lidocaine strengthens the oppressing action on a respiratory center of anesthetics (hexobarbital, sodium thiopental intravenously), hypnotic drugs and sedatives.

At simultaneous use with hypnotic drugs and sedatives strengthening of the oppressing action on the central nervous system is possible. Ethanol strengthens the oppressing action influence of lidocaine on breath function. At simultaneous use with blockers of adrenoceptors reduction of a dose of lidocaine is necessary.

At simultaneous use with polymyxin B – breath function control is necessary. During treatment by MAO inhibitors it is not necessary to apply lidocaine parenterally as it increases risk of development of arterial hypotension. At simultaneous use with procaineamide hallucinations are possible.

Lidocaine can strengthen effect of the medicines causing neuromuscular transmission blockade as the last reduce conductivity of nervous impulses. At intoxication cardiac glycosides lidocaine can increase weight of AV blockade. Lidocaine weakens cardiotonic effect of cardiac glycosides.

With care appoint with:

- blockers of r-adrenoceptors – slow down metabolism of lidocaine in a liver, effects of lidocaine amplify (including toxic) and the risk of development of bradycardia and arterial hypertension increases;

- kurarepodobny medicines – muscle relaxation deepening is possible (to paralysis of respiratory muscles);

- Norepinephrinum, meksiletiny – toxicity of lidocaine amplifies (the clearance of lidocaine decreases);

- Isadrinum, a glucagon – the clearance of lidocaine increases;

- midazolam – concentration of lidocaine in a blood plasma increases;

- anticonvulsant drugs (PSP), barbiturates (including with phenobarbital) – acceleration of metabolism of lidocaine in a liver, decrease in concentration in blood is possible;

- antiarrhytmic means (Amiodaronum, verapamil, quinidine, Ajmalinum, Disopyramidum, propafenony), PSP (hydantoin derivatives) – amplifies cardiodepressive action; simultaneous use with Amiodaronum can lead to development of spasms;

- novocaine, novokainamidy – excitement of the central nervous system and developing of hallucinations is possible;

- morphine – strengthens analgeziruyushchy effect of morphine;

- Prenylaminum – increases risk of development of gastric arrhythmia like "pirouette";

- rifampicin – decrease in concentration of lidocaine in blood is possible;

- Phenytoinum – strengthens cardiodepressive effect of lidocaine;

- vasoconstrictors (Epinephrinum, метоксамин, Phenylephrinum) – promote delay of absorption of lidocaine and prolong its action.

Contraindications:

Hypersensitivity to medicine components, and also to other amide mestnoanesteziruyushchy medicines; instructions in the anamnesis on the epileptoformny spasms connected with administration of Lidocaine of a hydrochloride; AV-blockade of II and III degrees, a sick sinus syndrome, a WPW-syndrome, Adams-Stokes's syndrome, severe forms of heart failure, the expressed arterial hypotension, bradycardia, cardiogenic shock, a full cross heart block; myasthenia; hypovolemia; a porphyria, a heavy renal and/or liver failure, pregnancy, the feeding period a breast, age up to 12 years.

Overdose:

Symptoms: in cases of very bystry administration of drug there can be dizziness, arrhythmia, spasms, they can also be overdose symptoms.

Treatment: carry out symptomatic therapy.

Lidocaine overdose: the main symptoms connected with oppression of the central nervous system and cardiovascular system: general weakness, dizziness, disorientation, toniko-clonic spasms, coma, tremor, vision disorder, atrioventricular block, asphyxia, nausea vomiting, euphoria, psychomotor excitement, adynamy, apnoea, bradycardia, lowering of arterial pressure, collapse.

The first symptoms of overdose at healthy people arise at concentration of lidocaine of a hydrochloride in blood more than 0,006 mg/kg, spasms – at 0,01 mg/kg.

Treatment: termination of administration of medicine, oxygenotherapy, vasoconstrictors (noradrenaline, phenylephine hydrochloride), anticonvulsants, cholinolytics. The patient should be in horizontal position; it is necessary to provide access of fresh air, supply of oxygen and/or carrying out an artificial respiration. Symptoms from the central nervous system are adjusted by use of benzodiazepines or barbiturates of short-term action. Apply atropine (0,5-1,0 mg) to correction of bradycardia and disturbances of conductivity, at arterial hypotension - sympathomimetics in a combination with agonists of r-adrenoceptors. At a cardiac standstill immediate holding resuscitation actions is shown. Carrying out an intubation, artificial ventilation of the lungs is possible. In an acute phase of overdose by lidocaine dialysis is not effective.

There is no special antidote.

Storage conditions:

In the place protected from light, at a temperature from 8 °C to 15 °C. Not to freeze. To store in the place, unavailable to children. A period of validity - 2 years. Medicine cannot be used after the termination of a period of validity.

Issue conditions:

According to the recipe

Packaging:

On 2 ml in ampoules, on 10 ampoules together with a knife or the scarificator for opening of ampoules and a leaf insert place in a box from a cardboard (packaging No. 10; No. 10х1).