Lidokain-Zdorovye, solution for infection 10% on 2 ml No. 10

General characteristics. Structure:

International and chemical name: lidocaine, 2 - (dietilamino-2', to 6 acetoxylidine a hydrochloride); main physical and chemical properties: the transparent, colourless or slightly painted liquid; structure: 1 ml of lidocaine of a hydrochloride (in terms of 100% substance) 100 mg; Excipients: sodium of hydroxide of 1 M solution, water for injections.

Pharmacological properties:

Antiarrhytmic activity of drug is caused by oppression of a phase 4 (diastolic depolarization) in Purkinye's fibers, automatism reduction, suppression of the ectopic centers of excitement. At the same time lidocaine suppresses electric activity depolarized, aritmogenny sites, but minimum influences electric conductivity of normal fabrics. Does not influence the speed of fast depolarization (phase 0) or reduces slightly. Increases permeability of membranes for potassium ions, accelerates process of repolarization of cellular membranes, shortens duration of action potential and the effective refractory period. At use in average therapeutic doses practically does not change contractility of a myocardium, does not slow down AV conductivity, does not reduce arterial pressure is considerable. At use as antiarrhytmic means at intravenous administration action develops - through 45 - 90 with, continues - 10 - 20 min., at intramuscular introduction action develops - in 5 - 15 min. continues - 60 - 90 min.

Has mestnoanesteziruyushchy the activity caused by stabilization of a neyronalny membrane, decrease in its permeability for sodium ions that interferes with emergence of action potential and carrying out impulses.

Pharmacokinetics. At intravenous administration the maximum concentration is reached through 45 - 90 with, at intramuscular - in 5 - 15 min. Linkng with proteins of plasma - 60 - 80% (depending on a dose). Stable concentration in blood is established in 3-4 hours at continuous introduction (at patients with an acute myocardial infarction - in 8-10 hours). Easily passes through gistogematichesky barriers, including hematoencephalic. At first comes to fabrics with good blood supply (heart, lungs, a brain, a liver, a spleen), then - to fatty and muscular fabrics. Gets through a placenta, in an organism of the newborn there are 40 - 55% of concentration of the drug used women in labor. Therapeutic concentration in blood on average - 0,0035 mg/ml.

It is metabolized for 90% in a liver by oxidizing N-dezalkilyuvannya with formation of active metabolites: to a monoyetilglitsinksilidin and a glitsinksilidina, 2 hours and 10 hours having an elimination half-life respectively. Has effect of "the first passing". The elimination half-life after bolyusny introduction makes 1,5 - 2 hours (newborns have 3 hours), at long intravenous infusions till 3 o'clock and more. At an abnormal liver function the elimination half-life can increase more than twice. In not changed view with urine 5 - 20% are removed.

Indications to use:

Ventricular arrhythmias (premature ventricular contraction, tachycardia, trembling, fibrillation), including during the acute period of a myocardial infarction, at implantation of an artificial pacemaker, glikozidny intoxication, an anesthesia.

Route of administration and doses:

Appoint intramusculary, intravenously struyno, kapelno. Solution of lidocaine of 10% is entered exclusively intramusculary! Intramusculary enter into a buttock or deltoid muscle. The adult intramusculary enter 10% solution in a dose of 2 - 4 mg/kg (the maximum single dose - no more than 200 mg (2 ml) with an interval of 4 - 6 hours. Intramuscular introduction is not recommended to children.

Apply 10% to jet introduction the lidocaine solution divorced to concentration of 20 mg/ml of sterile 0,9% solution of sodium of chloride or 5% glucose solution.

Drop introduction apply the solution containing 2 mg of lidocaine in 1 ml; for this purpose 2 ml (1 ampoule) of Lidokain-Zdorovye, solution for injections of 10%, dilute sterile 0,9% of solution of sodium of chloride or 5% of solution of glucose in 100 ml. Total quantity of the entered solution the adult intravenously kapelno per day - no more than 1200 ml. Infusion is carried out under continuous ECG monitoring.

The adult at introduction of a dose of loading (bolyusny) intravenously struyno 0,5 - 2 mg/kg within 3 - 4 minutes; an average single dose - 80 mg, the maximum single dose - 100 mg. Then at once pass to drop infusion with a speed of 0,02 - 0,055 mg/kg/min. (the maximum speed - 2 mg/min.) into 0,9% solution of sodium of chloride or into 5% glucose solution (before drop introduction pass only after jet). Drop infusion can be carried out within 24 - 36 hours (before improvement of a condition of the patient), duration of infusion depends on a condition of the patient and results of use of drug. At introduction within more than 24 hours it is necessary to reduce infusion speed. On a neobkhidnostin a background of drop infusion it is possible to repeat intravenous jet administration of lidocaine in a dose of 40 mg in 10 min. after the first dose of loading.

The maximum dose at intravenous administration of a dose loading - 100 mg, at the subsequent drop infusion - 300 mg (4,5 mg/kg) in 1 hour.

At elderly patients the dose is reduced on 1/3.

At a myocardial infarction before hospitalization as the single preventive dose is entered usually by 4 mg/kg once (as much as possible - 200 - 300 mg (2 - 3 ml of 10% of solution)).

To children 12 years at arrhythmias are more senior appoint only at urgent need with extra care; drug is dissolved as and for adults. Enter intravenously struyno a dose of loading of 1 mg/kg within 5-10 min., if necessary perhaps repeated introduction in 5 min. (the total dose should not exceed 3 mg/kg). For continuous infusion (usually after introduction of a dose of loading) - 0,02 - 0,03 mg/kg/min. The maximum dose for children in case of repeated introduction of a dose of loading with an interval of 5 min. - 3 mg/kg; at continuous infusion (usually after introduction of a dose of loading) - 0,05 mg/kg/min. The maximum daily dose for children - 4 mg/kg.

Features of use:

Before lidocaine use obligatory conducting skin test on individual sensitivity to drug to which hypostasis and reddening of the place of an injection testifies.

With care and in smaller doses apply the patient with heart failure, arterial hypotension, a sinus bradycardia, an incomplete atrioventricular block, disturbances of intra ventricular conductivity, a WPW-syndrome, abnormal liver functions and kidneys, epilepsy, after heart operations, at genetic predisposition to a malignant hyperthermia, the weakened and elderly patients.

During treatment ECG monitoring is necessary. At sinus dysfunction, lengthening of an interval of PQ, the QRS expansion or new arrhythmia it is necessary to reduce a dose of drug or to stop treatment.

At simultaneous use with  adrenoceptors, with Cimetidinum reduction of a dose of lidocaine is required; with polymyxin B - breath function control. During treatment by MAO inhibitors it is not necessary to apply lidocaine parenterally.

Lidocaine cannot be added to blood for transfusion.

Use during pregnancy and feeding by a breast. During pregnancy drug is contraindicated. In need of use in the period of a lactation feeding by a breast should be stopped.

Influence on ability to manage vehicles or to work with mechanisms. After use of lidocaine it is not recommended to be engaged in the types of activity demanding speed of psychomotor reactions.

Side effects:

From the central and peripheral nervous systems and sense bodys: before eyes, a photophobia, a headache, dizziness, a sleep disorder, a diplopia, confusion of consciousness, oppression or an apnoea, muscular twitchings, at excessively bystry intravenous administration and patients with hypersensitivity have an oppression or excitement of the central nervous system, concern, flashing of "front sights" a sonitus, a bradyarthria, euphoria, a tremor, a disorientation, paresthesias, spasms.

From cardiovascular system: at use in high doses - bradycardia, delay of conductivity of heart, a cross heart block, arterial hypotension, a collapse, it is very rare - arterial hypertension.

From the alimentary system:

nausea, vomiting.

Allergic reactions: extremely seldom - skin rash, generalized exfoliative dermatitis, an acute anaphylaxis.

Others:

feeling of heat, cold or numbness of extremities, malignant hyperthermia, oppression of immune system.

At bystry intravenous administration arterial pressure can sharply decrease and develop a collapse (in these cases apply a phenylephine hydrochloride, ephedrine and other vasoconstrictors).

Interaction with other medicines:

Contraindications:

Hypersensitivity to lidocaine, existence in the anamnesis of epileptiform spasms on lidocaine, the expressed bradycardia, the expressed arterial hypotension, cardiogenic shock, severe forms of chronic heart failure, a sick sinus syndrome at elderly, an atrioventricular block of II and III degrees (except for cases when the probe for stimulation of ventricles is entered), a full cross heart block, a hypovolemia, heavy abnormal liver functions, a porphyria, a myasthenia, the period of pregnancy and feeding by a breast, age up to 12 years.

Overdose:

Symptoms: psychomotor excitement, dizziness, the general weakness, a lowering of arterial pressure, a tremor, a vision disorder, toniko-clonic spasms, a coma, a collapse, blockade, oppression of TsNS, an apnoea is possible. The first symptoms of overdose at healthy people arise at concentration of lidocaine in blood more than 0,006 mg/kg, spasms - at 0,01 mg/kg. Treatment: the termination of administration of drug, lung ventilation, an oxygenotherapy, anticonvulsants, vasoconstrictors (noradrenaline, a phenylephine hydrochloride), at bradycardia - cholinolytics (0,5 - 1 mg of atropine). Carrying out an intubation, artificial ventilation of the lungs, resuscitation actions is possible. Dialysis is not effective.

Storage conditions:

To store in the place protected from light at a temperature from 8 °Сдо 25 °C. To store in the place, unavailable to children.

Period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 10% on 2 ml in ampoules, No. 10 in a box, No. 5х2 in the blister in a box, No. 10 in the blister in a box; No. 10 in the blister folding with a latch in a box.