Lidocaine hydrochloride

General characteristics. Structure:

Active ingredient: lidocaine hydrochloride;

1 ml of solution contains hydrochloride lidocaine in recalculation on anhydrous substance 20 mg;

excipients: sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Mestnoanesteziruyushchy means, for implementation of all types of local anesthesia: terminal, infiltration, conduction. Relative toxicity of Lidocaine of a hydrochloride depends on concentration of solutions. In small concentration (0,5%) it significantly does not differ on toxicity from novocaine, with increase in concentration (1% and 2%) toxicity increases (on

40-50%).

Pharmacokinetics. At topical administration on mucous membranes lidocaine is soaked up in different degree,  depending on  a dose  and    a site of application  (the maximum  concentration  is reached  through

10-20 minutes); absorption is influenced by perfusion speed through a mucous membrane. At intramuscular introduction the maximum concentration is reached in 5-15 minutes. Linkng with proteins of a blood plasma – 60-80% (depending on a dose). Easily gets through gistogematichesky barriers, including hematoencephalic. In the beginning 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 40-55% of concentration of drug, concerning the woman in labor are defined.

It Metabilizirutsya for 90% in a liver by oxidizing N-dealkylation with formation of active metabolites: a monoetilglitsinksilidina and a glitsinksilidina which have elimination half-lives of 2 and 10 hours respectively. There is an effect of "the first passing".

At an abnormal liver function the elimination half-life can increase more than twice. In not changed view with urine 5-20% are removed.

The main physical and chemical the svoystva:prozrachny colourless or slightly painted liquid.

Incompatibility.

Drug should not be mixed with other medicines in one capacity. Lidocaine drops out in a deposit when mixing with Amphotericinum, metogeksitony or sulfatiaziny. Depending on рН solution lidocaine can be incompatible with ampicillin.

Indications to use:

Local anesthesia (terminal, infiltrative, conduction) in surgery, ophthalmology, stomatology, otolaryngology; blockade of peripheral nerves and neuroplexes at various pain syndromes.

Route of administration and doses:

Before use of Lidocaine of a hydrochloride conducting skin test on the increased individual sensitivity to drug about which hypostasis and reddening of the place of an injection testifies is obligatory.

For local anesteziiprimenyat injektsionno (subcutaneously, intramusculary) and locally on mucous membranes. It is necessary to avoid intravascular administration of drug.

For conduction anesthesia (including for anesthesia of humeral and sacral textures) the usual dose for adults makes 5-10 ml of solution (100-200 mg of lidocaine).

For anesthesia of fingers of extremities, a nose, usheyvvodit 2-3 ml of solution (40-60 mg of Lidocaine of a hydrochloride). The maximum dose of solution of Lidocaine гидрохлоридадля adults when using for conduction anesthesia – 10 ml (200 mg of Lidocaine of a hydrochloride).

For all types of injection anesthesia the lidocaine combination to Epinephrinum (1:50000-1:100000) is possible, except for cases when systemic action which carries out

 

Epinephrinum (adrenaline), it is undesirable – hypersensitivity to Epinephrinum, arterial hypertension, a diabetes mellitus, glaucoma or is required short-term anesthetic effect. Epinephrinum promotes delay of absorption of lidocaine and prolongs its action.

For anesthesia in офтальмологиипо 2 drops of solution instilirut in a conjunctival sac 2-3 times with an interval of 30-60 seconds just before a research or surgical intervention.

For terminal to an anesteziislizistya of a cover grease with lidocaine solution of no more than 20 ml for adults in a dose up to 2 mg/kg of body weight, anesthesia duration –    15-30 minutes. The maximum dose of solution for adults makes 20 ml.

To children at all types of peripheral anesthesia the total dose of Lidocaine of a hydrochloride should not exceed 3 mg/kg of body weight.

Features of use:

Before use of lidocaine conducting skin test on individual sensitivity to drug to which hypostasis and reddening of the place of an injection testifies is obligatory. At introduction to vaskulyarizirovanny 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 of a hydrochloride 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.

In usage time of lidocaine ECG control is obligatory. In case of disturbance of activity of a sinus node, continuation of an interval of P-Q, the QRS expansion or at development of new arrhythmia it is necessary to reduce a dose or to cancel drug.

With care and in smaller doses apply at patients with heart failure, arterial hypertension, an incomplete atrioventricular block, disturbance of intra ventricular conductivity, abnormal liver functions and kidneys, epilepsy, after heart operations, at genetic tendency to a hyperthermia, the weakened patients. To apply with care to patients of old age, and also persons with arrhythmia in the anamnesis.

When carrying out planned subarachnoidal anesthesia it is necessary to cancel MAO inhibitors not less than in 10 days prior to carrying out anesthesia.

 

Ability to influence speed of response at control of motor transport or work with other mechanisms.

After use of Lidocaine of a hydrochloride it is not recommended to be engaged in activity which demands the speed of psychomotor reactions.

Side effects:

From central and a peripheral nervous sistemy:golovokruzhenia, a headache, weakness, motive concern, euphoria, a nystagmus, a loss of consciousness, drowsiness, sleep disorders, visual (a diplopia, a photophobia) and acoustical disturbances, a tremor, a lockjaw, spasms (the risk of their development increases at a hypercapnia and acidosis), paresthesias, paralysis of respiratory muscles, the motor block, sensitivity disturbance, respiratory paralysis (develops at subarachnoidal anesthesia), numbness of language and lips more often (when using in stomatology).

From cardiovascular system: when using in high doses – a lowering of arterial pressure, bradycardia, at introduction with a vasoconstrictor – tachycardia, delay of conductivity of heart, a cross heart block, a collapse, arterial hypertension, a peripheral vazodilatation, thorax pain, arrhythmias, a heart block, a stop of cordial activity.

From bodies breath dykhaniya:ugneteniye, apnoea, asthma.

From a gastrointestinal trakta:toshnot, vomiting.

Allergic reactions: skin rashes, urticaria, a skin itch, a Quincke's disease, generalized exfoliative dermatitis, anaphylactoid reactions, konyyuktivit, rhinitis.

Local reactions: feeling of easy burning which disappears with development of the anesthetizing effect.

Others: hypothermia, feeling of heat, cold or numbness of extremities. At use in high doses – a sonitus, a condition of excitement.

Interaction with other medicines:

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 impact of lidocaine on breath function.

At simultaneous use with β-blockers reduction of a dose of lidocaine is required. 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 at the same time the risk of development of arterial hypotension increases. At simultaneous use with procaineamide hallucinations are possible. Lidocaine can strengthen effect of drugs which cause 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 together with:

– β-adrenoblockers - - - - - - - - - – slow down metabolism of lidocaine in a liver, effects of lidocaine amplify (including toxic) and the risk of development of bradycardia and arterial hypotension increases;

– kurarepodobny drugs – muscle relaxation deepening (is possible up 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;

– anticonvulsants, barbiturates (т.ч. phenobarbital) – acceleration of metabolism of lidocaine in a liver, decrease in concentration in blood is possible;

– antiarrhytmic means (Amiodaronum, verapamil, quinidine, Ajmalinum, Disopyramidum, propafenony), anticonvulsant drugs (hydantoin derivatives) – kardiodepresivny action amplifies; 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 – the analgeziruyushchy effect of morphine amplifies;

– Prenylaminum – the risk of development of ventricular arrhythmia like "pirouette" increases;

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

– Phenytoinum – strengthens kardiodepresivny effect of lidocaine.

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

Contraindications:

Individual hypersensitivity to drug 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 ІІ and ІІІ degrees, a sick sinus syndrome, a WPW-syndrome, Adams-Stokes's syndrome, severe forms of heart failure (ІІ-ІІІ degrees), the expressed arterial hypotension, bradycardia, cardiogenic shock; full cross heart block; myasthenia; hypovolemia; porphyria; heavy renal and/or liver failure; retrobulbar introduction by the patient with glaucoma; pregnancy, feeding period breast; children's age up to 12 years.

Use during pregnancy or feeding by a breast.

Use of drug during pregnancy is contraindicated. In need of drug use feeding by a breast needs to be stopped.

Children. Do not use to children aged up to 12 years.

Overdose:

The main symptoms are connected with oppression of TsNS and cardiovascular system: general weakness, dizziness, disorientation, toniko-clonic spasms, coma, tremor, vision disorders, atrioventricular block, asphyxia, nausea, vomiting, euphoria, psychomotor excitement, adynamy, apnoea, bradycardia, decrease in the ABP, 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.

Lecheniye:prekrashcheny administrations of drug, oxygenotherapy, vasoconstrictors (noradrenaline, phenylephine hydrochloride), anticonvulsant drugs, cholinolytics. The patient has to 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 TsNS are adjusted by use of benzodiazepines or barbiturates of short-term action. If the overdose arises in the course of anesthesia, it is necessary to use a muscle relaxant of short action. For correction of bradycardia and disturbance of conductivity use atropine (0,5-1,0 mg intramusculary), at arterial hypotension – sympathomimetics in a combination with agonists of β-adrenoceptors.......... At a cardiac standstill urgent 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. The specific antidote is absent.

Storage conditions:

Period of storage 3 years. To store in the place protected from light at a temperature not above 25 °C. In the place unavailable to children.

Issue conditions:

According to the recipe

Packaging:

10 ampoules on 2 ml in a box.

10 ampoules in the planimetric cell-like packaging enclosed in a pack.