Lidocaine

General characteristics. Structure:

Active ingredient: 20 mg or 100 mg of lidocaine of a hydrochloride.

Excipients: sodium chloride (for parenteral dosage forms), water for injections.

The Mestnoanesteziruyushchy medicine intended for carrying out terminal, infiltration and conduction anesthesia and also possesses antiarrhytmic action.

Pharmacological properties:

Pharmacodynamics. Antiarrhytmic means of the class IB, local anesthetic derivative of acetanilide. Has membrane stabilizing activity. Causes blockade of natrium channels of excitable membranes of neurons and membranes of cardiomyocytes.

Reduces duration of action potential and the effective refractory period in Purkinye's fibers, suppresses their automatism. At the same time lidocaine suppresses electric activity of the depolarized, aritmogenny sites, but minimum influences electric activity of normal fabrics. At use in average therapeutic doses practically does not change contractility of a myocardium and does not slow down AV conductivity. At use as antiarrhytmic means at in introduction the beginning of action in 45-90 sec., duration - 10-20 min.; at introduction in oil the beginning of action in 5-15 min., duration - 60-90 min.

Causes all types of local anesthesia: terminal, infiltration, conduction.

Pharmacokinetics. After introduction in oil absorption almost full. Distribution is bystry, Vd makes about 1 l/kg (at patients with heart failure lower). Linkng with proteins depends on concentration of active agent in plasma and makes 60-80%. It is metabolized mainly in a liver with formation of active metabolites which can promote manifestation of therapeutic and toxic action, especially after infusion during 24 h and more.

T1/2 tends to two-staging with a phase of distribution of 7-9 min. In the whole T1/2 depends on a dose, makes 1-2 h and can increase to 3 h and more during long in/in infusions (more than 24 h). 10% in not changed look are removed by kidneys in the form of metabolites.

Indications to use:

In cardiological practice: treatment and prevention of ventricular arrhythmias (premature ventricular contraction, tachycardia, trembling, fibrillation), including in the acute period of a myocardial infarction, at implantation of an artificial pacemaker, at glikozidny intoxication, an anesthesia.

For anesthesia: terminal, infiltration, conduction, spinal (epidural) anesthesia in surgery, obstetrics and gynecology, urology, ophthalmology, stomatology, otorhinolaryngology; blockade of peripheral nerves and nerve knots.

Route of administration and doses:

As antiarrhytmic means the adult at introduction of a load dose in/in - 1-2 mg/kg within 3-4 min.; average single dose of 80 mg. Then at once pass to drop infusion with a speed of 20-55 mkg/kg/min. Drop infusion can be carried out during 24-36 h. If necessary against the background of drop infusion it is possible to repeat in/in jet administration of lidocaine in a dose 40 mg in 10 min. after the first load dose.

In oil enter 2-4 mg/kg, if necessary repeated introduction is possible in 60-90 min.

To children at in introduction of a load dose - 1 mg/kg, if necessary perhaps repeated introduction in 5 min. For continuous in/in infusion (usually after introduction of a load dose) - 20-30 mkg/kg/min.

For use in surgical and obstetric practice, stomatology, the LOR-expert the mode of dosing is set individually, depending on indications, a clinical situation and the used dosage form.

Maximum doses: the adult at in introduction a load dose - 100 mg, at the subsequent drop infusion - 2 mg/min.; at introduction in oil - 300 mg (about 4.5 mg/kg) during 1 h.

To children in case of repeated introduction of a load dose with an interval of 5 min. the total dose makes 3 mg/kg; at continuous in/in infusion (usually after introduction of a load dose) - 50 mkg/kg/min.

Features of use:

With care it is necessary to apply at the states which are followed by decrease in a hepatic blood-groove (including at chronic heart failure, liver diseases), the progressing cardiovascular insufficiency (usually owing to development of heart blocks and shock), at the heavy and weakened patients, at patients of advanced age (65 years are more senior); for epidural anesthesia - at neurologic diseases, a septicaemia, impossibility of carrying out a puncture because of deformation of a backbone; for subarachnoidal anesthesia - at a dorsodynia, brain infections, high-quality and malignant new growths of a brain, at coagulopathies of various genesis, migraine, subarachnoidal hemorrhage, arterial hypertension, arterial hypotension, paresthesia, psychosis, hysteria, at not contact patients, impossibility are carrying out a puncture because of deformation of a backbone.

It is necessary to enter with care lidocaine solutions into fabrics with plentiful vascularization (for example, into the area of a neck at a thyroid gland operations), in such cases lidocaine is applied in smaller doses.

At simultaneous use with beta adrenoblockers, with Cimetidinum reduction of a dose of lidocaine is required; with polymyxin B - it is necessary to control breath function.

During treatment by MAO inhibitors it is not necessary to apply lidocaine parenterally.

Solutions are not intended for injections which part Epinephrinum and Norepinephrinum are for in/in introductions.

Lidocaine cannot be added to the transfused blood.

Influence on ability to driving of motor transport and to control of mechanisms

After use of lidocaine it is not recommended to be engaged in the types of activity demanding high concentration of attention and bystry psychomotor reactions.

At pregnancy and in the period of a lactation to apply only according to vital indications. Lidocaine is emitted with breast milk.

In obstetric practice with care to apply paratservikalno at disturbances of pre-natal fetation, fetoplacental insufficiency, prematurity, postmaturity, a gestosis.

With care it is necessary to apply at the diseases of a liver which are followed by decrease in a hepatic blood-groove.

With care it is necessary to apply at patients of advanced age (65 years are more senior).

Side effects:

From TsNS and peripheral nervous system: dizziness, a headache, weakness, motive concern, a nystagmus, a loss of consciousness, drowsiness, visual and acoustical disturbances, a tremor, a lockjaw, spasms (the risk of their development increases against the background of a hypercapnia and acidosis), a syndrome of "a horse tail" (paralysis of legs, paresthesias), paralysis of respiratory muscles, an apnoea, the block motor and sensitive, respiratory paralysis (develops at subarachnoidal anesthesia), numbness of language more often (when using in stomatology).

From cardiovascular system: increase or decrease in the ABP, tachycardia - at introduction with a vasoconstrictor, a peripheral vazodilatation, a collapse, thorax pain.

From the alimentary system: nausea, vomiting, involuntary defecation.

Allergic reactions: skin rash, a small tortoiseshell (on skin and mucous membranes), a skin itch, a Quincke's disease, an acute anaphylaxis.

Local reactions: at spinal anesthesia - a dorsodynia, at epidural anesthesia - accidental hit in a subarachnoid space; at topical administration in urology - an urethritis.

Others: an involuntary urination, a methemoglobinemia, resistant anesthesia, decrease in a libido and/or a potentiality, respiratory depression, up to a stop, a hypothermia; at anesthesia in stomatology: anesthesia and paresthesias of lips and language, anesthesia lengthening.

Interaction with other medicines:

At simultaneous use with barbiturates (including with phenobarbital) increase in metabolism of lidocaine in a liver, decrease in concentration in a blood plasma and thereof, reduction of its therapeutic effectiveness is possible.

At simultaneous use with beta adrenoblockers (including with propranolol, Nadololum) strengthening of effects of lidocaine (including toxic), apparently, owing to delay of his metabolism in a liver is possible.

At simultaneous use with MAO inhibitors strengthening of mestnoanesteziruyushchy effect of lidocaine is possible.

At simultaneous use with the drugs causing neuromuscular transmission blockade (including from succinylcholine chloride) strengthening of effect of the drugs causing neuromuscular transmission blockade is possible.

At simultaneous use with hypnotic drugs and sedatives strengthening of the oppressing action on TsNS is possible; with Ajmalinum, quinidine - strengthening of cardiodepressive action is possible; with Amiodaronum - cases of development of spasms and SSSU are described.

At simultaneous use with hexenal, sodium thiopental (in/in) perhaps respiratory depression.

At simultaneous use with meksiletiny toxicity of lidocaine increases; with midazolam - moderate reduction of concentration of lidocaine in a blood plasma; with morphine - strengthening of analgeziruyushchy effect of morphine.

At simultaneous use with Prenylaminum the risk of development of ventricular arrhythmia like "pirouette" develops.

Cases of excitement, hallucinations at simultaneous use with procaineamide are described.

At simultaneous use with propafenony increase in duration and increase in severity of side effects from TsNS is possible.

Believe that under the influence of rifampicin reduction of concentration of lidocaine in a blood plasma is possible.

At simultaneous in/in infusion of lidocaine and Phenytoinum strengthening of side effects of the central genesis is possible; the case of sinuatrial blockade owing to the additive cardiodepressive effect of lidocaine and Phenytoinum is described.

At the patients receiving Phenytoinum as an anticonvulsant reduction of concentration of lidocaine in a blood plasma is possible that is caused by induction of microsomal enzymes of a liver under the influence of Phenytoinum.

At simultaneous use with Cimetidinum the clearance of lidocaine moderately decreases and its concentration in a blood plasma increases, there is a risk of strengthening of side effect of lidocaine.

Contraindications:

Heavy bleedings, shock, arterial hypotension, infection of the place of an estimated injection, the expressed bradycardia, cardiogenic shock, severe forms of chronic heart failure, SSSU at patients of advanced age, AV blockade of II and III degrees (except for cases when the probe for stimulation of ventricles is entered), heavy abnormal liver functions.

For subarachnoidal anesthesia - a total block of heart, bleeding, arterial hypotension, shock, infection of the venue of a lumbar puncture, a septicaemia.

Hypersensitivity to lidocaine and other local anesthetics of amide type.

Overdose:

Symptoms: the first signs intoxicationsof - dizziness, nausea, vomiting, euphoria, decrease in the ABP, an adynamy; then - spasms of mimic muscles with transition to toniko-clonic spasms of skeletal muscles, psychomotor excitement, bradycardia, an asystolia, a collapse; when using at childbirth at the newborn - bradycardia, oppression of a respiratory center, an apnoea.

Treatment: termination of administration of drug, inhalation by oxygen. Symptomatic therapy. At spasms in/in enter 10 mg of diazepam. At bradycardia - m-holinoblokatory (atropine), vasoconstrictors (Norepinephrinum, Phenylephrinum). The hemodialysis is inefficient.

Storage conditions:

List B. To store in the unavailable to children, protected from light place at a temperature not over 25 ºС.

Issue conditions:

According to the recipe

Packaging:

 On 5 ml - ampoules, on 10 ampoules in cardboard packs.