Insidious Lidocaine: friend or foe? When will lidocaine help: instructions for use

The drug "Lidocaine" is widely used in medicine in various forms. In the form of sprays and aerosols, it is used in the treatment and correction of teeth, minor operations in the oral cavity, the treatment of ENT organs, as well as putting on dentures. How is the drug used? The gel is applied in a thin layer to the diseased, inflamed area of ​​the mucous membrane several times a day. After application, the affected area should be gently massaged. When using dentures, irritated mucosa or bedsores, the gel is thinly applied to the skin, gums and prosthesis.

What is the medicine "Lidocaine" in ampoules? It is having a wide range of uses. Being a strong local anesthetic, the drug is used for all types of local anesthesia - conduction, terminal, infiltration. It stabilizes cell membranes, so it is sometimes used as a remedy for arrhythmias.

With sprains, bruises and other injuries, the drug "Lidocaine" (injections) brings quick relief, because this is the fastest way to influence the nerve endings. The drug is even used to alleviate labor pains. The drug "Lidocaine" for injection is used for various blockades in the treatment, and in other medical cases.

How does the drug "Lidocaine" in ampoules work? Getting into the blood and tissues, it makes the nerve endings insensitive, thereby eliminating pain. In contrast, it does not cause adverse reactions in the tissues. Sometimes allergic reactions are observed on the components of the drug.

The presence of dizziness, excessive sweating, headache, ringing in the ears or drowsiness indicates an overdose of the drug. With such symptoms, it is necessary to stop using the drug.

Who is contraindicated in the drug "Lidocaine" in ampoules? Pregnant and lactating women, children under ten years of age, debilitated patients and people who are hypersensitive to the components of the drug - this is a list of people who should not be given such injections.

How and in what doses is the drug "Lidocaine" used? It can be administered in different ways - intravenously or intramuscularly. As a local anesthetic, different percentage solutions are used, depending on the situation. Usually, no more than 50 ml of a 0.5-1 or 2% solution of the drug is used. For the treatment of the mucous membrane, a 1-2% solution is suitable, very rarely 5%, in a volume of not more than 20 ml. As a medicine, "Lidocaine" is administered intravenously in a stream in the first four minutes at a dosage of 50 to 100 ml, and then - by drip at 2 mg per minute. No more than 1200 mg of the solution can be administered per day.

The drug "Lidocaine" in ampoules in medical practice is used very often. And in most household cases, the use of an aerosol or gel is sufficient. For example, there is another interesting way to use this tool - anesthesia of the epilation process. Yes, yes, smart women realized this a long time ago and began to use gels and creams based on lidocaine during such a far from pleasant procedure. Creams are applied to the body an hour before epilation and wrapped so that it penetrates deeper and acts on the nerve endings. Sprays act much more slowly, and if you use them, then you need to spray the product on the body three to four hours before the scheduled epilation.

But it must be remembered that with arrhythmias and liver diseases, such drugs cannot be used. In general, "Lidocaine" is a rather strong remedy, and therefore it is still not worth using it without consulting a doctor, especially if you are already taking other medications. But when taking vitamin complexes and nutritional supplements of plant origin, it does not pose a danger.

In this medical article, you can get acquainted with the drug Lidocaine. The instructions for use will explain in which cases you can take injections, ointment or aerosol, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the form of release of the drug and its composition.

In the article, doctors and consumers can only leave real reviews about Lidocaine, from which you can find out if the drug helped in the treatment of arrhythmias and anesthesia (pain relief) in adults and children, for which it is also prescribed. The instructions list analogues of Lidocaine, drug prices in pharmacies, as well as its use during pregnancy.

The local anesthetic for superficial anesthesia is Lidocaine. Instructions for use informs that injections in ampoules for injection and dilution in solution, spray, gel or ointment 5% provide terminal, infiltration, conduction anesthesia.

Release form and composition

Lidocaine is produced in the following dosage forms:

1. The solution intended for injection is odorless and colorless, it is poured into ampoules of 2 ml, in blister packs - 5 such ampoules. A solution of 10%, 2%, 1% is produced.
2. The solution, which is administered intravenously, is colorless and odorless. The solution is poured into ampoules of 2 ml, 5 pcs. in cell contour packaging. Two such packages are put into a pack of cardboard.
3. Eye drops 2% are colorless and odorless, but sometimes they can be slightly colored. It is contained in 5 ml polyethylene bottles.
4. A gel is also available.
5. Lidocaine 10% Spray is a colorless alcohol solution that has a menthol flavor. Contained in vials (650 doses), it is equipped with a special pump and nozzle for spraying. The bottle is enclosed in a cardboard box.

Compound

• The active ingredient included in the solution for injection is also lidocaine hydrochloride (monohydrate form), additional components are sodium chloride, water.
• The composition of the solution for intravenous administration includes the active component of lidocaine hydrochloride (monohydrate form). An additional component is water for injection.
• Spray 10% for topical application contains lidocaine, as well as additional components: propylene glycol, peppermint oil, 96% ethanol.
• The composition of the gel for external use also contains a similar active substance.
• Eye drops contain lidocaine hydrochloride, as well as benzethonium chloride, sodium chloride, water.

pharmachologic effect

Lidocaine is used for conduction, infiltration, terminal anesthesia. The drug has a local anesthetic, antiarrhythmic effect. As an anesthetic, the drug acts by inhibiting nerve conduction by blocking sodium channels in nerve fibers and endings.

Lidocaine is significantly superior to procaine, its action is faster and longer - up to 75 minutes (in combination with epinephrine - more than two hours). Lidocaine, when applied topically, dilates blood vessels, does not have a local irritating effect.

The antiarrhythmic effect of the drug is due to the ability to increase the permeability of membranes for potassium, block sodium channels, and stabilize cell membranes. The drug does not have a significant effect on contractility, myocardial conduction (affects only in large doses).

The level of absorption when applied topically depends on the dosage of the agent and the place of treatment (for example, it is absorbed better on mucous membranes than on the skin). After intramuscular injections, Lidocaine reaches its maximum concentration 5-15 minutes after injection.

Indications for use

What helps Lidocaine? Injections have the following indications for use intravenously and intramuscularly:

• with ventricular arrhythmias associated with glycoside intoxication.
• for the relief and prevention of the development of recurrent ventricular fibrillation in patients with acute coronary syndrome, as well as recurrent paroxysms of ventricular tachycardia.
• for infiltration, spinal, epidural, conduction anesthesia.
• for terminal anesthesia (also used in ophthalmology).

Application in ophthalmology:

• in preparation for ophthalmic surgery.
• for pain relief during short-term interventions on the conjunctiva and cornea.
• for anesthesia, if necessary, apply contact research methods.

In dentistry, Lidocaine in ampoules is used for local anesthesia, during surgical interventions in the oral cavity:

• when opening superficial abscesses.
• for anesthesia of the gums in order to fix the prosthesis or crown.
• in order to suppress or lower the enhanced pharyngeal reflex during preparation for an x-ray examination.
• when removing bone fragments and suturing wounds.
• for opening cysts of the salivary glands and frenuloectomy in children.
• before removal or excision of the enlarged papilla of the tongue.
• during the extraction of milk teeth.
• before excision of benign superficial mucosal tumors.

Application in obstetrics and gynecology:

• for anesthesia when suturing in case of abscesses.
• for pain relief during excision and treatment of rupture of the hymen.
• for anesthesia of the operating field during a number of surgical interventions.
• for the purpose of anesthetizing the perineum to perform an episiotomy or treatment.

Application in ENT practice:

• for anesthesia before washing the sinuses.
• for additional pain relief before opening a paratonsillar abscess.
• as an additional anesthesia before the puncture of the maxillary sinus.
• before a tonsillectomy to relieve pain and reduce the pharyngeal reflex (not applicable for adenectomy and tonsillectomy in children under eight years of age).
• before septectomy, electrocoagulation, resection of nasal polyps.

Use for examinations and endoscopy:

• for anesthesia before performing rectoscopy and, if necessary, replacing catheters.
• for anesthesia, if necessary, insert a probe through the mouth or nose.

Application in dermatology: for anesthesia of mucous membranes before minor surgical operations.

Instructions for use

Lidocaine solution

• For blockade of peripheral nerves and nerve plexuses: perineurally, 10-20 ml of a 10 mg / ml solution or 5-10 ml of a 20 mg / ml solution (no more than 400 mg).
• For conduction anesthesia: perineurally apply solutions of 10 mg / ml and 20 mg / ml (no more than 400 mg).
• For infiltration anesthesia: intradermally, subcutaneously, intramuscularly. Apply a solution of lidocaine 5 mg / ml (max daily dose 400 mg).
• For spinal anesthesia: subarachnoid, 3-4 ml of a 20 mg/ml solution (60-80 mg). In ophthalmology: a solution of 20 mg / ml is instilled into the conjunctival sac, 2 drops 2-3 times with an interval of 30-60 seconds immediately before surgery or examination.
• For epidural anesthesia: epidural, solutions of 10 mg / ml or 20 mg / ml (no more than 300 mg).

To prolong the action of lidocaine, it is possible to add an extempore 0.1% solution of adrenaline (1 drop per 5-10 ml of lidocaine solution, but not more than 5 drops for the entire volume of the solution). It is recommended to reduce the dose of lidocaine in elderly patients and patients with liver diseases (cirrhosis, hepatitis) or with reduced hepatic blood flow (chronic heart failure) by 40-50%.

As an antiarrhythmic agent: intravenously. Lidocaine solution for intravenous administration 100 mg/ml can only be used after dilution. 25 ml of a 100 mg/ml solution should be diluted with 100 ml of physiological saline to a concentration of lidocaine of 20 mg/ml. This diluted solution is used to administer the loading dose.

The introduction begins with a loading dose of 1 mg / kg (for 2-4 minutes at a rate of 25-50 mg / min) with an immediate connection to a constant infusion at a rate of 1-4 mg / min. Due to the rapid distribution (T1 / 2 approximately 8 minutes), 10-20 minutes after the first dose, the concentration of the drug in the blood plasma decreases, which may require repeated bolus administration (against the background of constant infusion) at a dose equal to 1 / 2-1 / 3 loading doses, with an interval of 8-10 minutes. The maximum dose in 1 hour is 300 mg, per day - 2000 mg.

The IV infusion is usually given for 12-24 hours with continuous ECG monitoring, after which the infusion is stopped to evaluate the need to change the patient's antiarrhythmic therapy. The rate of excretion of the drug is reduced in heart failure and impaired liver function (cirrhosis, hepatitis) and in elderly patients, which requires a reduction in the dose and rate of drug administration by 25-50%. In chronic renal failure dose adjustment is not required.

Eye drops

Locally, by installation in the conjunctival sac immediately before the study or surgery, 1-2 drops. 2-3 times with an interval of 30-60 seconds.

Spray

The dose may vary depending on the indication and the size of the area to be anesthetized. One dose of spray, released by pressing the dosing valve, contains 3.8 mg of lidocaine. In order to avoid reaching high plasma concentrations of the drug, the lowest doses at which a satisfactory effect is observed should be used.

Usually 1-2 valve strokes are sufficient, but in obstetric practice, 15-20 or more doses are applied (maximum 40 doses per 70 kg of body weight).

Contraindications

Lidocaine is contraindicated for use in:

• heart block.
• with a history of epileptiform seizures as a reaction to lidocaine.
• Adams-Stokes syndrome.
• violations of intraventricular conduction.
• myasthenia.
• severe liver disease.
• cardiogenic shock.
• WPW syndrome.
• heavy bleeding.
• hypersensitivity to the active substance.
• weakness of the sinus node.

With caution, injections of Lidocaine and other dosage forms of the drug are used in conditions accompanied by a decrease in hepatic blood flow, such as chronic heart failure and liver disease, progression of cardiovascular insufficiency, severe weakening of the body, in old age, with violations of the integrity of the skin in the area of ​​application (when using plates).

The restriction to the use of this drug is pregnancy and lactation, use is possible only if the expected effect of therapy outweighs the potential risk to the fetus and child. Lidocaine is also used with caution in children under 18 years of age. Slow metabolism can lead to accumulation of the drug.

Side effects

• general weakness;
• angioedema;
• decrease in blood pressure;
• convulsions;
• disorientation;
• dizziness;
• feeling hot or cold;
• anxiety;
• skin rash;
• nausea, vomiting;
• neurotic reactions;
• erectile dysfunction;
• confusion or loss of consciousness;
• anaphylactic shock;
• drowsiness;
• noise in ears;
• euphoria;
• hives;
• headache;
• persistent anesthesia;
• bradycardia (up to cardiac arrest);
• paresthesia;
• chest pain.

Children, during pregnancy and lactation

Carefully prescribe the drug to children under 18 years of age, because due to too slow metabolism, the active substance may accumulate. For children under 2 years of age, it is recommended to apply the product with a cotton swab, and not by spraying.

Lidocaine during pregnancy and lactation

This drug is contraindicated for use during pregnancy, as well as for women who are breastfeeding. It is possible to use lidocaine in an aerosol during pregnancy, but this should be done only under medical supervision and with a clear benefit-risk ratio.

It should be borne in mind when using Lidocaine Bufus that this remedy during pregnancy is used only for health reasons.

special instructions

When using Lidocaine Spray, it is important to avoid contact with the eyes and respiratory tract. Special care is required when applying the drug to the back wall of the pharynx.

When using Lidocaine in ampoules for injection into tissues with abundant vascularization, for example, in the neck, special care should be taken and a lower dose should be used.

drug interaction

When used with other drugs, a number of interaction reactions may develop:

• With the simultaneous use of mecamylamine, guanethidine, trimetafan and guanadrel, the risk of a marked decrease in blood pressure and bradycardia increases.
• When using phenytoin and lidocaine together, a decrease in the resorptive effect of lidocaine is likely, and an undesirable cardiodepressive effect may also develop.
• If the sites where the injection of lidocaine was injected were treated with disinfection solutions that contain heavy metals, the likelihood of local reactions increases.
• The effectiveness of lidocaine is reduced by inducers of microsomal liver enzymes.
• With the simultaneous administration of vasoconstrictors (methoxamine, epinephrine, phenylephrine), the local anesthetic effect of lidocaine may increase, and pressure may also increase and tachycardia may occur.
• Extends and enhances the effect of muscle relaxants.
• With simultaneous use with procainamide, the manifestation of CNS excitation, hallucinations is possible.
• If intravenous lidocaine is administered to people who take cimetidine, a number of negative effects may occur - drowsiness, stupor, paresthesia, bradycardia. If there is a need to combine these agents, it is necessary to reduce the dose of lidocaine.
• If polymyxin B and lidocaine are given concomitantly, it is important to monitor the patient's respiratory function.
• When taking MAO inhibitors at the same time, the local anesthetic effect of lidocaine may increase, and there is also a decrease in blood pressure. Do not prescribe parenteral lidocaine to patients who are taking MAO inhibitors.
• With simultaneous use, the cardiotonic effect of digitoxin decreases.
• The inhibitory effect on respiration and the central nervous system may be enhanced if lidocaine is taken in conjunction with sedative and hypnotic drugs, as well as with hexenal, sodium thiopental, and opioid analgesics.
• The negative inotropic effect is enhanced by the simultaneous administration of Verapamil, Aymalin, quinidine and amiodarone.
• Enhances muscle relaxation of curare-like drugs.
• Lidocaine reduces the effect of antimyasthenic drugs.
• When taking Cimetidine and beta-blockers, the risk of toxic effects increases.

Analogues of the drug Lidocaine

According to the structure, analogues are determined:

1. Dineksan.
2. Lidocaine hydrochloride.
3. Luan.
4. Helikain.
5. Lidocaine-Vial.
6. Lidocaine Hydrochloride Brown.
7. Lidocaine Bufus.
8. Xylocaine.
9. Versatis.

Which is better: Lidocaine or Ultracaine?

Ultracaine is a less toxic drug. It provides longer anesthesia, but also has a number of contraindications for use.

Lidocaine or Novocaine - which is better?

Novocaine is a drug that demonstrates moderate analgesic activity, while Lidocaine is an effective anesthetic. However, Novocain is a less toxic drug.

Holiday conditions and price

The average cost of Lidocaine (injections in ampoules of 2 ml No. 10) in Moscow is 27 rubles. The price of eye drops is 30 rubles per pack of 5 tubes - bottles. Released by prescription.

Keep out of the reach of children at a temperature of 15 - 25 C. Shelf life - 5 years.

Formula: C14H22N2O, chemical name: (2-Diethylamino)-N-(2,6-dimethylphenyl)acetamide (and as hydrochloride).
Pharmacological group: organotropic/cardiovascular/class 1B antiarrhythmics;
Neurotropic drugs / local anesthetics / acetanilide derivative.
Pharmachologic effect: antiarrhythmic, local anesthetic.

Pharmacological properties

The antiarrhythmic properties of lidocaine are due to the inhibition of diastolic depolarization in the Purkinje fibers, the suppression of ectopic foci of excitation, and a decrease in automatism. Lidocaine does not affect the rate of rapid depolarization or slightly lowers it. Lidocaine increases the permeability of the cell membrane for potassium ions, makes the process of repolarization faster and the action potential shorter. Lidocaine does not change the excitability of the sinoatrial node, slightly affects the contractility and conduction of the myocardium. When administered intravenously, it acts briefly and quickly (10–20 minutes). The mechanism of the local anesthetic properties of lidocaine is to stabilize the membranes of neurons, reducing their permeability to sodium ions, which prevents the occurrence of an action potential and the conduction of impulses. In a slightly alkaline environment of tissues, lidocaine is rapidly hydrolyzed and, after a short latent period, has an effect within 1–1.5 hours. With inflammation, the anesthetic activity of lidocaine is reduced due to the acidic environment at the site of inflammation.
With all types of local anesthesia, lidocaine is effective. Lidocaine does not have an irritating effect on tissues, dilates blood vessels; possible antagonism with calcium ions. When administered intravenously, the maximum concentration is created after 45 - 90 seconds, when administered intramuscularly - after 5 - 15 minutes. Quite quickly, lidocaine is absorbed from the mucous membrane of the oral cavity or upper respiratory tract (the maximum concentration is reached after 10-20 minutes). When taking lidocaine orally, bioavailability is only 15-35% (due to the effects of "first pass" through the liver). It binds to plasma proteins by 50-80%. In the blood, a stable concentration is reached after 3-4 hours with continuous intravenous administration (in patients with acute myocardial infarction - after 8-10 hours). The therapeutic effect develops at a concentration of 1.5–5 µg/ml. Lidocaine easily crosses various barriers, including the blood-brain, placental barriers, enters breast milk. First, lidocaine enters well-perfused tissues (lungs, heart, brain, spleen, liver), then into muscle and adipose tissue.
The half-life with intravenous bolus administration is 1.5–2 hours (3 hours in newborns), with prolonged intravenous infusions - up to 3 hours and even more. In case of violation of the liver, the half-life of lidocaine can increase by more than 2 times. Lidocaine is almost completely and rapidly metabolized in the liver (less than 10% is excreted unchanged in the urine) during oxidative N-dealkylation, in this process active metabolites (glycinexylidine and monoethylglycinexylidine) are formed, which have a half-life of 10 hours and 2 hours, respectively. In patients with chronic renal failure, lidocaine metabolites may accumulate in the body. The duration of action of intravenous lidocaine is 10–20 minutes for intramuscular administration and 60–90 minutes. When used topically in the form of plates on intact skin, a therapeutic effect sufficient to relieve pain occurs, while systemic effects do not develop.

Indications

ventricular fibrillation; ventricular tachyarrhythmias and extrasystoles, including in the postoperative period, and in acute myocardial infarction; all types of local anesthesia, including superficial, infiltration, conduction, epidural, spinal, intraligamentary during painful manipulations, surgical interventions, instrumental and endoscopic studies; in the form of plates - myositis, pain syndrome with lesions of the spine, postherpetic neuralgia.

Method of application of lidocaine and dose

The dosage regimen is set individually, depending on the clinical situation, indications and dosage form used. With arrhythmias: intravenously (within 3-4 minutes) bolus 50-100 mg at a rate of 25-50 mg / min, then at a rate of 1-4 mg / min drip; intramuscularly 4.3 mg / kg of body weight, it is possible to re-introduce after 1 - 1.5 hours; for intravenous and intramuscular administration, the maximum dose for adults is up to 300–400 mg over 1 hour; the maximum daily dose is 2000 mg. Children are injected with a stream of 1 mg/kg at a rate of 25–50 mg / min, after 5 minutes it is possible to repeat the administration (the total dose should not be more than 3 mg / kg), then it is administered at a rate of 30 μg / kg / min; the maximum daily dose is 4 mg/kg. Surface anesthesia - 2-10% solution (no more than 200 mg - 2 ml). Infiltration anesthesia for adults is used 0.5% solution, conductor anesthesia - 1-2% solution. The maximum total dose is 300–400 mg. In ophthalmology, 1-2 drops are administered 2-3 times with an interval of 30-60 seconds. Topically (aerosol, gel, spray, plates). For children under 2 years old, for surface anesthesia, 1–2 aerosol doses (4.8–9.6 mg) are prescribed, having previously been applied to a cotton swab. The plates are glued to the skin, covering the painful surface. After applying the plate, wash your hands immediately. Within 12 hours, the plate can be on the skin. Then they take it off and take a break at 12 hours. A maximum of 3 plates can be used at the same time.
To prolong the action of lidocaine, you can add 1 drop of 0.1% adrenaline solution to 5-10 ml of lidocaine. Care must be taken when taking lidocaine in patients with kidney disease, liver disease, severe heart failure with impaired contractility, hypovolemia, and a genetic predisposition to malignant hyperthermia. Children, debilitated patients, elderly patients need dose adjustment in accordance with the physical status and age. With the introduction of lidocaine into vascularized tissues, it is necessary to conduct an aspiration test. Use of lidocaine topically in the area of ​​infection or injury must be done with caution. If during the use of the plate there is reddening of the skin or a burning sensation, then the plate must be removed and not used until the redness or burning has passed. Immediately after use, the plates must be destroyed so that they cannot be reached by children or pets.

Contraindications for use

Hypersensitivity, heart block (intraventricular, AV, sinoatrial), sinus node weakness, cardiogenic shock, WPW syndrome, myasthenia gravis, severe liver disease, a history of epileptiform seizures when using lidocaine.

Application restrictions

Breastfeeding, pregnancy, age over 65 years, progression of cardiovascular insufficiency, debilitated patients, conditions that are accompanied by a decrease in hepatic blood flow; violations of the integrity of the skin (at the site of use of the plates).

Use during pregnancy and lactation

You can use lidocaine during breastfeeding and during pregnancy if the expected effects of therapy for the mother outweigh the possible risk to the child or fetus.

Side effects of lidocaine

Nervous system and sense organs: excitation or depression of the central nervous system, nervousness, flashing "flies" before the eyes, euphoria, photophobia, headache, drowsiness, dizziness, diplopia, tinnitus, impaired consciousness, respiratory arrest or depression, tremor, disorientation, muscle twitching, convulsions ( the possibility of their development increases with hypercapnia and acidosis);
circulatory system: violation of the conduction of the heart, sinus bradycardia, transverse heart block, increase or decrease in blood pressure, collapse;
digestive system: nausea, vomiting;
allergic reactions: anaphylactic shock, generalized exfoliative dermatitis, contact dermatitis (skin rash, hyperemia at the site of application, itching, urticaria), angioedema, short-term burning sensation at the site of aerosol action or at the site of application of the plate;
others: sensation of cold, heat or numbness of the extremities, suppression of the immune system, malignant hyperthermia.

Interaction of lidocaine with other substances

Beta-blockers increase the possibility of hypotension and bradycardia when used together with lidocaine. Beta-blockers and norepinephrine, by reducing hepatic blood flow, reduce the clearance of lidocaine (the toxicity of lidocaine increases), glucagon, isoprenaline - increase the clearance of lidocaine. Cimetidine increases the content of lidocaine in plasma. Barbiturates, due to the induction of microsomal enzymes, activate the degradation of lidocaine and, thereby, reduce its activity. Anticonvulsants (hydantoin derivatives) accelerate the biotransformation of lidocaine in the liver. Antiarrhythmics (verapamil, aimaline, amiodarone, quinidine) potentiate cardiodepression when used in combination with lidocaine. The combined use of lidocaine and novocainamide can cause hallucinations and excitation of the central nervous system. Lidocaine enhances the inhibitory effect of hypnotics and narcotic drugs on the respiratory center, deepens myorelaxation, which is caused by curare-like drugs, and weakens the cardiotonic effect of digitoxin. MAO inhibitors prolong local anesthesia with lidocaine.

Overdose

With an overdose of lidocaine, psychomotor agitation, general weakness, dizziness, hypotension, tremor, coma, tonic-clonic convulsions, collapse, depression of the central nervous system, AV blockade, respiratory arrest occur. It is necessary: ​​discontinuation of lidocaine, oxygen therapy, pulmonary ventilation, taking anticonvulsants, vasoconstrictors (mezaton, norepinephrine), with the development of bradycardia - anticholinergics (atropine); if necessary, resuscitation, pulmonary intubation, mechanical ventilation. Dialysis is ineffective.

Trade names of drugs with the active ingredient lidocaine

N.01.B.B Amides

N.01.B.B.02 Lidocaine

C.01.B.B.01 Lidocaine

C.01.B.B Class Ib antiarrhythmic drugs

Antiarrhythmic drug. Class I B
local anesthetic. Antiarrhythmic drug. Class I B.

Active substance

Release form, composition and packaging

Injection transparent, colorless or almost colorless, odorless.

Excipients: for parenteral forms - 12 mg, water for injection - up to 2 ml.

2 ml - ampoules with a break point and a green code ring (5) - blister packs (20) - cardboard boxes.

pharmachologic effect

Lidocaine is a short-acting local anesthetic of the amide type. Its mechanism of action is based on a decrease in the permeability of the neuron membrane for sodium ions. As a result, the rate of depolarization decreases and the excitation threshold increases, leading to reversible local numbness. Lidocaine is used to achieve conduction anesthesia in various parts of the body and control arrhythmias. It has a rapid onset of action (about one minute after intravenous administration and 15 minutes after intramuscular injection), quickly spreads into surrounding tissues. The action lasts 10-20 minutes and about 60-90 minutes after i.v. and i.m. administration, respectively.

Pharmacokinetics

Suction

Lidocaine is rapidly absorbed from the gastrointestinal tract, but due to the "first pass" effect through the liver, only a small amount of it reaches the systemic circulation. Systemic absorption of lidocaine is determined by the site of administration, dose, and its pharmacological profile. C max in the blood is achieved after intercostal blockade, then (in descending order of concentration), after injection into the lumbar epidural space, brachial plexus and subcutaneous tissues. The main factor determining the rate of absorption and concentration in the blood is the total dose administered, regardless of the site of administration. There is a linear relationship between the amount of lidocaine administered and Cmax of the anesthetic in the blood.

Distribution

Lidocaine binds to proteins including α 1 -acid glycoprotein (AKG) and albumin. The degree of binding is variable, being approximately 66%. The plasma concentration of AKG in newborns is low, so they have a relatively high content of the free biologically active fraction of lidocaine.

Lidocaine crosses the BBB and the placental barrier, probably through passive diffusion.

Metabolism

Lidocaine is metabolized in the liver, about 90% of the administered dose undergoes N-dealkylation to form monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which contribute to the therapeutic and toxic effects of lidocaine. The pharmacological and toxic effects of MEGX and GX are comparable to those of lidocaine, but less pronounced. GX has a longer T 1/2 (about 10 hours) than lidocaine and can accumulate with repeated administration.

Metabolites resulting from subsequent metabolism are excreted in the urine.

breeding

Terminal T 1/2 lidocaine after intravenous bolus administration to healthy adult volunteers is 1-2 hours. Terminal T 1/2 GX is about 10 hours, MEGX - 2 hours. The content of unchanged lidocaine in the urine does not exceed 10%

Pharmacokinetics in special groups of patients

Due to its rapid metabolism, the pharmacokinetics of lidocaine may be affected by conditions that impair liver function. In patients with impaired liver function, T 1/2 of lidocaine may increase by 2 or more times.

Impaired renal function does not affect the pharmacokinetics of lidocaine, but may lead to accumulation of its metabolites.

Newborns have a low concentration of AKG, so plasma protein binding may decrease. Due to the potentially high concentration of the free fraction, the use of lidocaine in neonates is not recommended.

Indications

- local and regional anesthesia, conduction anesthesia for large and small interventions.

Contraindications

- AV blockade of the III degree;

- hypovolemia;

- hypersensitivity to any of the components of the drug and to amide-type anesthetics.

Dosage

The dosage regimen should be selected depending on the response of the patient and the site of administration. The drug should be administered at the lowest concentration and lowest dose that gives the desired effect. The maximum dose for adults should not exceed 300 mg.

The volume of solution to be administered depends on the size of the anesthetized area. If there is a need to administer a larger volume with a low concentration, then the standard solution is diluted with physiological saline (0.9% sodium chloride solution). Breeding is carried out immediately before the introduction.

Children, elderly and debilitated patients the drug is administered in smaller doses appropriate to their age and physical condition.

At adults and adolescents aged 12-18 years a single dose of lidocaine should not exceed 5 mg/kg with a maximum dose of 300 mg.

Experience with children under 1 year old limited. The maximum dose for children aged 1-12 years- no more than 5 mg/kg of body weight of 1% solution.

Side effects

Adverse reactions are described according to the MedDRA System Organ Classes. Like other local anesthetics, adverse reactions to lidocaine are rare and are usually due to elevated plasma concentrations due to accidental intravascular administration, overdose, or rapid absorption from areas with abundant blood supply, or due to hypersensitivity, idiosyncrasy, or reduced patient tolerance to the drug. Systemic toxicity reactions are mainly manifested by the central nervous system and / or the cardiovascular system.

From the side of the immune system

Hypersensitivity reactions (allergic or anaphylactoid reactions, anaphylactic shock) - see also skin and subcutaneous tissue disorders. A skin allergy test for lidocaine is considered unreliable.

From the nervous system and mental disorders

Neurological symptoms of systemic toxicity include dizziness, nervousness, tremor, paresthesia around the mouth, numbness of the tongue, drowsiness, convulsions, and coma.

Reactions from the nervous system can be manifested by its excitation or depression. Signs of CNS stimulation may be of short duration or not occur at all, as a result of which the first manifestations of toxicity may be confusion and drowsiness, followed by coma and respiratory failure.

Neurological complications of spinal anesthesia include transient neurological symptoms such as pain in the lower back, buttocks, and legs. These symptoms usually develop within 24 hours of anesthesia and resolve within a few days.

After spinal anesthesia with lidocaine and similar agents, isolated cases of arachnoiditis and cauda equina syndrome with persistent paresthesia, bowel and urinary tract dysfunction, or paralysis of the lower extremities have been described. Most cases are due to hyperbaric lidocaine or prolonged spinal infusion.

From the organ of vision

Signs of lidocaine toxicity may include blurred vision, diplopia, and transient amaurosis. Bilateral amaurosis can also result from accidental injection of lidocaine into the optic nerve bed during ophthalmic procedures. Ocular inflammation and diplopia have been reported following retro- or peribulbar anesthesia.

From the organ of hearing and the labyrinth: ringing in the ears, hyperacusis.

From the side of the cardiovascular system

Cardiovascular reactions are manifested by arterial hypotension, bradycardia, myocardial depression (negative inotropic effect), arrhythmias, cardiac arrest or circulatory failure are possible.

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

From the digestive system: nausea, vomiting.

From the skin and subcutaneous tissues: rash, urticaria, angioedema, swelling of the face.

Reporting adverse reactions suspected of being related to treatment

Reporting suspected treatment-related adverse reactions after drug registration is very important. These measures allow the monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals should report any suspected treatment-related adverse reactions through the pharmacovigilance system.

Overdose

Symptoms

CNS toxicity is manifested by symptoms that increase in severity. First, paresthesia around the mouth, numbness of the tongue, dizziness, hyperacusis, and tinnitus may develop. Visual impairment and muscle tremors or muscle twitches are indicative of more severe toxicity and precede generalized seizures. These signs should not be confused with neurotic behavior. Then loss of consciousness and large convulsive seizures lasting from a few seconds to several minutes may occur. Convulsions lead to a rapid increase in hypoxia and hypercapnia due to increased muscle activity and respiratory failure. In severe cases, sleep apnea may develop. Acidosis enhances the toxic effects of local anesthetics. In severe cases, there are violations of the cardiovascular system. At high systemic concentrations, arterial hypotension, bradycardia, arrhythmia and cardiac arrest can develop, which can be fatal.

Overdose resolution occurs due to redistribution of the local anesthetic from the CNS and its metabolism, it can proceed quite quickly (unless a very large dose of the drug has been administered).

Treatment

If signs of overdose occur, the administration of the anesthetic should be stopped immediately.

Seizures, CNS depression, and cardiotoxicity require medical attention. The main goals of therapy are to maintain oxygenation, stop seizures, maintain circulation and stop acidosis (if it develops). In appropriate cases, it is necessary to ensure the patency of the respiratory tract and prescribe oxygen, as well as establish assisted ventilation (mask or using an Ambu bag). Maintaining blood circulation is carried out by infusion of plasma or infusion solutions. If long-term circulatory maintenance is required, vasopressors should be considered, but they increase the risk of CNS excitation. Seizure control can be achieved by intravenous administration of diazepam (0.1 mg/kg) or sodium (1-3 mg/kg), while taking into account that anticonvulsants can also depress breathing and circulation. Prolonged seizures may interfere with ventilation and oxygenation of the patient, and therefore, early endotracheal intubation should be considered. If the heart stops, start standard cardiopulmonary resuscitation. The effectiveness of dialysis in the treatment of acute lidocaine overdose is very low.

drug interaction

The toxicity of lidocaine increases with its simultaneous use with and propranolol due to an increase in the concentration of lidocaine, this requires a decrease in the dose of lidocaine. Both drugs reduce hepatic blood flow. In addition, cimetidine inhibits microsomal activity. slightly reduces the clearance of lidocaine, which leads to an increase in its concentration.

An increase in the serum concentration of lidocaine can also cause antiretroviral agents (eg, amprenavir, atazanavir, darunavir, lopinavir).

Hypokalemia caused by diuretics may reduce the effect of lidocaine when they are used simultaneously.

Lidocaine should be used with caution in patients receiving other local anesthetics or agents structurally similar to amide-type local anesthetics (eg, antiarrhythmic agents such as mexiletine, tocainide) because systemic toxic effects are additive.

Separate drug interaction studies between lidocaine and class III antiarrhythmic drugs (eg, amiodarone) have not been conducted, but caution is advised.

In patients receiving concomitant antipsychotics that prolong or may prolong the QT interval (eg, pimozide, sertindole, olanzapine, quetiapine, zotepine), prenylamine, epinephrine (if given by accident), or serotonin 5HT3 receptor antagonists (eg, tropisetron , dolasetron), may increase the risk of ventricular arrhythmias.

The simultaneous use of quinupristin / dalfopristin may increase the concentration of lidocaine and thus increase the risk of ventricular arrhythmias; simultaneous use should be avoided.

In patients receiving concomitant muscle relaxants (eg, suxamethonium), the risk of increased and prolonged neuromuscular blockade may be increased.

After the use of bupivacaine in patients treated with verapamil and timolol, the development of cardiovascular insufficiency was reported; lidocaine is similar in structure to bupivacaine.

Dopamine and 5-hydroxytryptamine lower the seizure threshold for lidocaine.

Opioids are likely to have a proconvulsant effect, as supported by evidence that lidocaine lowers the seizure threshold for fentanyl in humans.

The combination of opioids and antiemetics, sometimes used to sedate children, may lower the seizure threshold and increase the CNS depressant effect of lidocaine.

The use of epinephrine together with lidocaine can reduce systemic absorption, but with accidental IV administration, the risk of ventricular tachycardia and ventricular fibrillation increases dramatically.

The simultaneous use of other antiarrhythmic drugs, beta-blockers and slow calcium channel blockers can further reduce AV conduction, intraventricular conduction and contractility.

The simultaneous use of vasoconstrictors increases the duration of action of lidocaine.

The simultaneous use of lidocaine and ergot alkaloids (eg, ergotamine) can cause severe arterial hypotension.

Care must be taken when using sedatives, as they may interfere with the action of local anesthetics on the CNS.

Caution should be exercised with long-term use of antiepileptic drugs (phenytoin), barbiturates and other inhibitors of microsomal liver enzymes, as this may lead to a decrease in effectiveness and, as a result, an increased need for lidocaine. On the other hand, intravenous administration of phenytoin may increase the inhibitory effect of lidocaine on the heart.

The analgesic effect of local anesthetics may be enhanced by opioids and clonidine.

Ethanol, especially with prolonged abuse, can reduce the effect of local anesthetics.

Lidocaine is not compatible with amphotericin B, methohexitone and nitroglycerin.

Mixing lidocaine with other drugs is not recommended.

special instructions

The introduction of lidocaine should be carried out by specialists with experience and equipment for resuscitation. With the introduction of local anesthetics, it is necessary to have equipment for resuscitation.

Lidocaine should be used with caution in patients with myasthenia gravis, epilepsy, congestive heart failure, bradycardia, and respiratory depression, and in combination with drugs that interact with lidocaine and lead to increased bioavailability, potentiation of effects (eg, phenytoin), or prolongation of excretion ( for example, in hepatic or end-stage renal failure, in which lidocaine metabolites can accumulate).

Patients receiving class III antiarrhythmic drugs (eg, amiodarone) should be carefully observed and monitored by ECG, as the effect on the heart may be potentiated.

In the post-registration period, there have been reports of chondrolysis in patients who underwent prolonged intra-articular infusion of local anesthetics after surgery. In most cases, chondrolysis was observed in the shoulder joint. Due to the many contributing factors and the inconsistency of the scientific literature regarding the mechanism of the effect, a causal relationship has not been identified. Long-term intra-articular infusion is not a valid indication for the use of lidocaine.

IM administration of lidocaine may increase the activity of creatine phosphokinase, which may complicate the diagnosis of acute myocardial infarction.

Lidocaine has been shown to cause porphyria in animals; the use of the drug in patients with porphyria should be avoided.

When injected into inflamed or infected tissues, the effect of lidocaine may be reduced. Before starting intravenous administration of lidocaine, it is necessary to eliminate hypokalemia, hypoxia and a violation of the acid-base state.

Some local anesthesia procedures can lead to serious adverse reactions, regardless of the local anesthetic used.

Conduction anesthesia of the spinal nerves can lead to depression of the cardiovascular system, especially against the background of hypovolemia, therefore, when performing epidural anesthesia in patients with cardiovascular disorders, care should be taken.

Epidural anesthesia can lead to arterial hypotension and bradycardia. The risk can be reduced by prior administration of crystalloid or colloid solutions. It is necessary to stop arterial hypotension immediately.

In some cases, paracervical blockade during pregnancy can lead to bradycardia or tachycardia in the fetus, and therefore, careful monitoring of fetal heart rate is required.

Introduction to the head and neck area can lead to inadvertent entry into the artery with the development of cerebral symptoms (even at low doses).

Retrobulbar injection can rarely enter the subarachnoid space of the skull, resulting in serious/severe reactions including cardiovascular failure, apnea, seizures, and temporary blindness.

Retro- and peribulbar administration of local anesthetics carries a low risk of persistent oculomotor dysfunction. The main causes include trauma and/or local toxic effects on muscles and/or nerves.

The severity of such reactions depends on the degree of injury, the concentration of the local anesthetic and the duration of its exposure in the tissues. In this regard, any local anesthetic must be used at the lowest effective concentration and dose.

Intravascular administration should be avoided unless directly indicated.

The drug should be used with caution:

In patients with coagulopathy. Therapy with anticoagulants (eg, heparin), NSAIDs, or plasma expanders increases the tendency to bleed. Accidental damage to blood vessels can lead to severe bleeding. If necessary, check bleeding time, activated partial thromboplastin time (APTT) and platelet count;

In patients with complete and incomplete blockade of intracardiac conduction, since local anesthetics can inhibit AV conduction;

Patients with seizure disorders should be closely monitored for CNS symptoms. Low doses of lidocaine may also increase seizures. In patients with Melkersson-Rosenthal syndrome, allergic and toxic reactions from the nervous system in response to the administration of local anesthetics may develop more often;

In the III trimester of pregnancy.

Lidocaine injection 10 mg/ml and 20 mg/ml is not approved for intrathecal administration (subarachnoid anesthesia).

Influence on the ability to drive vehicles and control mechanisms

After the introduction of local anesthetics, a temporary sensory and / or motor blockade may develop. Until the disappearance of these effects, patients should not drive vehicles and work with mechanisms.

Pregnancy and lactation

Lidocaine is allowed to be used during pregnancy and during breastfeeding. It is necessary to strictly adhere to the prescribed dosing regimen. In case of complications or a history of bleeding, epidural anesthesia with lidocaine in obstetrics is contraindicated.

Lidocaine has been used in a large number of pregnant women and women of childbearing age. No reproductive disorders have been registered, ie. there was no increase in the incidence of malformations.

Due to the potential for reaching high concentrations of local anesthetics in the fetus after paracervical blockade, adverse reactions such as fetal bradycardia may develop in the fetus. In this regard, lidocaine in concentrations exceeding 1% is not used in obstetrics.

No adverse effects on the fetus have been found in animal studies.

Lidocaine passes into breast milk in a small amount, the bioavailability is very low, so the amount expected in breast milk is very small, therefore, the potential harm to the baby is very low. The decision on the possibility of using lidocaine during breastfeeding is made by the doctor.

Data on the effect of lidocaine on fertility in humans are not available.

Application in childhood

Experience with children under 1 year old limited.

For impaired renal function

Lidocaine should be used with caution in end-stage renal disease, because may accumulate metabolites of lidocaine.