Lidocaine: instructions for use, analogues and prices. Medicinal reference book geotar

"Lidocaine" is produced in the form of an injection solution () and in the form of a spray. Injections of a 2% solution are used for local anesthesia. The drug is administered subcutaneously, intramuscularly, instilled into the conjunctival sac, and treated with the mucous membranes. For conduction anesthesia, 100-200 mg of the drug is used. To relieve pain in the ears, nose, and fingers, 40-60 mg is administered. To achieve the greatest therapeutic effect, Epinephrine can be additionally used.

In ophthalmology, the drug is instilled 4-6 drops into each eye, 2 drops every 30-60 seconds. For the purpose of terminal anesthesia, Lidocaine is used to the maximum extent possible. permissible dose– 20 ml, treatment should last 15-30 minutes. 10% Lidocaine is used during operations and diagnostic procedures. It is administered intramuscularly and also used in the form of applications. The maximum permissible volume for applications is 2 ml.

Before using Lidocaine, you need to conduct an allergy test to determine sensitivity to the drug. If swelling or redness occurs, the anesthetic should not be used. When using Lidocaine, you need to monitor the ECG; you cannot disinfect the injection site with solutions containing heavy metals. The drug inhibits nerve conduction by blocking sodium channels in nerve endings and fibers. The effect of Lidocaine can last up to 75 minutes, and in combination with Epinephrine - longer than 2 hours.

"Lidocaine": side effects, contraindications

Lidocaine can cause the following: side effects: weakness, headache, fatigue, photophobia, euphoria, nystagmus, numbness of the tongue, lips, hearing impairment, nightmares, drowsiness, double vision, low blood pressure, transverse heart block, cardiac rhythm and conduction disturbances, chest pain, respiratory paralysis muscles, sensory disturbances, tremors, convulsions. The drug can also cause allergic reactions, shortness of breath, vomiting, nausea, decreased body temperature, chills, and fever.

"Lidocaine" is contraindicated in cases of atrioventricular block of the 2nd and 3rd degree, heart failure of the 2nd and 3rd degree, arterial hypertension, severe bradycardia, cardiogenic shock, complete transverse heart block, myasthenia gravis, porphyria, severe hepatic, renal pathologies, glaucoma (for eye injections), hypovolemia, hypersensitivity, during pregnancy and lactation.

Dosage form:  injection Compound:

1 ml of solution for injection 20 mg/ml contains:

active substance- lidocaine hydrochloride (in terms of anhydrous substance) 20.0 mg;

Excipients- sodium chloride 6.0 mg, sodium hydroxide 1 M solution to pH 5.0-7.0. water for injections up to 1 ml.

Description: Transparent colorless or slightly colored liquid. Pharmacotherapeutic group:Local anesthetic ATX:  

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

Pharmacodynamics: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 to sodium ions. As a result, the rate of depolarization decreases and the excitation threshold increases. leading to reversible local numbness. 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 fifteen minutes after intramuscular administration), and quickly spreads into surrounding tissues. The action lasts 10-20 minutes and about 60-90 minutes after intravenous and intramuscular injection respectively. Pharmacokinetics:

Absorption

Lidocaine is rapidly absorbed from gastrointestinal tract, however, due to the “first pass” effect through the liver, only a small amount reaches the systemic circulation.

Systemic absorption of lidocaine is determined by the site of administration and dose. The maximum concentration in the blood is achieved after intercostal blockade, then (in order of decreasing concentration), after injection into the lumbar epidural space, brachial plexus and subcutaneous tissue. 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 the resulting maximum concentration of anesthetic in the blood.

Distribution

Lidocaine binds to plasma proteins, including acid glycoprotein (ACG) and albumin. The degree of binding is variable, being approximately 66%. The plasma concentration of ACG in newborns is low, so they have a relatively high content of the free biologically active fraction of lidocaine. penetrates the blood-brain and placental barriers, probably through passive diffusion.

Metabolism

Lidocaine is metabolized in the liver, about 90% of the administered dose is N- dealkylation to form monoethylglycine xylidide(MEGX) and glycinxylidide(GX). both contribute to the therapeutic and toxic effects of lidocaine. Pharmacological and toxic effects MEGX and GX comparable to those of lidocaine. but less pronounced. GX has a longer half-life than . (about 10 hours) and can accumulate with repeated administration.

Metabolites resulting from subsequent metabolism are excreted in the urine.

Removal

The terminal half-life of lidocaine after intravenous bolus administration to healthy adult volunteers is 1-2 hours. Terminal half-life GX is about 10 hours. MEGX - 2 hours.

Special groups patients

Due to its rapid metabolism, the pharmacokinetics of lidocaine may be influenced by conditions that impair liver function. In patients with hepatic dysfunction, the half-life of lidocaine may increase by 2 or more times.

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

In newborns, the concentration of AKG is low, so the connection with plasma proteins may be reduced. Due to the potentially high concentration of the free fraction, the use of lidocaine in newborns is not recommended.

Indications: Local and regional anesthesia, conduction anesthesia for major and minor surgical interventions. Contraindications:Hypersensitivity to the components of the drug and to amide-type anesthetics; atrioventricular (AV) block 3 degrees; hypovolemia. Carefully:The administration of lidocaine should be carried out with caution in patients with myasthenia gravis, epilepsy, chronic heart failure, bradycardia and respiratory depression, coagulopathy, complete and incomplete block of intracardiac conduction, convulsive disorders, Melkersson-Rosenthal syndrome, porphyria, as well as in the third trimester of pregnancy (see . section "Special instructions"). Pregnancy and lactation:

Fertility

There are no data on the effect of lidocaine on human fertility.

Pregnancy

Lidokaia is allowed to be used during pregnancy and breastfeeding. It is necessary to strictly adhere to the prescribed dosage regimen. If there are complications or a history of bleeding, epidural anesthesia with lidocaine in obstetrics is contraindicated.

Lidocaine was used in large number pregnant women and women of childbearing age. No reproductive disorders were registered, i.e. no increase in the incidence of malformations was observed.

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

No harmful effects on the fetus were found in animal studies.

Breast-feeding

Lidocaine penetrates in small quantities into breast milk, its oral bioavailability is very low. Thus, the expected amount obtained through breast milk is very small, therefore potential harm very low for a child.

The decision about the possibility of using lidocaine during breastfeeding is made by the doctor.

Directions for use and dosage:

The dosage regimen should be adjusted based on patient response and site of administration. The drug should be administered in 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 injected depends on the size of the area to be anesthetized. If there is a need to administer a large volume with a low concentration, then the standard solution is diluted saline solution(0.9% sodium chloride solution). Dilution is carried out immediately before administration.

For children, elderly and weakened patients, the drug is administered in smaller doses appropriate to their age and physical condition.

In adults and children 12-18 years of age, a single dose of lidocaine (except spinal anesthesia) should not exceed 5 mg/kg. at maximum - 300 mg.

	10 mg/ml	20 mg/ml
Infiltration anesthesia:
Small interventions	2-10 ml (20-100 mg)
Major interventions	10-20 ml (100-200 mg)	5-10 ml (100-200 mg)
Conduction anesthesia	3-20 ml (30-200 mg)	1.5-10 ml (30-200 mg)
Anesthesia of fingers/toes	2-4 ml (20-40 mg)	2-4 ml (40-80 mg)
Epidural, lumbar	25-30 ml (250-300 mg)
Caudal, chest block	20-30 ml (200-300 mg)
Regional anesthesia	No more than 5 ml (50 mg)	No more than 2.5 ml (50 mg)

Children under 1 year old

Experience with children under 1 year of age is limited. The maximum dose in children 1-12 years old is 5 mg/kg body weight of a 1% solution.

Concomitant use with epinephrine

To prolong the action of lidocaine and reduce its systemic effect, it is possible to add ex tempore 0.1% epinephrine solution in a ratio of 1:100000 to 1:200000.

Side effects:

Adverse reactions are described according to systemic organ classes MedDRA.

Like other local anesthetics, adverse reactions are rare. usually due to elevated plasma concentrations due to accidental intravascular administration, overdose, or rapid absorption from areas of abundant blood supply, or due to hypersensitivity, idiosyncrasy, or reduced patient tolerance. Systemic toxicity reactions mainly occur in the central nervous and/or of cardio-vascular system(see also section "Overdose").

Violations by immune system: hypersensitivity reactions (allergic or anaphylactoid reactions, anaphylactic shock) - see also disorders of the skin and subcutaneous tissues. The allergy skin test is not considered reliable.

Nervous system disorders and mental disorders: Neurological signs of systemic toxicity include dizziness, nervousness, tremor, and paresthesia around the mouth. numbness of the tongue, drowsiness, convulsions, coma. Reactions from the nervous system can manifest themselves as either excitation or depression. Signs of stimulation of the central nervous system (CNS) may be short-lived or not occur at all, as a result of which the first manifestations of toxicity may be signs of CNS depression - confusion and drowsiness, followed by coma and respiratory failure.

TO neurological complications spinal anesthesia includes transient neurological symptoms such as pain in the lower back, buttocks and legs. These symptoms develop. usually 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 have been described. Most cases are due to hyperbaric lidocaine or prolonged spinal infusion.

Visual disorders: Signs of lidocaine toxicity may include blurred vision, diplopia, and transient amaurosis.

Bilateral amaurosis may also result from accidental insertion of the optic nerve into the optic nerve bed during ophthalmic procedures. After retro- and peribulbar anesthesia, ocular inflammation and diplopia have been reported (see section "Special Instructions").

Disorders of the hearing organ and labyrinth: tinnitus, hyperacusis.

Cardiovascular system disorders: cardiovascular reactions are manifested by arterial hypotheisia, bradycardia, inhibition of myocardial contractile function (negative inotropic effect), arrhythmias, possible cardiac arrest or circulatory failure.

Violations by respiratory system, organs chest and mediastinum: shortness of breath, bronchospasm, respiratory depression, respiratory arrest.

Gastrointestinal disorders: nausea, vomiting.

Disorders of the skin and subcutaneous tissues: rash, urticaria, angioedema, facial swelling.

Overdose:

Symptoms:Central nervous system toxicity is manifested by symptoms. increasing in severity. Paresthesia around the mouth may develop first. numbness of the tongue, dizziness, hyperacusis and tinnitus. Visual disturbances and muscle tremors or muscle twitching indicate more serious toxicity and precede generalized seizures. Loss of consciousness and grand mal seizures may then occur, lasting from a few seconds to several minutes. Convulsions lead to a rapid increase in hypoxia and hypercapnia, caused by increased muscle activity and respiratory failure. In severe cases, apnea may develop. Acidosis enhances the toxic effects of local anesthetics. In severe cases, disorders of the cardiovascular system occur. At high systemic concentrations, hypotension, bradcardia, arrhythmia and cardiac arrest may develop, which can be fatal.

Resolution of an overdose occurs due to the redistribution of the local anesthetic from the central nervous system and its metabolism; it can occur quite quickly (if very high dose drug).

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 adequate circulation and relieve acidosis (if it develops). In appropriate cases, it is necessary to ensure patency respiratory tract and prescribe, as well as establish auxiliary ventilation (mask or using an Ambu bag). Blood circulation is maintained through the influence of plasma or infusion solutions. If long-term circulatory maintenance is necessary, vasopressors should be considered, but they increase the risk of CNS stimulation. Seizure control can be achieved by intravenous diazepam (0.1 mg/kg) or sodium thiopental (1-3 mg/kg). It should be borne in mind that anticonvulsants may also depress respiration and circulation. Prolonged seizures may interfere with the patient's ventilation and oxygenation, and early endotracheal intubation should be considered. If the heart stops, standard cardiopulmonary resuscitation begins.

The effectiveness of dialysis in the treatment of acute lidocaine overdose is very low.

Interaction:

The toxicity of lidocaine increases with its simultaneous use with cimetidiom and propranolol due to an increase in the concentration of lidocaine, this requires a reduction in the dose of lidocaine. Both drugs reduce hepatic blood flow. In addition, it inhibits microsomal activity.

Ranitidine slightly reduces the clearance of lidocaine, which leads to an increase in its concentration. Increased serum concentrations of lidocaine may also cause antivirals(eg, ., lopinavir). Hypokalemia. caused by diuretics, may reduce the effect of lidocaine when used simultaneously (see section "Special Instructions").

Lidocaine should be used with caution in patients receiving other local anesthetics or agents structurally similar to amide-type local anesthetics (eg, antiarrhythmics such as tocainide). since systemic toxic effects are additive. Selected studies drug interactions No studies have been conducted between lidocaine and class III antiarrhythmics (eg, amiodarone), but caution is advised.

In patients simultaneously receiving antipsychotics, prolonging or capable of prolonging the OT interval (for example, pimozide, zotepine), prenylamine. (at random intravenous administration) or 5-HT3-serotonin receptor antagonists ( , dolasetron), the risk of ventricular arrhythmias may increase.

Concomitant use of hipupristin/dalfopristin may increase lidocaine concentrations and thus increase the risk of ventricular arrhythmias; their simultaneous use should be avoided.

Patients receiving concomitant muscle relaxants (eg, suxamethonium) may have an increased risk of enhanced and prolonged neuromuscular blockade. After the use of bupivacaine in patients receiving and, the development of cardiovascular failure was reported: it is similar in structure to bupivacaine. and 5-hydroxytryptamia reduce the threshold of convulsive readiness to lidocaine. Opoids appear to have a proconvulsant effect, supported by evidence, which lowers the seizure threshold to fentanyl in humans.

A combination of opioids and antiemetics, sometimes used for sedation in children, may lower the seizure threshold to lidocaine and increase its CNS depressant effect.

Use of epinephrine with lidocaine may reduce systemic absorption, but accidental intravenous administration increases the risk ventricular tachycardia and ventricular fibrillation.

Concomitant use of other antiarrhythmics, β-blockers and slow blockers calcium channels may further reduce AV conduction, ventricular conduction, and contractility.

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

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

Care must be taken when using sedatives, since they can affect the action of local anesthetics on the central nervous system.

Caution should be exercised with long-term use of antiepileptic drugs (), barbiturates and other inhibitors of microsomal liver enzymes. as this may result in reduced efficiency and. as a consequence, an increased need for lidocaine.

On the other hand, intravenous administration of phenytoin may enhance the depressant effect of lidocaine on the heart.

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

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

Lidocaine is not compatible with amphogerycin B, methohexitone and nitroglycerin. When using lidocaine simultaneously with narcotic analgesics an additive effect develops, which is used when performing epidural anesthesia, but increases the depression of the central nervous system and respiration.

Vasoconstrictors (methoxamine) prolong the local anesthetic effect of lidocaine and can cause an increase in blood pressure and tachycardia.

Use with monoamine oxidase inhibitors (seleginine) probably enhances the local anesthetic effect of lidocaine and increases the risk of lowering blood pressure.

Guanadrel, guanethidine. mecamylamine, trimethaphan camsylate increase the risk of a pronounced decrease in blood pressure and bradycardia.

Anticoagulants (including ardeparin sodium, danaparoid sodium, heparin, etc.) increase the risk of bleeding. reduces the cardiotonic effect of digitoxin.

Lidocaine reduces the effect of antimyasthenic drugs medicines, enhances and prolongs the effect of muscle relaxant drugs.

When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing local reaction in the form of pain and swelling. Mixing with other medications is not recommended.

Special instructions:

Regional and local anesthesia should be carried out by experienced specialists in an appropriately equipped room with the availability of equipment and drugs necessary for cardiac monitoring and resuscitation, ready for immediate use. Anesthesia personnel. must be qualified and trained in anesthesia techniques, must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions and other complications.

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

For patients receiving antiarrhythmic drugs Class III (for example,) requires careful observation and ECG monitoring, since the effect on the heart may be potentiated.

There have been post-marketing reports of chondrolysis in patients who received prolonged intra-articular infusion of local anesthetics after surgery. In most cases, chondrolysis was observed in shoulder joint. Due to the many contributing factors and the inconsistency in the scientific literature regarding the mechanism by which the effect is realized, a cause-and-effect relationship has not been identified. Long-term intra-articular infusion is not an approved indication for the use of lidocaine. Intramuscular administration of lidocaine can increase the activity of creatine phosphokinase. which may complicate the diagnosis of acute myocardial infarction.

Shown to cause porphyria in animals, its use in persons with porphyria should be avoided.

When injected into inflamed or infected tissues, the effect of lidocaine may be reduced.

Before starting intravenous lidocaine, it is necessary to eliminate hypokalemia, hypoxia and acid-base imbalance.

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

Conduction anesthesia spinal nerves may lead to depression of the cardiovascular system, especially against the background of hypovolemia, so caution should be exercised when administering epidural anesthesia to patients with cardiovascular disorders.

Epidural anesthesia can lead to arterial hypotension and bradycardia. The risk can be reduced by pre-administration of crystalloid or colloid solutions. Arterial hypotension must be stopped immediately.

In some cases, paracervical blockade during pregnancy can lead to bradycardia or tachycardia in the fetus, which requires careful monitoring of the fetal heart rate (see section "Use during pregnancy and breastfeeding").

Administration to the head and neck area may result in inadvertent arterial entry leading to cerebral symptoms, even at low doses.

Retrobulbar administration may rarely result in entry into the subarachnoid space of the skull, resulting in serious/severe reactions including cardiovascular collapse, 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 effect 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 in the lowest effective concentration and dose. Lidocaine injection solution is not recommended for use in newborns. The optimal serum concentration of lidocaine to avoid toxicities such as seizures and arrhythmias has not been established in neonates.

Intravascular administration should be avoided unless directly indicated. Use with caution:

In patients with coagulopathy. Therapy with anticoagulants (eg, heparin), nonsteroidal anti-inflammatory drugs (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;

Patients with complete and incomplete block 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 seizure activity. 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; -third trimester of pregnancy.

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

Impact on the ability to drive vehicles. Wed and fur.:After administration of local anesthetics, a transient decrease in sensitivity and/or motor block may occur. Until these effects resolve, patients are not advised to administer vehicles and work with machinery. Release form/dosage:

Solution for injection 20 mg/ml.

Package:

2 ml in ampoules. 10 ampoules per cardboard box along with instructions for use and an ampoule scarifier. 5 ampoules per blister pack. 2 blister packs each, along with instructions for use and an ampoule scarifier in a cardboard pack.

When using ampoules with a break point or ring, do not insert an ampoule scarifier.

Storage conditions:

In a place protected from light at a temperature of 8 ° C to 25 ° C.

Avoid freezing.

Keep out of the reach of children.

Best before date:

Do not use after the expiration date stated on the packaging.

Conditions for dispensing from pharmacies: On prescription Registration number: P N000318/01 Registration date: 19.11.2007 Expiration date: Indefinite Owner of the Registration Certificate:MOSKHIMPHARMPREPARATY im. N.A. Semashko, JSC Russia Manufacturer:   Information update date:   26.02.2018 Illustrated instructions

Lidocaine is an effective analgesic (pain reliever) for local anesthesia.

This drug is widely used in dentistry, ophthalmology, as well as surgery during various operations or diagnostic procedures.

In addition to the local anesthetic effect, Lidocaine also has pronounced antiarrhythmic properties, which allow you to quickly normalize the heart rate.

The anesthetic (pain-relieving) effect is observed, as a rule, after 3-5 minutes. after local administration medicinal product and at the same time lasts more than 70-90 minutes.

Before starting to use Lidocaine, it is recommended to do an allergy test for individual sensitivity to the drug, and if local redness or swelling occurs at the injection site, then use this remedy strictly contraindicated!

Main indications for the use of Lidocaine:

• local anesthesia before various surgical or diagnostic procedures;
• pain from various injuries or diseases that are accompanied by severe pain;
• dental procedures (tooth extraction, installation of crowns, etc.);
• various surgical procedures in otolaryngology (tonsillectomy);
• performing gastroduodenoscopy;
• gynecological manipulations.

Attention: Before starting to use Lidocaine, it is recommended to consult with a qualified physician!

The drug is produced in the form of a solution for injection, as well as a spray for topical use.

How to use Lidocaine?

For local anesthesia, adults are usually prescribed 2% Lidocaine in a total dose of 2-4 ml. for intramuscular or subcutaneous administration.

Quite often used this drug in the form of a spray for topical application to the area of ​​the body that needs to be numbed, while avoiding possible contact with this medicinal substance into the eyes or respiratory tract of the body.

For children, the required dose of the drug is determined absolutely individually for each child, depending on age, body weight, as well as the specific situation.

Contraindications to the use of lidocaine

• hypersensitivity (increased sensitivity of the body to the main active ingredient of the drug);
• acute heart failure;
• hypovolemia;
• severe form of bradycardia;
• arterial hypotension (low blood pressure);
• severe liver and kidney diseases;
• glaucoma;
• pregnancy and lactation (breastfeeding).

Side effects of Lidocaine

• headache;
• increased dry mouth;
• general weakness;
• increased fatigue;
• hearing loss;
• drowsiness;
• numbness of the tongue;
• convulsions;
• local allergic reactions (increased itchy skin, urticaria, allergic rhinitis);
• increased irritability;
• sleep disturbance (insomnia);
• nausea or vomiting (occurs extremely rarely, mainly with a significant overdose of the drug).

With the development of any allergic reaction After using Lidocaine, it is recommended to consult your doctor!

In this article, we looked at what Lidocaine helps with, as well as how to inject it correctly.

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

Pharmacological properties

The antiarrhythmic properties of lidocaine are due to inhibition of diastolic depolarization in Purkinje fibers, suppression of ectopic foci of excitation, and reduction of automaticity. Lidocaine does not affect the rate of rapid depolarization or slightly reduces it. Lidocaine increases the permeability of the cell membrane to potassium ions, speeds up the repolarization process and shortens the action potential. Lidocaine does not change the excitability of the sinoatrial node; it has a slight effect on myocardial contractility and conductivity. 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, this prevents the occurrence of action potentials and the conduction of impulses. In a slightly alkaline tissue environment, lidocaine is quickly hydrolyzed and, after a short latent period, has an effect within 1 - 1.5 hours. During inflammation, the anesthetic activity of lidocaine is reduced due to the acidic environment at the site of inflammation.
Lidocaine is effective for all types of local anesthesia. Lidocaine does not irritate tissues and dilates blood vessels; antagonism with calcium ions is possible. When administered intravenously, the maximum concentration is created after 45 - 90 seconds, when administered intramuscularly - after 5 - 15 minutes. Lidocaine is absorbed quite quickly from the mucous membrane of the oral cavity or upper respiratory tract (maximum concentration is reached after 10–20 minutes). When lidocaine is taken orally, bioavailability is only 15–35% (due to first-pass effects through the liver). 50–80% bound to plasma proteins. In the blood, a stable concentration is achieved 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 penetrates various barriers, including the blood-brain and placental barriers, and enters breast milk. First, lidocaine enters well-supplied tissues (lungs, heart, brain, spleen, liver), then into muscle and adipose tissue.
The half-life of intravenous bolus administration is 1.5–2 hours (3 hours in newborns), with long-term intravenous infusions it is up to 3 hours or even more. If liver function is impaired, the half-life of lidocaine may increase by more than 2 times. Lidocaine is almost completely and quickly metabolized in the liver (less than 10% is excreted unchanged in the urine) through the process of oxidative N-dealkylation; in this process, active metabolites are formed (glycine xylidine and monoethylglycine xylidine), which have a half-life of 10 hours and 2 hours, respectively. In patients with chronic renal failure accumulation of lidocaine metabolites in the body is possible. The duration of action of lidocaine when administered intravenously is 10–20 minutes when administered intramuscularly and 60–90 minutes. When used topically in the form of plates on intact skin, a therapeutic effect sufficient to relieve pain occurs without systemic effects developing.

Indications

Ventricular fibrillation; ventricular tachyarrhythmias and extrasystoles, including in 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 administration of lidocaine and dose

The dosage regimen is set individually, depending on the clinical situation, indications and dosage form used. For arrhythmias: intravenously (over 3–4 minutes) 50–100 mg in a stream at a rate of 25–50 mg/min, then drip at a rate of 1–4 mg/min; intramuscularly 4.3 mg/kg body weight, possible repeated administration after 1 – 1.5 hours; for intravenous and intramuscular administration maximum dose for adults equal to 300–400 mg for 1 hour; maximum daily dose is 2000 mg. Children are injected with 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 injected at a rate of 30 mcg/kg/min; the maximum daily dose is 4 mg/kg. Superficial anesthesia - 2–10% solution (no more than 200 mg - 2 ml). Infiltration anesthesia for adults uses a 0.5% solution, and conduction anesthesia uses a 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. Locally (aerosol, gel, spray, plates). For children under 2 years of age, 1–2 aerosol doses (4.8–9.6 mg) are prescribed for superficial anesthesia, first applied to a cotton swab. The plates are glued to the skin, covering the painful surface. After applying the plate, you should immediately wash your hands. The plate can remain on the skin for 12 hours. Then it is removed and a break of 12 hours is taken. No more than 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. Caution must be exercised 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, and elderly patients require dose adjustment in accordance with their physical status and age. When introducing lidocaine into vascularized tissues, an aspiration test must be performed. Use topical lidocaine to an area of ​​infection or injury with caution. If, while using the plate, skin redness or a burning sensation occurs, the plate must be removed and not used until the redness or burning sensation 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 blocks (intraventricular, AV, sinoatrial), sinus node weakness, cardiogenic shock, WPW syndrome, myasthenia gravis, serious illnesses liver, a history of epileptiform seizures when using lidocaine.

Restrictions on use

Breastfeeding, pregnancy, age over 65 years, progression of cardiovascular failure, debilitated patients, conditions that are accompanied by decreased hepatic blood flow; violation of the integrity of the skin (at the site of use of the plates).

Use during pregnancy and breastfeeding

Lidocaine can be used during breastfeeding and pregnancy if the expected effects of therapy on the mother are higher possible risk for a child or fetus.

Side effects of lidocaine

Nervous system and sense organs: excitement or depression of the central nervous system, nervousness, flashing “floaters” before the eyes, euphoria, photophobia, headache, drowsiness, dizziness, diplopia, tinnitus, impaired consciousness, stopping or depression of breathing, tremor, disorientation, muscle twitching, convulsions ( the possibility of their development increases with hypercapnia and acidosis);
circulatory system: cardiac conduction disturbances, sinus bradycardia, transverse heart block, increased or decreased 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 at the site of action of the aerosol 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 potential for 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 plasma level of lidocaine. 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, ajmaline, amiodarone, quinidine) potentiate cardiodepression when used together with lidocaine. The combined use of lidocaine and procainamide can cause hallucinations and stimulation of the central nervous system. Lidocaine enhances the inhibitory effect of hypnotic and anesthetic drugs on the respiratory center, deepens muscle relaxation, which is caused by curare-like drugs, and weakens the cardiotonic effect of digitoxin. MAO inhibitors prolong the local anesthesia of lidocaine.

Overdose

An overdose of lidocaine causes psychomotor agitation, general weakness, dizziness, hypotension, tremor, coma, tonic-clonic seizures, collapse, depression of the central nervous system, AV block, and respiratory arrest. It is necessary: ​​stopping the use of lidocaine, oxygen therapy, pulmonary ventilation, taking anticonvulsants, vasoconstrictors (mesaton, norepinephrine), if bradycardia develops - anticholinergics (atropine); if necessary, carrying out resuscitation measures, pulmonary intubation, mechanical ventilation. Dialysis is ineffective.

Trade names of drugs with the active ingredient lidocaine

Versatis Helikain Dinexan Xylocaine

Lidocaine Lidocaine Bufus Lidocaine-Vial Lidocaine hydrochloride

Lidocaine hydrochloride 1% Brown Lidocaine hydrochloride 2% Brown Lidocaine hydrochloride injection solution Luan

Lidocaine is a short-acting local anesthetic. The drug is available in several dosage forms and is used in many medical industries to obtain a lasting analgesic effect during various manipulations.

In the article you will receive instructions on the use of this medicine, and also become familiar with the indications and contraindications.

What kind of drug is this?

Lidocaine is one of the most common medical practice local anesthetic. It is characterized by a rapid onset of action, relatively low toxicity and an average duration of effect.

Lidocaine is used for all types of local anesthesia. In the presence of inflammation in the tissues, the analgesic activity is slightly reduced. In addition to the analgesic effect, it has antiarrhythmic properties.

What's in the solution?

Active substance drug – lidocaine hydrochloride. It is an acetanilide derivative. Each ampoule contains sodium chloride and hydroxide, and water for injection as auxiliary components.

Lidocaine is a colorless or yellowish transparent solution, without foreign impurities or inclusions.

Possible forms of release of Lidocaine

The drug is presented in several forms of release:

1. Spray 10% in a special bottle.
2. 1% and 2% solutions for injection in ampoules or cylinders
3. gel, ointment
4. solutions in dropper tubes for use in ophthalmology (eye drops).
5. 2% and 10% solution for injection in buffus (special plastic ampoules).
6. solution in syringe pens and capsules-ampoules.

Important! Lidocaine is included in some creams, such as Emla. It is used for venipuncture - spread on skin covering a few hours before the manipulation. Ledocaine gel is also used in adults on the mucous membrane before getting rid of genital warts (10-15 minutes before the intervention).

How does it work?

The mechanism of the analgesic effect is based on membrane stabilization nerve cells and a decrease in its penetrating ability for sodium ions. Due to this, an action potential does not occur, and the transmission of nerve impulses is temporarily blocked.

The active substance does not irritate tissues, leads to vasodilation and reduces its effectiveness in the presence of inflammation in tissues

Important! The antiarrhythmic effect of Lidocaine is due to its stabilizing effect on cardiac muscle cells.

In what cases is it used?

The drug in ampoules is prescribed in the following situations:

Lidocaine is used as an antiarrhythmic for ventricular extrasystole, in the acute phase of myocardial infarction, as well as for the prevention of ventricular fibrillation.

Instructions for use of Lidocaine in ampoules

The exact dosage and quantity depend on the type of anesthesia and nature surgical intervention.

Instructions for use:

Before using it for the first time, the patient must undergo an allergy test.

For these purposes, 0.1 ml of Lidocaine is injected subcutaneously and the reaction is observed for half an hour. If the reaction is negative, then the medicine can be administered in full intravenously or intramuscularly.

Use in pregnant and nursing mothers

Should not be used on early stages pregnancy, except in situations where the benefit to the woman significantly outweighs the risk to the fetus.

Active substance penetrates into breast milk in small quantities and causes adverse reactions in children, so during treatment breastfeeding should be stopped for a while.

The drug is approved for use in childhood after consultation with your doctor. The first administration is performed after an allergy test in an outpatient or inpatient conditions to prevent the consequences of a possible allergic reaction.

Contraindications, overdose and negative reactions

The drug is not prescribed:

When using Lidocaine, undesirable effects may occur:

1. Nervous system: drowsiness, fatigue, nystagmus, dizziness, spots before the eyes, impaired consciousness, respiratory arrest.
2. Heart and blood vessels: sudden change in blood pressure (fall or rise), arrhythmia, blockade, rapid heartbeat, heart pain.
3. Digestive tract: nausea, diarrhea, vomiting.
4. Kidneys: involuntary act of urination.
5. Other: fever, feeling of heat, chills, rash, urticaria, swelling, dermatitis.

Uncontrolled use of the medicine can lead to an overdose. This condition is manifested by nausea, drop in blood pressure, convulsions, vomiting, weakness and respiratory arrest.

How and where is it stored?

Store in a dry place, inaccessible to direct sun rays, at a temperature not higher than 25 degrees. Shelf life under storage conditions is up to 5 years.

Interaction with other drugs

Combined use with beta blockers increases the toxicity of lidocaine, increasing the likelihood of a decrease in blood pressure and the development of bradycardia. Barbiturates and rifampicin reduce its activity.

In combination with procainamide, hallucinations and agitation may occur. Anticoagulants increase the risk of bleeding.

Lidocaine potentiates the effect of anesthetic and sedatives, when administered simultaneously with narcotic analgesics, its effectiveness increases.

Concomitant use with epinephrine prolongs the effect of local anesthesia, but increases the risk of developing ventricular fibrillation.

Prescribed with caution in patients receiving drugs of similar chemical structure (some antiarrhythmics) to avoid combined toxic reactions.

Price and analogues

The average cost of the product in ampoules is from 20 rubles per 1 ampoule. A medicine with a similar effect is Novocain, which costs 19 rubles per ampoule.

In addition, you can replace Lidocaine with Ultracaine D-S, the price of which is from 100 rubles. per ampoule.