Long-term use of lidocaine. Domestic and foreign analogues

In this article, you can read the instructions for using the drug Lidocaine. Reviews of site visitors - consumers of this medicine, as well as opinions of doctors of specialists on the use of Lidocaine in their practice are presented. We kindly ask you to actively add your reviews about the drug: the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Analogues of Lidocaine in the presence of existing structural analogues. Use for the treatment of arrhythmias and anesthesia (pain relief) in adults, children, as well as during pregnancy and lactation.

Lidocaine- according to the chemical structure, it belongs to acetanilide derivatives. It has a pronounced local anesthetic and antiarrhythmic effect. The local anesthetic effect is due to the inhibition of nerve conduction due to the blockade of sodium channels in the nerve endings and nerve fibers. In its anesthetic effect, lidocaine is significantly (2-6 times) superior to procaine; the action of lidocaine develops faster and lasts longer - up to 75 minutes, and when used simultaneously with epinephrine - more than 2 hours. When applied topically, it dilates blood vessels, does not have a local irritating effect.

The antiarrhythmic properties of lidocaine are due to its ability to stabilize the cell membrane, block sodium channels, and increase membrane permeability to potassium ions. With virtually no effect on the electrophysiological state of the atria, lidocaine accelerates repolarization in the ventricles, inhibits the 4th phase of depolarization in the Purkinje fibers (diastolic depolarization phase), reducing their automatism and the duration of the action potential, increases the minimum potential difference at which myofibrils respond to premature stimulation. The rate of rapid depolarization (phase 0) is not affected or slightly reduced. Does not have a significant effect on the conductivity and contractility of the myocardium (inhibits conduction only in large, close to toxic doses). Intervals PQ, QRS and QT under its influence on the ECG do not change. The negative inotropic effect is also insignificantly expressed and manifests itself for a short time only with the rapid administration of the drug in large doses.

Pharmacokinetics

It is rapidly distributed in organs and tissues with good perfusion, incl. in the heart, lungs, liver, kidneys, then in muscle and adipose tissue. Penetrates through the blood-brain and placental barriers, secreted with breast milk (up to 40% of the concentration in the mother's plasma). It is metabolized mainly in the liver (90-95% of the dose) with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycine xylidide and glycine xylidide. Excreted with bile and urine (up to 10% unchanged).

Indications

infiltration, conduction, spinal and epidural anesthesia;
terminal anesthesia (including in ophthalmology);
relief and prevention of recurrent ventricular fibrillation in acute coronary syndrome and recurrent paroxysms of ventricular tachycardia (usually within 12-24 hours);
ventricular arrhythmias due to glycoside intoxication.

Release form

Solution (injections in ampoules for injection and dilution).

Spray dosed (aerosol) 10%.

Eye drops 2%.

Gel or ointment 5%.

Instructions for use and dosage

Solution

For infiltration anesthesia: intradermally, subcutaneously, intramuscularly. Apply a solution of lidocaine 5 mg / ml (maximum dose 400 mg).

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 epidural anesthesia: epidural, solutions of 10 mg / ml or 20 mg / ml (no more than 300 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.

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, however, in obstetric practice, 15-20 or more doses are applied (the maximum number is 40 doses per 70 kg of body weight).

Side effect

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

Contraindications

sick sinus syndrome;
severe bradycardia;
AV blockade 2-3 degrees (except when a probe is inserted to stimulate the ventricles);
sinoatrial blockade;
WPW syndrome;
acute and chronic heart failure (3-4 FC);
cardiogenic shock;
pronounced decrease in blood pressure;
Adams-Stokes syndrome;
violations of intraventricular conduction;
retrobulbar administration to patients with glaucoma;
pregnancy;
lactation period (penetrates the placental barrier, excreted in breast milk);
hypersensitivity to any of the components of the drug.

Use during pregnancy and lactation

Contraindicated for use during pregnancy and lactation.

Use in children

The drug should be used with caution in children.

special instructions

It is necessary to cancel MAO inhibitors at least 10 days in advance, in case of planned use of lidocaine.

Caution should be exercised when administering local anesthesia to highly vascularized tissues, and an aspiration test is recommended to avoid intravascular injection.

Influence on the ability to drive vehicles and control mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

drug interaction

Beta-blockers and cimetidine increase the risk of developing toxic effects.

Reduces the cardiotonic effect of digitoxin.

Enhances muscle relaxation of curare-like drugs.

Aymalin, amiodarone, verapamil and quinidine increase the negative inotropic effect.

Inducers of microsomal liver enzymes (barbiturates, phenytoin, rifampicin) reduce the effectiveness of lidocaine.

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

Lidocaine reduces the effect of antimyasthenic drugs.

Combined use with procainamide can cause CNS excitation, hallucinations.

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

Enhances and prolongs the action of muscle relaxants.

The combined use of lidocaine and phenytoin should be used with caution, because. it is possible to reduce the resorptive effect of lidocaine, as well as the development of an undesirable cardiodepressive effect.

Under the influence of MAO inhibitors, an increase in the local anesthetic effect of lidocaine and a decrease in blood pressure is likely. Patients taking MAO inhibitors should not be given parenteral lidocaine.

With the simultaneous appointment of lidocaine and polymykisin B, it is necessary to monitor the patient's respiratory function.

With the combined use of lidocaine with hypnotics or sedatives, opioid analgesics, hexenal or sodium thiopental, it is possible to increase the inhibitory effect on the central nervous system and respiration.

With intravenous administration of lidocaine to patients taking cimetidine, undesirable effects such as state of stupor, drowsiness, bradycardia, paresthesia are possible. This is due to an increase in the level of lidocaine in the blood plasma, which is explained by the release of lidocaine from its association with blood proteins, as well as a slowdown in its inactivation in the liver. If combination therapy with these drugs is necessary, the dose of lidocaine should be reduced.

When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.

Analogues of the drug Lidocaine

Structural analogues for the active substance:

Versatis;
Helikain;
Dinexan;
Xylocaine;
Lidocaine Bufus;
Lidocaine-Vial;
Lidocaine hydrochloride;
Lidocaine Hydrochloride Brown;
Luan.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases that the corresponding drug helps with and see the available analogues for the therapeutic effect.

Dosage form: solution for intravenous administration; injection Compound:

Solution for intravenous administration: active substance: 2 ml of solution contains 200 mg of anhydrous lidocaine hydrochloride (in the form of lidocaine hydrochloride monohydrate 213.31 mg); excipients: water for injection

Injection: active substance: 2 ml of solution contains 40 mg of anhydrous lidocaine hydrochloride (in the form of lidocaine hydrochloride monohydrate 43 mg), excipients: sodium chloride for parenteral dosage forms, water for injection.

Description: Clear, colorless or almost colorless aqueous solution, odorless. Pharmacotherapeutic group:Local anesthetic, antiarrhythmic agent 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:

Lidocaine, according to its chemical structure, belongs to acetanilide derivatives. It has a pronounced local anesthetic and antiarrhythmic (lb class) action. The local anesthetic effect is due to the inhibition of nerve conduction due to the blockade of sodium channels in the nerve endings and nerve fibers. In terms of its anesthetic effect, it significantly (2-6 times) exceeds; the action of lidocaine develops faster and lasts longer - up to 75 minutes, and when used simultaneously with epinephrine - more than 2 hours. When applied topically, it dilates blood vessels, does not have a local irritating effect.

The antiarrhythmic properties of lidocaine are due to its ability to stabilize the cell membrane, block sodium channels, and increase membrane permeability to potassium ions. With virtually no effect on the electrophysiological state of the atria, it accelerates repolarization in the ventricles, inhibits the IV phase of depolarization in the Purkinje fibers (diastolic depolarization phase), reducing their automatism and the duration of the action potential, increases the minimum potential difference at which myofibrils respond to premature stimulation. The rate of rapid depolarization (phase 0) is not affected or slightly reduced. Does not have a significant effect on the conductivity and contractility of the myocardium (inhibits conduction only in large, close to toxic doses). Intervals PQ, QRS and QT under its influence on the ECG do not change. The negative inotropic effect is also insignificantly expressed and manifests itself for a short time only with the rapid administration of the drug in large doses.

Pharmacokinetics:The time to reach maximum plasma concentration after intramuscular injection is 5-15 minutes, with slow intravenous infusion without an initial saturating dose - after 5-6 hours (in patients with acute myocardial infarction - up to 10 hours). Plasma proteins bind 50-80% of the drug. It is rapidly distributed (T1 / 2 distribution phase - 6-9 minutes) in organs and tissues with good perfusion, incl. in the heart, lungs, liver, kidneys, then in muscle and adipose tissue. Penetrates through the blood-brain and placental barriers, secreted with breast milk (up to 40% of the concentration in the mother's plasma). It is metabolized mainly in the liver (90-95% of the dose) with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycinexylidide glycinexylidide, having a half-life of 2 hours and 10 hours, respectively. The intensity of metabolism decreases with liver diseases (may be from 50 to 10% of the normal value); in violation of liver perfusion in patients after myocardial infarction and / or with congestive heart failure. The half-life with continuous infusion for 24-48 hours is about 3 hours; in case of impaired renal function, it can increase by 2 or more times. Excreted with bile and urine (up to 10% unchanged). Acidification of urine increases the excretion of lidocaine. Indications:

Infiltration, conduction, spinal and epidural anesthesia. Terminal anesthesia (including in ophthalmology).

Relief and prevention of recurrent ventricular fibrillation in acute coronary syndrome and recurrent paroxysms of ventricular tachycardia (usually within 12-24 hours).

Ventricular arrhythmias due to glycoside intoxication.

Contraindications:

Sick sinus syndrome; severe bradycardia; atrioventricular block II-III degree (except when a probe is inserted to stimulate the ventricles); sinoatrial blockade, WPW syndrome, acute and chronic heart failure (III-IV FK); cardiogenic shock; pronounced decrease in blood pressure, Adams-Stokes syndrome; intraventricular conduction disorders

Hypersensitivity to any of the components of the drug;

Retrobulbar administration to patients with glaucoma;

Pregnancy, breastfeeding (penetrates the placental barrier, excreted in breast milk).

Carefully:

Chronic heart failure II-III degree, arterial hypotension, hypovolemia, atrioventricular block I degree, sinus bradycardia, severe hepatic and / or renal failure, severe myasthenia gravis, epileptiform convulsions (including history), reduced hepatic blood flow, weakened or elderly patients (over 65 years of age), children under 18 years of age (due to slow metabolism, accumulation of the drug is possible), history of hypersensitivity to other amide local anesthetics.

It is also necessary to take into account the general contraindications to the conduct of a particular type of anesthesia.

Dosage and administration:

For infiltration anesthesia: intradermal, subcutaneous, intramuscular. Apply a solution of lidocaine 5 mg / ml (maximum dose 400 mg)

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 epidural anesthesia: epidural, solutions 10 mg / ml or 20 mg / ml (no more than 300 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 research.

To prolong the action of lidocaine, it is possible to add ex tempore a 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).

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 (half-life of 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 dose, with an interval of 8-10 minutes.

The maximum dose in 1 hour is 300 mg, per day - 2000 mg.

The intravenous infusion is usually given for 12-24 hours with continuous ECG monitoring, after which the infusion is stopped to evaluate the need for changing the patient's antiarrhythmic therapy.

In chronic renal failure dose adjustment is not required.

Side effects:

From the nervous system, sensory organs:euphoria, headache, dizziness, drowsiness, general weakness, neurotic reactions, confusion or loss of consciousness, disorientation, convulsions, tinnitus, paresthesia, diplopia, nystagmus, photophobia, tremor, trismus of mimic muscles, anxiety.

From the side of the cardiovascular system:decrease in blood pressure, peripheral vasodilation, collapse, chest pain, bradycardia (up to cardiac arrest).

Allergic reactions: skin rash, urticaria, itching, angioedema, anaphylactic shock.

From the digestive system: nausea, vomiting.

Others:sensation of "heat" or "cold", persistent anesthesia, erectile dysfunction, hypothermia, methemoglobinemia.

Overdose:

Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria, lowering blood pressure, asthenia; then - convulsions of mimic muscles with a transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, bradycardia, asystole, collapse; when used during childbirth in a newborn - bradycardia, depression of the respiratory center, apnea.

Treatment: termination of drug administration, oxygen inhalation. Symptomatic therapy. With convulsions, 10 mg of diazepam is administered intravenously. With bradycardia - m-anticholinergics (), vasoconstrictors (,). Hemodialysis is ineffective.

Interaction:

Beta-blockers and increase the risk of developing toxic effects.

Reduces the cardiotonic effect of digitoxin.

Enhances muscle relaxation of curare-like drugs.

Aymalin, and enhance the negative inotropic effect. Inducers of microsomal liver enzymes (barbiturates,) reduce the effectiveness of lidocaine.

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

Lidocaine reduces the effect of antimyasthenic drugs.

Joint use with procainamide can cause excitation of the central nervous system, hallucinations.

Guanadrel, guanethidine, mecamylamine, trimethaphan increase the risk of a pronounced decrease in blood pressure and bradycardia. Enhances and prolongs the action of muscle relaxants.

The combined use of lidocaine and phenytoin should be used with caution, since it is possible to reduce the resorptive effect of lidocaine, as well as the development of an undesirable cardiodepressive effect.

Under the influence of monoamine oxidase inhibitors, an increase in the local anesthetic effect of lidocaine and a decrease in blood pressure is likely. Patients taking monoamine oxidase inhibitors should not be administered parenterally.

With the simultaneous appointment of lidocaine and polymykisin B, it is necessary to monitor the patient's respiratory function.

With the combined use of lidocaine with hypnotics or sedatives, narcotic analgesics, hexenal or sodium thiopental, it is possible to increase the inhibitory effect on the central nervous system and respiration.

With intravenous administration of lidocaine to patients taking, undesirable effects such as a state of stupor, drowsiness, bradycardia, paresthesia, etc. are possible. This is due to an increase in the level of lidocaine in the blood plasma, which is explained by the release of lidocaine from its association with blood proteins, as well as a slowdown in its inactivation in the liver. If combination therapy with these drugs is necessary, the dose of lidocaine should be reduced.

When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.

Special instructions:

It is necessary to cancel MAO inhibitors at least 10 days in advance, in case of planned use of lidocaine.

Caution should be exercised when administering local anesthesia to highly vascularized tissues, and an aspiration test is recommended to avoid intravascular injection.

Influence on the ability to drive transport. cf. and fur.:During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions. Release form / dosage:Solution for intravenous administration 100 mg/ml. Package: 2 ml of the drug in colorless glass ampoules of hydrolytic class I with two code rings (red and green) and a white fault line. 5 ampoules in a blister pack. 2 blister packs together with instructions for medical use are placed in a cardboard box. Solution for injections 20 mg/ml. 2 ml per vial with a notch and with a green code ring, 5 ampoules in a blister pack sealed with a transparent PE film, 20 blister packs in a cardboard box with a sealed label along with instructions for use. Storage conditions:At a temperature of 15 to 25 ° C, out of the reach of children. Best before date: 5 years. Do not use after the expiration date stated on the packaging. Conditions for dispensing from pharmacies: On prescription Registration number: P N014235/03 Date of registration: 26.09.2008 Expiration date: Perpetual Registration certificate holder: Hungary Manufacturer: Representation: EGIS CJSC Pharmaceutical Plant Hungary Information update date: 26.02.2018 Illustrated Instructions

In ophthalmic practice

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

Side effects

From the nervous system and sensory organs

From the side of the blood

Local reactions

With spinal anesthesia - back pain, with epidural anesthesia - accidental entry into the subarachnoid space.

allergic reactions

Other

Heat, sensation of cold. With anesthesia - persistent anesthesia, respiratory depression, up to stopping, hypothermia. When used in ophthalmic practice - irritation of the conjunctiva, with prolonged use - corneal epitheliopathy.

Overdose

Symptoms

special instructions

Prophylactic administration of all patients with acute myocardial infarction without exception is not recommended (routine prophylactic administration of lidocaine may increase the risk of death by increasing the incidence

The majority of medical and many diagnostic procedures are painful for the patient, so manipulations are often performed with anesthesia. Anesthesia for medicinal purposes has been used for almost two hundred years, having developed into a separate branch of medicine - anesthesiology.

Currently, there are several types of anesthesia, for example, for extensive abdominal operations, general anesthesia is used - anesthesia, it is performed using narcotic drugs that affect the central nervous system. For manipulations of a smaller scale (in dentistry and outpatient surgery), local anesthesia is often sufficient, which is carried out with the help of anesthetics - anesthetics.

Lidocaine is the most popular local anesthetic

The most common anesthetics are Novocaine (Procaine) and Lidocaine. The latter has a number of advantages over Novocaine: it rarely causes allergic reactions, acts faster and lasts longer, and does not cause local irritating effects.

Lidocaine blocks sodium channels in nerve endings and fibers, as a result, a temporary cessation of the transmission of the nerve impulse occurs, pain sensitivity is completely lost. To prolong the action of the drug, it is often combined with adrenaline (epinephrine), opioid analgesics and steroid hormones.

Types of anesthesia Lidocaine

infiltration

This method is used for minor surgical interventions (opening abscesses, removal of small benign formations, reduction of an inguinal or umbilical hernia, in dentistry). For infiltrations, Lidocaine is used at a concentration of 2.5; 5; 10 and 20 mg / ml, at a dose of up to 200 mg. It is administered intradermally, subcutaneously and intramuscularly, depending on the required depth of anesthesia. With the infiltrative method, the effect develops immediately after a dose of the drug is administered.

Lidocaine in infiltration anesthesia is used for minor surgical interventions

One of the varieties of infiltration anesthesia is application anesthesia or in another way it is called terminal. With this method of anesthesia, the drug is applied to the skin or mucous membranes, blocking the pain sensitivity of superficial nerve endings. Application anesthesia allows you to anesthetize tissues to a depth of several millimeters.

The application technique is used for manipulations in the nasal cavity, in the throat, as well as in dentistry and ophthalmology. For application, Lidocaine is used in the form of a spray or drops, depending on the technique, the anesthetic is used at a dose of 1 to 2 ml of a 10% solution (100 mg / ml) or at a dose of 10–20 ml if a 1–2% solution is used (10 –20 mg/ml). In dentistry, application anesthesia is also used in the form of gels, which help with teething in children, and also help relieve pain after oral surgery.

Conductor

It is performed along the nerve trunk with Lidocaine at a concentration of 20 mg / ml (2%) in a dose of up to 10 ml of solution, depending on the size of the nerve trunk and the place of its innervation. Unlike the infiltration method, the loss of pain sensitivity with conduction technique occurs after 10-15 minutes. Conduction technique is used when carrying out deeper and larger-scale operations on the limbs, the method is used in dentistry and maxillofacial surgery. A special type of conduction anesthesia is the introduction of Lidocaine under the conjunctiva of the eye.

Conduction anesthesia is often used in dentistry

To successfully perform local conduction anesthesia, the doctor needs to accurately select the localization of the injection, sometimes ultrasound or neurological testing is used for this purpose; in dentistry, the doctor can determine the right point for the injection during examination and palpation. Some methods of conduction anesthesia use the addition of a small dose of adrenaline, narcotic analgesics and hormones to enhance the effect.

Epidural and spinal

Epidural and spinal analgesia, in fact, are also conductive techniques, allowing you to block pain impulses at the level of nerve trunks emerging from the spinal cord. Performing spinal and epidural anesthesia allows for full-fledged surgical interventions on the limbs, in the lower abdominal cavity and small pelvis. The advantage of epidural anesthesia over anesthesia is that the effect on the brain in this case is minimal. Epidural and spinal analgesia is performed with anesthetics, the dose of narcotic analgesics is minimized, the patient is conscious, which avoids side effects and complications of anesthesia.

The epidural technique is also used for operations on the chest, in which case the technique of thoracic access is performed, which is more difficult than lumbar epidural analgesia, since the spinal cord passes in the thoracic spine, and there is a risk of damage, in the lumbar spinal cord there is no longer , there are only nerve fibers.

For epidural and spinal techniques, solutions of 10 and 20 mg / ml (1 - 2%) Lidocaine are used. The drug is administered at a dose of 1-2 ml per one segment of the spine, so for the blockade of pain sensitivity of the limbs or for epidural analgesia of childbirth, 2-4 ml of the solution is needed, but the dose of 10-15 ml of the drug can anesthetize the operation on the abdominal cavity.

The epidural technique is widely used in the world for postoperative pain relief, allowing you to relieve pain after surgery for a long time (up to 10 hours). In order to carry out epidural analgesia for several days, a spinal catheter is installed, through which the medicine enters the spinal canal by drip.

Other types of pain relief

With the help of Lidocaine, intraosseous, intraligamentous anesthesia is performed in traumatology and orthopedics; in dentistry, an intraseptal technique is used. For all species, working concentrations of 10–20 mg/ml are used.

The use of the drug in cardiology

Lidocaine is a powerful antiarrhythmic agent. In cardiology practice, the drug is used in a 10% concentration (100 mg / ml), administered diluted intramuscularly or intravenously by drip to stop arrhythmias.

Side effects of local anesthesia with Lidocaine

Adverse drug reactions are rare and usually mild. However, after local analgesia, neurological symptoms (tremor, nystagmus, dizziness, headache, convulsions, tinnitus, photophobia, anxiety) may occur. Being a powerful antiarrhythmic drug, Lidocaine can cause heart rhythm (bradycardia) and conduction disturbances (blockade).

Contraindications for local anesthesia

Severe disturbances of rhythm and conduction of the heart, severe heart failure and cardiogenic shock.
The presence of an infectious process at the site of the proposed anesthesia.
Blood clotting disorders.
Reduced blood pressure.

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:

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.
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.
Eye drops 2% are colorless and odorless, but sometimes they can be slightly colored. It is contained in 5 ml polyethylene bottles.
A gel is also available.
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 administration.

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

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:

Dineksan.
Lidocaine hydrochloride.
Luan.
Helikain.
Lidocaine-Vial.
Lidocaine Hydrochloride Brown.
Lidocaine Bufus.
Xylocaine.
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 Novocain - 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.