Detailed instructions for the use of lidocaine. Lidocaine 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 oral cavity, 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 mucous membranes or the presence of bedsores, the gel is thinly applied to the skin, gums and denture.

What is the medicine "Lidocaine" in ampoules? This is having wide range use. Being a strong local anesthetic, the drug is used for all types of local anesthesia- conductive, terminal, infiltration. It stabilizes cell membranes, which is why it is sometimes used as a remedy against arrhythmia.

For sprains, bruises and other injuries, the drug "Lidocaine" (injections) brings quick relief, because it is the most quick way effects on nerve endings. The drug is even used to relieve labor pain. The medicine "Lidocaine" for injection is used for various blockades in 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 tissues. Sometimes the components of the drug are observed allergic reactions.

Presence of dizziness, increased sweating, headache, ringing in the ears or drowsiness indicates an overdose of the drug. If such symptoms occur, you should stop using the drug.

Who is contraindicated for the medicine "Lidocaine" in ampoules? Pregnant and lactating women, children under ten years of age, weakened patients and people with hypersensitivity 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 Lidocaine used? It can be entered different ways- intravenously or intramuscularly. Solutions of different percentages are used as a local anesthetic, depending on the situation. Typically, no more than 50 ml of a 0.5-1 or 2 percent solution of the drug is used. A 1-2% solution is suitable for treating the mucous membrane, very rarely 5%, in a volume of no more than 20 ml. As a medicine, "Lidocaine" is administered intravenously in a stream in the first four minutes in a dosage of 50 to 100 ml, and then - by drip 2 mg per minute. No more than 1200 mg of solution can be administered per day.

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

But it must be remembered that such drugs cannot be used in case of arrhythmia and liver diseases. In general, Lidocaine is quite strong remedy, and therefore you should not use it without consulting a doctor, especially if you are already taking other medications. But upon reception vitamin complexes And food additives plant origin he poses no danger.

Lidocaine hydrochloride- local anesthetic drug intended for terminal, infiltration and conduction anesthesia.
At local application solution, the degree of absorption depends on the dose of lidocaine and the place of application (when applied to mucous membranes, absorption is higher than when applied to the skin). At intramuscular injection The maximum plasma concentration of lidocaine is observed 5-15 minutes after injection. Depending on the dose, about 60-80% of lidocaine is bound to plasma proteins.
Lidocaine penetrates the blood-brain and hematoplacental barrier.
Lidocaine hydrochloride is metabolized in the liver and excreted primarily in the form of metabolites by the kidneys. Some metabolites of lidocaine have pharmacological activity. The average half-life of lidocaine and its active components is 4-5 hours.

Indications for use

Solution Lidocaine 2% is used for local anesthesia in ophthalmological, dental, surgical and otolaryngological practices.
In addition, a 2% lidocaine solution can be used to block peripheral nerves and nerve plexuses in patients with pain.
Solution Lidocaine 10% is used for topical anesthesia of mucous membranes in various areas medicine (including gynecology, dentistry, gastroenterology, pulmonology, ENT practice) when conducting diagnostic procedures and surgical interventions.
A 10% solution of lidocaine hydrochloride is also used as an antiarrhythmic agent.

Mode of application

Before using lidocaine hydrochloride, you should skin test to identify possible hypersensitivity to the active component (in patients with hypersensitivity, when performing a skin test, the development of edema and hyperemia at the injection site is noted). When administering the solution intramuscularly, before starting to inject the drug into the muscle, the syringe plunger should be slightly pulled back to avoid accidental intravascular injection of lidocaine.
Lidocaine hydrochloride solution 2%:
The drug is intended for intramuscular, subcutaneous administration, as well as for conduction anesthesia, instillation into the conjunctival sac and treatment of mucous membranes. The method of use and dose of lidocaine hydrochloride is determined by the attending physician individually.
For local anesthesia, as a rule, subcutaneous, intramuscular or local (for mucous membranes) application of lidocaine solution is prescribed.
For conduction anesthesia, as a rule, 100-200 mg of lidocaine hydrochloride is prescribed.
For pain relief in the fingers, ear and nose, 40-60 mg of lidocaine hydrochloride is usually prescribed.
Maximum recommended daily dose lidocaine for adults (with regional anesthesia) is 200 mg.
At injection solution to increase the time of the therapeutic effect of lidocaine, the drug can be administered in combination with epinephrine (1: 50,000-1: 100,000) in the absence of contraindications to the use of epinephrine in patients.
In ophthalmic practice, 2 drops of lidocaine hydrochloride solution are usually prescribed into the conjunctival sac up to 3 times with an interval of 30-60 seconds. As a rule, 4-6 drops in one eye are enough for sufficient anesthesia during diagnostic procedures and surgical interventions.
For terminal anesthesia, the mucous membranes are lubricated with 2-20 ml of lidocaine hydrochloride solution. The duration of terminal anesthesia is 15-30 minutes.
The maximum daily dose of lidocaine hydrochloride solution for terminal anesthesia is 20 ml.
For children with any type of peripheral anesthesia, the total dose of lidocaine should not exceed 3 mg/kg body weight.
Lidocaine hydrochloride solution 10%:
The drug is intended for intramuscular administration, as well as for topical anesthesia. The method of use and dose of lidocaine hydrochloride is determined by the attending physician individually.
For topical anesthesia, the maximum recommended volume of a 10% lidocaine solution is 2 ml. If longer-term anesthesia is required, a lidocaine solution is used in combination with a 0.1% adrenaline hydrochloride solution (1 drop of adrenaline solution per 5-10 ml of lidocaine solution).
To relieve an attack of arrhythmia, the drug is administered intramuscularly at a dose of 200-400 mg. If necessary, the administration is repeated after 3 hours.
For arrhythmia, it is also possible to administer a 1% or 2% solution of lidocaine hydrochloride intravenously in a bolus at a dose of 50-100 mg, after which they switch to intramuscular administration of a 10% solution of lidocaine hydrochloride according to the standard regimen.
When using the drug Lidocaine hydrochloride 2% and Lidocaine hydrochloride 10%, it is recommended to monitor the ECG.
Solutions containing heavy metals should not be used to disinfect the injection site.
When using high doses of the drug, barbiturates are recommended before injection of lidocaine.

Side effects

Undesirable effects when using the solution Lidocaine are rare, but the development of such side effects cannot be excluded:
From the sense organs, central and peripheral nervous system: weakness, increased fatigue, headache, nystagmus, euphoria, drowsiness, photophobia, diplopia, hearing impairment, nightmares, numbness of the lips and tongue.

In addition, the development of limb tremors, convulsions, paresthesia, motor block, paralysis of the respiratory muscles and sensory disturbances is possible.
From the heart and blood vessels: disorders heart rate, decrease blood pressure, transverse heart block, cardiac conduction disturbances, pain in chest, peripheral vasodilation. In addition, mainly when using high doses of lidocaine, the development of collapse, heart block and cardiac arrest is possible.
From the outside respiratory system: dyspnea, apnea, shortness of breath.
Allergic reactions: itchy skin, allergic rhinitis or conjunctivitis, exfoliative dermatitis, Quincke's edema, urticaria, anaphylactic shock. Others: vomiting, nausea, pain at the injection site, decreased body temperature, feeling of heat and numbness of the extremities, chills.

Contraindications

:
Solution Lidocaine do not use for the treatment of patients with individual intolerance to the components of the drug, as well as other amide local anesthetic drugs (including a history of seizures that developed in response to the administration of lidocaine hydrochloride).
Lidocaine hydrochloride is contraindicated in patients suffering from atrioventricular block II and III degrees, heart failure II and III degrees, weakness syndrome sinus node, Wolff-Parkinson-White syndrome and Adams-Stokes syndrome.
It is not recommended to prescribe lidocaine to patients with severe bradycardia, arterial hypotension (systolic blood pressure less than 90 mmHg), cardiogenic shock and complete transverse heart block.
Do not use lidocaine hydrochloride solution for myasthenia gravis, porphyria, hypovolemia, as well as severe dysfunction of the liver and kidneys.
Pregnant and lactating women, as well as children under 12 years of age, the use of lidocaine hydrochloride is not recommended.
For patients suffering from glaucoma, lidocaine hydrochloride solution is not administered retrobulbarly.
It is recommended to be careful when prescribing lidocaine hydrochloride solution to patients with heart failure, incomplete atrioventricular block, epilepsy, arrhythmia (history).
Only after careful study of the risk/benefit ratio is lidocaine used for surgical interventions on the heart, and is also prescribed to patients with a genetic tendency to hyperthermia and elderly patients.
You should not drive a car or perform work that requires increased attention while using lidocaine hydrochloride solution.

Pregnancy

:
Lidocaine It is forbidden to prescribe to pregnant women. If it is impossible to avoid the use of lidocaine during lactation, the issue of temporary interruption should be resolved. breastfeeding. Breastfeeding can be resumed after consulting a doctor.

Interaction with other drugs

Lidocaine hydrochloride can be mixed in one syringe only with medicines, the description of which specifically states the possibility of mixing with lidocaine. If the drug is available in powder form, then the lidocaine solution cannot be used for initial dilution.
It is strictly forbidden to mix a solution of lidocaine hydrochloride with amphotericin, sulfathiazine and methohexitone (when mixing these solutions, lidocaine precipitates).
Lidocaine may be incompatible with ampicillin (depending on the pH of the solution).
Contraindicated parenteral administration lidocaine in patients receiving therapy with monoamine oxidase inhibitors. Lidocaine hydrochloride enhances the effect on the central nervous system, including the respiratory center, hypnotics and sedatives, as well as anesthetics, and also potentiates the effects of drugs that cause blockade of neuromuscular transmission. Ethyl alcohol enhances the severity of the effect of lidocaine on respiratory function. The dose of lidocaine hydrochloride should be adjusted when used in combination with beta-adrenergic blockers, chlorpromazine, propanolol, cimetidine, quinidine, amiodarone, verapamil, phenytoin, pethidine and disopyramide. It is recommended to carefully monitor respiratory function when using lidocaine in combination with polymyxin B. Lidocaine reduces the severity of the cardiotonic effect of cardiac glycosides, and with an overdose of cardiac glycosides increases the severity of atrioventricular block. Hallucinations may develop when simultaneous use procainamide and lidocaine hydrochloride. Caution should be exercised when combining lidocaine hydrochloride with curare-like drugs, mexiletine, norepinephrine, isadrine, midazolam, glucagon, barbiturates, anticonvulsants and antiarrhythmics. medicines, morphine, novocaine and novocainamide, as well as rifampicin, prenylamine, phenytoin and vasoconstrictor drugs. Such combinations may lead to changes in the pharmacokinetic parameters of lidocaine and increase the risk of developing undesirable effects.

Overdose

:
In case of overdose Lidocaine patients experience the development of symptoms of depression of the cardiovascular and central nervous systems, including general weakness, tonic-clonic convulsions, dizziness, loss of consciousness, tremors of the limbs, asphyxia, bradycardia, arterial hypotension. With a further increase in dose, loss of consciousness, atrioventricular block, collapse, respiratory arrest and coma may develop. In addition, excessive doses of lidocaine can cause a temporary decrease in visual acuity, the development of vomiting, psychomotor agitation and euphoria.
There is no specific antidote. If symptoms of overdose develop, stop the administration of lidocaine hydrochloride, place the patient on his back and ensure an influx of fresh air. In case of severe overdose, oxygen therapy is carried out, vasoconstrictor and anticonvulsant drugs, as well as anticholinergic drugs are prescribed.
Disorders of the central nervous system with an overdose of lidocaine are treated with barbiturates short acting or benzodiazepines.
In case of overdose during anesthesia, it is recommended to prescribe short-acting muscle relaxants. With the development of bradycardia and atrioventricular conduction disorders, patients are prescribed intravenous administration atropine in a dose of 0.5-1 mg.
In case of arterial hypotension, sympathomimetic agents in combination with beta-agonists are indicated.
In case of severe intoxication, resuscitation measures are carried out. Hemodialysis to reduce the plasma concentration of lidocaine in case of overdose is ineffective.

Storage conditions

Lidocaine hydrochloride injection solution 2% should be stored for 3 years in rooms with a temperature not exceeding 25 degrees Celsius.
Solution for injection Lidocaine hydrochloride 10% should be stored for 2 years in rooms with a temperature not exceeding 25 degrees Celsius.

Release form

Lidocaine hydrochloride solution 2%
Lidocaine hydrochloride solution 10% 2 ml in glass ampoules, 10 ampoules in a contour package, 1 contour package included in a cardboard box.

Compound

:
1ml solution for injection Lidocaine hydrochloride 2% contains:
Lidocaine hydrochloride in terms of dry matter - 20 mg; additional ingredients.

1ml solution for injection Lidocaine hydrochloride 10% contains:
Lidocaine hydrochloride in terms of dry matter - 100 mg; additional ingredients.

"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 in the maximum 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, rhythm and conduction disturbances heart disease, chest pain, respiratory muscle paralysis, 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.

Gross formula

C14H22N2O

Pharmacological group of the substance Lidocaine

Nosological classification (ICD-10)

CAS Code

137-58-6

Characteristics of the substance Lidocaine

White or almost white crystalline powder, poorly soluble in water. It is used in the form of hydrochloric acid salt, easily soluble in water.

Pharmacology

pharmachologic effect- local anesthetic, antiarrhythmic.

Antiarrhythmic activity is due to inhibition of phase 4 (diastolic depolarization) in Purkinje fibers, a decrease in automaticity, and suppression of ectopic foci of excitation. The rate of rapid depolarization (phase 0) is not affected or slightly reduced. Increases membrane permeability for potassium ions, accelerates the repolarization process and shortens the action potential. Does not change the excitability of the sinoatrial node, has little effect on the conductivity and contractility of the myocardium. When administered intravenously, it acts quickly and briefly (10-20 minutes).

The mechanism of the local anesthetic effect is to stabilize the neuronal membrane, reducing its permeability to sodium ions, which prevents the occurrence of action potentials and the conduction of impulses. Antagonism with calcium ions is possible. It hydrolyzes quickly in a slightly alkaline environment of tissues and, after a short latent period, acts for 60-90 minutes. With inflammation (tissue acidosis), anesthetic activity decreases. Effective for all types of local anesthesia. Dilates blood vessels. Does not irritate fabrics.

With intravenous administration, Cmax is created almost “on the needle” (after 45-90 s), with intramuscular injection - after 5-15 minutes. Absorbed quite quickly from the mucous membrane of the upper respiratory tract or oral cavity (Cmax is reached in 10-20 minutes). After oral administration, bioavailability is 15-35%, since 70% of the absorbed drug undergoes biotransformation during the “first pass” through the liver. In plasma, it is 50-80% protein bound. A stable concentration in the blood is established 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 mcg/ml. Easily passes through histohematic barriers, including the BBB. First it enters well-supplied tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. Penetrates through the placenta, 40-55% of the mother's concentration is found in the newborn's body. Excreted in breast milk. T1/2 after IV bolus administration is 1.5-2 hours (in newborns - 3 hours), with long-term IV infusions - up to 3 hours or more. If liver function is impaired, T1/2 may increase by 2 times or more. It is quickly and almost completely metabolized in the liver (less than 10% is excreted unchanged in the urine). The main degradation pathway is oxidative N-dealkylation, which produces active metabolites (monoethylglycine xylidine and glycine xylidine) with half-life of 2 hours and 10 hours, respectively. For chronic renal failure accumulation of metabolites is possible. Duration of action is 10-20 minutes with intravenous administration and 60-90 minutes with intramuscular administration.

When applied topically to intact skin (in the form of plates), a therapeutic effect occurs that is sufficient to relieve pain without developing a systemic effect.

Application of the substance Lidocaine

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

Contraindications

Hypersensitivity, history of epileptiform seizures to lidocaine, WPW syndrome, cardiogenic shock, sinus node weakness, heart block (AV, intraventricular, sinoatrial), serious illnesses liver, myasthenia.

Restrictions on use

Conditions accompanied by a decrease in hepatic blood flow (for example, chronic heart failure, liver diseases), progression cardiovascular failure(usually due to the development of heart block and shock), weakened patients, elderly age(over 65 years old), integrity violation skin(at the place where the plate is applied), pregnancy, breastfeeding.

Use during pregnancy and breastfeeding

During pregnancy and breastfeeding, it is possible if the expected effect of therapy exceeds the potential risk to the fetus and child.

Side effects of the substance Lidocaine

From the nervous system and sensory organs: depression or stimulation of the central nervous system, nervousness, euphoria, flashing of “floaters” before the eyes, photophobia, drowsiness, headache, dizziness, tinnitus, diplopia, impaired consciousness, depression or cessation of breathing, muscle twitching, tremor, disorientation, convulsions (risk of development increases against the background of hypercapnia and acidosis).

From the outside of cardio-vascular system and blood (hematopoiesis, hemostasis): sinus bradycardia, cardiac conduction disturbance, transverse heart block, decreased or increased blood pressure, collapse.

From the gastrointestinal tract: nausea, vomiting.

Allergic reactions: generalized exfoliative dermatitis, anaphylactic shock, angioedema, contact dermatitis(hyperemia at the application site, skin rash, urticaria, itching), a short-term burning sensation in the area of ​​action of the aerosol or at the site of application of the plate.

Others: feeling of heat, cold or numbness in the extremities, malignant hyperthermia, depression immune system.

Interaction

Beta blockers increase the likelihood of bradycardia and hypotension. Norepinephrine and beta-blockers, reducing hepatic blood flow, reduce (toxicity increases), isoprenaline and glucagon increase the clearance of lidocaine. Cimetidine increases plasma concentrations (displaces it from protein binding and slows down inactivation in the liver). Barbiturates, causing the induction of microsomal enzymes, stimulate the degradation of lidocaine and reduce its activity. Anticonvulsants (hydantoin derivatives) accelerate biotransformation in the liver (the concentration in the blood decreases); with intravenous administration, the cardiodepressive effect of lidocaine may be enhanced. Antiarrhythmics (amiodarone, verapamil, quinidine, ajmaline) potentiate cardiodepression. Combination with procainamide can cause central nervous system stimulation and hallucinations. Strengthens the inhibitory effect of anesthesia (hexobarbital, sodium thiopental) and sleeping pills on the respiratory center, weakens the cardiotonic effect of digitoxin, deepens muscle relaxation caused by curare-like drugs (paralysis of the respiratory muscles is possible). MAO inhibitors prolong local anesthesia.

Overdose

Symptoms: psychomotor agitation, dizziness, general weakness, decreased blood pressure, tremor, tonic-clonic convulsions, coma, collapse, possible AV blockade, central nervous system depression, respiratory arrest.

Treatment: cessation of use, pulmonary ventilation, oxygen therapy, anticonvulsants, vasoconstrictors (norepinephrine, mezaton), for bradycardia - anticholinergics (atropine). Intubation, mechanical ventilation, and resuscitation measures are possible. Dialysis is ineffective.

Routes of administration

IV, IM, locally (in the form of an aerosol, gel, spray, plate).

Precautions for the substance Lidocaine

Caution should be exercised in case of liver and kidney diseases, hypovolemia, severe heart failure with impaired contractility, genetic predisposition to malignant hyperthermia. In children, debilitated patients, and elderly patients, dose adjustment is necessary in accordance with age and physical status. When injecting into vascularized tissues, an aspiration test is recommended.

When applied topically, use with caution in case of infection or injury at the site of application.

If during use of the plate a burning sensation or redness of the skin occurs, it must be removed and not used until the redness disappears. Used plates should not be accessible to children or pets. The plate should be destroyed immediately after use.

special instructions

To prolong the action of the anesthetic, it is possible to add 1 drop of 0.1% adrenaline solution to 5-10 ml of lidocaine (with a maximum permissible dose increases to 500 mg).

Pharmacokinetics

When administered intramuscularly, the maximum concentration in the blood is achieved after 5-15 minutes. In plasma it binds to blood proteins by 33-80%. The degree of binding largely depends on the concentration of the drug and the content of alpha-1-acid glycoprotein in the blood plasma. Plasma protein binding is increased in uremic patients and recipients kidney transplant and increases after acute myocardial infarction, which is characterized by an increase in the level of alpha-1-acidglycoprotein. High protein binding may reduce the effect of free lidocaine or cause an overall increase in drug plasma concentrations. The therapeutic effect develops at a concentration of 1.5-5 mcg/ml. It is quickly distributed in tissues, the volume of distribution is 1 l/kg. First it enters tissues with a high rate of blood supply: heart, brain, kidneys, lungs, liver, spleen, then into adipose and muscle tissue. Easily penetrates histohematic barriers, including blood-brain and placental. In organism infant it turns out to be 40-55% of the concentration of the drug in the mother’s body. Metabolized in the liver with the participation of microsomal enzymes with the formation of metabolites: monoethylglycine exilidide and glycine exilidide. Metabolic rate is determined by hepatic blood flow and, as a result, may be impaired in patients following myocardial infarction and/or patients with congestive heart failure. It is excreted from the body by the kidneys in the form of metabolites (about 90%) and unchanged (10%). Excretion of unchanged drug in urine depends in part on urine pH. Acidic urine leads to an increase in the proportion excreted in urine. The half-life after intravenous bolus administration is 1.5-2 hours. The half-life of metabolites is 2 and 10 hours, respectively. If liver function is impaired, the half-life may increase.

Pharmacodynamics

Lidocaine is a local anesthetic. The local anesthetic effect is due to the stabilization of the neuronal membrane by reducing its permeability to sodium ions, which prevents the occurrence of an action potential and the conduction of nerve impulses. Antagonism with calcium ions is possible. Effective for all types of local anesthesia. It inhibits the conduction of not only pain impulses, but also impulses of other modalities. It quickly hydrolyzes in a slightly alkaline environment of tissues and, after a short latent period, acts for 1-1.5 hours. The anesthetic effect of lidocaine is 2-6 times stronger than procaine. With inflammation, anesthetic activity decreases. When applied topically, it dilates blood vessels and does not have a local irritating effect.

Indications for use

Local anesthesia (terminal, infiltration, conduction) in surgery, ophthalmology, dentistry, otolaryngology

Peripheral nerve blocks and nerve ganglia

Directions for use and doses

The drug is used by injection (subcutaneously, intramuscularly) and topically on the mucous membranes.

Intravascular administration of the drug should be avoided.

The administration of lidocaine involves a test to determine individual sensitivity to this drug.

For terminal anesthesia lubricate the mucous membrane of adults with the drug in a dose of up to 2 mg/kg lidocaine, the duration of anesthesia is 15-30 minutes.

Maximum dose for adults – 20 ml.

For conduction anesthesia(including for anesthesia of the brachial and sacral plexuses) administer 5-10 ml (100-200 mg of lidocaine) of the drug, for anesthesia of the fingers, nose, ears - 2-3 ml (40-60 mg). The maximum dose for adults is 10 ml (200 mg).

For anesthesia in ophthalmology Instill 2 drops of the drug into the conjunctival sac 2-3 times at intervals of 30-60 seconds immediately before the examination or surgery.

	Lidocaine
Interventions	Concentration
Infiltration ‒ Through the skin ‒ Intravenously	5 mg/ml (0.5%) or 10 mg/ml (1%)
	5 mg/ml (0.5%)
Peripheral nerve block ‒ Brachial plexus ‒ Dentistry ‒ Intercostal ‒ Paravertebral ‒ Genitourinary system	15 mg/ml (1.5%) 20 mg/ml (2%) 10 mg/ml (1%) 10 mg/ml (1%) 10 mg/ml (1%)
Paracervical ‒ Anesthesia in obstetrics	10 mg/ml (1%)
Sympathetic nerve blockade: ‒ Cervical ‒ Lumbarno	10 mg/ml (1%) 10 mg/ml (1%)
Blockade of the central nervous system: ‒ Epidural * ‒ Lumbarno: ‒ Pain relief ‒ Anesthesia * Dose depends on the number of dermatomes (skin areas) that need anesthesia (2-3 ml/dermatome)	10 mg/ml (1%) 10 mg/ml (1%) 15 mg/ml (1.5%) 20 mg/ml (2%)
Caudal anesthesia – Anesthesia in obstetrics – Anesthesia in surgery	10 mg/ml (1%) 15 mg/ml (1.5%)

Procedure for working with the ampoule.

1. Separate one ampoule from the block and shake it, holding it by the neck.

2. Squeeze the ampoule with your hand (this should not release the drug) and roll it up with rotational movements and separate the head.

3. Immediately connect the syringe to the ampoule through the resulting hole.

4. Turn the ampoule over and slowly draw its contents into the syringe.

5. Place the needle on the syringe.

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Side effects

Restlessness, drowsiness, dizziness, headache, sleep disturbance, confusion, loss of consciousness, even coma, sensory disturbance, muscle twitching, convulsions, motor block, dysarthria, dysphagia, persistent anesthesia, paresis or plegia lower limbs and loss of sphincter control (eg, cauda equina syndrome), skin tingling

Numbness of tongue and lips

Anorexia, irritability, restlessness, hallucinations, depression, agitation, euphoria

Visual impairment, nystagmus, reversible blindness, diplopia, floaters, photophobia, conjunctivitis

Vertigo, hearing impairment, noise or ringing in the ears, hyperacusis

When used in high doses– arrhythmia, bradycardia, cardiac conduction slowing, transverse heart block, cardiac arrest, peripheral vasodilation, collapse

Tachycardia, increase/decrease in blood pressure, pain in the heart, hot flashes

Nausea, vomiting

Dyspnea, rhinitis, depression or respiratory arrest

Allergic reactions: skin reactions, urticaria, itching, angioedema, hypersensitivity reactions, including anaphylactoid reactions (including anaphylactic shock), generalized exfoliative dermatitis

Suppression of the immune system

Feelings of heat, cold or numbness in the extremities, malignant hyperthermia, edema, weakness

Reactions at the injection site feeling of lightness burning sensation, disappearing with increasing anesthetic effect within 1 minute, thrombophlebitis, hyperemia

During spinal or epidural anesthesia, pain in the back, legs, partial/complete spinal block may be observed, accompanied by arterial hypotension, defecation disturbance, involuntary urination, impotence and loss of sensation in the perineal area (the likelihood of these effects increases when using higher doses or in case of accidental administration lidocaine into the spinal space when the dose intended for administration into the epidural space penetrates into the spinal space). In some cases, after such an intervention, restoration of motor, sensory and/or autonomic function occurs slowly (after several months) or incompletely.

Contraindications

– individual increased sensitivity to the components of the drug, as well as to other amide local anesthetic drugs

– a history of epileptoform seizures associated with the administration of lidocaine

– AV blockade II and III degrees, sick sinus syndrome, Wolff-Parkinson-White syndrome, Adam-Stokes syndrome, severe forms of heart failure (II-III degrees), severe arterial hypotension, bradycardia, cardiogenic shock

– myasthenia gravis

– hypovolemia

– porphyria

– severe renal and/or liver failure

– retrobulbar administration to patients with glaucoma

– the period in the first three months after myocardial infarction with reduced cardiac output of the left ventricle (less than 35% of normal)

– bleeding disorders, anticoagulant therapy

– infections at the injection site

– non-contact patients

– significant decrease in left ventricular function

– childhood up to 12 years

Drug interactions"type="checkbox">

Drug interactions

At combined use lidocaine with drugs such as chlorpromazine, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, notriptyline, the concentration of lidocaine in the blood plasma decreases.

Prescribe with caution in combination with:

Antiarrhythmic drugs (including amiodarone, verapamil, disopyramide , ajmaline) – the cardiodepressive effect is enhanced (the QT interval is prolonged and, in rare cases, AV block or ventricular fibrillation may develop); simultaneous use with amiodarone can lead to the development of seizures

Novocaine, novocainamide, procainamide - possible stimulation of the central nervous system, delirium, hallucinations

Curare-like drugs – enhances muscle relaxation (possible paralysis of respiratory muscles)

Ethanol – enhances the inhibitory effect of lidocaine on breathing

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) – help slow down the absorption of lidocaine and prolong the effect of the latter

Cimetidine - reduces the hepatic clearance of lidocaine (reduction due to inhibition of microsomal oxidation), increases its concentration and the risk of developing toxic effects. Also has a synergistic effect when interacting with lidocaine

Guanadrel, guanethidine, micamalamine, trimetaphan - when used in combination for spinal and epidural anesthesia, the risk of severe arterial hypotension and bradycardia increases

- β-adrenergic blockers (for example, propranolol, metopronol) – slow down the metabolism of lidocaine in the liver, enhance the effects of lidocaine (including toxic ones) and increase the risk of developing bradycardia and arterial hypotension. With the simultaneous use of beta-blockers and lidocaine, it is necessary to reduce the dose of the latter. Also, β-blockers have a synergistic effect when interacting with lidocaine; there is an inhibitory effect on cardiac conduction, which can lead to increased myocardial contractility

Cardiac glycosides – the cardiotonic effect of cardiac glycosides is weakened

Sleeping pills or sedative drugs – the inhibitory effect on the central nervous system of hypnotic and sedative drugs may be enhanced

Narcotic analgesics (morphine) - enhances the analgesic effect of narcotic analgesics, respiratory depression

MAO inhibitors (furazolidone, procarbazine, selegiline) increase the risk of developing arterial hypotension and prolong the local anesthetic effect of the latter. Lidocaine should not be used parenterally during treatment with MAO inhibitors.

Anticoagulants (including ardeparin, dalteparin, danaparoid, enotoxaparin, heparin, warfarin) - increase the risk of bleeding

Anesthesia - increases the inhibitory effect on the respiratory center (hexobarbital, sodium thiopental intravenously)

Polymyxin B – monitoring of respiratory function is necessary

Rifampicin – possible decrease in the concentration of the latter in the blood

Propafenone – possible increase in duration and severity of side effects from the central nervous system

Prenylamine – increases the risk of developing ventricular arrhythmia such as “pirouette”

Anticonvulsants, barbiturates (phenobarbital) - possible acceleration of the metabolism of lidocaine in the liver, decreased concentration in the blood, increased cardiodepressive effect

Isadrin, glucagon - increases the clearance of lidocaine

Norepinephrine, mexiletine – the clearance of lidocaine decreases (toxicity increases); hepatic blood flow decreases

Acetazolamide, thiazide and loop diuretics - reduce the effect of lidocaine as a result of hypokalemia

Midazolam – increases the concentration of lidocaine in the blood plasma

Drugs that block neuromuscular transmission - the effect of these drugs is enhanced because they reduce the conduction of nerve impulses

Norepinephrine – has a synergistic effect when interacting with lidocaine

With acidosis, the concentration of free lidocaine in the blood plasma increases and there is a risk of developing toxic effects.

When lidocaine interacts with other antiarrhythmic drugs, for example, calcium antagonists, an inhibitory effect on cardiac conduction occurs, which can lead to increased myocardial contractility.

Drugs that affect hepatic metabolism and microsomal enzyme induction (eg, phenytoin) may reduce the effectiveness of lidocaine.

With simultaneous use of muscle relaxants (for example, suxamethonium), there may be a synergistic effect.

Use with caution with diazepam.

For all types of injection anesthesia, it is possible to combine lidocaine with epinephrine (1: 50,000-1: 100,000; prepare ex tempore, add 1 drop of 0.1% epinephrine solution to 5-10 ml of lidocaine solution), except for cases where there is a systemic effect, which has epinephrine (adrenaline), undesirable – hypersensitivity to epinephrine, arterial hypertension, diabetes, glaucoma or a short-term anesthetic effect is required. Epinephrine helps slow down the absorption of lidocaine and prolongs its action.

It is not advisable to mix the drug with other drugs.

Lidocaine precipitates when mixed with amphotericin, methohexitone or sulfadiazine. Depending on the pH of the solution, lidocaine may be incompatible with ampicillin.

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special instructions

Before using lidocaine, it is necessary to conduct a skin test for individual sensitivity to the drug, which is indicated by swelling and redness of the injection site.

Lidocaine should only be administered by medical professionals.

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. Personnel performing anesthesia must be qualified and trained in anesthesia techniques and must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions and other complications.

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

When using lidocaine, ECG monitoring is mandatory. In case of disturbances in the activity of the sinus node, lengthening P-Q interval, QRS widening or if a new arrhythmia develops, the dose should be reduced or the drug discontinued.

Before using lidocaine for heart disease (hypokalemia reduces the effectiveness of lidocaine), it is necessary to normalize the level of potassium in the blood.

Before administering lidocaine in high doses, barbiturates are recommended. When performing planned subarachnoid anesthesia, it is necessary to discontinue MAO inhibitors no later than 10 days before anesthesia.

Care should be taken to avoid accidental intravasal application (especially when administering local anesthesia to areas containing a lot of blood vessels) or subdural administration of the drug. It is necessary to establish strict control over the system toxic effect the drug on the cardiovascular and central nervous systems (since the doses intended for epidural anesthesia are always higher than for subdural); when injecting into vascularized tissues, an aspiration test is recommended.

Extreme caution should be used when administering anesthesia around the spinal region in patients with neurological diseases, spinal deformity, septicemia and severe arterial hypertension.

Smaller doses of the drug should be administered to the head and neck region, including retrobulbar and dental administration, as well as use for blockade of the stellate ganglion, since the systemic toxic effects of the drug through retrograde flow can enter the cerebral circulation.

Extreme caution should be used during retrobulbar administration, as possible side effects: collapse, shortness of breath, convulsions, reversible blindness.

Since lidocaine has a pronounced antiarrhythmic effect and can itself act as an arrhythmogenic factor that can cause the development of arrhythmia, before administering the drug it is necessary to collect an anamnesis and use the drug with caution to persons with complaints of arrhythmias in the past.

Use with caution and in smaller doses in patients with moderate heart failure, moderate arterial hypotension, incomplete AV block, impaired intraventricular conduction, moderate liver and kidney dysfunction (creatinine clearance less than 10 ml/min), impaired respiratory function, epilepsy , after heart surgery, with a genetic predisposition to malignant hyperthermia, debilitated and elderly patients.

Intramuscular administration of lidocaine may increase the concentration of creatinine, which may lead to an error in diagnosing acute myocardial infarction.

With local anesthesia of tissues with pronounced vascularization (for example, the neck in case of surgery on thyroid gland) special care should be taken to avoid the drug entering the blood vessels.

The safety of using amide anesthetics is questionable in patients prone to malignant hyperthermia, so their use in such cases should be avoided.

Particular caution should be exercised when using lidocaine in patients with circulatory insufficiency, hypovolemia, arterial hypotension, hepatic and renal insufficiency.

Use with caution in patients with central nervous system disorders who are using narcotics, as sudden cardiac side effects may occur. With long-term use, it is necessary to monitor the level of electrolytes in the blood. Use with caution in patients with a tendency to convulsions, in a state of shock, or hypoxia.

Use during pregnancy and lactation

The drug crosses the placental barrier and can cause fetal bradycardia, so it is not recommended for use during pregnancy. If it is necessary to use the drug, breastfeeding should be discontinued.

Features of the influence on the ability to manage vehicle or potentially dangerous mechanisms

The drug affects the function of the central nervous system, therefore, after using lidocaine, it is not recommended to drive vehicles or operate other mechanisms.

Overdose

Possible increased adverse reactions.

Symptoms: psychomotor agitation, dizziness, general weakness, decreased blood pressure, tremor, blurred vision, tonic-clonic seizures, coma, collapse, AV block, asphyxia, apnea, depression, drowsiness, anxiety, ringing in the ears. With a significant overdose, impaired consciousness, respiratory depression, shock, and myocardial infarction are possible. The first symptoms of overdose in healthy volunteers occur when the concentration of lidocaine in the blood is more than 0.006 mg/kg; convulsions – at 0.01 mg/kg.

Treatment: cessation of drug administration, oxygen therapy, vasoconstrictors (norepinephrine, mezaton), anticonvulsants, anticholinergics.

The patient must be in horizontal position; it is necessary to ensure access to fresh air, oxygen supply and/or artificial respiration. Symptoms from the central nervous system are corrected by the use of benzodiazepines or short-acting barbiturates. If overdose occurs during anesthesia, a short-acting muscle relaxant should be used. To correct bradycardia and conduction disturbances, use atropine (0.5-1 mg intravenously); for arterial hypotension, use sympathomimetics in combination with β-adrenergic receptor agonists.

In case of cardiac arrest, immediate resuscitation measures are indicated. In the acute phase of lidocaine overdose, dialysis is ineffective. There is no specific antidote.

Conditions for dispensing from pharmacies

On prescription

Manufacturer

LLC "NIKO", Ukraine, 86123, Donetsk region, Makeevka, st. Tayozhnaya, 1-1