Lidocaine - side effects, dosage and overdose

As Life reported, a ten-year-old girl died in Omsk. According to investigators, the child suffered a severe allergic reaction after being injected with lidocaine. According to investigators, during treatment, doctors were not convinced that the little patient tolerated lidocaine normally, which led to the tragedy.

This is far from the only case. As Life reported, in December in Moscow, a 36-year-old woman died after being injected with lidocaine.

Pharmacological properties

The antiarrhythmic activity of the drug is due to the inhibition of phase 4 (diastolic depolarization) in Purkinje fibers, a decrease in automaticity, and suppression of ectopic foci of excitation.
In this case, lidocaine suppresses the electrical activity of depolarized, arrhythmogenic areas, but has minimal effect on the electrical conductivity of normal tissues. The speed of rapid depolarization (phase 0) is not affected or reduced slightly. Increases membrane permeability for potassium ions, accelerates the process of repolarization of cell membranes, shortens the duration of the action potential and the effective refractory period. When used in average therapeutic doses, it practically does not change myocardial contractility, does not slow down AV conduction, and does not significantly reduce blood pressure. When used as an antiarrhythmic drug with intravenous administration, the effect develops after 45-90 s, lasts 10-20 minutes, with intramuscular administration the effect develops after 5-15 minutes, lasts 60-90 minutes. It has local anesthetic activity due to the stabilization of the neuronal membrane, reducing its permeability to sodium ions, which prevents the occurrence of action potentials and the conduction of impulses.

Pharmacokinetics. With intravenous administration, the maximum concentration is achieved after 45 - 90 s, with intramuscular administration - after 5 - 15 minutes. Plasma protein binding - 60 - 80% (depending on dose). A stable concentration in the blood is established after 3-4 hours with continuous administration (in patients with acute myocardial infarction - after 8-10 hours). Easily passes through histohematic barriers, including the blood-brain barrier. First it enters tissues with a good blood supply (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. Penetrates through the placenta, 40 - 55% of the concentration of the drug used by the mother appears in the newborn's body. The average therapeutic concentration in the blood is 0.0035 mg/ml.

Metabolized 90% in the liver by oxidative N-dealkylation to form active metabolites: monoethylglycine xylidine and glycine xylidine, which have a half-life of 2 hours and 10 hours, respectively. It has a “first pass” effect. The half-life after bolus administration is 1.5 - 2 hours (in newborns - 3 hours), with long-term intravenous infusions up to 3 hours or more. If liver function is impaired, the half-life may increase by more than 2 times. 5-20% is excreted unchanged in the urine.

Pharmacological action and indications for use

The pharmacological action of lidocaine is local anesthetic. This substance suppresses sodium channels, preventing the conduction of impulses along the axons - not only pain, but also others, completely blocking the sensitivity of the anesthetized area. In addition, this drug dilates blood vessels in the area of ​​application.

Indications for the use of this substance in dental practice include:

  • anesthesia of the mucous membranes before tooth extraction;
  • suturing the mucous membrane;
  • various orthodontic interventions;
  • removal of tartar;
  • removal of superficial benign neoplasms;
  • opening of superficial abscesses;
  • anesthesia of the gums before fixing bridges;
  • excision of an enlarged dental papilla;
  • suppression of the pharyngeal reflex before taking a plaster cast.

Lidocaine in the form of a spray is used for skin anesthesia when removing minor tumors, such as nevi (birthmarks). In cardiology, lidocaine is also used as an antiarrhythmic agent for ventricular tachycardia and extrasystole.

Lidocaine is considered a fairly safe anesthetic. The likelihood of side effects when using it is lower than that of other anesthetics of the same group (novocaine, prilocaine).

Pharmacological properties

The analgesic effect of Lidocaine is not the only option for its use in medicine. Very often the drug is used as an antiarrhythmic agent during manipulations with patients suffering from cardiovascular diseases.

The popularity of Lidocaine is understandable, because it retains its effect for about one hour and fifteen minutes. Therefore, other popular means for local anesthesia cannot compete with it. It is known that when lidocaine and epinephrine are used together, the duration of action increases to two hours.

It is noteworthy that the active component of the drug is absorbed better and faster on the mucous membranes. If you use the product on other tissues, its penetration into the body will depend primarily on the dosage.

Lidocaine injections are given intramuscularly. In this case, it begins to act within fifteen minutes, approximately during the same time interval the maximum concentration of the active substance in the patient’s tissues is reached.

pharmachologic effect

Lidocaine is a local remedy. An anti-arrhythmic effect is added to the analgesic effect. It is better in every sense than Novocaine. Compared to other painkillers, they are associated with a small percentage of allergic reactions. The effectiveness of lidocaine is 70-95%.

Lidocaine is used together with vasoconstrictors in the form of a 1-2% solution. It works quite quickly. The maximum concentration of the drug is achieved within 5-10 minutes.

How does lidocaine work? It blocks nerve conduction due to damage to nerve endings and fibers. The anesthetic drug dilates blood vessels well and does not irritate the tissue. As a result, the medicine is smoothly and evenly distributed throughout the vessels of the body.

In what cases is the use of the drug indicated?

The drug is indicated for use in the following types of anesthesia:

  1. Infiltration. One of the most widely used analgesic techniques. This method in medicine is called freezing, and is used mainly in dental treatment.
  2. Terminal. It allows you to eliminate the sensation of pain only temporarily, which is achieved by blocking pain receptors.
  3. Conductor. Based on this anesthesia, nerve transmission to a specific area is blocked. This is the area in which surgical intervention is planned.
  4. Spinal. The anesthetic is applied to the subarachnoid space, thereby blocking impulses by the roots of the spinal centers.
  5. Epidural. Inserted into the epidural space of the spine.

Let us consider in more detail which indications favor the use of the drug by intravenous and intramuscular routes.

  1. Carrying out various types of anesthesia that were mentioned above.
  2. With the development of ventricular arrhythmias that occur against the background of glycoside intoxication.
  3. For preventive purposes, as well as to relieve the occurrence of recurrent ventricular fibrillation in patients with coronary syndrome.

Lidocaine is actively used in dentistry, as well as during operations in the oral cavity. The following indications are available for this:

  1. Removal of baby teeth in children.
  2. When removing bones and suturing wounds in the mouth.
  3. To perform autopsies of emerging abscesses.
  4. For gum pain relief, which is necessary when installing dentures or crowns.
  5. When removing a papilla on the tongue.
  6. When opening cysts of the salivary glands, as well as during frenulectomy in children.

Lidocaine is popular in ENT practice, as it is prescribed for the following indications:

  1. When performing procedures such as resection of nasal polyps, septectomies, as well as electrocoagulation.
  2. Before performing the procedure for opening a peritonsillar abscess.
  3. During the puncture procedure of the maxillary sinuses.
  4. For analgesic effect before rinsing the nose.
  5. When performing tonsillectomy, as well as adenectomy.

Lidocaine is used during examinations, as well as before endoscopic diagnostics:

  • Anesthesia of the oral cavity when there is a need to pass a probe through the nose or mouth.
  • When performing a rectoscopy procedure, as well as in case of need to replace catheters.

Lidocaine has gained popularity in gynecology, obstetrics, ophthalmology and dermatology. Every doctor of any specialty should know not only about the presence of such a drug as Lidocaine, but also about its features.

Dosage and overdose

In dental practice, lidocaine is used for infiltration anesthesia in concentrations:

  • 0,125%
  • 0,25%
  • 0,5%.

If other types of anesthesia are necessary, use a 1–2% solution.

One spray dose (released by pressing the valve once) contains 4.6 mg of active substance.

In dental practice, one or two presses are enough to achieve an anesthetic effect; in dental surgery, higher doses may be required, and the number of presses may be up to four.

The maximum dosage of lidocaine is 400 mg, or 40 doses when using a spray.

In case of overdose, the following phenomena are observed:

  • dizziness;
  • nausea;
  • euphoria;
  • asthenia;
  • lowering blood pressure;
  • bradycardia;
  • headache;
  • breathing problems;
  • convulsions.

Severe intoxication can lead to cardiac paralysis, respiratory arrest, and coma.

In case of intoxication, after stopping the administration of the drug, it is necessary to place the patient in a horizontal position and restore respiratory functions: relieve single spasms with intravenous injections of 5-15 mg of diazepam, if necessary, use pulmonary ventilation and oxygen inhalation. For bradycardia, m-anticholinergic blockers are used, in particular atropine (0.5-1 mg). Hemodialysis for intoxication is ineffective.

Solution 10 Lidocaine in ampoules

The drug is administered intramuscularly and used in the form of applications. The permissible volume for the latter type of procedure is 2 milliliters. To prevent an attack of arrhythmia, an intramuscular injection of Lidocaine is performed - 200-400 milligrams.

If the problem is not resolved, then three hours later they give a second injection. During an arrhythmic attack, you can administer either a one-percent or two-percent solution intravenously in a bolus - 50-100 milligrams, after which, according to the annotation, Lidocaine is administered intramuscularly.

Using Lidocaine injection solution 2 and 10%, it is necessary to monitor the electrocardiogram, and you should also refrain from disinfecting the injection site with solutions containing heavy metals. When using the drug in high concentrations, barbiturates are used before the procedure.

The spray is used only locally. The medication is sprayed from a short distance, usually to the area that requires anesthesia, avoiding its penetration into the visual organs and respiratory tract.

When irrigating the mouth, due to decreased sensitivity, special care must be taken to avoid damaging the tongue with the teeth.

In dentistry and dermatology, one or two ampoules of a 10% solution are used. In otolaryngology, as well as craniofacial surgery - from one to four doses of 10% Lidocaine. To carry out an endoscopic examination, two or three ampoules are used; in gynecology, up to five doses are used.

When treating large areas of the skin, you can use a swab moistened with Lidocaine from a can. Thus, it is necessary to use a spray when administering anesthesia to children (the permitted dosage is 3 milligrams per kilogram of weight).

Signs of overdose

In case of an overdose of Lidocaine, victims experience symptoms of depression of the central nervous and cardiovascular systems. Characteristic is the progressive development of intoxication, a gradual increase in the severity of the process:

  • tingling and “crawling” around the mouth;
  • increased sweating;
  • pale skin;
  • chills;
  • drowsiness or, conversely, psychomotor agitation, a state of agitation;
  • numbness of the tongue;
  • dizziness, headache;
  • painful sensitivity to sounds and tinnitus;
  • visual impairment (inability to focus, double vision);
  • tremor, muscle twitching, sometimes turning into generalized convulsive seizures lasting from several seconds to several minutes;
  • episodes of spontaneous respiratory arrest;
  • decreased blood pressure, decreased heart rate;
  • heart rhythm disturbances, in severe cases – cardiac arrest.

Source: depositphotos.com

The risk of overdose increases with intravenous administration of the drug.

An acute overdose of lidocaine during spinal and epidural anesthesia during childbirth can lead to depression of the fetal heart rate, severe hypotension and depression of the respiratory center, including respiratory arrest.

The US Food and Drug Administration (FDA) issued a Safety Announcement on June 26, 2019, providing information that gel containing 2% lidocaine, previously recommended as a teething analgesic in infants, is dangerous because its use has caused a number of hospitalizations and deaths.

Side effects

When using the medicine, the following side effects described in the instructions may occur:

  • allergic, anaphylactoid reactions, sensitivity disorders;
  • dizziness, tremor, drowsiness, convulsions, nervousness, coma, respiratory failure, hallucinations;
  • pain in the lower back, legs or buttocks, intestinal dysfunction, paralysis of the lower limbs, tachycardia;
  • blurred vision, diplopia, amaurosis, inflammation of the eye, ringing in the ears;
  • hypotension, bradycardia, myocardial depression, arrhythmia, cardiac arrest;
  • nausea, vomiting, shortness of breath, bronchospasm, respiratory arrest;
  • rash, angioedema, urticaria, facial swelling.

Side effects of Lidocaine

The nervous and cardiovascular systems react most acutely to the effects of the drug.

Side effects related to the functions of the nervous system and sensory organs:

  • stimulation (less often - depression) of the central nervous system;
  • euphoria;
  • nervousness;
  • neurotic reactions;
  • dizziness;
  • headache;
  • drowsiness;
  • myasthenia gravis;
  • confusion;
  • decreased visual acuity, double vision;
  • photophobia;
  • nystagmus (rhythmic twitching of the eyeball);
  • tremor.

The cardiovascular system is characterized by the following reactions:

  • decreased (less commonly, hypertension) blood pressure;
  • cardiac conduction dysfunction;
  • arrhythmia;
  • bradycardia.

Sometimes reactions from the digestive system in the form of nausea and vomiting may occur.

When performing injection anesthesia, you may experience a feeling of heat or cold with an objective decrease in body temperature.

Very rarely, when using the drug, allergic reactions develop: redness, itching, hyperemia in the area of ​​its administration, swelling, anaphylaxis.

Side effects are usually observed when the drug is injected too quickly; their occurrence when using an aerosol is unlikely.

Interaction with other drugs

Lidocaine enhances the inhibitory effect on the respiratory center of anesthetics (hexobarbital, sodium thiopental intravenously), hypnotics and sedatives; weakens the cardiotonic effect of digitoxin. When used simultaneously with hypnotics and sedatives, the inhibitory effect on the central nervous system may be enhanced.

Ethanol enhances the inhibitory effect of lidocaine on respiratory function. Prescribe with caution in combination with:

  • -adrenoreceptors (including propranolol, nadolol) - the metabolism of lidocaine in the liver slows down, the effects of lidocaine increase (including toxic ones) and the risk of developing bradycardia and hypotension increases; curare-like drugs - possible deepening of muscle relaxation (up to paralysis of the respiratory muscles);
  • norepinephrine, mexiletine - the toxicity of lidocaine increases (the clearance of lidocaine decreases); isadrine and glucagon - the clearance of lidocaine increases;
  • cimetidine, midazolam - the plasma concentration of lidocaine increases. Cimetidine displaces lidocaine from binding to proteins and slows down the inactivation of lidocaine in the liver, which leads to an increased risk of increased side effects of lidocaine. Midazolam moderately increases the concentration of lidocaine in the blood;
  • anticonvulsants, barbiturates (including phenobarbital) - possible acceleration of lidocaine metabolism in the liver, decreased concentration in the blood, and as a result - a decrease in its therapeutic effectiveness;
  • antiarrhythmic drugs (amiodarone, verapamil, quinidine, ajmaline, disopyramide), anticonvulsants (hydantoin derivatives) - the cardiodepressive effect is enhanced; simultaneous use with amiodarone may lead to the development of seizures;
  • novocaine, novocainamide - possible stimulation of the central nervous system and the occurrence of hallucinations;
  • MAO inhibitors, aminazine, bupivacaine, amitriptyline, nortriptyline, imipramine - the local anesthetic effect of lidocaine is prolonged;
  • morphine - the analgesic effect of morphine is enhanced;
  • prenylamine - increases the risk of developing ventricular arrhythmias; propafenone - possible increase in duration and severity of side effects from the central nervous system;
  • rifampicin - a decrease in the concentration of lidocaine in the blood is possible;
  • with simultaneous infusion of lidocaine and phenytoin, side effects of central origin may be increased (cardiodepressive effects, inhibition of atrioventricular conduction). In patients using phenytoin as an anticonvulsant, a decrease in the concentration of lidocaine in the blood plasma is possible (due to the induction of lidocaine metabolism in the liver by phenytoin);
  • polymyxin B - respiratory function should be monitored.

Interaction with other drugs

Before you start taking the drug, you must inform your doctor about the medications you are currently using. It is necessary to remember about the interaction of drugs with each other, for example, Lidocaine:

  • When taken simultaneously with Cimetidine, the risk of toxic effects increases.
  • Muscle relaxation increases when taken with curare-like drugs.
  • When taken with Methoxamine and Epinephrine, the anesthetic effect of Lidocaine is enhanced.
  • The drug reduces the effects of antimyasthenic drugs.
  • Concomitant use with Procainamide may cause hallucinations.
  • It is necessary to monitor the patient's respiratory function if prescribed simultaneously with Polymyxin B.
  • If the patient uses Cimetidine and Lidocaine is administered intravenously, drowsiness, bradycardia, and hearing impairment may occur.

How to inject lidocaine

The instructions for use of the drug warn that before injecting lidocaine, you need to conduct a tolerance test. To do this, a small amount of solution is injected under the skin in the forearm area. The result is assessed after 15 minutes. If redness and swelling appear, the drug should not be used.

A two percent lidocaine solution is used for conduction anesthesia, treatment of mucous membranes and instillation into the conjunctival area. Administered intramuscularly and subcutaneously. This dosage is also used in dental practice.

There are maximum permissible doses for medical procedures, which are not recommended to be exceeded:

  1. Conduction anesthesia - 100-200 mg.
  2. Anesthesia of the phalanges of the fingers, ears, nose - 40, 60 mg.
  3. Ophthalmic practice is to instill 2 drops into the eye every minute. It is allowed to use no more than 6 drops. This amount is sufficient for short-term surgical interventions and diagnostic procedures.
  4. Terminal anesthesia - use lidocaine solution for injection 20 mg ml (2%) in an amount of 20 ml.

If necessary, lidocaine is combined with epinephrine to enhance the analgesic effect. But this is only possible if there are no contraindications.

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A 10% solution of lidocaine is intended for intramuscular administration and in the form of applications.

  1. Relief of an attack of arrhythmia - 200-400 mg intramuscularly. If necessary, re-administration of the product used is possible no earlier than after 3 hours.
  2. For applications use 2 ml of the drug. If lidocaine is used in ampoules for external use, then a tolerance test is still carried out. To do this, a small amount of the drug is applied to the skin of the forearm and the result is expected within 10-15 minutes.

Intramuscular administration of 2% and 10% lidocaine solution is recommended under ECG monitoring. If it is necessary to use large doses of the drug, then take drugs from the barbiturate group first. If everything is done correctly, the risk of side effects will be lower.

The drug is also used as a solvent for injectable antibiotics, which must be diluted with 2% lidocaine.

A doctor gives a prescription for diluting antibiotics.

If lidocaine solution is prescribed to children, the amount of the drug administered should not exceed a dose of 3 mg per 1 kg of weight. First of all, a tolerance test is carried out. The use of antibiotics for children should be under medical supervision. Sometimes, even with a negative test for lidocaine, an allergic reaction can develop. Therefore, injections for children are carried out in the manipulation room of the clinic.

What happens if you inject the drug into a vein?

Lidocaine is administered intravenously only as an emergency aid to relieve an acute attack of arrhythmia. This method is used in the case of diagnosing an increase in heart rate, when other treatment methods are ineffective.

In surgical practice, the injection of a 2% lidocaine solution into a vein is allowed to prevent postoperative pain syndrome. This helps reduce the dosage of opioid analgesics. It has been proven that if an anesthetic is administered before surgery, in the period after the operation there is an improvement in intestinal motility.

Is it possible to drink

Lidocaine injections are not intended for oral administration. This is a local anesthetic and not a pain reliever.

Ingestion of the drug can cause numbness of the tongue and throat. There is also a risk of developing respiratory paralysis.

Usually a strong reaction occurs to a companion drug

According to a member of the American Association of Anesthesiologists (ASA), an anesthesiologist at the Central Military Clinical Hospital No. 3 named after A.A. Vishnevsky Alexander Rabukhin, an allergy usually occurs not to lidocaine itself, but to a companion medicine. As the specialist says, lidocaine is usually administered with some other drug.

“The body can give an allergic reaction if lidocaine is administered with an antibiotic or adrenaline,” he said. — The classic option is when the antibiotic is diluted with lidocaine and injected into a vein. Sensitization occurs (the body acquires a specific increased sensitivity to foreign substances - allergens). When the drug is repeatedly administered with this antibiotic, a person develops anaphylactic shock. And for there to be a reaction to lidocaine - I have never seen this in 35 years. A side effect that can occur from lidocaine is an overdose.

Contraindications

The drug is prohibited for use in patients with acute and chronic heart failure
. Most contraindications relate to the injection form of the drug. It is prohibited to use for the following diagnoses:

  • Bradycardia,
  • Sinoatrial blockade,
  • Sick sinus syndrome,
  • AV block of the second and third degree,
  • WPW syndrome,
  • Myasthenia gravis,
  • Cardiogenic shock
  • Acute and chronic heart failure,
  • Very low blood pressure,
  • Adams-Stokes syndrome,
  • Violation of intraventricular conduction,
  • Retrobulbar administration.

The medication should not be used during pregnancy and lactation, as well as in case of individual intolerance

Injections are used with caution in case of sinus bradycardia, high blood pressure and hypovolemia. Relative contraindications also include:

  • Kidney and liver failure,
  • Decreased hepatic blood flow
  • First degree AV block,
  • Epileptiform seizures.

Lidocaine is not recommended for use by persons under eighteen years of age or the elderly. Before use, it is necessary to consider the possibility of contraindications to specific types of anesthesia. Lidocaine aerosol cannot be used in dentistry as an impression material because there is a risk of aspiration. The spray can be used during pregnancy, but the doctor must limit the dosage.

Lidocaine hydrochloride solution 1% 3.5 ml No. 5

Instructions for medical use of the drug
Lidocaine hydrochloride Trade name
Lidocaine hydrochloride

International nonproprietary name

Lidocaine

Dosage form

Solution for injection 1% 3.5 ml

Compound

One ampoule contains
the active substance
- lidocaine hydrochloride (in terms of 100% substance) 35 mg,
excipients:
0.1 M sodium hydroxide solution, water for injection.

Description

Transparent, colorless or slightly colored liquid.

Pharmacotherapeutic group

Drugs for the treatment of diseases of the nervous system. Local anesthetics. Amides. Lidocaine Code ATX N01BB02

Pharmacological properties
Pharmacokinetics
After intramuscular administration, absorption is almost complete.
Distribution is rapid, the volume of distribution is about 1 l/kg (lower in patients with heart failure). Protein binding depends on the concentration of the active substance in plasma and is 60-80%. Metabolized mainly in the liver with the formation of active metabolites, which can contribute to the manifestation of therapeutic and toxic effects, especially after infusion for 24 hours or more. The half-life of the drug tends to be biphasic with a distribution phase of 7-9 minutes. In general, the half-life of the drug depends on the dose, is 1-2 hours and can increase to 3 hours or more during long-term intravenous infusions (more than 24 hours). Excreted by the kidneys in the form of metabolites, 10% unchanged. Pharmacodynamics
Acetanilide derivative. Antiarrhythmic, local anesthetic. Causes all types of local anesthesia: terminal, infiltration, conduction. Stabilizes cell membranes, blocks sodium channels. In the myocardium, it suppresses the automaticity of ectopic foci, mainly in the ventricles; practically does not inhibit the conductivity and contractility of the myocardium. Promotes the release of potassium ions from myocardial cells and accelerates the process of repolarization of cell membranes, shortens the duration of the action potential and the effective refractory period.

Indications for use

- conduction anesthesia - spinal anesthesia - epidural anesthesia - for lubrication of mucous membranes: (for tracheal intubation, bronchoesophagoscopy, removal of polyps, punctures of the maxillary sinus) - as a solvent for cephalosporin antibiotics

Directions for use and doses

The drug is intended for intramuscular, subcutaneous administration, as well as for conduction anesthesia 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 local anesthesia,
the usual dose is from 5 ml to 10 ml of a 1% lidocaine solution.
To anesthetize the brachial and sacral plexus,
5-10 ml of a 1% solution is injected.
To numb the fingers and toes,
use 2 ml to 3 ml of a 1% solution. The maximum dose of a 1% lidocaine solution is 10 ml; this dose cannot be re-administered within 24 hours. With local anesthesia, the drug should be administered into highly vascularized tissues with caution to avoid it entering the bloodstream. For children receiving any type of peripheral anesthesia, the total dose of lidocaine should not exceed 3 mg/kg body weight. As a solvent for cephalosporin antibiotics: for intramuscular injection, no more than 1 g of antibiotic (Cef III) is dissolved in 3.5 ml of a 1% lidocaine solution and injected deep into the gluteal muscle. A solution containing lidocaine and a cephalosporin antibiotic (Cef III) cannot be administered intravenously.

Side effects

- depression or excitement of the central nervous system - nervousness, euphoria, anxiety - general weakness, drowsiness - headache, dizziness, tinnitus - diplopia, nystagmus - photophobia - convulsions (the risk of development increases against the background of hypercapnia and acidosis) - tremor, facial trismus muscles, paresthesia - disorientation, confusion or loss of consciousness - depression or cessation of breathing - decrease or increase in blood pressure - cardiac conduction disturbance, arrhythmia, sinus bradycardia, peripheral vasodilation, collapse - chest pain - cardiac arrest - nausea, vomiting - involuntary urination - generalized exfoliative dermatitis - angioedema, anaphylactic shock - contact dermatitis (hyperemia at the site of application, skin rash, urticaria, itching)
Others
- sensation of “hot”, “cold” or numbness of the extremities - persistent anesthesia - erectile dysfunction - malignant hyperthermia - methemoglobinemia - flickering of “floaters” before the eyes and tachycardia when administered simultaneously with a vasoconstrictor

Contraindications

- hypersensitivity (including to other amide local anesthetic drugs) - infection of the intended injection site - sick sinus syndrome, bradycardia - acute and chronic heart failure - atrioventricular block II-III degree (except when an artificial pacemaker is installed), sinoauricular blockade - Wolff-Parkinson-White syndrome, cardiogenic shock, intraventricular conduction disorders - angle-closure glaucoma (with retrobulbar administration) - liver dysfunction - arterial hypotension - myasthenia gravis - epileptiform convulsions - pregnancy and lactation - children under 12 years of age It is also necessary to take into account general contraindications to this or that type of anesthesia. If you have one of the listed diseases, be sure to consult your doctor before taking the drug. When using 1% lidocaine solution as a solvent, intravenous administration is contraindicated

Drug interactions

With the simultaneous use of lidocaine and beta-blockers, the toxic effects of lidocaine may be enhanced. It is irrational to prescribe lidocaine together with ajmaline, amiodarone, verapamil or quinidine due to increased cardiodepressive effects. The combined use of lidocaine and procainamide can cause stimulation of the central nervous system and hallucinations. With intravenous administration of hexenal or thiopental sodium against the background of the action of lidocaine, respiratory depression is possible. The combined use of lidocaine and definin should be used with caution, as 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, the local anesthetic effect of lidocaine is likely to be enhanced. Patients taking monoamine oxidase inhibitors should not be prescribed parenteral lidocaine. With the simultaneous administration of lidocaine and polymykisin B, under the influence of the latter, it is possible to increase the inhibitory effect on neuromuscular transmission, used as an antiarrhythmic agent, therefore in this case it is necessary to monitor the patient’s respiratory function. When lidocaine is used in combination with hypnotics or sedatives, the inhibitory effect on the central nervous system may be enhanced. Under the influence of cimetidine, intravenous administration of lidocaine causes undesirable effects (stunning, drowsiness, bradycardia, etc.). If combination therapy is necessary, the dose of lidocaine should be reduced. Chlorpromazine, cimetidine, propranolol, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline increase the concentration of lidocaine in the blood serum. An increase in serum lidocaine levels can also occur with antiviral drugs (for example, amprenavir, atazanavir, darunavir, lopinavir). Alcohol enhances the inhibitory effect of lidocaine on the respiratory center.

special instructions

Use with caution in case of heart failure stage II-III, severe liver and/or renal failure, hypovolemia, AV blockade stage I-II, sinus bradycardia, arterial hypotension, myasthenia gravis, epileptiform seizures (including in history), genetic predisposition to malignant hyperthermia, acute diseases, debilitated patients, and the elderly.
Lidocaine should be administered carefully into highly vascularized tissues to avoid intravasal exposure of the drug; in such cases, smaller doses of lidocaine are indicated. Caution should be used when administering local anesthesia to organs rich in blood vessels; Intravascular injection should be avoided during administration. With dilution, toxicity decreases. When injecting into vascularized tissues, an aspiration test is recommended. Prophylactic administration to 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 of asystole). If lidocaine is ineffective, it is necessary first to exclude hypokalemia; in emergency situations, there are several options for further action: carefully increasing the dose until side effects from the central nervous system appear (lethargy, difficulty speaking); prescription, sometimes combined, of class IA drugs (procainamide), transition to class III drugs (amiodarone, bretylium tosylate). It is prohibited to administer retrobulbar lidocaine solutions to patients with glaucoma. Features of the effect of the drug on the ability to drive a vehicle or potentially dangerous mechanisms
During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Overdose
Symptoms:
the first signs of intoxication are dizziness, nausea, vomiting, euphoria, convulsions of facial muscles with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, general weakness, apnea, bradycardia, decreased blood pressure, collapse, methemoglobinemia.
Treatment:
the patient should be in a horizontal position; Oxygen inhalation is prescribed and diazepam 10 mg is administered. In cases of skeletal muscle spasms, the latter are relieved by slow intravenous administration of a 1% solution of hexobarbital or sodium thiopental. For bradycardia - M-anticholinergics (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is ineffective.

Release form and packaging

3.5 ml in ampoules with a capacity of 5 ml made of neutral glass or sterile ampoules for syringe filling. 5 ampoules are packed in a contoured cell packaging made of polyvinyl chloride film and aluminum foil. A label made of label or writing paper is glued onto each ampoule, or the text is applied directly to the ampoule using intaglio printing ink for glass products. 2 contour blister packs, together with approved instructions for medical use in the state and Russian languages, are placed in a pack of cardboard boxes. It is allowed that contour blister packs (without being placed in a pack of cardboard) together with approved instructions for medical use in the state and Russian languages ​​are placed in cardboard boxes.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 30 °C. Keep out of the reach of children!

Shelf life

3 years After the expiration date, do not use the drug.

Conditions for dispensing from pharmacies

On prescription

, Republic of Kazakhstan, Shymkent, Al-Farabi district, st. Sh. Rashidova, No. 81, t/f: 560882

Registration Certificate Holder

JSC "Khimpharm", Republic of Kazakhstan

Address of the organization that accepts claims from consumers regarding the quality of products (products) on the territory of the Republic of Kazakhstan

JSC "Khimpharm", Shymkent, REPUBLIC OF KAZAKHSTAN, Al-Farabi district, st. Sh. Rashidova, No. 81, t/f: 560882 Phone number 7252 (561342) Fax number 7252 (561342) Email address

Release form

Lidocaine anesthetizes very effectively, and therefore the manufacturer has provided different forms of release. This is done so that it can be conveniently used in different areas of medicine and in situations where pain relief is required.

The most common is Lidocaine for injection. It is produced in ampoules, each of which contains one milliliter of active substance. In addition to it, the drug also includes auxiliary components, so the manufacturer sells the medicine in a two-milliliter solution. Twenty ampoules are included in a cardboard package. Each has a break point at the top and a green ring, which is a kind of quality sign.

"Lidocaine" in ampoules is a colorless, odorless liquid. Pharmacists note that the solution should be clear, but in some cases slight turbidity is allowed.

Lidocaine spray can be found on sale in pharmacies. It is very often used in dentistry, when it is necessary to quickly numb some areas of the oral cavity. The aerosol packaging indicates that the bottle contains a ten percent solution of the drug. One dose contains almost five milligrams of the active substance; in addition, the spray consists of a number of auxiliary components, which we will talk about a little later. Most often, the aerosol goes on sale in a dark glass bottle.

For some problems, patients are advised to use ointment with lidocaine. It is available in two and five percent versions. A tube of ointment can have a volume of fifteen, twenty-five and thirty grams. The composition includes almost two grams of the active substance and four additional components.

When is medical attention required?

Medical attention is required in 100% of cases of lidocaine overdose, as cardiac arrest and death are possible.

Of particular concern when using Lidocaine are:

  • the appearance of neurological symptoms (loss of orientation in time and place, lethargy or excessive agitation, convulsions, etc.);
  • change in heart rhythm, sudden decrease in blood pressure;
  • state of depressed consciousness, the patient’s inaccessibility to contact;
  • severe cyanosis of the skin and mucous membranes;
  • breathing disorders.

After providing emergency care, if necessary, the victim is hospitalized in a specialized department of the hospital, where he receives special treatment:

  • intubation, artificial ventilation and oxygen therapy in case of coma and respiratory depression;
  • intravenous administration of electrolyte solutions (sodium chloride, Lactasol, polarizing mixture) or plasma substitutes (Reomacrodex, Reopoliglyukin, Poliglyukin);
  • anticonvulsants – intravenous Diazepam, sodium thiopental;
  • for bradycardia - m-anticholinergic blockers (Atropine), vasoconstrictors (norepinephrine, phenylephrine).

basic information

This drug is a local anesthetic that also has antiarrhythmic properties. The essence of its work is to locally block nerve signals. The drug is used to completely relieve pain or reduce pain (discomfort) in a certain area of ​​the body, for example, during operations, punctures or insertion of a catheter. The use of lidocaine hydrochloride solution is sometimes found in cardiology when it is necessary to stop a heart attack.

Epidural anesthesia using this substance is often performed during labor to relieve pain in women in labor. The drug is often used to dilute antibiotics produced in the form of a dry substrate, for example, Ceftriaxone. This method of administration has not been used in world medicine for a long time, but in the post-Soviet space it is still quite common.

Precautions and side effects

Before administering lidocaine solution, the patient must inform the doctor about serious illnesses that he has suffered or currently has, as well as previous cases of allergic reactions to drugs, dyes or other substances

An approximate list of conditions in which the drug should be administered with caution:

  • heart blocks such as atrioventricular and others;
  • heart rhythm disturbances, such as Stokes-Adams or Wolff-Parkinson-White syndrome;
  • allergic reactions to corn;
  • liver and kidney diseases;
  • cardiac pathologies (if Lidocaine is not used to treat them);
  • circulatory disorders and pathologies of the coronary arteries;
  • hyperthermia (malignant form).

Obviously, if the patient has an allergic reaction to other anesthetics, it leads to the selection of another method of pain relief. Since the effect of Lidocaine on the fetus has not been studied, its use for pregnant women (except for childbirth) is undesirable. The main side effects of the drug may be:

  • convulsions, tremors;
  • dizziness, drowsiness;
  • slowing heart rate;
  • weak or shallow breathing;
  • sudden feeling of heat and muscle stiffness;
  • cyanosis of the skin;
  • anxiety, inexplicable feeling of fear, impaired consciousness;
  • tinnitus;
  • decreased visual acuity, diplopia;
  • allergic reactions up to anaphylactic shock.

Interaction with other substances

The simultaneous use of Lidocaine with Anaprilin increases the risk of developing side effects of Lidocaine, and barbiturates and rifampicin can reduce the effectiveness of the anesthetic. Cardiodepression is provoked by a combination with antiarrhythmics, and a cocktail with procainamide can cause hallucinations. Bradycardia will become more severe in situations where the patient is taking beta blockers.

Intravenous administration of lidocaine solution, coupled with sleeping pills or anesthesia, enhances muscle relaxation up to paralysis of the respiratory muscles. Substances such as vasoconstrictors prolong the local effect of the anesthetic. The risk of bleeding increases when combined with anticoagulants.

Dosage regimens

For intravenous administration, use ampoules with a 10% solution of Lidocaine, diluted in 0.9% saline so that the concentration of the substance is 20 mg/ml. This composition is administered dropwise under ECG control and is used in cardiological practice for the treatment of ventricular arrhythmias that occur during cardiac manipulation (cardiac surgery), as well as as intensive therapy for acute myocardial infarction. The maximum daily dose for an adult should not exceed 2 thousand mg of the substance.

Infiltration anesthesia is carried out with a 0.5%, 0.25% and 0.125% solution, and a 1 or 2% concentration of Lidocaine is used to anesthetize peripheral nerves. For epidural analgesia, 200-300 mg of 1% anesthetic is used, in obstetric practice - 2%, in surgery - 1.5%. The specific doses of the substance, as well as the actual concentrations and volumes that are used, directly depend on the type and extent of surgery, the duration of the procedure and the condition of the patient.

Interaction with other drugs

Sometimes it is necessary to use Lidocaine in parallel with other drugs. Some drugs complement each other, but others significantly reduce the effectiveness of pain relief. For example, the use of Novocainamide and Lidocaine simultaneously increases the risk of side effects from the central nervous system.

Beta blockers, together with local anesthesia, lead to arrhythmia and a decrease in blood pressure. The toxicity of the drug may also increase, which leads to a worsening of the patient’s condition.

If you take diuretics, then the dosage of Lidocaine must be increased, since the effectiveness of the drug in this case is significantly reduced. Viral agents, on the contrary, increase the concentration of the anesthetic and enhance its effect several times.

Doctors mention that the simultaneous use of Lidocaine and other drugs for local anesthesia is not indicated for most patients. Medicines for the same purpose can increase each other's toxicity and cause side effects.

Experts try not to use Lidocaine with the following medications:

  • "Propanorm";
  • "Cimetidine";
  • "Ranitidine".

Because of them, it is quite difficult to calculate the required dosage of the anesthetic, since not only its toxicity increases, but also its concentration in the blood.

Patients regularly taking medications for epilepsy should inform their doctor about this. In their total mass, they reduce the effect of Lidocaine, which may force the specialist to increase its dose. In turn, this will lead to a possible overdose and undesirable consequences.

You should not use this remedy in cases where you take sedatives. It is also prohibited to mix the anesthetic with any other medications. This rule should be taken extremely seriously and not violated.

Lidocaine in carpules

Modern anesthetics are switching to carpules, but ampoules are a thing of the past.
Carpools are easy to use. The carpule already includes the required dose of anesthetic and is inserted into the carpule syringe, a needle is inserted and an injection is given. An injection with such a needle is more painless for the patient.

In addition to Lidocaine, anesthetic carpules may contain additional drugs and additives, such as adrenaline and epinephrine. Lidocaine in combination with such additives will be washed out of the mouth more slowly.

The average volume of one carpule is 1.7 ml. An example of anesthesia with Lidocaine in carpules can be a drug such as Xylonor, which is produced in France.

Thus, modern medicine is switching to a completely new type of packaging - carpules, which is very convenient for the doctor and also helps the patient endure the injection less painfully, thanks to a thinner needle.

Lidocaine spray

This is a 10% metered spray that is used for local anesthesia.
The can contains 38 grams of Lidocaine. One bottle is enough for 650 doses. In addition to being easy to use, the spray also tastes good and also contains excipients. It begins to work 60 seconds after spraying and lasts for five minutes.

The spray can also be used by children under two years of age. In dentistry, Lidocaine spray anesthetizes the oral mucosa and reduces the gag reflex. It is not difficult to purchase it at any pharmacy; you just need to take a prescription from your doctor with you. However, most often, sellers in pharmacies do not require it.

Lidocaine in dentistry

Lidocaine is used less and less in dentistry, because there are more popular and effective pain relievers. Of course, lidocaine is not used in dental practice as an antiarrhythmic agent, however, this property of the drug should not be ignored or forgotten!

Instructions for the use of lidocaine in dentistry do not have any special features. All important points will be discussed in this article below. Most often, a dentist uses lidocaine in ampoules or carpules, less often - gel and spray.

  • Lidocaine gel is used for topical anesthesia. It is simply impossible to find the drug in its pure form. The most famous gel with lidocaine - Kamistad - is a combination of an anesthetic with a tincture of chamomile. Naturally, the composition also includes other components, such as formic acid, benzalkonium chloride and ethyl alcohol. Kamistad has an anesthetic and anti-inflammatory effect due to the presence of chamomile. Used by the dentist for inflammatory diseases of the oral cavity (gingivitis, stomatitis, cheilitis, etc.) for short-term relief of pain symptoms. Apply with massaging movements to the entire area that needs to be numbed. Available in pharmacies without a prescription.

Kamistad gel with lidocaine

  • Lidocaine spray can be used in children under 2 years of age. Indications for the use of this drug are: temporary elimination of the gag reflex, for treatment/removal of teeth, anesthesia of the oral mucosa for the treatment of inflammatory diseases, elimination of pain during conduction anesthesia. The analgesic effect occurs in approximately 30-60 seconds and lasts 15 minutes. A single exposure of the spray contains 4.8 mg of lidocaine. Sold without a prescription.

Spray 10% lidocaine

  • Lidocaine in 2% ampoules, 2 ml . Most often used in “budget” dentistry. For conduction anesthesia, a 2% solution is used, but 1% in a higher dosage can be used. For infiltration anesthesia, weaker solutions are suitable: 0.125%, 0.25%, 0.5% Administered with a regular disposable syringe. The effect of anesthesia depends on the anesthesia technique and the patient’s condition; on average, the analgesic effect lasts 40-60 minutes.

Lidocaine in ampoules

On many sites you can find information that lidocaine is less toxic than novocaine - this is a myth! At the lowest concentrations 0.125%, 0.25%, 0.5% will be equal in toxicity to novocaine! At higher concentrations it is 40-50% more toxic than novocaine! At the same time, lidocaine hydrochloride is 2-3 times stronger than a novocaine solution, 3 times longer in action and acts 2 times faster.

Lidocaine in carpules for dentistry . Modern form of release of an anesthetic. It is worth paying attention to the fact that it will simply be impossible to find “pure” lidocaine in carpules in a pharmacy, since it is sold under other names.

Synonyms of lidocaine: Lidestin, Lidocard, Lidocaton, Leostesin, Lignocaine, Nulicain, Octocaine, Remicaine, Xylocetin, Xylocaine, Xylocard, Xylonor, etc.

A carpule is a glass cartridge from which an anesthetic is injected using a special device - a carpule syringe.

Carpule syringe

The advantage of anesthesia using a carpule syringe is not that the carpule is disposable, but that the needle on the carpule syringe is only 0.3 mm in diameter, in the usual 2 ml. syringe needle diameter 0.6 mm. The carpule needle is more flexible and 2 times thinner, which allows you to give an injection with minimal discomfort and completely painless!

Needles for carpule syringe

An analogue of lidocaine in carpules, which can be found in a pharmacy, is called Xylocaine, a 2% solution with a vasoconstrictor - adrenaline (epinephrine), a drug that is added to the anesthetic to constrict blood vessels and prolong its action.

Lidocaine in carpules – Xylocaine 2%

Directions for use and dosage

Doctors often use Lidocaine in practice - the instructions for use of the drug include information on the dosage depending on the form of release, and on methods of use. For example, gel and ointment with Lidocaine are used externally, the solution can be administered parenterally (intravenously and into muscles), the spray is used to treat mucous membranes, and drops are used only for ophthalmic purposes.

Lidocaine for injection

According to the instructions, Lidocaine in ampoules is used for intramuscular injections. The maximum dose for adults is 300 mg of the drug; for children and the elderly this dose is reduced. A single dosage for adults and adolescents over 12 years of age is considered to be 5 mg/kg. Before administration, the solution can be diluted with physiological 0.9% sodium chloride solution. The maximum dose for children 1-12 years old is considered to be no more than 5 mcg per body weight of a 1% lidocaine solution.

Lidocaine intravenously

Lidocaine 2 percent, which is administered intravenously, is used as an antiarrhythmic agent. The loading dose for adults is 1-2 mg/kg body weight over 3-4 minutes. The average single dosage is 80 mg. After this, patients are transferred to a drip infusion of 20-55 mcg/kg/minute, which lasts for 24-36 hours.

10 minutes after the first loading dose, intravenous bolus administration at a dose of 40 mg can be repeated. Children receiving a loading dose of 1 mg/kg may be given a repeat dose after five minutes. Continuous intravenous infusion has parameters of 20-30 mcg/kg/minute. In surgery, dentistry, ENT and obstetric practice, the dosage is set by the doctor.

Gel for external use

According to the instructions, Lidocaine gel is an external agent that is applied to the surface of the skin 3-4 times a day. It can be used to lubricate the mucous membranes of the esophagus, larynx, trachea, and treat the oral cavity with a cotton swab or swab, applying 0.2-2 g of gel. If anesthesia is not enough, it is repeated after 2-3 minutes. The maximum dose for adults is 300 mg (6 g of gel) per 12 hours, for women in urology - 3-5 ml, for men - 100-200 mg (5-10 ml), before cystoscopy - 600 mg (30 ml) in two doses .

Children are prescribed up to 4.5 mg/kg body weight. In urology in men, the gel is used to wash the opening of the external urethra. To do this, the contents of the tube are injected inside and the canal is clamped for several minutes. With catheterization, the numbing effect is achieved immediately. To relieve pain due to cystitis, 10 g of gel is administered once a day for a course of 5-7 days. In dentistry, the gel is used for anesthesia when removing tartar - rubbed into the gingival margin for 2-3 minutes. The product can be used under a bandage or applied in the form of applications to areas of erosion.

Eye drops

According to the instructions, the use of eye drops with Lidocaine should be local. They are instilled by installation into the conjunctival sac immediately before conducting studies on the cornea or conjunctiva, or before surgical interventions on them. The number of drops is 1-2, they are applied 2-3 times with an interval between each administration of 30-60 seconds.

Spray

A local external spray is used in the same way, the dosage of which depends on the area to be anesthetized. One dose of the product contains 4.8 mg of active substance. According to the instructions, use 1-2 sprays, in obstetric practice - up to 15-20. The maximum dose of the spray is 40 sprays per 70 kg of body weight. It is allowed to soak a cotton swab with the drug and apply anesthesia with it - this is done for children to eliminate the fear of spraying and eliminate the side effect of tingling.

Instructions for use

Using lidocaine topically allows you to dilate blood vessels without causing irritation. Using the drug on the entire skin relieves pain, but does not lead to the development of a systemic effect. When administered intravenously, the effect can be observed within a few minutes, as rapid absorption by organs and tissues occurs.

Lidocaine is metabolized almost completely in the liver, therefore, in the presence of diseases of this organ, the intensity of metabolism decreases. The drug is excreted from the body through urine and bile. The drug is available in various dosage forms.

Method and dosage of injections

The solution is often prescribed for infiltration anesthesia. Based on 5 mg/ml, but the permissible dose should not exceed 400 mg. If the solution is used to block the nerve plexuses, then it is administered in an amount of 10-20 ml with a concentration of 10 mg/ml. If a more concentrated solution is used, the dosage is reduced.

For epidural anesthesia, take 10-20 mg/ml, and for spinal anesthesia, 3-4 ml of a 2% solution. Since Lidocaine does not have a long effect time, a 0.1% solution of Adrenaline is often added to prolong it. It is administered intravenously only after dilution with 100 mg/ml saline solution. To do this, 25 ml of solution is diluted in 100 ml of saline and administered to the patient. The initial dosage should be 1 mg per kilogram of body weight. The rate of administration should be controlled and is 25-50 mg per minute.

The intravenous infusion can last from 12 to 24 hours, but it is necessary to constantly monitor the work of the heart, that is, do an ECG. It must be remembered that according to the instructions, the drug can be taken only after an allergic reaction to it has been ruled out. If there is even the slightest suspicion of an allergy, then anesthesia using the product is prohibited.

Spray method and dosage

The instructions note that the spray is intended for spraying on mucous membranes. The dosage will depend on how large an area will be treated. With a single spray, approximately 4.8 mg of active substance is released. But the dose must be taken that will give the desired analgesic effect. This usually happens after 2-3 sprays.

The largest dosages are usually used in gynecology and obstetrics, when the dose can be up to 40 sprays depending on the weight of the patient. Please note that the bottle must be held vertically during use.

Method and dosage of eye drops

Most often, the use of the drug in the form of eye drops is justified before surgery in the eye area. To do this, before the operation, 2 drops of a 2% solution are instilled into the conjunctival sac 2-3 times.

Lidocaine for children

As a rule, they try to carefully prescribe the medicine to children under 18 years of age. This is taking into account the fact that the drug has a slow metabolism and the active substance can accumulate in the child’s body. For children under 2 years of age, if there is an urgent need to use this product, take the product as an application with a cotton swab rather than spraying it.

Doctors generally do not use this medication for local anesthesia in children before undergoing tonsillectomy or adenoid removal. The dosage of the drug when used in children should be calculated based on the fact that the amount of the drug should not exceed 3 mg per kilogram of the baby’s weight.

special instructions

According to the instructions, when using the drug, you must exercise some caution and adhere to the following recommendations:

  • If a spray is used, do not allow it to come into contact with the eyes or respiratory system.
  • Apply with extreme caution to the back of the throat.
  • If Lidocaine solution is used for injection into an area with strong vascularity, for example, in the neck, then the dosage must be reduced.
  • While using the drug, you must be extremely careful when driving.
  • You should always consult your doctor before using the drug.

How to give an antibiotic injection with lidocaine

Cephalosporins are currently one of the most effective antibiotics used in the treatment of various infectious and inflammatory diseases. The most popular representative of cephalosporin antibiotics is Ceftriaxone. As a rule, doctors prescribe 1 g of Ceftriaxone twice a day for adults. How to properly dilute the antibiotic Lidocaine?

The solution must be prepared immediately before the injection. It is not worth preparing the solution for future use, because it has a very short shelf life. To prepare the solution, use 1 g of Ceftriaxone and 3.5 ml of 1% lidocaine solution. It’s worth noting right away that Lidocaine is available in ampoules of 2 ml, that is, you will have to take two ampoules of Lidocaine - this will result in a total of 4 ml of anesthetic. So, you need to draw 4 ml of Lidocaine into a syringe and insert the contents of the syringe into a bottle with 1 g of Ceftriaxone. Next, you need to take a bottle of solution and vigorously shake until the powder is completely dissolved.

It is worth noting that it is not always possible to purchase exactly 1% lidocaine solution in pharmacies. In this case, to prepare 4 ml of 1% lidocaine solution, you can mix 2 ml of 2% lidocaine with 2 ml of water for injection.

note

Ceftriaxone prepared with lidocaine is administered only intramuscularly. For intravenous injections, water for injection is used as a solvent.

Valeria Grigorova, doctor, medical columnist

9, total, today

Indications for the use of lidocaine

  • Anesthesia of the oral mucosa during stomatitis . Local administration (ointment, solution or gel). Adults and children: apply a solution or ointment (2-5%) or 15 ml of viscous lidocaine (2%) to the mucous membranes every 3-4 hours.
  • Anesthesia for laryngoscopic, bronchoscopic and endotracheal intubation . Adults: spray 4% lidocaine 1.5 ml into the throat. (40-200 mg or 0.6-3 mg/kg).
  • Preventing toothache . Lidocaine is used as a local anesthetic for short-term operations in the oral cavity, for example: tooth extraction. To achieve an analgesic effect during conduction anesthesia on the upper or lower jaw, it is enough to use a 2% lidocaine solution in a dose of 4 ml. On average, the analgesic effect lasts 30-40 minutes.
  • Treatment of neuropathic pain associated with postherpetic neuralgia . For adults, an intravenous dose of 5 mcg/kg/day is suggested.
  • Transtracheal anesthesia. Adults: 2-3 ml of sterile 4% lidocaine solution is administered quickly transtracheally during inspiration. You should use a needle that is large enough to give the injection quickly. When performing an injection during inhalation, part of the dose reaches the bronchi, a provoked cough will contribute to the distribution of the drug along the vocal cords and epiglottis. Occasionally, pharyngeal atomization with an oropharyngeal spray may be necessary to achieve complete analgesia. For the combination of injection and aerosol, total doses greater than 5 mL (200 mg or 3 mg/kg) are rarely necessary.
  • For ophthalmic anesthesia. Adults: For retrobulbar injection, the dose is 3.5 ml (120 to 200 mg or 1.7 to 3 mg/kg) 4% lidocaine. Part of this dose is given retrobularly, and the rest can be used to block the facial nerve.

The dose depends on many factors, such as the depth of anesthesia, the extent of the surgical procedure, the degree of muscle relaxation required, the duration of anesthesia and the physical condition of the patients.

special instructions

First of all, it must be said that the administration of the drug should be carried out by doctors who have experience working with resuscitation equipment

Manipulation requires special care and practice

The medicine is prescribed with extreme caution to patients diagnosed with heart failure, bradycardia and other heart rhythm disorders. In addition, the drug is not indicated for people who have epileptic seizures.

Patients taking antiarrhythmic drugs should be closely monitored by a physician. They are constantly monitored and ECG monitoring is organized.

The drug can change the activity of creatine phosphokinase, which can “blur” the picture of acute myocardial infarction.

Prescribing Lidocaine to patients with porphyria should be avoided in order to avoid progression of the pathology, since such a pattern was present in clinical studies on rodents.

In old age

The drug can be used in elderly people. However, all manipulations must be carried out under the strict supervision of medical personnel in conjunction with monitoring data from the cardiovascular system.

During pregnancy and lactation

When performing anesthesia in pregnant women, it is necessary to carefully monitor the heart rate of the fetus, since the administration of lidocaine can provoke a slowdown in the child’s heart rate.

Lidocaine should not be administered to newborns due to the risk of bradycardia and sinus arrhythmias.

In pediatrics

The instructions for use contain a warning about caution in using the drug for children. The harm/benefit indicator is assessed before prescribing

The drug is contraindicated for children under one year of age.

Effect on reaction

The body's response to medication may vary. It all depends on the patient’s chronic diseases and his age. It has been clinically proven that the incidence of adverse reactions is higher in patients over 50 years of age and under 3 years of age. Doctors have noted that Lidocaine in the form of an injection solution at a dosage of 20 mg/ml is more likely to cause adverse reactions than the same drug, but at a lower dose.

Interaction with other drugs

A lidocaine injection can reduce the activity of antiretroviral drugs, so combination with drugs such as Atazanavir, Lopinavir and others is not recommended.

The use of loop diuretics in combination with lidocaine reduces the effect of the latter.

Do not combine a 10% solution of Lidocaine with amide-type compounds. Due to the similarity in their structure, systemic toxic reactions may occur.

Ranitidine is able to increase the percentage of lidocaine in the liquid part of the blood.

The combination of antiarrhythmic drugs with lidocaine is not recommended, since there are no clinical studies proving their compatibility.

In patients receiving antipsychotic therapy, lidocaine increases the risk of mitral valve problems.

Injection lidocaine reduces the seizure response rate for opioid analgesics. The combination of the drug with opioids lowers the conduction limit of nerve cells and can lead to the development of seizures.

Ethyl alcohol reduces the effect of local anesthetics.

The drug is not compatible with nitrates, barbiturates and macrocyclic antibiotics.

Antibiotics should be diluted with Lidocaine with extreme caution, as drug incompatibility is possible.

Pain management and childbirth

Since adequate controlled studies have not been conducted in pregnant women, it is recommended to avoid the use of drugs containing lidocaine as much as possible in the first trimester of pregnancy (when organogenesis occurs). It should be noted that local anesthetics penetrate into the blood quite quickly when used in epidural or caudal anesthesia and can be toxic to the fetus and mother.

The degree of toxicity of Lidocaine will depend on the type of procedure, method and site of administration of the drug. As a rule, side effects in the mother and newborn are associated with changes in the functioning of the central nervous system, cardiac function and peripheral vascular tone.

Spinal and paracervical anesthesia can affect labor by changing the contractility of the uterus or weakening the woman's pushing efforts. The use of obstetric analgesia may increase the second stage of labor and lead to the use of forceps. In the first two days of life, children born with the use of local anesthesia by the mother may experience a decrease in tone and muscle strength.

Long-term follow-up has not been carried out, but it is clear that during paracervical anesthesia, the fetal heart rate must be strictly monitored, and the physician must weigh the risks and benefits of pain management for each individual woman, based on her condition and medical history. It is worth noting that it is not entirely clear whether lidocaine passes into breast milk, but since almost all drugs that the mother uses are found in milk, it is better to avoid the use of this drug during breastfeeding due to its specific effect on the conduction of nerve impulses.

Lidocaine gel

A well-known gel containing lidocaine is Kamistad.
In addition to the lidocaine base, it contains chamomile extract. It is used specifically for the oral cavity and does not cause irritation. There are professional gels for dental clinics, the rest can be purchased at any pharmacy kiosk. An analogue of such a gel is Cholisal. It relieves pain well and has an anti-inflammatory effect.

Reviews about Lidocaine can be found on the Internet. As a rule, they are positive. After all, the correct dosage will help any patient tolerate surgery well.

The price of the drug depends on the manufacturer. Lidocaine in ampoules can be purchased for 40 rubles per package containing 10 ampoules. In carpools - approximately 70 rubles per carpool. Spray - 300–400 rubles 50 ml. The gel costs from 200 rubles.

The list of Lidocaine analogues includes such drugs as Versatis, Xylocaine, Helicain, Dinexan and others.

Lidocaine is able to retain its properties for five years when stored at a temperature of 15–25 degrees Celsius.

Before surgery, the patient is required to be examined by an allergist.

If the patient’s chart indicates that he has an allergy (to medications, food, dust, pollen), then before the administration of the anesthetic he needs to go to an allergist.

“The allergist will draw up a list of drugs that are suitable for the patient,” says Dmitry Davydov.

Lidocaine has analogues, for example, propofol and ultracaine. As a rule, they are tens of times more expensive.

“There are a lot of analogues, but an allergic reaction can happen in any case, it all depends on the individual sensitivity to the component of the drug,” says Dmitry Davydov.

Release forms and composition

There are many manufacturers of Lidocaine in ampoules or bottles. The drug can be used in all types of anesthesia and as a solvent for other drugs and is in demand in medical practice. Active ingredient: lidocaine hydrochloride.

There are 3 concentrations of industrial production:

  • ampoules with a solution of 1% concentration (10 mg/ml);
  • and 2% solutions (20 mg of substance in 1 ml);
  • 10% liquid (100 mg/ml).

The volume of containers is 2, 5 or 10 ml.

The solution is clear, colorless or slightly yellowish. Auxiliary components in the ampoule can be: sodium chloride, caustic soda and others, solvent water for injection.

Contraindications for use

A contraindication to the use of Ledocaine is considered to be hypersensitivity to the components of the drug. Ledocaine is also not used for the treatment of patients with a history of epileptic seizures, complex cardiac pathologies, or liver pathologies.

Restrictions on the use of an anesthetic and on use under close supervision of specialists are:

  • chronic pathologies and heart diseases;
  • complex liver pathologies;
  • malfunctions of the immune system;
  • old age;
  • pregnancy period, especially the last trimester;
  • lactation.

Use during pregnancy and lactation

During pregnancy, Lidocaine Bufus should be used with caution and only in cases where the benefit to the mother is clearly higher than the possible risks to the fetus.

Lidocaine is excreted in small amounts into breast milk, so the potential harm to the baby is very low. The drug can be used during lactation, but the decision to prescribe it is made only by the doctor.

Dosage recommendations should be strictly followed.

In obstetrics, if there are complications or a history of bleeding, the use of Lidocaine Bufus as epidural anesthesia is prohibited. Also, the use of lidocaine in concentrations exceeding 1% is not allowed, since this can lead to the development of fetal bradycardia in the fetus, resulting from the potential for high concentrations of local anesthetics to be achieved after paracervical blockade.

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

What is Lidocaine used for?

The drug is administered both intramuscularly and intravenously. But it can also be used as a dropper. This achieves maximum effect after 10 – 20 minutes.

The active substance of the drug, after the injection, begins to affect the membranes of neurons. This allows the movement of sodium ions to be blocked by the membrane. In this case, all exciting processes are inhibited. But complications may arise with calcium ions.

If an alkaline or slightly alkaline environment occurs, all components of the drug may dissolve. Lidocaine has two functions. It dilates blood vessels and reduces the pain threshold. Provided that the solution is administered via injection, it is quickly absorbed and the anesthetic begins to act immediately.

The active substance (Lidocaine hydrochloride) accumulates in the liver after the effect of the medicine ends. Then it is excreted naturally along with urine or bile. This process takes about 10 hours.

Indications of the drug

The drug can be used only as prescribed by a doctor. Self-use may adversely affect your health. Lidocaine is widely used in medicine. It is used to administer various methods of anesthesia.

  1. Infiltration. It is commonly used to “freeze” certain tissues. This approach is mainly used in dentistry.
  2. Terminal. Pain receptors are temporarily blocked. The effect is short-lived.
  3. Conductor. Used during operations. Nerve impulses are blocked in a certain area.
  4. Spinal. It is used if it is necessary to reduce the pain threshold in the spinal center. To do this, an injection is made into the subarachnoid space. In this case, the roots of the spinal center are blocked.
  5. Epidural. In this case, it is necessary to give an injection into the epidural space.

The drug is indicated for the following types of pathologies:

  • when the patient begins to develop ventricular arrhythmia, the causative agent of which is considered to be glycoside intoxication;
  • for patients who suffer from coronary syndrome for preventive purposes;

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It is widely used in dentistry:

  • for removing baby teeth in preschool children;
  • when it is necessary to remove bones or apply sutures to wounds in the oral cavity;
  • if there is a need to perform an autopsy during sudden abscesses;
  • when installing a prosthesis or crown on the gum, to relieve pain in the gum itself;
  • to destroy the papilla on the tongue;
  • if there is a need to open a cyst in the salivary glands;
  • in children, when a frenulectomy is needed.

Doctors treating ENT diseases use lidocaine injections in the following cases:

  • when it is necessary to perform surgery to remove nasal polyps;
  • for the treatment of deviated nasal septum;
  • during electrocoagulation;
  • before performing an operation to open a peritonsillar abscess;
  • to administer anesthesia before performing a puncture of the maxillary sinuses;
  • analgesic effect before rinsing the nasopharynx;
  • before removing the tonsils (tonsillectomy);
  • before removing the adenoids (adenoidectomy).

Not only before surgery, injections of the drug are used. He is appointed:

  • when you need to numb the nasopharynx or mouth before inserting a probe;
  • before examining the rectum with a probe;
  • if there is a need to replace catheters.

This is only a small part of the procedures where the drug is used. Gynecology, ophthalmology, obstetrics, plastic surgery - its functions as an anesthetic are currently used in all areas of medicine.

Contraindications

The anesthetic has contraindications:

  • in the presence of atrioventricular block (in this case, the conduction of the drug is impaired);
  • diseases associated with the work of the heart (heart failure, decreased heart rate, low blood pressure);
  • porphyria, or as it is also called “scientific vampirism”;
  • the presence of neuromuscular malaise (myasthenia gravis) (striated and transverse muscles get tired very quickly);
  • problems with the liver and kidneys, which impairs the excretion of lidocaine hydrochloride;
  • allergic reactions to any of the components of the drug;

Allergies can cause anaphylactic shock. This is very dangerous as it can be fatal.

  • breastfeeding and any trimester of pregnancy;
  • low blood volume circulation rates.

Not only Lidocaine - drugs of similar action are strictly contraindicated for the patient.

Adverse reactions

  • Allergic reactions may develop (anaphylactic shock, Quincke's edema, urticaria).
  • Impaired cardiac conduction.
  • Collapse.
  • Sinus bradycardia.
  • Central nervous system disorders - dizziness, tinnitus, convulsions, tremors, respiratory depression, nervousness, euphoria.
  • Nausea, vomiting.

Before using this anesthetic (as with any other drug), it is necessary to obtain a complete patient history.

We recommend reading: Local anesthesia in dentistry, types and rules

Causes of poisoning

Poisoning with a drug with the development of negative symptoms can occur for the following reasons:

  • individual intolerance to the drug;
  • intravenous administration;
  • rapid absorption into an area with a rich circulatory system;
  • exceeding the permissible dosage.

Note! Diseases of internal organs can cause poisoning even with a normal dose of administration. Therefore, it is recommended to calculate the amount of the drug taking into account the individual characteristics of the patient and use the minimum concentration of the drug.

Overdose

Lidocaine hydrochloride can be used for infiltration anesthesia intramuscularly, intradermally, subcutaneously. A lidocaine solution of 5 mg/ml is used (the maximum allowable dose is 400 mg).

To block the nerve plexuses and peripheral nerves, it is administered perineurally, 10-20 ml of solution is used. 10 mg/ml or 5-10 ml solution. 20 mg/ml.

  • Conduction anesthesia involves the use of 10 mg/ml and 20 mg/ml perineurally.
  • Epidural anesthesia involves the use of epidural 10 mg/ml or 20 mg/ml.
  • Spinal anesthesia involves the use of subarachnoid 3-4 ml of a solution. 20 mg/ml.

To prolong the effect of lidocaine, it is practiced to add a 0.1% solution of adrenaline.

It is administered intravenously as an antiarrhythmic drug.

A solution of 100 mg/ml is used intravenously only after it is diluted with saline.

25 ml sol. 100 mg/ml is diluted with 100 ml of saline to obtain a concentration of 20 mg/ml. This solution is administered to the patient as a loading dose. Initially, it is 1 mg per kg of weight (injected over 2-4 minutes, the rate is 25-50 mg per minute). Next, a constant infusion is started, the rate of which is 1-4 mg/min. Next, the doctor adjusts the administration individually.

As a rule, the intravenous infusion lasts 12-24 hours, while ECG monitoring is carried out continuously.

The spray must be sprayed onto the mucous membranes. The dosage depends on how large the surface area needs to be numbed. With a single spray, 4.8 mg of the active component is released. The minimum dose that provides the desired effect should be used. As a rule, the expected effect appears after 1-3 sprays.

The bottle should be held vertically while spraying the aerosol.

Some drugs (Cathegel with lidocaine, Lidocaine Asept spray) should only be administered by specialists.

If it is necessary to use an aerosol for children, it is applied with a cotton swab, as this avoids the burning sensation.

Ointment with lidocaine is applied to the surface in an amount that is determined individually.

Eye drops are used before interventions in ophthalmology; 20 mg/ml solution is instilled into the conjunctival sac. 2 drops each 2-3 times.

If an overdose is noted, the patient's first signs of intoxication may be nausea, dizziness, vomiting, a feeling of euphoria, asthenia, and a decrease in blood pressure. Later, spasms of facial muscles develop, turning into spasms of skeletal muscles. The patient also has bradycardia, psychomotor agitation, collapse, and asystole. If an overdose occurs during childbirth, the newborn may develop bradycardia, apnea, and depression of the respiratory center.

In case of overdose, it is necessary to stop administering the drug and inhale oxygen. Next, symptomatic breathing is carried out. If seizures develop, 10 mg of diazepam should be administered. In case of bradycardia, the administration of m-anticholinergic blockers (atropine) and vasoconstrictors is practiced. Hemodialysis will be ineffective.

Treatment of intoxication with anesthetic

When the body is intoxicated by a medication, the patient requires specialized care, which is provided in the toxicology department.

Treatment is aimed at removing intoxication from the body and restoring respiratory and cardiac activity, and relieving neurological symptoms.

Solutions for intravenous administration

Therapeutic measures include:

  • intravenous administration of sodium thiosulfate as an antidote;
  • with the development of a coma and depression of the respiratory center, intubation and mechanical ventilation (artificial ventilation), oxygen therapy are carried out;
  • intravenous administration of saline solutions, plasma;
  • for muscle twitching or contraction of individual muscle groups, in order to prevent seizures - anticonvulsants;
  • for bradycardia (slow pulse) to stimulate cardiac activity - M-anticholinergics;
  • if the rhythm of the heart muscle is disturbed - drugs that contain potassium and magnesium.

Intensive therapy is to prevent the development of congestive pneumonia. With timely treatment, the prognosis for the restoration of important body functions and the normalization of cardiac activity improves.

How to recognize an overdose?

Lidocaine overdose is a terrible thing. Not only does the patient have problems with the heart and blood vessels, but also the central nervous system is in a depressed state. Among other things, general weakness of the body appears, convulsions, dizziness, loss of consciousness, asphyxia and many other unpleasant symptoms are possible.

If, having such symptoms, you increase the dose, then such manipulations will lead to loss of consciousness, coma or even death. Exceeding the permissible limit causes temporary loss of vision, leads to vomiting or euphoria.

If at least one symptom appears, the administration of the drug should be suspended. Next, we act quickly and harmoniously:

  1. We place the patient on his back.
  2. We provide it with an influx of fresh air.
  3. If the problem is serious, we do oxygen therapy (administration of anticonvulsants).

Usually, in case of overdose, muscle relaxants are prescribed. For bradycardia, intravenous atropine is administered (the dosage is chosen by the doctor). In case of severe poisoning, the patient is taken to intensive care.

Who is contraindicated for Lidocaine hydrochloride?

The drug is a potent drug, therefore it is prescribed individually, taking into account the various diseases that the patient has.

The use of idocaine is contraindicated in pathological processes:

  • chronic heart and kidney failure;
  • liver dysfunction;
  • arterial pressure;
  • epileptiform syndrome;
  • allergic mood of the body;
  • infection of the intended site of anesthesia;
  • changes in intraventricular conduction, atrioventricular block of 2-3 degrees;
  • myasthenia gravis in severe form;
  • bearing a child and the period of breastfeeding.

If the patient has one of the above types of abnormalities, another pain medication is selected that does not cause severe complications when used.

Lethal dose

It is important to select the correct dosage of the drug, which is calculated per 1 kg of weight. The amount of the drug for parenteral administration to an adult patient is 5 mg/kg of body weight, but not more than 300 mg per hour.

Apnea

The dose is 2000 mg. If it is exceeded, an overdose of lidocaine occurs, in which clinical symptoms rapidly progress. Severe intoxication develops and can be fatal:

  • collapse, drop in blood pressure and cardiac activity;
  • apnea due to paralysis of the diaphragm;
  • cardiac arrest as a result of conduction disturbances.

Blood tests of patients who died from an overdose of the drug indicate elevated levels of the substance - 15 mcg/ml.

Required dosages

Each problem requires a certain dose of the drug. For example. To anesthetize the brachial and sacral plexuses, take up to 10 ml of a 2% solution. For pain relief in the fingers, nose or intimate area – up to 3 ml. It is prohibited to inject the solution into vessels.

When performing surgery on polyps or puncture of the maxillary sinuses, use up to 20 ml of a 2% solution.

Maximum volume of injected solution:

  • at 0.125% - 300 ml;
  • at 0.25% - 100 ml;
  • at 0.5% - 40 ml;
  • at 1% - 20 ml;
  • at 2% - 10 ml.

Repeated administration of the maximum dose on the same day is prohibited. If it is necessary to administer a large amount of medication, it is necessary to combine it with adrenaline, since the second substance reduces the absorption of lidocaine.

Cardiologists usually administer up to 2 mg per 1 kilogram of patient body weight. 20 mcg per kilogram is administered intravenously over 1 minute, and intramuscularly at 4 mg per kilogram every 6 hours.

First aid for lidocaine poisoning

The toxic reaction to the administration of lidocaine manifests itself very quickly. There is no specific antidote, so the victim needs to be helped symptomatically.

First you should stop administering the drug. For urticaria and other skin manifestations, antihistamines and a cold compress on the site of the rash are indicated. Bronchodilators will make breathing easier, and you can improve blood circulation by simply taking a lying position with your legs raised above head level.

Since Lidocaine is not taken orally, there is no point in gastric lavage, as well as in taking enterosorbents. Drinking plenty of liquid will help quickly get rid of the toxic substance that has entered the stomach.

In severe cases, artificial ventilation is performed

Due to the specificity of the drug, medical care and observation in the first days after an overdose are recommended for everyone, because Lidocaine can cause sudden cardiac arrest and death.

In a hospital hospital, the victim is intubated and artificially ventilated, and in parallel, electrolyte solutions or plasma substitutes, anticonvulsants and M-choline blockers are administered.

Storage

The storage temperature of the drug is from 8 to 25 ° C. In this case, all ampoules must be in the packaging. If any capsule is opened or the seal is broken, the solution is not suitable for injection. Always check the expiration date at the pharmacy. Usually it is 3 years from the date of issue. It is strictly prohibited to use expired goods.

Lidocaine in ampoules is an anesthetic that has been proven over the years. The only disadvantage of this drug is that it still remains toxic. But, nevertheless, many private clinics, dental offices and plastic surgeons order it for local anesthesia.

Who is contraindicated for lidocaine anesthesia?

Lidocaine is an old but proven method. But it has special rules of application that must be followed. This drug has a number of contraindications. That is why before administering the medicine, the doctor asks the patient’s age and whether he has liver or heart problems.

When injecting an anesthetic into the spine, the doctor will definitely ask about problems with the vertebrae. Doctors also use Lidocaine with extreme caution in cases of poor blood clotting. It is not recommended to administer anesthesia to nursing mothers.

The main reason remains individual intolerance to the drug. It is worth considering when administering lidocaine if you have low blood pressure or if there is an infection in the treated area.

Pregnant women are prohibited from injecting the drug into the uterus if toxicosis began too late, the baby is premature or, conversely, post-term.

Don’t worry, doctors know all the contraindications, just trust a professional.

Maximum dosage of the drug

The dosage of Lidocaine is calculated individually and depends on the size of the body area that needs to be anesthetized. Doses of minimal concentration are administered first. For adults, the maximum permissible dose is 200 mg of a two percent solution, and for topical anesthesia with ten percent Lidocaine, the permissible dose is 2 ml. It is noteworthy that the maximum and lethal dose have a very blurred line, and exceeding the norms specified in the instructions is strictly prohibited.

The manifestation of any symptoms of overdose should alert you. In such cases, the drug is immediately discontinued and actions aimed at neutralizing the toxic-allergic reaction are carried out.

Pharmacokinetics and pharmacodynamics

The highest concentration in the blood after intravenous administration is observed after 5-15 minutes, if the infusion is carried out slowly without a saturating initial dose, the maximum concentration is observed after 5-6 hours, and in people with acute myocardial infarction it can be achieved after a long time - up to 10 hours.
Binds to plasma proteins by 50-80%. It is distributed quickly in the body and penetrates the placental and blood-brain barriers. Metabolism mainly occurs in the liver, microsomal enzymes take part in the metabolic process, and active metabolites are formed - glycine xylidide monoethylglycine xylidide. People with liver disease have a slower metabolism. Excretion occurs in bile and urine.

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If lidocaine cream or other agents are applied topically, absorption depends on the dose and also on the site where the lidocaine cream or gel is applied. Absorption is affected by the rate of perfusion in the mucosa.

There is good absorption in the respiratory tract, so care must be taken to prevent the administration of the drug in toxic doses.

After injections of lidocaine intramuscularly, almost complete absorption is noted. It is distributed quickly and binds to proteins, depending on the concentration of the active ingredient, by 60-80%.

The half-life depends on the dose administered, it is 1-2 hours.

If an aerosol is used, its effect appears within 1 minute and lasts 1-2 minutes. There is a gradual disappearance of the achieved decrease in sensitivity over 15 minutes.

Lidocaine tolerance test

Allergic reactions are observed infrequently, and even if nothing like this has happened to a person before, this does not mean that a reaction will not occur under conditions of illness (for example, while taking another medication). The structure of Lidocaine is complex, and if there is the slightest danger, it is better to abandon it and replace it with an alternative drug.

If the drug is taken for the first time, the doctor is obliged to do an intolerance test : 0.1 ml of Lidocaine is injected subcutaneously, if after 15-30 minutes there are no negative reactions, then it can be used. Under no circumstances should lidocaine be combined with adrenaline during a provocative test, so as not to cause a false negative reaction.

It is not recommended to carry out the procedure on your own, because without the knowledge and skills of a healthcare worker, you may not be able to save yourself from unwanted reactions such as anaphylactic shock. The danger of Lidocaine lies in the rapid reaction of the human body. Due to insensitivity to pain signals, a person may not even realize that something is wrong with him.

Before the injection, you need to do a Lidocaine tolerance test.

You should immediately report any unpleasant sensations to your doctor, rather than endure them. The doctor will quickly stop anaphylaxis and take measures to eliminate the consequences of the drug.

If during a tolerance test it turns out that the patient’s body has at least the slightest intolerance, Lidocaine is replaced with another drug of the same effect, fortunately, in our time there is a wide choice for an alternative.

The cause of an undesirable reaction can be either hereditary or individual intolerance to the drug, or undesirable compatibility of the active substance with another drug. Therefore, before the pain relief procedure, you must inform your doctor about the medications you are taking.

Lidocaine is strictly prohibited for people suffering from the following diseases:

  • heart failure of II and III degrees;
  • bradycardia;
  • atrioventricular block II and III degrees;
  • hypotension;
  • epilepsy;
  • myasthenia gravis;
  • problems with blood clotting;
  • chronic and acute renal failure.

Release forms, composition and scope of their application

Lidocaine has several forms of release. Which one is best to use is usually decided by the doctor depending on the procedure being performed.

Lidocaine spray

A clear liquid with a strong menthol odor and an unpleasant bitter taste.

The aerosol contains the active component - lidocaine hydrochloride, propylene glycol and mint oil.

The concentration of the active substance in the spray is quite high - 10%, due to which the anesthetic effect occurs in a few minutes, but it does not last long, so re-application of the product to the mucous membranes is often required.

The spray is usually used in the following cases:

  • The need to numb the mouth before an injection or minor surgery.
  • Decreased gag reflex during manipulations in the depths of the oral cavity.
  • Relief of pain during teething, including wisdom teeth.

It can be used in pediatric dentistry to remove baby teeth when an injection of the main anesthetic is not required.

Lidocaine in the form of a solution for injection

The most common option. The solution contains distilled water, lidocaine hydrochloride, sodium chloride. The concentration of the active substance is most often 2%, but can be higher. The dosage is chosen by the dentist depending on the operation. Unlike the spray, Lidocaine in ampoules is odorless. The effect lasts from half an hour to an hour. Lidocaine injections have a great advantage over Novocaine - the product is allowed to be used for inflammation, since Lidocaine does not have a negative effect on the tissues affected by the process.

Applicable for:

  • removal of simple teeth;
  • removing the stone;
  • opening of purulent foci in the oral cavity;
  • in cases where for some reason it is not possible to use Novocain.

Lidocaine in gel form

It is used much less frequently than spray or injections. The gel is colorless, smells faint and has a characteristic taste. It is used to treat the oral cavity during dental treatment or inflammatory processes. The composition includes chamomile extract, due to which the product, in addition to pain relief, also has a calming, anti-inflammatory effect.

Despite the effectiveness of lidocaine, it is not the most powerful anesthetic for topical use in dentistry. If you are undergoing a serious and lengthy operation, it is better to give preference to new generation painkillers, such as Ultracaine.

How does Lidocaine affect our body?

Doctors recommend using lidocaine for pain relief, as they consider it the best.
After all, it is able to restore heart rhythm and prevent rapid heartbeat. When injected under the skin, the drug acts very quickly. Many patients have noticed more than once how the pain-relieving part goes numb. As a result, the nervous system is blocked. Typically, the duration of such anesthesia is 1 hour. Almost all the medicine is excreted from the body by the kidneys.

It is also important to know which medications Lidocaine is compatible with and which it is not. If this is not controlled, complications may arise. After all, with some medications, lidocaine reduces its effects, and with others it increases. To avoid negative consequences, it is better to inform your doctor in advance about taking certain medications.

Very important! During treatment with Lidocaine, it is extremely important to stop drinking alcohol, otherwise it can cause cardiac arrest, that is, death!

Pharmacological effects

Since lidocaine hydrochloride is a representative of a subgroup of anesthetics, it has the following pharmacological effects:

  • conduction and infiltration anesthesia;
  • epidural anesthesia.

The drug not only has a local anesthetic effect by suppressing impulse conduction while blocking sodium ion channels directly in the nerve fiber, but also has an antiarrhythmic effect.

When distributed locally, the drug "Lidocaine", the instructions for use confirms this, dilates blood vessels, while no locally irritating effect is observed. Due to increased permeability of potassium membranes, the antiarrhythmic mechanism of the drug is possible.

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