Why the action of lidocaine does not pass. Death from lidocaine

13.08.2020

Lidocaine is an antiarrhythmic, local anesthetic that is used in many branches of medicine. It is actively used for intramuscular, intravenous administration in the form of a hydrochloride solution.

In addition, you can use the drug in the form of a spray 10%. Ointments, gels and eye drops with Lidocaine are also produced.

Lidocaine is an analgesic drug, anesthetic, but not general, but local. It can be used to carry out small surgical interventions, some painful studies.

Lidocaine is actively used during cesarean section and childbirth. Many people are familiar with a similar drug from visits to the dentist, since children and adults are often given local anesthesia during dental treatment, which lasts a certain time. Lidocaine is even used to remove or apply surgical stitches.

The mechanism of action of Lidocaine on a child, an adult:

suppression of the automatism of Purkinje fibers;
blocking of sodium channels of membranes of neurons, cardiocytes;
local anesthetic effect, which can be explained by the stabilization of cell membranes, which is why there is a decrease in impulse conduction;
oppression in the myocardium of ectopic foci of excitation, provoking the development of arrhythmia.

First, the drug penetrates into those organs in which there is a fairly good blood circulation, namely the lungs, heart and brain. In case of infusion, it can pass into breast milk, placenta. If there is chronic renal failure, then the drug can accumulate in the body.

Taking lidocaine inside is contraindicated!

The drug relieves pain, after which it reduces tactile sensitivity. It is important to note that in a therapeutic dosage it has no effect on myocardial contraction. To relieve an attack of arrhythmia, you need to perform intravenous administration. The effect comes on quickly, does not last very long. In the case of intramuscular injection, the effect appears after 5-15 minutes. When the spray is applied to the skin or mucous membranes, anesthesia appears after 15 minutes. Knowing what effect and for how long lidocaine has, you can avoid many complications and overdose.

Side effects of Lidocaine:

Dysfunction of the digestive system, which manifests itself in the form of nausea, vomiting and dyspepsia.
Allergic reactions in the form of urticaria, Quincke's edema, anaphylactic shock.
The cardiovascular system also suffers: bradycardia, conduction disturbances, blockade appear; blood pressure rises or falls.
Disturbances from the nervous system: consciousness is inhibited or excited, euphoria, dizziness appear. If the case is too severe, cramps and twitching of the muscles may occur.

In addition to the listed symptoms, numbness of the arms and legs, as well as a feeling of heat and cold, may occur.

The clinical picture of overdose

In case of an overdose of Lidocaine, symptoms of depression of the nervous system and the activity of the heart muscle occur. It is important to note that the symptomatology increases gradually, with a parallel deterioration in the patient's condition.

The first signs of a lidocaine overdose:

tremor of the limbs;
numbness of the tongue;
excessive sweating;
dizziness and migraine;
feeling of "goose bumps" around the lips;
pallor of the skin;
severe weakness, lethargy and apathy;
excessive excitement or, conversely, inhibition of the reaction;
episodes of short-term respiratory arrest;
a sharp drop in blood pressure.

If the listed signs begin to appear, the use of this drug should be urgently discontinued. When the condition worsens, the clinical picture becomes significantly more complicated.

Symptoms of lidocaine poisoning:

convulsions and tremors;
strong depression of consciousness with the impossibility of contact;
violation of the rhythm of the heartbeat;
decrease in pressure;
development of pathological types of breathing;
pronounced cyanosis of the skin, mucous membranes.

In the event of the above symptoms, the victim will need emergency medical care and hospitalization in a hospital, and sometimes it is impossible to do without resuscitation measures.

Video

The specifics of first aid and treatment of anesthetic overdose

If an overdose has occurred at home, you must immediately call an ambulance.

Algorithm of actions:

stop using lidocaine;
lay the patient in a horizontal position;
provide him with a sufficient amount of oxygen;
call the ambulance team.

As for washing the stomach and taking laxatives, then this is not worth doing. The fact is that Lidocaine is not taken orally, so such measures are meaningless. It is important to immediately deliver the victim to the hospital, where specialists will be able to provide him with highly qualified assistance.

In the conditions of resuscitation, a number of important actions are performed: intubation of the trachea is performed in order to join the mechanical ventilation; anticonvulsants are introduced - Thiopental sodium and Diazepam. Then intravenous administration of plasma substitutes is carried out - Polyglyukin, Reopoliglyukin. If there is bradycardia, then you cannot do without Atropine.

As a specific antidote, a thirty percent solution of sodium thiosulfate acts, it is administered intravenously.

Lidocaine: consequences of an overdose

An overdose of the drug leads to severe and immediate consequences:

collapse;
paralysis of the diaphragm, followed by respiratory arrest;
cardiac arrest due to conduction disturbances;
death.

The lethal dose of the drug is about 2 g.
But the death of a patient can occur without an overdose, in case of allergy to the drug or individual intolerance to it. The development of anaphylactic shock in such a situation does not depend on the administered dose of Lidocaine.

Thus, Lidocaine is not an anesthetic for home use; its use should only take place under the supervision of a physician.

Lidocaine belongs to pharmacy drugs, local anesthetics and heart depressants used as an antiarrhythmic agent. This drug has a more intense and lasting effect compared to Novocaine. The total duration of action is shorter than that of Bupivacaine or Prilocaine.

Pharmacology and pharmacokinetics

Lidocaine has a local anesthetic effect by blocking voltage-gated sodium channels, which prevents impulse generation inside sensitive nerve endings and prevents impulse conduction along the nerves. The agent suppresses the conduction of pain and other impulses. Local application promotes vasodilation, but there is no irritating effect. The level of absorption for parenteral administration depends on the dose and the site of administration.

The substance is metabolized in the liver tissues with the participation of microsomal enzymes and dealkylation of the amino group under conditions of rupture of amide bonds with the formation of active metabolites. With liver disease, the level of metabolic intensity decreases markedly. Long-term infusion of lidocaine for a couple of days increases significantly. This drug is excreted from the human body by the kidneys and bile. Chronic renal failure can be the cause of the accumulation of metabolites, and with acidification of urine, the rate of excretion of Lidocaine increases.

Interaction of lidocaine with other drugs

When interacting with other drugs, it is necessary to take into account the features and mechanism of action of the funds:

a decrease in hepatic clearance and an increase in the risk of developing a toxic effect with the simultaneous use of lidocaine with cimetidine and propranolol;
decrease in effectiveness when taken simultaneously with barbiturates and phenytoin, as well as Rifampicin;
increased inotropic negative effect when administered together with Aimalin, Verapamil, Phenytoin, Quinidine and Amiodarone;
increased risk of developing severe bradycardia when administered together with any beta-blockers;
a noticeable weakening of the cardiotonic effect when used simultaneously with cardiac glycosides;
an increase in the risk of developing arousal of the central nervous system and the appearance of hallucinations when prescribing Lidocaine with Procainamide;
increasing the depressing effect on the central nervous system while prescribing with hypnotics and sedative drugs;
respiratory depression with intravenous administration of Thiopental sodium or Hexobarbital against the background of exposure to lidocaine;
an increase in the risk of a sharp decrease in blood pressure indicators when used together with MAO inhibitors represented by Furazolidone, Procarbazine and Selegilin;
the risk of severe inhibition of neuromuscular transmission when used simultaneously with polymyxin B;
lengthening of local anesthetic effects when used with vasoconstrictors such as Epinephrine, Methoxamine and Phenylephrine.

When prescribing, it must be remembered that combined use with narcotic analgesics provokes the development of an additive effect, and the simultaneous use of Lidoaquin with anticoagulants can cause bleeding.

Side effects

The undesirable consequences that may occur when using lidocaine are most often presented:

euphoria and dizziness;
flashing "flies" and points in front of the eyes;
photophobia;
neurotic reactions;
headaches;
anxiety and tinnitus;
diplopia;
convulsions and tremors;
drowsiness;
paresthesia;
disorientation and confusion;
paralysis of the respiratory muscles;
respiratory arrest and respiratory paralysis;
collapse and tachycardia;
peripheral vasodilation and bradycardia up to cardiac arrest;
involuntary urination and defecation.

From the side of the hematopoietic organs, the development of methemoglobinemia may be noted. Allergic reactions can often develop in the form of urticaria and itching, up to anaphylactic shock. An overdose of Lidocaine causes more serious complications, including death.

The reasons for the development of side effects

The appearance of side effects is associated with improper use of lidocaine and its high plasma concentration. Overdose directly depends on the amount of the drug, and the symptoms are the result of:

intravenous anesthesia;
patient hypersensitivity;
individual intolerance;
intravascular administration;
application to damaged skin;
rapid absorption from loci with an abundant vascular system;
use not for the main purpose.

Signs of overdose

Lidocaine overdose often has very serious consequences. Symptoms of intoxication can be presented:

inhibition of the activity of the cardiovascular and central nervous system with a gradual increase in the severity of the process;
tingling and "creeping" in the area around the mouth;
increased sweating;
blanching of the skin;
chills;
drowsiness or, conversely, psychomotor agitation, a state of agitation;
numbness of the tongue;
dizziness and headaches;
painful sensitivity to sounds and tinnitus;
visual impairment with inability to focus the gaze and double vision;
tremors and muscle twitching, sometimes turning into a generalized convulsive seizure;
episodic and spontaneous respiratory arrest;
lowering blood pressure;
slowing down the pulse;
heart rhythm disturbances with the risk of cardiac arrest.

The danger of an overdose with lidocaine increases significantly under conditions of intravenous administration of the drug. In case of acute overdose in the process of carrying out spinal or epidural anesthesia during childbirth, there may be an inhibition of the heart rate in the fetus, the development of severe hypotension or depression of respiratory function.

The clinical picture of poisoning

Symptoms of drug overdose are accompanied by a number of signs of toxic effects on the central nervous system:

numbness of the tongue;
a feeling of creeping in the face;
sharp dizziness;
growing noise in the ears.

Further symptoms are typical for a severe overdose. In this case, convulsions and breathing disorders develop, as well as muscle twitching, preceding the generalization of the toxic process. Most often, acidosis and hypoxia progress rapidly. As a symptomatology of the heart and vascular system, it is considered:

a sharp and sharp drop in pressure;
arrhythmic contraction of the myocardium.

Death develops during cardiac arrest and cessation of respiratory activity. In case of an overdose of a spray based on Lidocaine, increased sweating, rapid blanching of the skin, double vision and convulsions are noted.

First aid for overdose

At the first sign of poisoning, the victim should sit in a horizontal position with an influx of fresh air. At risk of developing severe complications, hospitalization is required.

Intoxication therapy

There is no specific antidote. The appearance of small or large seizures requires the introduction of Phenazepam. Stopping cardiac activity involves resuscitation. Therapy for an overdose with Lidocaine involves 100% oxygenation, restoration and normalization of blood circulation, prevention of convulsive state, ensuring full patency of all airways.

If necessary, the patient is prescribed vasoconstrictors, anticonvulsants and m-anticholinergics. Also, according to indications, intubation and mechanical ventilation are allowed. Violation of cardiac activity involves the use of Epinephrine and resuscitation measures. In order to prevent an overdose, the patient's age, the list of contraindications and compatibility with other drugs, and also the dosage is correctly selected.

Dosage Form: & nbspinjection Composition:

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

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

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

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

N.01.B.B Amides

N.01.B.B.02 Lidocaine

C.01.B.B.01 Lidocaine

C.01.B.B Class Ib antiarrhythmic drugs

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

Absorption

Lidocaine is rapidly absorbed from the gastrointestinal tract, but due to the "primary passage" effect through the liver, only a small amount reaches the systemic circulation.

Systemic absorption of lidocaine is determined by the site of administration and dose. The maximum concentration in the blood is achieved after intercostal blockade, then (in order of decreasing concentration), after injection into the lumbar epidural space, brachial plexus and subcutaneous tissues. The main factor that determines the rate of absorption and concentration in the blood is the total dose administered, regardless of the site of administration. There is a linear relationship between the amount of lidocaine administered and the resulting maximum concentration of anesthetic in the blood.

Distribution

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

Metabolism

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

Metabolites resulting from subsequent metabolism are excreted in the urine.

Withdrawal

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

Special patient groups

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

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

In newborns, a low concentration of ACG is noted, therefore, the connection with plasma proteins may decrease. Due to the potentially high concentration of the free fraction, the use of lidocaine in neonates is not recommended.

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

Fertility

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

Pregnancy

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

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

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

In animal studies, no harmful effects on the fetus were found.

Breast-feeding

A small amount of lidocaine passes into breast milk, its oral bioavailability is very low. Thus, the expected amount entering breast milk is very small, hence the potential harm to the baby is very low.

The doctor makes the decision about the possibility of using lidocaine during breastfeeding.

Method of administration and dosage:

The dosage regimen should be selected based on the patient's response and the site of administration. The drug should be administered at the lowest concentration and the lowest dose that gives the desired effect. The maximum adult dose should not exceed 300 mg. The volume of solution to be administered depends on the size of the area to be anesthetized. If there is a need for the introduction of a large volume with a low concentration, then the standard solution is diluted with saline (0.9% sodium chloride solution). Dilution is carried out immediately prior to administration.

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

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

	10 mg / ml	20 mg / ml
Infiltration anesthesia:
Small interventions	2-10 ml (20-100 mg)
Big interventions	10-20 ml (100-200 mg)	5-10 ml (100-200 mg)

Conductive anesthesia	3-20 ml (30-200 mg)	1.5-10 ml (30-200 mg)
Finger / toe anesthesia	2-4 ml (20-40 mg)	2-4 ml (40-80 mg)
Epidural, lumbar	25-30 ml (250-300 mg)

Caudal, chest block	20-30 ml (200-300 mg)

Regional anesthesia	No more than 5 ml (50 mg)	Not more than 2.5 ml (50 mg)

Children under 1 year old

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

Combined use with epinephrine

To lengthen the action of lidocaine and reduce its systemic action, it is possible to addex tempore 0.1% epinephrine solution in a ratio from 1: 100,000 to 1: 200,000.

Side effects:

Adverse reactions are described according to system organ classes.MedDRA.

Like other local anesthetics, adverse reactions are rare. usually due to increased plasma concentration due to inadvertent intravascular administration, overdose or rapid absorption from areas with abundant blood supply, or due to hypersensitivity, idiosyncrasy, or reduced patient tolerance. Systemic toxicity reactions are mainly manifested by the central nervous and (or) cardiovascular system (see also the "Overdose" section).

Immune system disorders: hypersensitivity reactions (allergic or anaphylactoid reactions, anaphylactic shock) - see also disorders of the skin and subcutaneous tissues. An allergy skin test is not considered unreliable.

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

Neurological complications of spinal anesthesia include transient neurological symptoms such as pain in the lower back, buttocks, and legs. These symptoms develop. usually within 24 hours after anesthesia and resolve within a few days. After spinal anesthesia with lidocaine and similar agents, isolated cases of arachnoiditis and cauda equina syndrome with persistent paresthesia, intestinal and urinary tract dysfunction, or paralysis of the lower extremities have been described. Most cases are due to hyperbaric lidocaine concentration or prolonged spinal infusion.

Violations of the organ of vision: blurred vision, diplopia, and transient amaurosis may be a sign of lidocaine toxicity.

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

Hearing and labyrinth disorders: tinnitus, hyperacusis.

Cardiovascular disorders: cardiovascular reactions are manifested by arterial hypotheisia, bradycardia, suppression of the contractile function of the myocardium (negative inotropic effect), arrhythmias, possibly cardiac arrest or circulatory failure.

Respiratory, chest and mediastinal disorders: shortness of breath, bronchospasm, respiratory depression, respiratory arrest.

Gastrointestinal disorders: nausea, vomiting.

Skin and subcutaneous tissue disorders: rash, urticaria, angioedema, facial edema.

Overdose:

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

Overdose resolution occurs due to the redistribution of the local anesthetic from the central nervous system and its metabolism; it can proceed quite quickly (if a very large dose of the drug has not been administered).

Treatment: if there are signs of an overdose, the administration of the anesthetic should be stopped immediately.

Convulsions, CNS depression, and cardiotoxicity require medical attention. The main goals of therapy are to maintain oxygenation, stop seizures, maintain adequate blood circulation and stop acidosis (if it develops). In appropriate cases, it is necessary to ensure the patency of the airways and prescribe, as well as establish an auxiliary ventilation of the lungs (mask or using an Ambu bag). The maintenance of blood circulation is carried out through the influence of plasma or infusion solutions. If long-term maintenance of blood circulation is necessary, the possibility of introducing vasopressors should be considered, but they increase the risk of CNS excitation. Seizure control can be achieved with intravenous diazepam (0.1 mg / kg) or sodium thiopental (1-3 mg / kg). it should be borne in mind that anticonvulsants can also depress respiration and blood circulation. Prolonged seizures may interfere with ventilation and oxygenation of the patient, and early endotracheal intubation should be considered. When cardiac arrest occurs, standard cardiopulmonary resuscitation is initiated.

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

Interaction:

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

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

Lidocaine should be used with caution in patients receiving other local anesthetics or agents that are structurally similar to local anesthetics of the amide type (for example, antiarrhythmics such as tocainide). since systemic toxic effects are additive. Separate studies of drug interactions between lidocaine and class III antiarrhythmics (eg, amiodarone) have not been conducted, but caution is advised.

In patients who are simultaneously receiving antipsychotics that prolong or can prolong the OT interval (eg, pimozide, zotepin), prenylamine. (if accidentally administered intravenously) or antagonists of 5-HT3-serotonin receptors (eg, dolasetron) may increase the risk of ventricular arrhythmias.

The simultaneous use of hipupristin / dalfopristin can increase the concentration of lidocaine and, thus, increase the risk of ventricular arrhythmias; their simultaneous use should be avoided.

Patients concurrently receiving muscle relaxants (eg, suxamethonium) may have an increased risk of increased and prolonged neuromuscular blockade. After using bupivacaine in patients receiving and, it was reported the development of cardiovascular failure: it is similar in structure to bupivacaine. and 5-hydroxytryptomy reduce the seizure threshold for lidocaine. Opoids are likely to have a pro-convulsive effect, as evidenced by the evidence that the seizure threshold to fentanyl is lowered in humans.

The combination of opioids and antiemetics, used for sedation in children, can lower the seizure threshold for lidocaine and increase its depressant effect on the central nervous system.

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

The simultaneous use of other antiarrhythmics, β-blockers and blockers of "slow" calcium channels can further reduce AV conduction, ventricular conduction and contractility.

The simultaneous use of vasoconstrictor agents increases the duration of the action of lidocaine.

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

Care must be taken when using sedatives because they can affect the effect of local anesthetics on the central nervous system.

Care should be taken with long-term use of antiepileptic drugs (), barbiturates and other inhibitors of liver microsomal enzymes. since this can lead to a decrease in efficiency and. as a result, an increased need for lidocaine.

On the other hand, intravenous administration of phenytoin may increase the inhibitory effect of lidocaine on the heart.

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

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

Lidocaine is not compatible with amphohericin B. methohexitone and nitroglycerin. With the simultaneous use of lidocaine with narcotic analgesics, an additive effect develops, which is used when conducting epidural anesthesia, but increases the depression of the central nervous system and respiration.

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

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

Guanadrel, guanethidine. mecamylamine, trimetaphan kamzilate increase the risk of severe lowering of blood pressure and bradycardia.

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

Lidocaine reduces the effect of anti-myasthenic drugs, enhances and lengthens the effect of muscle relaxant drugs.

When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases. It is not recommended to mix with other medicinal products.

Special instructions:

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

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

For patients receiving class III antiarrhythmic drugs (for example), close observation and ECG monitoring should be established, since the effect on the heart can be potentiated.

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

It has been shown to cause porphyria in animals and should be avoided in individuals with porphyria.

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

Before starting the intravenous administration of lidocaine, it is necessary to eliminate hypokalemia, hypoxia and violation of the acid-base state.

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

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

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

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

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

Retrobulbar administration can rarely enter the subarachnoid space of the skull, leading to serious / severe reactions including cardiovascular failure, apnea, seizures, and temporary blindness.

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

The severity of these reactions depends on the severity of the injury, the concentration of the local anesthetic and the duration of tissue exposure. In this regard, any local anesthetic should be used in the lowest effective concentration and dose. Lidocaine injection solution is not recommended for use in newborns. The optimal serum concentration of lidocaine to avoid toxicity such as seizures and arrhythmias has not been established in neonates.

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

In patients with coagulopathy. Treatment with anticoagulants (eg, heparin), nonsteroidal anti-inflammatory drugs (NSAIDs), or plasma substitutes increases the tendency to bleed. Accidental vascular damage can lead to severe bleeding. If necessary, check bleeding time, activated partial thromboplastin time (APTT) and platelet count;

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

Patients with seizure disorders should be closely monitored for central nervous system symptoms. Low doses of lidocaine can also increase convulsive readiness. In patients with Melkersson-Rosenthal syndrome, allergic and toxic reactions from the nervous system in response to the introduction of local anesthetics may develop more often; - the third trimester of pregnancy.

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

Impact on the ability to drive vehicles. Wed and fur .:Transient sensory loss and / or motor block may occur after administration of local anesthetics. Until these effects are resolved, patients are not recommended to drive vehicles and operate machinery. Release form / dosage:

Solution for injection 20 mg / ml.

Packaging:

2 ml ampoules. 10 ampoules in a cardboard box together with instructions for use and ampoule scarifier. 5 ampoules in a blister strip packaging. 2 blister packs each with instructions for use and ampoule scarifier in a cardboard box.

When using ampoules with a point or a break ring, the ampoule scarifier is not inserted.

Storage conditions:

In a dark place at a temperature of 8 ° C to 25 ° C.

Avoid freezing.

Keep out of the reach of children.

Shelf life:

Do not use after the expiration date printed on the package.

Pharmacy dispensing conditions:On prescription Registration number:R N000318 / 01 Registration date:19.11.2007 Expiration date:Indefinite Marketing Authorization Holder:MOSKHIMFARMPREPARATY them. N.A. Semashko, JSC Russia Manufacturer: & nbsp Date of information update: & nbsp26.02.2018 Illustrated instructions

Lidocaine is a drug that can be harmful to health. Not so long ago it became known that a ten-year-old child died in the city of Omsk. The girl was undergoing treatment for renal failure. She was injected with lidocaine, after which the child fell into a coma, and died in the morning.

It is worth noting that allergic reactions to lidocaine are not common, but similar cases have occurred in the capital and in Yakutia. In Moscow, a 36-year-old woman died from an injection of lidocaine, in Yakutia - Christina Hyde, a journalist. When the outraged public raised a wave of discussion about this, it turned out that in practice there were other cases of strong reactions to lidocaine, which led to the death of children.

What is lidocaine?

Lidocaine is a substance that has analgesic effects. It is used to dilute intramuscular antibiotics, which are quite painful for normal administration, as well as to relieve pain during various medical procedures. In a sense, diluting an intramuscular antibiotic with lidocaine is less dangerous than diluting it with water for injection.

Parents should be aware that any medication can cause anaphylaxis or idiosyncrasy. Medical intervention is a risk, but the risk must of course be justified.

By the way, for children, the option with oral antibiotics is more preferable, since the introduction of an antibiotic into the muscle is indicated only if the person is unconscious, or cannot absorb the medicine through the digestive tract.

Lidocaine, in addition to anaphylaxis, can lead to overdose, which in turn will cause rhythm disruption and cardiac arrest.

It is impossible to know whether a person will have a reaction. Neither by passing tests, nor by making samples. It's individual. And this is very bad, both for us, patients, and for doctors. Therefore, the doctor cannot be blamed for the death of the child. At the very least, this is unfair. The doctor's fault may lie in the fact that the treatment could have been carried out without an injection. But, if we talk about an overdose, then you need to read the instructions for the drugs and know the material well.

The conclusions can be made as follows:

An antibiotic should be prescribed for a child only when indicated. Oral administration should be preferred over intramuscular administration.

Despite the well-known tragic cases, there is no need to be afraid of lidocaine, doctors and antibiotics. According to statistics, the probability of dying at a pedestrian crossing, crossing the road at a permitted traffic light, is higher than dying from lidocaine.

Every medical intervention has risks and harms. Thus, it is only possible to intervene if the harm from non-intervention is much greater than the likely harm caused by the intervention. It is not known how to find the line, but only a doctor can get close to it and understand how to act in a specific situation. Look for good doctors and trust them.

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Lidocaine is a common drug primarily used as a local anesthetic and antiarrhythmic drug. Despite the relatively short period of action, this substance is the main alternative to novocaine due to its rapid, intense effect.

How exactly does lidocaine affect the body and is it harmful? What are the symptoms of an overdose and is it dangerous? What first aid can be given to the victim? You will read about this and much more in our article.

How does lidocaine affect the body?

The mechanism of action of lidocaine is that the drug has a pronounced, anesthetic effect by blocking potentially dependent sodium channels, which prevents the generation of impulses in the nerves and slows down their conduction through the fibers.

Clinical practice shows that lidocaine not only suppresses pain, but can also inhibit impulse responses of other modalities. The action of lidocaine in time reaches one and a half hours (when combined with epinephrine up to 2.5 hours), while the blocking intensity is up to 5 times higher than that of classic procaine.

The drug at the local level dilates blood vessels and does not irritate the skin and mucous membranes.

In cases of parenteral administration, it is rapidly absorbed and distributed in the body (within 5-10 minutes), binding to plasma proteins and entering the internal organs first, and then affecting muscle and adipose tissues.

Overdose reasons

As a rule, subject to all norms of use in the local treatment of the skin and mucous membranes, an overdose of lidocaine does not occur.

However, in the case of long-term medical events in the field of dentistry, surgery, ophthalmology, obstetrics, urology, etc. lidocaine can accumulate in the body for a short period of time (especially with a slow metabolism) and cause a number of side effects.

Most often, an overdose of lidocaine is observed with its intramuscular or intravenous administration when stopping ventricular fibrillations and arrhythmias, preventive measures to counteract tachycardia and the formation of paroxysm, as well as in cases of systemic anesthesia.

The maximum daily permitted dose of the drug for adults administered parenterally is 2,000 mg, but not more than 400 milligrams per hour.

For children, the highest limit of the single use rate is no more than 1.25 milliliters of the product.

When administered intravenously, the norms are calculated based on body weight - 1 milligram per kilogram of weight.

Symptoms and signs of poisoning

In cases of lidocaine overdose, various pathologies and syndromes are observed associated with disruption of the nervous system and inhibition of the normal functioning of the cardiovascular system.

As a rule, signs of a negative state are initially insignificant, but with further accumulation of the drug in the body, the severity of the overdose state begins to gradually increase.

The main primary symptoms of a lidocaine overdose:

Blanching of the skin;
Sweating, creeping or itching in the area where lidocaine is applied;
Severe numbness of the localization of application of the drug;
Weakness, slight decrease in blood pressure;
Dizziness, tremors, lethargy, or vice versa - excitability;
Breathing problems, up to and including short-term stops.

An overdose of lidocaine as negative symptoms develop is accompanied by additional signs:

First aid for lidocaine overdose

As modern medical statistics show, most cases of lidocaine overdose occur mainly within the walls of medical institutions.

Qualified assistance

Poisoning with lidocaine, especially in moderate or severe form, causes in the patient not only severe hypotension, but also depression of the respiratory center, which can lead to a halt in the work of the system associated with it.

Despite the fact that pathological symptoms increase in this case gradually, even adults are at a potential risk of death.

Small children are in a special danger group (lidocaine acts on them faster and stronger), as well as the elderly (slow metabolism provokes the accumulation of the drug and its overdose).

The exact lethal dose of lidocaine is not known. Systemic pathological reactions from the central nervous system and the cardiovascular apparatus are observed with a single administration of more than 800 milligrams of the drug in absolute equivalent or more than 3 thousand milligrams throughout the day.

With the simultaneous use of lidocaine with a number of other medications (for example, epinephrine), the chances of a severe overdose with a potential death increase significantly.

In addition, a quick lethal outcome is possible in the presence of intolerance to lidocaine (anaphylactic shock), as well as in the case of an incorrect method of its administration (for example, a normal dose for intramuscular administration that has penetrated into a blood vessel can be fatal for a person).

Inpatient treatment

After the provision of first aid and the arrival of the ambulance team, given the serious condition of the patient, a decision can be made to hospitalize the victim in a hospital.

Specialists of the intensive care unit, if necessary, will carry out emergency measures aimed at stabilizing the basic vital signs of the patient, and will perform symptomatic and pathogenetic treatment.

Major activities include:

Consequences and complications

An overdose of lidocaine in high concentrations often causes a number of complications, mainly of an acute nature.

In some cases, negative consequences develop during the first days after the incident and directly threaten the patient's life.

Consequences of an overdose of lidocaine:

Stop breathingcaused by paralysis of the diaphragm and requiring immediate intubation and the use of artificial ventilation in the acute period;
Systemic pathologies of the cardiovascular systemcaused by persistent violation of intracardiac conduction and requiring prompt resuscitation;
A sharp drop in blood pressure and deterioration or cessation of blood supply to all the most important organs and systems of a person due to collapse.