Lidocaine Darnytsia solution for injection 20 mg/ml in 2 ml ampoules 10 pcs.

Active ingredient: lidocaine.

Composition

• 1 ml of solution contains lidocaine hydrochloride 20 mg;
• excipients: sodium chloride, sodium hydroxide, water for injections.

Release form

Solution for injection.

Pharmacodynamics. Local anesthetic for terminal, infiltration, and conduction anesthesia. The relative toxicity of lidocaine hydrochloride depends on the concentration of the solution. At low concentrations (0.5%) it does not differ significantly in toxicity from novocaine, with increasing concentration (1 and 2%), toxicity increases.

Pharmacokinetics. When applied topically to mucous membranes, lidocaine is absorbed to varying degrees depending on the dose and site of application (C _max is reached after 10-20 min); absorption is affected by the rate of perfusion through the mucous membrane. With i / m administration, C _max is reached after 5-15 min. Binding to blood plasma proteins is 60-80% (depending on the dose).

Easily passes through histohematological barriers, including the blood-brain barrier. First enters tissues with good blood supply (heart, lungs, brain, liver, spleen), then – into adipose and muscle tissue. Penetrates through the placenta, in the body of the newborn is found 40-55% of the concentration of the drug administered to the woman in labor.

It is metabolized by 90% in the liver by oxidative N-dealkylation with the formation of active metabolites: monoethylglycine xylidine and glycine xylidine with T _½ 2 and 10 hours, respectively. It exhibits a first-pass effect.

In case of impaired liver function, T _½ may increase more than 2 times. 5-20% is excreted unchanged in the urine.

Local anesthesia (terminal, infiltration, conduction) in surgery, ophthalmology, dentistry, otorhinolaryngology; blockade of peripheral nerves and nerve plexuses for various pain syndromes.

Before using lidocaine hydrochloride, a skin test for hypersensitivity to the drug is mandatory, as evidenced by swelling and redness at the injection site.

For local anesthesia, use by injection (s/c, i/m) and topically on mucous membranes. Intravascular administration of the drug should be avoided.

For conduction anesthesia (including for anesthesia of the brachial and sacral plexuses), administer 5-10 ml of solution (100-200 mg of the drug).

For anesthesia of fingers, extremities, nose, ears, enter 2-3 ml of solution (40-60 mg of the drug). The maximum dose of the drug for adults when used for conduction anesthesia is 10 ml (200 mg of lidocaine hydrochloride).

For all types of injection anesthesia, it is possible to combine lidocaine with adrenaline (1:50,000-1:100,000; prepare ex tempore, add 1 drop of 0.1% epinephrine solution to 5-10 ml of 2% lidocaine solution), except in cases where the systemic effect of adrenaline (adrenaline) is undesirable (hypersensitivity to epinephrine, hypertension, diabetes mellitus, glaucoma) or a short-term anesthetic effect is necessary. Epinephrine helps to slow the absorption of lidocaine and prolongs its effect.

For anesthesia in ophthalmology, instill 2 drops of the solution into the conjunctival sac 2-3 times with an interval of 30-60 seconds immediately before the examination or surgical intervention.

For terminal anesthesia, apply a lidocaine solution to the mucous membranes in a volume of no more than 20 ml for adults at a dose of up to 2 mg/kg of body weight, the duration of anesthesia is 15-30 minutes. The maximum dose of the solution for adults is 20 ml.

In children, for all types of peripheral anesthesia, the total dose of lidocaine hydrochloride should not exceed 3 mg/kg body weight.

Individual hypersensitivity to the components of the drug, as well as to other amide local anesthetic drugs; history of epileptiform seizures associated with the administration of lidocaine hydrochloride; AV block II and III degree, complete transverse heart block; sick sinus syndrome; Wolff-Parkinson-White syndrome, Adams-Stokes syndrome; severe forms of heart failure (II-III degree); severe arterial hypotension; severe bradycardia; cardiogenic shock; myasthenia gravis; hypovolemia; porphyria; severe renal and / or hepatic failure; retrobulbar administration to patients with glaucoma; blood coagulation disorders, anticoagulant therapy; infections at the injection site; non-contact patients.

When using the drug, side effects are possible:

from the cardiovascular system: decreased blood pressure, tachycardia – when administered with a vasoconstrictor, bradycardia, peripheral vasodilation, collapse, tachycardia, palpitations, chest pain, heart pain, arrhythmia, slowing of cardiac conduction, transverse heart block, ventricular fibrillation, cardiac arrest; very rarely – arterial hypertension;

from the central and peripheral nervous system: excitation of the central nervous system (when used in high doses), anxiety, dizziness, confusion, drowsiness, sleep disturbances, headache, weakness, motor restlessness, euphoria, nystagmus, loss of consciousness, sensory disturbances, paresthesia, numbness of the tongue and lips (when used in dentistry); in patients with increased sensitivity – euphoria, tremor, trismus, muscle twitching, motor restlessness, convulsions (the risk of their development increases against the background of hypercapnia and acidosis); persistent anesthesia, paresis or plegia of the lower extremities and loss of sphincter control (for example, cauda equina syndrome) – causes more often than other local anesthetics, motor and sensory block, dysarthria, dysphagia, coma;

on the part of the organs of vision: visual impairment, blurred vision, diplopia, nystagmus, flashing flies before the eyes, dilated pupils, photophobia, reversible blindness, conjunctivitis;

from the organ of hearing: hearing impairment, tinnitus, hyperacusis;

mental disorders: anorexia, irritability, restlessness, hallucinations, depression, feelings of anxiety, sleep disturbances, state of excitement;

from the respiratory system, chest and mediastinal organs: rhinitis, shortness of breath, difficulty breathing, feeling of suffocation, respiratory depression, bronchospasm, paralysis of the respiratory muscles, respiratory paralysis (more often develops during subarachnoid anesthesia), respiratory arrest;

from the digestive tract: nausea, vomiting, involuntary defecation, abdominal pain;

Urinary system: involuntary urination;

Skin and subcutaneous tissue disorders: hyperemia, itching, rash, urticaria;

from the reproductive system: decreased libido and/or potency;

Immune system disorders: hypersensitivity reactions, including angioedema, generalized exfoliative dermatitis, anaphylactic shock, anaphylactic reaction, immune system suppression;

reactions at the injection site: a slight burning sensation that disappears with the development of the anesthetic effect (within 1 min), edema, hyperemia, itching, rash, thrombophlebitis, local nerve damage at the injection site; with spinal or epidural anesthesia, pain in the back, lower extremities, partial / complete spinal blockade may be observed, which is accompanied by a decrease in blood pressure, impaired defecation, involuntary urination, impotence, loss of sensitivity in the perineum (the likelihood of these effects increases when using high doses or in the event of accidental injection of lidocaine into the spinal space, when the dose intended for injection into the epidural space enters the spinal space); in some cases, after such an intervention, the restoration of motor, sensory and / or vegetative function occurs slowly (after several months) or incompletely;

general disorders: persistent anesthesia, hypothermia, sensation of heat, cold or numbness of the extremities, malignant hyperthermia, increased sweating, pale skin, edema, weakness.

Lidocaine can only be administered by medical professionals.

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

ECG monitoring is mandatory during the use of lidocaine. In case of sinus node dysfunction, prolongation of the PQ interval, widening of the QRS complex, or the development of a new arrhythmia, the dose should be reduced or the drug should be discontinued.

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

When performing planned subarachnoid anesthesia, MAO inhibitors must be discontinued at least 10 days before anesthesia.

When administering local anesthesia, special care should be taken when injecting the drug into areas with a large number of blood vessels. During the injection, it is necessary to avoid getting into the vessels.

When administered into vascularized tissues, an aspiration test is recommended.

Before the introduction of lidocaine in high doses, it is recommended to prescribe barbiturates. Care should be taken to prevent accidental subdural or intravasal administration of the drug. It is necessary to establish close monitoring for systemic toxic effects of the drug on the cardiovascular system and the central nervous system (since the doses prescribed for epidural anesthesia are always higher than for subdural).

Extreme caution should be exercised when performing paravertebral anesthesia in patients with neurological diseases, spinal deformity, septicemia, and severe hypertension.

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

Extreme caution should be exercised with retrobulbar administration, as severe side effects are possible: collapse, shortness of breath, seizures, reversible blindness.

It should be remembered that lidocaine has a pronounced antiarrhythmic effect and can itself act as an arrhythmogenic factor. Therefore, before administering the drug, it is necessary to collect a history of signs of arrhythmia and use the drug with caution in people with complaints of arrhythmias in the past.

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

With the intramuscular administration of lidocaine, the concentration of creatinine may increase, which may lead to an error in the diagnosis of acute myocardial infarction.

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

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

Special caution should be exercised when using lidocaine in patients with circulatory failure, hypovolemia, hypotension, hepatic and renal failure.

Use with caution in patients with CNS disorders who are taking narcotics, as sudden side effects from the cardiovascular system may occur. With prolonged use, blood electrolyte levels should be monitored. Use with caution in patients with a tendency to seizures, in a state of shock, in hypoxia.

Use during pregnancy and breastfeeding. Use during pregnancy is contraindicated.

If necessary, use of the drug should be discontinued.

Children: The drug is not used in children under 12 years of age.

The ability to influence the reaction rate when driving vehicles or other mechanisms. After using the drug, you should not engage in activities that require speed of psychomotor reactions.

Chlorpromazine, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline – when combined with lidocaine, the concentration of the latter in the blood plasma decreases.

Antiarrhythmic drugs (including amiodarone, verapamil, quinidine, disopyramide, ajmalin) – when combined with lidocaine, the cardiodepressive effect is enhanced, in particular, the QT interval is prolonged and in rare cases, AV blockade or ventricular fibrillation may develop. Simultaneous use with amiodarone may lead to the development of seizures.

Procainamide – when used in combination with lidocaine, delusions and hallucinations are possible.

Procaine, novocainamide – when used in combination with lidocaine, CNS disorders and hallucinations are possible.

Curare-like drugs – when used in combination with lidocaine, muscle relaxation increases (paralysis of the respiratory muscles is possible).

Ethanol – when used in combination with lidocaine, it enhances the predominant effect of the latter on breathing.

Vasoconstrictors (adrenaline, methoxamine, phenylephrine) – when used in combination with lidocaine, they help slow down the absorption of lidocaine and prolong the effect of the latter.

Cimetidine – when used in combination, it reduces the hepatic clearance of lidocaine (reduced metabolism as a result of inhibition of microsomal oxidation) and increases its concentration and the risk of developing toxic effects.

Guanadrel, guanethidine, mecamylamine, trimetaphan – when used in combination with lidocaine for spinal and epidural anesthesia, the risk of severe hypotension and bradycardia increases.

β-adrenergic blockers – when used in combination, they slow down the metabolism of lidocaine in the liver, enhance the effects of lidocaine (including toxic ones) and increase the risk of developing bradycardia and hypotension. When using β-adrenergic blockers and lidocaine simultaneously, it is necessary to reduce the dose of the latter.

Cardiac glycosides – when combined with lidocaine, the cardiotonic effect of cardiac glycosides is weakened.

Digitalis glycosides – against the background of lidocaine intoxication, it can increase the severity of AV blockade.

Hypnotics or sedatives – when used in combination with lidocaine, the predominant CNS effects of hypnotics and sedatives may be enhanced.

Narcotic analgesics (morphine) – when used in combination with lidocaine, the analgesic effect of narcotic analgesics is enhanced, but respiratory depression is also increased.

MAO inhibitors (furazolidone, procarbazine, selegiline) – when used in combination with lidocaine, the risk of developing arterial hypotension increases and the local anesthetic effect of the latter is prolonged. Lidocaine should not be used parenterally during treatment with MAO inhibitors.

Anticoagulants (including ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) – when used in combination with lidocaine, the risk of bleeding increases.

Anesthetics – when used in combination with lidocaine, the latter enhances the inhibitory effect on the respiratory center of anesthetics (hexobarbital, thiopental sodium intravenously).

Polymyxin B – when used in combination with lidocaine, respiratory function must be monitored.

Rifampicin – when used in combination with lidocaine, a decrease in the concentration of the latter in the blood is possible.

Propafenone – when used in combination with lidocaine, the duration and severity of CNS side effects may increase.

Prenylamine – when used in combination with lidocaine, the risk of developing torsades de pointes increases.

Anticonvulsants, barbiturates (phenytoin) – when used in combination with lidocaine, it is possible to accelerate the metabolism of lidocaine in the liver, reduce its concentration in the blood, and increase the cardiodepressive effect.

Isadrin, glucagon – when used in combination with lidocaine, the clearance of lidocaine increases.

Norepinephrine, mexiletine – when used in combination with lidocaine, the clearance of the latter decreases (toxicity increases); hepatic blood flow decreases.

Acetazolamide, thiazide and loop diuretics – when used in combination with lidocaine, as a result of hypokalemia, reduce the severity of the effect of the latter.

Midazolam – when used in combination with lidocaine, the concentration of the latter in the blood plasma increases.

Drugs that block neuromuscular transmission – when used in combination with lidocaine, the effect of drugs that block neuromuscular transmission is enhanced, since the latter reduce the conductivity of nerve impulses.

Incompatibility: The drug should not be mixed with other drugs in the same container, except for the solvents listed in the APPLICATION section.

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

The main symptoms are associated with depression of the central nervous system and cardiovascular system: general weakness, drowsiness, depression, dizziness, disorientation, tonic-clonic convulsions, coma, tremor, visual impairment, tinnitus, AV block, asphyxia, nausea, vomiting, euphoria, psychomotor agitation, asthenia, apnea, bradycardia, decreased blood pressure, collapse. The first symptoms of overdose in healthy people occur at a concentration of lidocaine hydrochloride in the blood of 0.006 mg/kg; convulsions – at 0.01 mg/kg.

Treatment: discontinuation of the drug, oxygen therapy, vasoconstrictors (noradrenaline, mezaton), anticonvulsants, anticholinergics. The patient should be in a horizontal position; it is necessary to ensure access to fresh air, oxygen supply and / or artificial respiration. Symptoms from the central nervous system should be corrected by using benzodiazepines or short-acting barbiturates. If an overdose occurs during anesthesia, a short-acting muscle relaxant should be used. To correct bradycardia and conduction disorders, use atropine (0.5-1 mg i.v.), with arterial hypotension – sympathomimetics in combination with β-blocker agonists. In case of cardiac arrest, immediate resuscitation measures are indicated. Intubation and mechanical ventilation are possible. In the acute phase of lidocaine overdose, dialysis is ineffective. There is no specific antidote.

In the original packaging at a temperature not exceeding 25 °C. Do not freeze.