Lidocaine-SOLofarm Politvist solution for injection 20mg/ml 2ml ampoules plastic, 10pcs

Composition

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1 ml contains:

Active ingredients:

lidocaine hydrochloride (in terms of anhydrous substance) 20 mg

Auxiliary substances:

sodium chloride – 3 mg,

d/i water-up to 1 ml

Pharmacological action

Pharmacotherapeutic group: Local anesthetic. ATX:

N. 01. B. B Amides

N. 01. B. B. 02 Lidocaine

C. 01. B. B. 01 Lidocaine

C. 01. B. B Class Ib Antiarrhythmic drugs

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

Pharmacokinetics:

Absorption rate

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

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

Distribution

Lidocaine binds to plasma proteins, including α1-acid glycoprotein (AKT) and albumin. The degree of binding is variable, amounting to approximately 66%. The plasma concentration of AKT in newborns is low, so they have a relatively high content of the free biologically active fraction of lidocaine.

Lidocaine penetrates the blood-brain and placental barriers, probably through passive diffusion.

Metabolism

Lidocaine is metabolized in the liver, and about 90% of the administered dose undergoes N-dealkylation to form monoethylglycine xylidide (MEGX) and glycine silidide (GX), both contribute to the therapeutic and toxic effects of lidocaine. The pharmacological and toxic effects of MEGX and GX are comparable to those of lidocaine, but are less pronounced. GX has a longer half-life than lidocaine (about 10 hours) and can accumulate with repeated use.

Metabolites formed as a result of subsequent metabolism are excreted in the urine, the content of unchanged lidocaine in the urine does not exceed 10%.

Deduction

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

Special patient groups

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

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

In newborns, there is a low concentration of AKT, so the connection with plasma proteins may decrease. Due to the potentially high concentration of the free fraction, the use of lidocaine in newborns is not recommended.

Indications

Infiltration (including subconjunctival), conduction (including retro-bulbar, parabulbar anesthesia), spinal and epidural anesthesia.

Treatment of persistent paroxysms of ventricular tachycardia (including myocardial infarction and cardiac surgery), prevention of repeated ventricular fibrillation in acute coronary syndrome and repeated paroxysms of ventricular tachycardia (usually within 12-24 hours), ventricular arrhythmias caused by glycoside intoxication (use a solution with a concentration of 100 mg/ml).

Contraindications

syndrome of weakness of the sinus node, bradycardia, atrioventricular block degree II-III (except in cases when the probe is introduced to stimulate the ventricles), sinoatrial blockade, syndrome Wolff-Parkinson-white, acute and chronic heart failure (III-IV functional class), cardiogenic shock syndrome, Morgagni-Adams-Stokes, disorders of intraventricular conduction; hypersensitivity to any component of the drug;

pregnancy, lactation (crosses the placental barrier, excreted in breast milk).

It is also necessary to take into account the general contraindications to this or that type of anesthesia.

With caution: Chronic heart failure (functional class II), hypotension, hypovolemia, grade I atrioventricular block, sinus bradycardia, severe hepatic and/or renal failure, severe myasthenia gravis, epileptiform seizures (including in the anamnesis), reduced hepatic blood flow, weakened or elderly patients (over 65 years of age), children under 18 years of age (due to delayed metabolism, lidocaine accumulation is possible), hypersensitivity to other amide local anesthetics in the anamnesis.

Side effects

From the nervous system, sensory organs and psyche:  depression or agitation of the central nervous system, nervousness, euphoria, headache, dizziness, drowsiness, general weakness, neurotic reactions, confusion or loss of consciousness, respiratory depression or arrest, disorientation, convulsions (the risk of development increases against the background of hypercapnia and acidosis), tinnitus, paresthesia, diplopia, nystagmus, photophobia, tremor, trismus of facial muscles, anxiety.

From the cardiovascular system:  reduced or increased blood pressure, impaired cardiac conduction, arrhythmia, sinus bradycardia, peripheral vasodilation, collapse, chest pain, cardiac arrest.

Allergic reactions:  generalized exfoliative dermatitis, anaphylactic shock, angioedema, contact dermatitis (hyperemia at the application site, skin rash, urticaria, pruritus).

From the digestive system: nausea, vomiting.

Other services:  sensation of “heat”, “cold” or numbness of the extremities, persistent anesthesia, erectile dysfunction, malignant hyperthermia, methemoglobinemia, flickering of “flies” in front of the eyes and tachycardia when administered simultaneously with a vasoconstrictor.

Interaction

of Beta-blockers and cimetidine increases the risk of toxic effects. Aimalin, amiodarone, verapamil and quinidine enhance the negative inotropic effect.

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

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

Lidocaine reduces the effect of antimiasthenic drugs.

Concomitant use with procainamide may cause central nervous system arousal and hallucinations.

Guanadrel, guanethidine, mecamylamine, trimetafan camzilate increase the risk of severe lowering of blood pressure and bradycardia. Enhances and lengthens the effect of muscle relaxants.

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

Under the influence of monoamine oxidase inhibitors, the local anesthetic effect of lidocaine and blood pressure reduction are likely to increase. Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine.

With simultaneous use of lidocaine and polymyxin B, it is possible to increase the depressing effect on neuromuscular transmission. In this case, it is necessary to monitor the patient’s respiratory function.

With the combined use of lidocaine with sleeping pills or sedatives, narcotic analgesics, hexenal or thiopental sodium, it is possible to increase the depressing effect on the central nervous system and respiration. When lidocaine is administered intravenously to patients taking cimetidine, undesirable effects such as a state of deafness, drowsiness, bradycardia, paresthesia, etc. are possible. This is due to an increase in the concentration of lidocaine in blood plasma, which is explained by the release of lidocaine from binding to blood proteins, as well as a slowdown in its inactivation in the liver. If it is necessary to conduct a combination therapy with these drugs, the dose of lidocaine should be reduced.

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

How to take it, course of use and dosage

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

For blockade of peripheral nerves and nerve plexuses: perineurally,10-20 ml of 10 mg/ml solution or 5-10 ml of 20 mg/ml solution (no more than 400 mg).

For conducting anesthesia: solutions of 10 mg/ml and 20 mg/ml (no more than 400 mg) are used perineurally.

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

For spinal anesthesia: subarachnoid,3-4 ml of 20 mg/ml solution (60-80 mg). Parabulbar anesthesia: parabulbar,1-2 ml of lidocaine solution 20 mg / ml. Retrobulbar anesthesia: retrobulbar,3-4 ml of lidocaine solution 20 mg / ml. Subconjunctival anesthesia: use under the conjunctiva,0.5-1 ml of lidocaine solution 20 mg / ml.

To prolong the action of lidocaine, it is possible to add ex tempore 0.1% solution of epinephrine (epinephrine) (1 drop per 5-10 ml of lidocaine solution, but not more than 5 drops per the entire volume of the solution).

It is recommended to reduce the dose of lidocaine in elderly patients and patients with liver diseases (cirrhosis, hepatitis) or with reduced hepatic blood flow (chronic heart failure) by 40-50%.

In chronic renal failure, no dose adjustment is required.

For children under local anesthesia, the maximum dose in newborns is 4 mg / kg, in children

older than 1 year-5-7 mg/kg.

Lidocaine solution with a concentration of 100 mg / ml can be used only after dilution.

As an antiarrhythmic agent: intravenously,25 ml of a solution of 100 mg / ml should be diluted with 100 ml of 0.9% sodium chloride solution to a lidocaine concentration of 20 mg / ml. This diluted solution is used to administer a loading dose. use begins with a loading dose of 1 mg / kg (for 2-4 minutes at a rate of 25-50 mg / min) with immediate connection of a constant infusion at a rate of 1-4 mg / min. Due to the rapid distribution (half-life of approximately 8 minutes),10-20 minutes after the first dose, the concentration of the drug in the blood plasma decreases, which may require repeated bolus use (against the background of constant infusion) at a dose equal to 1/2-1/3 of the loading dose, with an interval of 8-10 minutes. The maximum dose in 1 hour is 300 mg, per day – 2000 mg.

Intravenous infusion is usually performed for 12-24 hours with continuous ECG monitoring, after which the infusion is stopped to assess the need for a change in antiarrhythmic therapy in the patient.

Intravenous jet in children – 1 mg / kg (usually 50-100 mg) as a loading dose at a rate of use of 25-50 mg / min (i. e. for 3-4 minutes); if necessary, the dose is repeated after 5 minutes, after which a continuous infusion is prescribed. Intravenous continuous infusion (usually after a loading dose): the maximum dose for children is 30 mcg/kg/min.

Overdose

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

Treatment – discontinuation of drug use, pulmonary ventilation, oxygen inhalation. Symptomatic therapy. For convulsions,10 mg of diazepam is administered intravenously. For bradycardia – m-cholinoblockers (atropine), vasoconstrictors (norepinephrine, phenylephrine). It is possible to perform intubation, artificial ventilation, resuscitation measures. Hemodialysis is ineffective.

Special instructions

Prophylactic use of the drug is not recommended for all patients with acute myocardial infarction without exception (routine prophylactic use of lidocaine may increase the risk of death by increasing the frequency of asystoles). If lidocaine is ineffective, first of all, hypokalemia should be excluded. In urgent situations, there are several options for further action: cautiously increasing the dose until side effects from the central nervous system appear (lethargy, difficult speech); prescribing, sometimes jointly, class IA drugs (procainamide), switching to class III drugs (amioarone, bretilia tosilate).

Monoamine oxidase inhibitors should be discontinued at least 10 days in advance if lidocaine is used as planned.

Caution should be exercised when performing local anesthesia of tissues with high vascularization, in order to avoid intravascular injection, it is recommended to conduct an aspiration test.

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

Form of production

The solution for injection is clear, colorless or slightly colored.

Storage conditions

In a dark place at a temperature of 15 to 25 °C. Keep out of reach of children.

Shelf

life is 4 years.. Do not use after the expiration date indicated on the package.

Active ingredient

Lidocaine

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection