Lidocaine, 20 mg/ml 2 ml 10 pcs

Pharmacodynamics:

Lidocaine is a short-acting local amide type anesthetic. Its mechanism of action is based on reduction of 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. Lidocaine is used to achieve conductive anesthesia in various parts of the body and to control arrhythmias. It has a rapid onset of action (about one minute after intravenous injection and fifteen minutes after intramuscular injection) and spreads quickly to surrounding tissues. The action lasts 10-20 minutes and about 60-90 minutes after intravenous and intramuscular injection, respectively.

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Indications

Infiltration (including subconjunctival), conduction (including retrobulbar, parabulbar anesthesia), spinal and epidural anesthesia.

. Constant paroxysms of ventricular tachycardia (including myocardial infarction and cardiac surgery), prevention of recurrent ventricular fibrillation in acute coronary syndrome and recurrent paroxysms of ventricular tachycardia (usually within 12-24 hours), ventricular arrhythmias due to glycoside intoxication (100 mg/ml solution is used).

Active ingredient

Composition

1 ml contains:

The active ingredients:

lidocaine hydrochloride (in terms of anhydrous substance) 20 mg

Associates:

Sodium chloride – 3 mg,

d/i water – up to 1 ml.

How to take, the dosage

For infiltration anesthesia: intramuscular, intradermal, subcutaneous. Lidocaine solution 5 mg/ml (maximum dose 400 mg) is used.

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 (maximum 400 mg).

For conduction anesthesia: 10 mg/ml and 20 mg/ml solutions (not more than 400 mg) are used perineurally.

For epidural anesthesia: epidurally, 10 mg/ml or 20 mg/ml solutions (not more than 300 mg).

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

In order to prolong the effect of lidocaine it is possible to add ex tempore 0.1% solution of epi- nephrine (adrenaline) (1 drop per 5-10 ml of lidocaine solution, but no more than 5 drops for the entire solution volume).

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

Dose adjustment is not required in chronic renal failure.

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

over 1 year of age, 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 100 mg/ml solution 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. The administration starts with a loading dose of 1 mg/kg (for 2-4 minutes at a rate of 25-50 mg/min) with immediate initiation of a continuous infusion at a rate of 1-4 mg/min. Due to rapid distribution (half-life of approximately 8 min), 10-20 minutes after the first dose, a decrease in plasma concentration of the drug occurs, which may require repeated bolus administration (against the background of continuous infusion) in a dose equal to 1/2-1/3 of the loading dose, at intervals of 8-10 minutes. The maximum dose in 1 hour is 300 mg, in a day – 2000 mg.

The intravenous infusion is usually given for 12-24 hours with continuous ECG monitoring, after which the infusion is stopped to assess whether the patient needs to change antiarrhythmic therapy.

Intravenously in children, 1 mg/kg (usually 50-100 mg) as a loading dose at a rate of 25-50 mg/min (i.e., within 3-4 min); if necessary, the dose is repeated after 5 min, after which a continuous infusion is given. Intravenously as a continuous infusion (usually after a loading dose): maximum dose for children is 30 µg/kg/min.

Interaction

Beta-adrenoblockers and cimetidine increase the risk of toxic effects. Aimalin, amiodarone, verapamil and quinidine increase the negative inotropic effect.

Hepatic microsomal enzyme inducers (barbiturates, phenytoin, rifampicin) reduce the effectiveness of lidocaine.

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

Lidocaine reduces the effect of antimiasthenic agents.

The combined use with procainamide may cause central nervous system agitation and hallucinations.

Guanadrel, guanethidine, mecamylamine, trimetaphane camsylate increase the risk of marked reduction of blood pressure and bradycardia. Increases and prolongs the effects of muscle relaxants.

The combined use of lidocaine and phenytoin should be used with caution because the resorptive effects of lidocaine may be reduced and an undesirable cardiodepressant effect may develop.

Monoamine oxidase inhibitors may increase the local anesthetic effect of lidocaine and decrease blood pressure. Patients taking monoamine oxidase inhibitors should not prescribe lidocaine.

The simultaneous administration of lidocaine and polymyxin B may increase the inhibitory effect on neuromuscular transmission. In this case the respiratory function of the patient should be monitored.

When lidocaine is used in combination with hypnotics or sedatives, narcotic analgesics, hexenal or sodium thiopental, the central nervous system and respiratory depression may be increased. When lidocaine is administered intravenously to patients taking cimetidine, such undesirable effects as stunned state, somnolence, bradycardia, paresthesias and others are possible. This is due to increased plasma concentration of lidocaine, which is explained by the release of lidocaine from bonding with blood proteins, as well as a slowdown of its inactivation in the liver. If combined therapy with these drugs is necessary, the dose of lidocaine should be reduced.

The treatment of the injection site with disinfectant solutions containing heavy metals increases the risk of local reaction in the form of soreness and swelling.

Special Instructions

The prophylactic administration of the drug 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 frequency of asystole). If lidocaine is ineffective, it is necessary to first rule out hypokalemia; in emergency situations, there are several options for further action: cautious increase in the dose until the appearance of side effects on the central nervous system (lethargy, difficult speech); prescription, sometimes jointly, of class IA drugs (procainamide), transition to class III drugs (amioarone, brettilia tozilate).

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

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

Period of treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Sinus node weakness syndrome, marked bradycardia, grade II-III atrioventricular block (except when a probe is inserted to stimulate the ventricles), sinoatrial block, Wolf-Parkinson-White syndrome, acute and chronic heart failure (functional class III-IV), cardiogenic shock, MorgagniAdams-Stokes syndrome, intraventricular conduction disorders; Hypersensitivity to any of the components of the drug;

Pregnancy, lactation (penetrates through the placental barrier, excreted with the breast milk).

You also need to consider the general contraindications to the particular type of anesthesia.

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

Side effects

Nervous system, sense organs and mental disorders: depression or agitation of the central nervous system, nervousness, euphoria, headache, dizziness, drowsiness, general weakness, neurotic reactions, confusion or loss of consciousness, depression or respiratory arrest, disorientation, convulsions (risk of development increases with hypercapnia and acidosis), tinnitus, paresthesias, diplopia, nystagmus, photophobia, tremor, trismus of mimic muscles, anxiety.

Cardiovascular system disorders: decreased or increased blood pressure, cardiac conduction disorders, 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, itching).

In the digestive system: nausea, vomiting.

Others: feeling of “heat”, “cold” or numbness of extremities, persistent anesthesia, erectile dysfunction, malignant hyperthermia, methemoglobinemia, flickering “flickers” before eyes and tachycardia when administered simultaneously with vasoconstrictor.

Overdose

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

The treatment is discontinuation of the drug, pulmonary ventilation, oxygen inhalation. Symptomatic therapy. In seizures, 10 mg of diazepam is administered intravenously. In bradycardia – m-cholinoblockers (atropine), vasoconstrictors (norepinephrine, phenylephrine). Intubation, artificial lung ventilation, resuscitation measures are possible. Hemodialysis is ineffective.

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