Lidocaine bufus Renewal solution for injection 10% 2ml ampoules, 10pcs

Composition

Active ingredient: Lidocaine hydrochloride (in terms of anhydrous substance) − 100 mg Excipients:  sodium chloride-6 mg sodium hydroxide (0.1 M sodium hydroxide solution) – up to pH 5.0-7.0 water for injection-up to 1 ml

Pharmacological action

It has an antiarrhythmic (Ib class) effect. It stabilizes cell membranes, blocks sodium channels, and increases the permeability of membranes to potassium ions. Practically without affecting the electrophysiological state of the atria, lidocaine accelerates repolarization in the ventricles, inhibits phase IV depolarization in Purkinje fibers (especially in ischemic myocardium), reduces their automatism and duration of the action potential, increases the minimum potential difference at which myofibrils respond to premature stimulation. Shortens the duration of the action potential and effective refractory period. It does not significantly affect the conduction and contractility of the myocardium (inhibition of conduction is noted when prescribed only in large, close to toxic doses) – the duration of the PQ, QT intervals and the width of the QRS complex do not change on the electrocardiogram. The negative inotropic effect is also expressed insignificantly and is manifested for a short time only with rapid use of the drug in large doses. Pharmacokinetics of absorption 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 drug in the blood. Distribution Lidocaine binds to plasma proteins, including α1-acid glycoprotein (AH) and albumin. The degree of binding is variable, approximately 66%. The plasma concentration of ACH 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. Metabolismlidocaine is metabolized in the liver, and about 90% of the administered dose undergoes N-dealkylation to form monoethylglycine xylidide (MEGX) and glycine xylidide (GX), both contributing 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%. Elimination 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 ACG, 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

Relief of persistent paroxysms of ventricular tachycardia, including during 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 during pregnancy and lactation

fertility There are no data on the effect of lidocaine on human fertility. Pregnancy is possible if the expected benefit to the mother exceeds the potential risk to the fetus and child. Breast-feedinglidocaine passes into breast milk in small amounts, and its oral bioavailability is very low. Therefore, the expected amount received in breast milk is very small, and therefore the potential harm to the baby is very low. The decision on the possibility of using lidocaine during breastfeeding is made by the doctor.

Contraindications

Hypersensitivity to the components of the drug; sinus node weakness syndrome, severe bradycardia (heart rate less than 50 beats per minute), atrioventricular (AV) block of II and III degrees (if an artificial pacemaker is not installed), sinoatrial block, WPW (Wolf-Parkinson-White syndrome), acute and chronic heart failure (NYHA functional class III-IV), cardiogenic shock, intraventricular conduction disorders; severe arterial hypotension, Morgagni Adams-Stokes syndrome. With caution Lidocaine should be administered with caution in patients with myasthenia gravis, epilepsy, grade II and III chronic heart failure, hypovolemia, grade I atrioventricular block, sinus bradycardia, severe hepatic and/or renal insufficiency, coagulopathy, complete and incomplete intracardiac conduction block, convulsive disorders, Melkerson – Rosenthal syndrome, porphyria, reduced hepatic blood flow weak or elderly patients (over 65 years of age), children under 18 years of age (due to slow metabolism, accumulation of the drug is possible), as well as the third trimester of pregnancy.

Side effects

Adverse reactions are described in accordance with MedDRA organ-system classes. Immune system disorders Hypersensitivity reactions (allergic or anaphylactoid reactions, anaphylactic shock – – see also skin and subcutaneous tissue disorders. A skin allergy test for lidocaine is considered unreliable. Nervous system disorders and psychiatric disorders Neurological signs of systemic toxicity include dizziness, nervousness, tremor, paresthesia around the mouth, tongue numbness, drowsiness, convulsions, coma. Reactions from the nervous system can be manifested by its agitation or depression. Signs of stimulation of the central nervous system may be short-lived or not occur at all, as a result of which the first manifestations of toxicity may be confusion and drowsiness, followed by coma and respiratory failure. Visual disturbances Signs of lidocaine toxicity may include blurred vision, diplopia, and transient amaurosis. Hearing impairment and labyrinth of tinnitus, hyperacusis. Disorders of the cardiovascular systemcardiovascular reactions are manifested by hypotension, bradycardia, inhibition of contractile function of the myocardium (negative inotropic effect), arrhythmias; cardiac arrest or circulatory failure are possible. Respiratory system, thoracic and mediastinal disorders: dyspnea, bronchospasm, respiratory depression, respiratory arrest. Disorders of the gastrointestinal tract Nausea, vomiting. Skin and subcutaneous tissue disorders Rash, urticaria, angioedema, facial edema.

Interaction

It is undesirable to combine lidocaine with the following drugs:  With beta-blockers, due to the increased toxic properties of lidocaine, with digitoxin – due to the weakening of the cardiotonic effect, with curare-like drugs-muscle relaxation is enhanced.

It is not rational to prescribe lidocaine together with aimalin, amiodarone, verapamil or quinidine due to the increased cardiodepressive effect. The combined use of lidocaine and novocainamide can cause excitement of the central nervous system, hallucinations.

With intravenous use of hexenal or thiopental sodium against the background of lidocaine, respiratory depression is possible.

Under the influence of MAO inhibitors, the local anesthetic effect of lidocaine is likely to increase. Patients taking MAO inhibitors should not be given lidocaine parenterally.

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

Concomitant use of lidocaine with sleeping pills or sedatives may increase their depressing effect on the central nervous system. When lidocaine is administered intravenously to patients taking cimetidine, undesirable effects such as a state of deafness, drowsiness, bradycardia, parastesias, etc. are possible. This is due to an increase in the level 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.

Pharmaceutical interaction When used concomitantly, the following drugs increase the concentration of lidocaine in the blood serum: aminazine, cimetidine, propranolol, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline.

How to take it, course of use and dosage

• For infiltration anesthesia: intradermal, subcutaneous, intramuscular. 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).

Overdose

Symptoms.Toxicity from the central nervous system is manifested by symptoms that increase in severity. First, you may develop paresthesia around the mouth, tongue numbness, dizziness, hyperacusis, and tinnitus. Visual disturbances and muscle tremors or muscle twitches indicate more serious toxicity and precede generalized seizures. Then loss of consciousness and large convulsive seizures lasting from a few seconds to several minutes may occur. Seizures lead to a rapid increase in hypoxia and hypercapnia due to increased muscle activity and respiratory disorders. Apnea may develop. In severe cases, there are disorders of the cardiovascular system. At high systemic concentrations, hypotension, bradycardia, arrhythmia, and cardiac arrest can develop, which can be fatal. Resolution of overdose occurs due to the redistribution of the drug from the central nervous system and its metabolism, it can occur quite quickly (if a very large dose of the drug has not been administered). Treatment. If signs of overdose occur, the drug should be discontinued immediately. Seizures, central nervous system depression, and cardiotoxicity require medical intervention. The main goals of therapy are to maintain oxygenation, stop seizures, maintain blood circulation, and stop acidosis (if it develops). In appropriate cases, it is necessary to ensure the patency of the airways and prescribe oxygen, as well as to establish auxiliary ventilation of the lungs (masked or with the help of an Ambu bag). Blood circulation is maintained by infusions of plasma or infusion solutions. If long-term circulatory maintenance is necessary, vasopressors should be considered, but they increase the risk of arousal of the central nervous system. Control of seizures can be achieved by intravenous use of diazepam (0.1 mg / kg) or sodium thiopental (1-3 mg/kg), but it should be borne in mind that anticonvulsants can also depress respiration and blood circulation. Prolonged seizures may interfere with the patient’s ventilation and oxygenation, and early endotracheal intubation should be considered. In case of cardiac arrest, standard cardiopulmonary resuscitation is initiated. The effectiveness of dialysis in the treatment of acute lidocaine overdose is very low.

Special instructions

Lidocaine 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 increased bioavailability, potentiation of effects (for example, phenytoin) or prolongation of excretion (for example, in hepatic or end-stage renal failure, in which lidocaine metabolites can accumulate). Patients receiving Class III antiarrhythmic drugs (for example, amiodarone) should be closely monitored and ECG monitored, as the effect on the heart may be potentiated. Lidocaine has been shown to cause porphyria in animals, and its use in individuals with porphyria should be avoided. When administered to inflammatory or infected tissues, the effect of lidocaine may be reduced. Before starting intravenous use of lidocaine, it is necessary to eliminate hypokalemia, hypoxia and violation of the acid-base state. Lidocaine injection solution is not recommended for use in newborns. The optimal serum concentration of lidocaine to avoid toxicity such as seizures and arrhythmias in newborns has not been established. The effect of a drug for medical use on the ability to drive vehicles, mechanisms, depending on the dose and method of use, lidocaine may have a temporary effect on motor ability and coordination. 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

Solution for injection.

Storage conditions

Store in a dry place protected from light.

Shelf

life is 3 years.

Active ingredient

Lidocaine

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection