Lidocaine - instructions for use, dose, side effects, contraindications

Lidocaine in chemical structure refers to acetanilide derivatives. Has a pronounced local anesthetic and antiarrhythmic (lb class) action. Local anesthetic action is caused by oppression of nerve conduction due to blockade, sodium channels in nerve endings and nerve fibers. By its anesthetic action lidocaine significantly (2-6 times) exceeds procaine; the action of lidocaine develops faster and lasts longer - up to 75 minutes, while with simultaneous application with epinephrine - more than 2 hours. With topical application dilates blood vessels, does not have a locally irritating effect.

Antiarrhythmic properties of lidocaine are due to its ability to stabilize the cell membrane, block sodium channels, increase the permeability of membranes for potassium ions. Virtually without affecting the electrophysiological state of the atria, lidocaine accelerates repolarization in the ventricles, depresses the IV depolarization phase in the Purkinje fibers (the phase of diastolic depolarization), reducing their automatism and the duration of the action potential, increases the minimal, potential difference at which the myofibrils react to premature stimulation. The speed of rapid depolarization (phase 0) does not affect or slightly reduces. Has no significant effect on conduction and contractility of the myocardium (inhibits conductivity only in large, close to toxic doses). Intervals PQ, QRS and QT under its influence on ECG do not change. Negative inotropic effect is also expressed slightly and manifests itself briefly only with the rapid administration of the drug in large doses.

Pharmacokinetics:The time to reach the maximum concentration in the blood plasma after intramuscular injection is 5-15 minutes, with slow intravenous infusion without the initial saturating dose in 5-6 hours (in patients with acute myocardial infarction, up to 10 hours).With blood plasma proteins bind 50-80% of the drug. Rapidly distributed (half-life of the distribution phase - 6-9 minutes) in organs and tissues with good perfusion, including in the heart, lungs, liver, kidneys, then in muscle and adipose tissue. Penetrates through the blood-brain and placental barriers, is secreted with the mother's milk (up to 40% of the concentration in the mother's plasma). It is metabolized primarily in the liver (90-95% of the dose) with the participation of microsomal enzymes with formation of active metabolites -monoetilglitsinksilidida glitsinksilidida and having a half-life of 2 hours or 10 hours, respectively. The intensity of metabolism decreases with liver diseases (can be from 50 to 10% of the normal value); if there is a violation of liver perfusion in patients after myocardial infarction and / or with congestive heart failure. Half-life with continuous infusion for 24 to 48 hours - about 3 hours; if the kidney function is impaired - can increase 2 or more times. It is excreted with bile and urine (up to 10% unchanged). Acidification increases the excretion of lidocaine.

Indications:

- Infiltration (including Subconjunctival), conductive (including retrobulbar, parabulbar anesthesia), spinal and epidural anesthesia;

- Terminal anesthesia in ophthalmology;

- Stimulation of resistant paroxysms of ventricular tachycardia, including myocardial infarction and cardiosurgical interventions;

- Prevention of recurrent ventricular fibrillation in acute coronary syndrome and repeated paroxysms of ventricular tachycardia (usually within 12-24 hours);

- Ventricular arrhythmias due to glycosidic intoxication.

Contraindications:

- syndrome of weakness of the sinus node; severe bradycardia; atrioventricular blockade of II-III degree (except for cases when a probe for ventricular stimulation has been introduced), sinoatrial blockade, WPW syndrome, acute and chronic heart failure (III-IV FK), cardiogenic shock, Adams-Stokes syndrome, intraventricular conductivity;

- hypersensitivity to any of the components of the drug;

- pregnancy, breastfeeding (penetrates the placental barrier, excreted in breast milk).

Carefully:

Chronic heart failure (II FK), arterial hypotension, hypovolemia, atrioventricular blockade of the 1st degree, sinus bradycardia, severe hepatic and / or renal insufficiency, severe myasthenia gravis, epileptiform convulsions (including in the anamnesis), decreased hepatic blood flow, weakened or elderly patients (over 65 years of age), children under 18 years of age (due to delayed metabolism, possible accumulation of the drug), hypersensitivity to other amide local anesthetics in history.

It is also necessary to take into account the general contraindications to the conduct of a particular type of anesthesia.

Dosing and Administration:

- for infiltration anesthesia: intradermal, subcutaneous, intramuscular. Apply a solution of lidocaine 5 mg / ml (maximum dose of 400 mg).

- for blockade of peripheral nerves and nerve plexuses: perineurally, 10-20 ml of a solution of 10 mg / ml or 5-10 ml of a solution of 20 mg / ml (not more than 400 mg).

- for conductive anesthesia: perineurally apply solutions of 10 mg / ml and 20 mg / ml (not more than 400 mg).

- for epidural anesthesia: epidural, solutions of 10 mg / ml or 20 mg / ml (not more than 300 mg).

- for spinal anesthesia: subarachnoid, 3-4 ml of a solution of 20 mg / ml (60-80 mg).

- terminal anesthesia in ophthalmology: a solution of 20 mg / ml is instilled in the conjunctival sac by 2 drops 2-3 times at intervals of 30-60 seconds immediately before surgery or examination.

- parabulbar anesthesia - parabulbar injection of 1.0-2.0 ml of lidocaine hydrochloride solution 20 mg / ml.

- retrobulbar anesthesia - the introduction of retrobulbarno 3.0-4.0 ml of a solution of lidocaine hydrochloride 20 mg / ml.

- subconjunctival - the injection of 0.5-1.0 ml of a solution of lidocaine hydrochloride 20 mg / ml under the conjunctiva.

To prolong the action of the lidocaine, it is possible to add ex tempore a 0.1% solution of epinephrine (adrenaline) (1 drop per 5-10 ml of lidocaine solution, but not more than 5 drops for 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%. With chronic renal failure, dose adjustment is not required. As an antiarrhythmic drug: intravenously, 25 ml of a solution of 100 mg / ml, 100 ml of physiological solution should be diluted to a lidocaine concentration of 20 mg / ml. This solution is used to introduce a loading dose.The administration 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 a repeated bolus administration (against a background of constant infusions) at a dose of 1 / 2-1 / 3 loading dose, with an interval of 8-10 minutes. The maximum dose at 1 hour is 300 mg, per day 2000 mg.

Intravenous infusion is usually performed for 12-24 hours with constant ECG monitoring, after which the infusion is discontinued to assess the need for changing antiarrhythmic therapy in the patient.

Side effects:

From the nervous, the system, the sense organs and the psyche: euphoria, headache, dizziness, drowsiness, general weakness, neurotic reactions, confusion or loss of consciousness, disorientation, convulsions, tinnitus, paresthesia, diplopia, nystagmus, photophobia, tremor, trimesus of facial muscles, anxiety.

From the side of the cardiovascular system: lowering blood pressure, arrhythmia,bradykirdia, peripheral vasodilation, collapse, chest pain, cardiac arrest, tachycardia with concomitant administration with a vasoconstrictor.

Allergic reactions: skin rash, hives, itching, angioedema, anaphylactic shock.

From the digestive system: nausea, vomiting.

Other: sensation of "heat" or "cold", persistent anesthesia, erectile dysfunction,

hypothermia, methemoglobinemia, flashing of "flies" before the eyes.

Overdose:Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria, lowering blood pressure, asthenia; then - convulsions of mimic muscles with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, bradycardia, asystole, collapse; when used during childbirth, a newborn can: bradycardia, respiratory center depression, apnea. Treatment: discontinuation of injection, inhalation with oxygen. Symptomatic therapy. With convulsions intravenously administered 10 mg of diazepam. With bradycardia, m holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Hemodialysis is ineffective.

Interaction:

Beta-blockers and cimetidine increase the risk of toxic effects. It enhances the muscle relaxation of curare-like drugs and muscle relaxants. Aymalin, amiodarone, verapamil and quinidine increase the negative inotropic effect.

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

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

Co-administration with procainamide can cause excitation of the central nervous system, hallucinations.

Guanadrel, guanethidine, mecamylamine, trimetaphane camsylate increase the risk of pronounced reduction in blood pressure and bradycardia.

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

Under the influence of monoamine oxidase inhibitors, it is likely that local anesthetic action of lidocaine and. lowering blood pressure.

Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine parenterally.

With the simultaneous administration of lidocaine and polymyxin B, the inhibitory effect on neuromuscular transmission may be enhanced. In this case, it is necessary to monitor the function of the patient's breathing.

With the combined use of lidocaine with hypnotics or sedatives, narcotic analgesics, hexenal or thiopental sodium, it is possible to intensify the inhibitory effect on the central nervous system and respiration. When intravenous lidocaine is administered to patients receiving cimetidine, such undesirable effects as stunnedness, drowsiness, bradycardia, paresthesia, etc. are possible. This is due to the increase in lidocaine in the blood plasma, which is explained by the release of lidocaine from the connection with blood proteins, as well as the slowing of its inactivation in the liver. If the need for combined therapy with these drugs should reduce the dose of lidocaine.

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

Special instructions:

It is necessary to abolish monoamine oxidase inhibitors in at least 10 days, in case of planned use of lidocaine.

Caution should be exercised when carrying out local anesthesia of tissues with high vascularity, an aspirate test is recommended to avoid intravascular injection.

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

Form release / dosage:

Solution for injection 20 mg / ml or 100 mg / ml.

Packaging:

To 2 ml in the ampoules of neutral glass HC-3. 10 ampoules together with the instruction for use are placed in a pack of cardboard. 5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film and aluminum foil lacquered, or wrapping paper with a polymer coating. 2 contour squares, together with instructions for use, are placed in a pack of cardboard.

In each pack insert knife ampoule or scarifier. When you pack the ampoules with a white point or a white rupture ring, the ampoule knife or scarifier does not insert.

Storage conditions:

In dry, dark place at a temperature of no higher than 30 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007747/09

Date of registration:02.10.2009/20.10.2014

The owner of the registration certificate:Armavir Biofactory, FKPArmavir Biofactory, FKP Russia

Manufacturer: & nbsp

Armavir Biofactory, FKP

Information update date: & nbsp13.04.2016

Illustrated instructions

Instructions

Lidocaine (Lidocaine)