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

Solution for intravenous administration: active substance: 2 ml of the solution contains 200 mg of lidocaine hydrochloride anhydrous (in the form of lidocaine hydrochloride monohydrate 213.31 mg); excipients: water for injection

Injection: active substance: in 2 ml of solution contains 40 mg of lidocaine hydrochloride anhydrous (in the form of lidocaine hydrochloride monohydrate 43 mg), auxiliary substances: sodium chloride for parenteral dosage forms, water for injection.

Description:Transparent colorless or almost colorless aqueous solution odorless.

Pharmacotherapeutic group:Local anesthetic, antiarrhythmic agent

ATX: & nbsp

N.01.B.B Amides

N.01.B.B.02 Lidocaine

C.01.B.B.01 Lidocaine

C.01.B.B Antiarrhythmic drugs Ib class

Pharmacodynamics:

Lidocaine in chemical structure refers to acetanilide derivatives. Has a pronounced local anesthetic and antiarrhythmic (lb class) action. The local anesthetic effect is due to the inhibition of nerve conduction by blocking the 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 Purkinje fibers (diastolic depolarization phase), reducing their automatism and duration of action potential, increases the minimal potential difference at which 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: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). Proteins of blood plasma bind 50 - 80% of the drug. It is quickly distributed (T1 / 2 phases of distribution - 6-9 minutes) in organs and tissues with good perfusion, incl. 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). Metabolized mainly in the liver (90-95% dose) with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycinexylide glycinexylidide, having a half-life of 2 hours and 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 24-48 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, conductive, spinal and epidural anesthesia. Terminal anesthesia (including in ophthalmology).

Coping and 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 (with the exception of cases when a probe is inserted to stimulate the ventricles); sinoatrial blockade, WPW syndrome, acute and chronic heart failure (III-IV FK); cardiogenic shock; marked reduction in blood pressure, Adams-Stokes syndrome; intraventricular conduction disorders

- hypersensitivity to any of the components of the drug;

- retrobulbar injection to patients with glaucoma;

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

Carefully:

Chronic heart failure of II-III degree, arterial hypotension, hypovolemia, atrioventricular blockade of I degree, sinus bradycardia, severe hepatic and / or renal failure, severe myasthenia gravis, epileptiform convulsions (including in 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 mestnoanesteziruyuschim in the anamnesis.

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: intradermally, subcutaneously, intramuscularly. 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).

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.

To prolong the action of lidocaine, it is possible to add ex tempore 0.1% adrenaline solution (1 drop per 5-10 ml 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%.

As an antiarrhythmic agent: intravenously. Lidocaine solution for intravenous administration of 100 mg / ml can be used only after dilution! 25 ml of 100 mg / ml solution should be diluted with 100 ml of physiological solution to a concentration of lidocaine 20 mg / ml. This diluted solution is used to administer 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 about 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 continuous infusion) 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.

The rate of excretion of the drug is reduced in heart failure and impaired liver function (cirrhosis, hepatitis) and in elderly patients, which requires a reduction in the dose and rate of drug administration by 25-50%.

With chronic renal failure, dose adjustment is not required.

Side effects:

From the nervous system, the sense organs: 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 cardiovascular system: reduction in blood pressure, peripheral vasodilation, collapse, chest pain, bradycardia (up to cardiac arrest).

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.

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 at birth in a newborn - bradycardia, oppression of the respiratory center, apnea.

Treatment: discontinuation of the drug, 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.

Reduces the cardiotonic effect of digitoxin.

It enhances the muscle relaxation of curare-like drugs.

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) lengthen the local anesthetic effect of lidocaine and can cause an increase in blood pressure and tachycardia.

Lidocaine reduces the effect of antimiasthenic drugs.

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

Guanadrel, guanethidine, mecamylamine, trimetaphan increase the risk of pronounced reduction in blood pressure and bradycardia. Strengthens and prolongs the action of muscle relaxants.

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 is enhanced and blood pressure is lowered. Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine parenterally.

With the simultaneous administration of lidocaine and polymiokisin B, 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 MAO inhibitors in at least 10 days, in case of planned use of lidocaine.

Care should be taken when carrying out local anesthesia of tissues with high vascularity, an aspiration test is recommended to avoid intravascular injection.

Effect on the ability to drive transp. cf. and fur: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 intravenous administration is 100 mg / ml.

Packaging:2 ml of the drug in ampoules of colorless glass of hydrolytic class I with two code rings (red and green) and a white line of the fault. 5 ampoules in the cell outline packaging. 2 contour squares, together with instructions for medical use, are placed in a cardboard box. Solution for injection 20 mg / ml. 2 ml per ampoule with a notch and with a green code ring, 5 ampoules in a contour acrylic package sealed with transparent PE film,20 contour mesh packages in a cardboard box with a sealed label together with instructions for use.

Storage conditions:At a temperature of 15 to 25 ° C, out of the reach of children.

Shelf life:5 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014235 / 03

Date of registration:26.09.2008

Expiration Date:Unlimited

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS Pharmaceutical Plant, ZAO Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp26.02.2018

Illustrated instructions

Instructions

Lidocaine (Lidocaine)