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

active ingredient: lidocaine hydrochloride monohydrate (in terms of lidocaine hydrochloride) - 10 mg, 20 mg, 100 mg; auxiliary substances: sodium chloride (for a dosage of 10 mg / ml and 20 mg / ml), sodium hydroxide 1M, water for injection.

Description:transparent colorless or slightly colored liquid.

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:

It has a local anesthetic effect, stabilizing the membranes of neurons, reducing their permeability for sodium ions, which prevents the generation and conduct of nerve impulses. It suppresses not only pain impulses, but also impulses of another modality.

The anesthetic effect of lidocaine is 2 to 6 times stronger than procaine (it acts faster and longer - up to 75 min, and after the addition of epinephrine - more than 2 h). With topical application dilates blood vessels, does not have a locally irritating effect on the tissue.

Has antiarrhythmic (lb class) properties. Stabilizes cell membranes, blocks sodium channels, increases membrane permeability for potassium ions. Almost without affecting the electrophysiological state of the atrium, accelerates repolarization in the ventricles, depresses the phase IV depolarization in the fibers

Purkinje (especially ischemic myocardium), reducing their automatism and duration of action potential, increases the minimum potential difference at which cardiomyocytes react to premature stimulation.

In therapeutic doses, it improves conductivity in Purkinje fibers and at the site of their connection with ventricular contractile myocardium, thereby helping to eliminate the conditions for the formation of the phenomenon of "re-entry", especially under conditions of ischemic damage to the heart muscle, for example, in myocardial infarction. Shortens the duration of the action potential and effective refractory period.

Virtually does not affect the conductance and contractility of the myocardium (conduction suppression is noted when administered only in large, close to toxic doses) - the duration of the intervals P-Q, Q-T and width of the QRS complex on the electrocardiogram (ECG) does 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:

For parenteral administration, the degree of absorption depends on the site of administration and the dose. ТСmах - 3 - 5 minutes. Connection with plasma proteins - 50 - 80%. It is distributed rapidly (T1 / 2 phases of distribution - 6-9 min), first it enters well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. It penetrates the blood-brain barrier, the placental barrier and into breast milk (40% of the concentration in the mother plasma).

Metabolised in the liver (90 - 95%) with the participation of cytochrome P450 by dealkylating the amino group and breaking the amide bond to form active metabolites (monoethylglycinexylidine and glycinexylidine), T1 / 2 of which are 2 h and 10 h respectively. With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value. T1 / 2 after IV bolus injection - 1,5 - 2 hours; in newborns - 3 hours. With prolonged infusion of lidocaine within 24-48 h, T1 / 2 significantly increases (up to 3 hours). If there is a violation of liver function, T1 / 2 increases 2 times or more.With constant infusion (without the introduction of the initial saturating dose), the therapeutically effective concentration (2-6 μg / ml) is achieved after 5-9 hours.

It is excreted with bile and kidneys (up to 10% unchanged). With chronic renal failure, cumulation of metabolites is possible. Acidification increases the excretion of lidocaine.

Indications:

- conductor (including retrobulbar, parabulbar anesthesia);

- local infiltration anesthesia (including subconjunctival);

- spinal anesthesia; -Epidural anesthesia;

- terminal anesthesia in ophthalmology;

relief of persistent 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 glycoside intoxication.

Contraindications:

Hypersensitivity (including other amide local anesthetic drugs); infection of the site of the proposed injection; syndrome of weakness of the sinus node; atrioventricular blockade of III degree (except for the case,when a probe was inserted to stimulate the ventricles); sinoauric blockade; Wolff-Parkinson-White syndrome; cardiogenic shock; violations of intraventricular conduction.

If you have any of these diseases, consult a doctor before taking the drug.

Carefully:

Chronic heart failure II - III grade, severe hepatic and / or renal failure, hypovolemia, atrioventricular blockade, sinus bradycardia, arterial hypotension, severe myasthenia gravis, epileptiform convulsions (including in anamnesis), pregnancy, lactation.

If you have any of the listed diseases / conditions, always consult a doctor before taking the drug.

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: perineural, 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: epidurally, 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) /

For parabulbar anesthesia: Parabulbar injection of 1.0-2.0 ml of a 20 mg / ml solution.

For retrobulbar anesthesia: the introduction of retrobulbarno 3.0-4.0 ml of 20 mg / ml solution.

For local infiltration anesthesia (subconjunctival): administration of 0.5-1.0 ml of a 20 mg / ml solution of lidocaine hydrochloride under the conjunctiva.

Terminal anesthesia in ophthalmology: a solution of 20 mg / ml is instilled into the W 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% 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%.

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 diluted solution is used to administer a loading dose. The introduction begins with a loading dose of 1-1.5 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 administration (against a background of constant infusion) at a dose of 1 / 2-1 / 3 loading dose, with an interval of 8-10 minutes.

The maximum dose per hour is 300 mg, per day 2000 mg. Intravenous infusion is usually carried out for 12-24 hours with a constant electrocardiogram monitoring, after which the infusion is stopped to assess the need for a change in 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 side of the nervous system and sensory organs: dizziness, headache, weakness, motor anxiety, nystagmus, loss of consciousness, drowsiness, visual and auditory disorders, tremor, trismus, convulsions (the risk of their development increases against hypercapnia and acidosis), respiratory muscle paralysis , respiratory arrest, motor and sensory block, respiratory paralysis (often develops with subarachnoid anesthesia).

From the cardiovascular system: increase or decrease in blood pressure, bradycardia, arrhythmia, tachycardia - when administered with a vasoconstrictor, peripheral vasodilation, collapse, pain in the chest. Allergic reactions: skin rash, urticaria (on the skin and mucous membranes), skin itching, angioedema, anaphylactic shock.

On the part of the organs of the gastrointestinal tract: nausea, vomiting, involuntary defecation.

From the side of the blood: methemoglobinemia.

Local reactions: with spinal anesthesia - pain in the back, with epidural anesthesia - accidental entry into the subarachnoid space. Other: persistent anesthesia, respiratory depression, up to a stop, hypothermia.

If any adverse side reaction occurs, consult a doctor as soon as possible.

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria, asthenia, lowering blood pressure, drowsiness, headache, paresthesia, disorientation, visual impairment, convulsions, coma; then - convulsions of mimic muscles of the face with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, bradycardia, collapse, asystole; in the newborn (when used in childbirth) - bradycardia, oppression of the respiratory center, until the respiratory arrest.

Treatment: when the first signs of intoxication appear, the administration is discontinued, the patient is transferred to a horizontal position; prescribe oxygen inhalation. When convulsions are administered intravenously, 10 mg of diazepam. With bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is ineffective.

Interaction:

Vase-converters (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

Cimetidine reduces hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation) and increases the risk of toxic effects.

Reduces the effect of antimiasthenic drugs.

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

With the use of local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimethofan camzilate, the risk of severe hypotension and bradycardia increases. Beta-adrenoblockers slow the metabolism of lidocaine, increasing its toxicity (lowering the value of hepatic blood flow). Cardiac glycosides weaken the cardiotonic effect. Strengthens and lengthens the effect of myorelaxing drugs. With the simultaneous administration of lidocaine and hypnotics and sedatives, it is possible to intensify their inhibitory effect on the central nervous system.

When combined with narcotic analgesics, an additive effect develops, which is used in epidural anesthesia, but respiratory depression is increased.

Use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of lowering blood pressure.

Anticoagulants (including ardeparin sodium, dalteparin sodium, sodium danaparoid, sodium enoxaparin, heparin sodium, warfarin and others) increase the risk of bleeding.

Special instructions:

Particular caution should be exercised when carrying out local anesthesia of vascular-rich organs; Avoid intravascular injection during administration. When administered to a vascularized tissue, an aspiration test is recommended. It is necessary to abolish monoamine oxidase (MAO) inhibitors no less than 10 days before planning a subarachnoid anesthetic with lidocaine.

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

Form release / dosage:

Solution for injection 10 mg / ml, 20 mg / ml, 100 mg / ml.

Packaging:

3.5 ml (for a solution of 10 mg / ml), 5 ml or 10 ml (for a solution of 10 mg / ml and 20 mg / ml) and 2 ml (for a solution of 20 mg / ml and 100 mg / ml) in ampoules of neutral glass.

For 10 ampoules, together with the instruction for use and the ampoule opening opener or ampoule scarifier, is placed in a cardboard box.

5 ampoules (for ampoules 2 ml, 3.5 ml) into a contiguous cell pack made of polyvinylchloride film and aluminum foil printed lacquered or foil-free.

2 contour squares, together with instructions for use and a knife for opening ampoules or a scarifier, are placed in a pack of cardboard.

When using ampoules with notches, rings and break points, the ampoule opener opener or ampoule scarifier is allowed not to be inserted.

Storage conditions:In the dark place at a temperature of 5 to 25 ° C. Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N001261 / 01

Date of registration:05.05.2008/08.07.2013

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp15.04.2016

Illustrated instructions

Instructions

Lidocaine (Lidocaine)