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

The local anesthetic effect is due to the inhibition of nerve conduction by blocking the sodium channels in the nerve endings, which prevents the generation of pulses in the endings of the sensory nerves and pain impulses along nerve fibers. With topical application dilates blood vessels, does not have a locally irritating effect.

The effect develops within 1-5 minutes after application to the mucous membranes or skin and persists for 10-15 minutes.

Pharmacokinetics:

Quickly absorbed from mucous membranes.The rate of absorption is determined by the degree of blood supply to the mucous membrane, the total dose of the drug, the site localization and the duration of the application. After application to the mucous membrane of the upper respiratory tract is partially swallowed and inactivated in the gastrointestinal tract. Time to reach the maximum concentration in the plasma, when applied to the mucosa of the oral cavity and upper respiratory tract -10-20 min. It is quickly distributed in well-blood-supplying organs (heart, lungs, brain, liver, spleen), then in adipose and muscle tissues. Penetrates through the blood-brain and placental barriers, is secreted with the mother's milk (40% of the concentration in the mother's plasma).

Metabolised in the liver (by 90-95%) with participation of microsomal enzymes by dealkylation of the amino group and breaking of the amide bond with the formation of metabolites less active than lidocaine (monoethylglycinexylidine and glycinoxylidine, the half-life of which is 2 h and 10 h respectively). With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value.It is excreted with bile and kidneys (up to 10% unchanged). With chronic renal failure, cumulation of metabolites is possible.

Indications:

The drug can be used for local anesthesia in the following cases:

In dentistry:

- for terminal (superficial) anesthesia:

- Anesthesia of the mucosa at the injection site of anesthetics;

-closure of superficial abscesses;

-before applying sutures on the mucous membrane;

- Before fixing crowns and bridges;

-in the treatment of inflammation of the gums, paradontopathies;

-Traction of calculus;

-extraction of milk teeth;

- When making impressions (in case of using elastic material)

In otorhinolaryngology:

-coagulation with an electric cautery in the treatment of nasal bleeding;

-resuscitation of injection injection site before removal of tonsils;

In obstetrics and gynecology:

- removal of seams;

- processing of filamentous suppuration.

In dermatology:

burns (including sunny); bites, small wounds (including scratches); contact dermatitis (including caused by irritating plants).

Contraindications:Hypersensitivity.

Carefully:Hemorrhoidal bleeding (with rectal examination); local infection in the field of application; trauma to the mucous membrane or skin in the field of application; acute diseases; weakened patients; younger children's age, advanced age; pregnancy, lactation.

Dosing and Administration:

Locally. Preliminary impregnated with lidocaine cotton swab drug is applied a thin layer on mucous membranes or skin. With insufficient anesthesia, the drug can be repeated. The amount of gel with a single application from 0.5 to 1.0 g. The maximum dose for adults is 300 mg of lidocaine (6 g of gel), for children the dose of the drug should not exceed 2 g.

Side effects:

In the place of application of the drug - a slight burning sensation, which stops after anesthesia (within 1 minute), erythema.

Allergic reactions are possible: skin rash, itching, bronchospasm, angioedema, anaphylactic shock.

From the central nervous system systemic reactions (dose-dependent) can occur: headache, dizziness, convulsions, tremor, visual impairment (diplopia), tinnitus, agitation and / or depression, fear, euphoria, anxiety, fever, cold sensation, respiratory depression.

From the side of the cardiovascular system: increased blood pressure, bradycardia.

Overdose:

Symptoms: nausea, vomiting, pallor of the skin, headache, blurred vision, ringing in the ears, diplopia, decreased blood pressure, bradycardia, arrhythmia, psychomotor agitation, tremor, clonic-tonic convulsions, collapse, cardiac arrest.

Treatment: at the appearance of the first signs of intoxication (dizziness, nausea, vomiting, euphoria), the patient is transferred to a horizontal position and oxygen inhalation begins. With psychomotor excitation - intravenous (iv) administration of 10 mg of diazepam, with convulsions in / in the introduction of 1% solution of hexobarbital or thiopental sodium; with bradycardia - atropine (0.5-1 mg intravenously), sympathomimetic agents. Dialysis is not effective.

Interaction:

Cimetidine and propranolol reduces hepatic clearance of lidocaine (decrease in metabolism by inhibiting microsomal oxidation and reduction of hepatic blood flow) and increase the risk of toxic effects (including stunned state, drowsiness, bradycardia, paresthesia et al.).

Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) reduce efficacy (an increase in dose may be required).

When administered with aymalin, phenytoin, verapamil, quinidine, amiodarone, an increase in the negative inotropic effect is possible.

Co-administration with beta-blockers increases the risk of bradycardia. Cardiac glycosides weaken the cardiotonic effect, curare-like drugs increase muscle relaxation.

Procainamide increases the risk of excitation of the central nervous system, hallucinations.

With the simultaneous use of lidocaine and hypnotics, sedatives, it is possible to intensify their inhibitory effect on the central nervous system.

Under the influence of MAO inhibitors, local anesthetic action of lidocaine may be enhanced.

With the simultaneous use of lidocaine and polymyxin, it is possible to intensify the inhibitory effect on neuromuscular transmission, so in this case it is necessary to monitor the function of the patient's breathing.

Special instructions:Avoid contact with eyes and respiratory tract (risk of aspiration).

Form release / dosage:Gel for topical application 5%.

Packaging:For 15 g and 30 g in aluminum tubes, or 25 in dark glass jars. A tube or a jar, together with an instruction for use, is placed in a pack of cardboard.

Storage conditions:

List B. At a temperature not higher than +20 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004166/07

Date of registration:26.11.2007

Expiration Date:Unlimited

The owner of the registration certificate:MOSCOW PHARMACEUTICAL FACTORY, CJSC MOSCOW PHARMACEUTICAL FACTORY, CJSC Russia

Manufacturer: & nbsp

MOSCOW PHARMACEUTICAL FACTORY, CJSC Russia

Information update date: & nbsp27.02.2018

Illustrated instructions

Instructions

Lidocaine (Lidocaine)