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

Excipients: Ethanol 96% (rectified ethyl alcohol, Extra grade) - 18.4 mg, propylene glycol 4.6 mg, sodium hydroxide (sodium hydroxide) 0.23 mg, sodium saccharinate dihydrate (saccharin sodium) 0.138 mg, racemetol (menthol racemic) - 0.092 mg, purified water - up to 0.046 g.

Description:Pcolorless or with a yellowish tinge.

Pharmacotherapeutic group:Local anesthetic

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 is a local anesthetic of the amide type.

Local anesthetic effect is caused by reversible inhibition of nerve conduction due to blockade of sodium channels in nerve endings, which prevents the generation of impulses in the endings of the sensory nerves and pain impulses along nerve fibers.

Lidocaine has a rapid onset of action, high anesthetic activity and low toxicity.

With topical application dilates blood vessels, does not have a locally irritating effect. Possesses an analgesic 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 the mucous membranes (especially the pharynx and respiratory tract), the degree of absorption of the drug is determined by the degree of blood supply to the mucosa, the total dose of the drug, the localization of the site 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 (TC_mOh) in plasma when applied to the mucosa of the oral cavity and upper respiratory tract - 10-20 min. The connection with proteins depends on the concentration of the drug and is 60-80% at a drug concentration of 1-4 μg / ml (4.3-17.2 μmol / L). Distributed quickly (half-life (T_1/2) of the distribution phase - 6-9 minutes), first enters the well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue.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 glycinexylidine), T_1/2which is 2 hours and 10 hours, 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. Acidification increases the release of lidocaine.

Indications:

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

in dentistry - for terminal (superficial) anesthesia: anesthesia of the injection site before local anesthesia; opening of superficial abscesses; Before suturing the mucosa; before fixing the crowns and bridges; in the treatment of gum disease, periodontitis; extirpation of infant teeth; removal of tartar;

in otorhinolaryngology - operations on the nasal septum and removal of polyps of the nose; electrocoagulation in the treatment of nasal bleeding; elimination of the pharyngeal reflex and anesthesia of the injection site of the injection needle before removal of the tonsils; opening of peritonsillar abscesses; puncture of the maxillary sinus;

in Obstetrics and Gynecology - ehsziotomy and processing of the incision; removal of stitches; small surgery on the vagina and cervix; breakthrough of the hymen; treatment of filamentous suppuration;

with instrumental and endoscopic studies - before inserting the probe through the nose or mouth (including duodenal sounding and fractional examination of gastric secretion); with rectoscopy, intubation;

radiographic examination - elimination of nausea and pharyngeal reflex;

as an analgesic (analgesic) drug for burns (including sunburn); bites; contact dermatitis (including caused by irritating plants); small wounds (including scratches);

superficial anesthesia of the skin with small surgical interventions.

Contraindications:

- Hypersensitivity to lidocaine or any other componentpreparation;

- the use of lidocaine in the form of a spray for tonsillectomy and adenotomy in children under 8 years old.

Carefully:

- Instrumental studies (rectoscopy) in patients with hemorrhoidal bleeding;

- local infection in the field of application;

- trauma of the mucous membrane or skin in the area of application;

- severe somatic pathology;

- epilepsy;

- bradycardia, impaired cardiac conduction;

- impaired liver function;

- heavy shock;

- associated acute diseases;

- weakened patients;

- pregnancy, the period of breastfeeding;

- younger children's age;

- elderly age.

Pregnancy and lactation:

The results of controlled clinical studies in pregnant women are absent.

If it is necessary to use local anesthesia and there is no more safe treatment, the drug can be used during pregnancy.

Lidocaine is excreted into breast milk, but after applying the usual therapeutic doses, its amount given off with milk is too small to harm any infant.

Dosing and Administration:

Apply topically, externally.

Dosage may vary depending on the indications and the size of the zone to be anesthetized.

One dose of the spray, released by pressing the dosing valve, contains 4.6 mg of lidocaine.

Recommendations for the number of clicks in various applications:

Application area	Number of clicks
Stomatology	1-4
Otorhinolaryngology	1-4
Endoscopic and instrumental studies	2-3
Obstetrics	15-20
Gynecology	4-5
Dermatology	1-3

The drug can also be applied with a cotton swab soaked in it.

To avoid absorption of the drug in the systemic circulation, the minimum dose providing the effect should be applied. Usually enough 1-3 clicks; it is possible to apply 15-20 or more pressures (the maximum dose is 40 pressures per 70 kg of body weight).

In dental practice, it is preferable to use children in the form of lubrication (in order to avoid the fright of the child during spraying) by pre-impregnating a cotton swab.

Side effects:

In the place of application: mild burning, which stops after anesthesia (within 1 minute), erythema, edema, impaired sensitivity.

Allergic reactions: possible allergic contact dermatitis (hyperemia at the site of application, skin rash, hives, itching), angioedema, anaphylactic shock.

The drug should be discontinued if any allergic reaction occurs.

Frequency of systemic reactions after aerosol application Lidocaine extremely small, because A very small amount of active drug is applied, which can enter the bloodstream.

In the case of large doses, as well as with rapid absorption, hypersensitivity, idiosyncrasy, poor drug tolerance, the following side effects from the central nervous system and cardiovascular system can be observed.

From the central nervous system there may be systemic reactions: headache, dizziness, convulsions, tremor, blurred vision, tinnitus, arousal and / or depression, a sense of fear, euphoria, anxiety, fever, a feeling of cold, respiratory depression.

From the cardiovascular system: increasing blood pressure, lowering blood pressure, bradycardia, arrhythmia, suppression of myocardial function.

Other: urethritis (after topical application).

Overdose:

Symptoms: increased sweating, pale skin, nausea, vomiting, dizziness, headache, blurred vision, ringing in the ears, diplopia, lowering blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness, tremor, anxiety, agitation, convulsions, methaemoglobinaemia, heart failure.

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 is prescribed; at psychomotor excitation - intravenously 10 mg of diazepam; with convulsions - in / in 1% solution of hexobarbital or thiopental sodium; at a bradycardia - in / in 0,5-1 mg atropine, sympathomimetic agents (norepinephrine, phenylephrine). Dialysis is ineffective.

Interaction:

Vasoconstrictors (epinephrine, phenylephrine, methoxamine) extend the local anesthetic effect of lidocaine.

Cimetidine and propranolol decrease liver lidocaine clearance (decrease in metabolism due to inhibition of microsomal oxidation and decrease in hepatic blood flow) and increase the risk of toxic effects (incl.state of deafness, drowsiness, bradycardia, paresthesia, etc.).

Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) reduce the effectiveness of lidocaine (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 administration of lidocaine and hypnotics and sedatives, it is possible to intensify their inhibitory effect on the central nervous system.

With intravenous injection of hexobarbital or thiopental sodium on the background of the action of lidocaine, respiratory depression is possible.

Under the influence of monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) it is possible to strengthen the local anesthetic action of lidocaine. Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine parenterally.

With the simultaneous use of lidocaine and nolimixin, 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:

When using the bottle, keep it in a vertical position.

Avoid contact with eyes and respiratory tract (risk of aspiration). It requires special care application of the drug in the region of the posterior pharyngeal wall.

Application on the mucous membrane of the cheeks is accompanied by a risk of dysphagia and subsequent aspiration, especially in children.

When the sensitivity of the tongue and the mucous membrane of the cheeks is impaired, the risk of their biting increases.

Lidocaine is well absorbed through the mucous membranes (especially in the trachea) and damaged skin. This should be taken into account, especially when treating large areas of tissue in children.

In case of spray application in surgical operations in the pharynx or nasopharynx, it should be taken into account that lidocaine, suppressing the pharyngeal reflex, falls into the larynx and trachea and suppresses the cough reflex, which can lead to bronchopneumonia. This is especially important in children, because they often cause a pharyngeal reflex.In this regard, the spray is not recommended for local anesthesia before tonsillectomy and adenotomy in children under the age of 8 years.

Care should be taken when applying lidocaine to the damaged mucosa and / or infected areas.

The drug should be used with caution in patients with epilepsy, as well as with bradycardia, impaired conduction in the heart, impaired liver function and severe shock, especially when you can expect absorption of a significant amount of the drug when treating large areas of tissue with high doses.

Lower doses should be used in attenuated and elderly patients, in acute diseases, and in children - in accordance with age and general condition.

In children under 2 years of age Lidocaine Spray is recommended to apply with a cotton swab dipped in the preparation.

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:

Spray for topical and topical use dosed, 4.6 mg / dose.

Packaging:

For 20 g (not less than 340 doses) or 38 g (not less than 650 doses) in plastic bottles, sealed with a nozzle-sprayer, complete with an adapter.

One bottle with instructions for use is placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-004021

Date of registration:13.12.2016

Expiration Date:13.12.2021

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

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp26.02.2018

Illustrated instructions

Instructions

Lidocaine (Lidocaine)