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

The local anesthetic effect is due to the blockade of voltage-dependent sodium channels, 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. Possesses an analgesic effect.

The effect develops after 1-5 min after application to the mucous membranes or skin and persists for 30-60 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 ingested and inactivated in the gastrointestinal tract (GIT). Time to reach the maximum concentration (TCmax) 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). 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 GEB and the placental barrier, is secreted with the mother's milk (40% of the concentration in the mother's plasma).

Metabolised in the liver (by 90-95%) with the 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), 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. It is excreted with bile and kidneys (up to 10% unchanged). With chronic renal failure, cumulation of metabolites is possible.

Indications:Terminal (surface) anesthesia of mucous membranes: in dentistry (analgesia field injection before local anesthesia, suturing to the mucosa, the removal of movable milk teeth, removing plaque and gingival anesthesia before fixation crown or bridge, in children at step excision tongue bridle and autopsies sialocele), otorhinolaryngology (nasal septum surgery holding electrocoagulation et al.), obstetrics and gynecology (episiotomy and cut processing, removing welds, intrude on the vagina and cervix of the uterus, etc.); with instrumental and endoscopic studies (probe insertion, rectoscopy, intubation, etc.), radiographic examination (elimination of nausea and pharyngeal reflex); as an analgesic drug for burns (including sunburn), small wounds (including scratches); superficial anesthesia of the skin with small surgical interventions.

Contraindications:Hypersensitivity to lidocaine or any other component of the drug. Use of lidocaine in the form of a spray for tonsillectomy and adenotomy in children under 8 years of age.section "Special instructions").

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 field of application, severe somatic pathology, epilepsy, bradycardia, cardiac conduction disorder, liver function disorders, severe shock (see " Special instructions "), younger children's age, advanced age, pregnancy, lactation.

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, lidocaine Spray 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.

To avoid high concentrations of the drug in the blood plasma should be used at the lowest dose, at which a satisfactory effect is observed.

Usually, 1 to 2 strokes per valve are sufficient, but in obstetric practice, 15 to 20 or more doses are applied (a maximum of 1 to 40 doses per 70 kg of body weight).

Recommended doses for different indications

Application Dose (number of valve strokes)

Dentistry 1-3

Dental surgery 1-4

Otorhinolaryngology 1-4

Endoscopy 2-3

Obstetrics 15-20

Gynecology 4-5

Dermatology 1-3

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

Children

When carrying out dental procedures and operations, use in children Lidocaine The spray is preferably used with a cotton swab, which avoids fright when spraying the product, as well as a tingling sensation (the usual side effect).

Side effects:

Local effects:

Light tingling sensation during application; This sensation passes after the development of the effect (after 1 minute).

Transient erythema, edema and sensitivity disorders can be observed at the site of application.

Allergic reactions:

Very rarely there may be allergic reactions: urticaria, angioedema, bronchospasm, extremely rare Lidocaine in the form of a spray can cause anaphylactic shock.

The drug should be discontinued immediately if any allergic reaction occurs.

System Action:

The frequency of systemic effects after topical administration of the drug is extremely low, Only a very small amount of active substance can enter the bloodstream. In very rare cases, there may be symptoms of central nervous system (CNS) excitation or depression: nervous excitement, systemic dizziness, insomnia, loss of consciousness and respiratory paralysis.

Cardiovascular side effects: lowering blood pressure, suppressing myocardial function, bradycardia, cardiac arrest.

Overdose:

Symptoms: increased sweating, pale skin, dizziness, headache, blurred vision, ringing in the ears, diplopia, lowering blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness, tremor, anxiety, agitation, convulsions, methhemoglobinaemia, cardiac arrest.

Treatment: Further administration was stopped, the patient is transferred to a horizontal position when the first signs of intoxication (dizziness, nausea, euphoria); prescribe oxygen inhalation; with convulsions - in / in 10 mg of diazepam; at a bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is ineffective.

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.

Curare like drugs enhance muscle relaxation.

Procainamide increases the risk of developing CNS excitement, 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 iv 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, local anesthetic action of lidocaine is possible.

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

Special instructions:

Regional and local anesthesia should be performed by experienced specialists in an appropriately equipped room with access to equipment and medicines needed to stop unwanted reactions. Personnel performing anesthesia should be qualified and trained in anesthesia, should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

It is important not to let lidocaine enter the respiratory tract (risk of aspiration).

Application to the throat requires special attention.

Application to the mucous membrane of the cheeks is accompanied by a risk of dysphagia and subsequent aspiration, especially in children. If the sensitivity of the tongue and the mucous membrane of the cheeks are 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 cases of application of a spray during 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 swallowing 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.

During application, the vial should be kept as vertically as possible. The spray should not fall on eyes. Do not open the bottle, do not heat it.

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 dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Spray for topical use dosed with 4.6 mg / dose.

Packaging:For 38 g (650 doses) in a bottle of brown glass, with a capacity of 50 ml, equipped with a metering pump with a spray head. The bottle is put together with instructions for use in a cardboard box.

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 / 02

Date of registration:01.11.2008 / 28.12.2017

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)