Lidocaine Asept (Spray) Instructions for Use

Marketing Authorization Holder

Biogen NPTs OU (Russia)

ATC Code

N01BB52 (Lidocaine in combination with other drugs)

Active Substances

Chlorhexidine (Rec.INN registered by WHO)

Lidocaine (Rec.INN registered by WHO)

Dosage Form

Lidocaine Asept

Spray for topical use 100 mg+500 mcg/1 ml: 25 ml bottle.

Dosage Form, Packaging, and Composition

25 ml – polyethylene bottles (1) with a spray nozzle – cardboard packs.

Clinical-Pharmacological Group

Agent for topical anesthesia of the skin and mucous membranes with antimicrobial action

Pharmacotherapeutic Group

Antiseptic + local anesthetic

Pharmacological Action

Combined medicinal product for topical use. It has antiseptic and local anesthetic action.

Lidocaine is a local anesthetic; its action is due to the inhibition of nerve conduction by blocking sodium channels in nerve endings, which prevents the generation of impulses in sensory nerve endings and the conduction of pain impulses along nerve fibers.

When applied topically, it dilates blood vessels and does not have a local irritant effect. The effect develops within 1-5 minutes after application to the mucous membranes or skin and lasts for 10-15 minutes.

Chlorhexidine is an antiseptic for topical use. It is active against protozoa, gram-positive and gram-negative bacteria, including Treponema spp., Neisseria gonorrhoeae, Chlamydia spp., Ureaplasma spp., Trichomonas vaginalis, Gardnerella vaginalis, Bacteroides fragilis.

Some strains of Pseudomonas spp., Proteus spp. are weakly sensitive to chlorhexidine, and acid-resistant forms of bacteria, bacterial spores are resistant.

Pharmacokinetics

Lidocaine is rapidly absorbed from the mucous membranes (especially the pharynx and respiratory tract).

The rate of absorption is determined by the degree of blood supply to the mucous membrane, the total dose of this agent, the location of the area and the duration of application. After application to the mucous membrane of the upper respiratory tract, it is partially swallowed and inactivated in the gastrointestinal tract.

The time to reach C_max in plasma when applied to the oral mucosa and upper respiratory tract is 10-20 minutes. Protein binding depends on the concentration of the drug and is 60-80% at a drug concentration of 1-4 mcg/ml (4.3-17.2 µmol/l).

It is rapidly distributed in well-perfused organs (heart, lungs, brain, liver, spleen), then in adipose and muscle tissues. It penetrates the blood-brain barrier and the placental barrier, and is secreted with breast milk (40% of the concentration in the maternal plasma).

It is metabolized in the liver (90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and cleavage of the amide bond with the formation of metabolites less active than lidocaine – monoethylglycinexylidide and glycinexylidide, the half-life of which is 2 hours and 10 hours, respectively.

In liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value. It is excreted with bile and by the kidneys (up to 10% unchanged). In chronic renal failure, accumulation of metabolites is possible. Acidification of urine promotes increased excretion of lidocaine.

Chlorhexidine is practically not absorbed when applied topically.

Indications

In dentistry – as a local anesthetic and antiseptic in the injection area before local anesthesia; in case of opening superficial abscesses, removal of loose milk teeth and bone fragments; when suturing the mucous membrane; before fixing crowns and bridges; in the treatment of gum inflammation, periodontopathies; when removing tartar; during extirpation of an enlarged interdental papilla; when making impressions of the dentition only in the case of using elastic material.

In radiographic examination – to eliminate nausea and the pharyngeal reflex.

In otorhinolaryngology – as a local anesthetic and antiseptic during coagulation using an electrocautery in the treatment of nosebleeds; operations on the nasal septum and removal of nasal polyps; to eliminate the pharyngeal reflex and for analgesia and disinfection of the injection site of the injection needle before tonsil removal; when opening peritonsillar abscesses and before puncture of the maxillary sinus (only for additional anesthesia); anesthesia of the mucous membrane before washing the maxillary sinus.

During instrumental and endoscopic examinations – before inserting a probe through the mouth or nose (including duodenal intubation and fractional examination of gastric secretion), during rectoscopy, intratracheal anesthesia, after tracheotomy and when changing the cannula.

In obstetrics and gynecology – episiotomy and treatment of the incision; removal of sutures; minor operations on the vagina and cervix; treatment of suture suppuration.

As an analgesic and antiseptic for burns (including sunburns), bites; contact dermatitis (including that caused by irritating plants); minor wounds (including scratches).

For superficial analgesia and disinfection of the skin during minor surgical interventions.

ICD codes

Dosage Regimen

Topically and externally.

The number of required doses of the drug containing this combination can vary widely depending on the size and nature of the treated surface.

To avoid absorption of active substances into the systemic circulation, the minimum dose that provides a sufficient effect should be used. Usually, 1-3 doses are sufficient; it is possible to use 15-20 or more doses; maximum – 40 doses per 70 kg of body weight.

Adverse Reactions

Local reactions mild burning, which stops after the onset of anesthesia (within 1 min), erythema, edema, sensitivity disturbance.

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

Systemic reactions (dose-dependent): possible in cases of application in high doses, as well as with rapid absorption, hypersensitivity, idiosyncrasy, poor tolerance of this agent – headache, dizziness, convulsions, tremor, visual impairment (diplopia), tinnitus, agitation and/or depression, feeling of fear, euphoria, anxiety, fever, feeling of cold, respiratory depression, increased blood pressure, decreased blood pressure, bradycardia, arrhythmia, depression of myocardial function.

Other urethritis (after topical application).

Contraindications

Hypersensitivity to lidocaine, chlorhexidine; sick sinus syndrome in elderly patients; AV block of II and III degree (except in cases where a probe for ventricular stimulation has been inserted); cardiogenic shock; severe liver dysfunction; severe myasthenia; history of epileptiform seizures; local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

With caution

Local infection in the application area; trauma to the mucous membrane or skin in the application area; acute diseases; debilitated patients; young children (under 3 years); elderly age; pregnancy, breastfeeding period.

Use in Pregnancy and Lactation

If local anesthesia is necessary and there is no safer treatment, this agent can be used during pregnancy. Lidocaine is excreted in breast milk, but after application in usual therapeutic doses, the amount excreted in milk is too small to cause any harm to the breastfed infant.

Use in Hepatic Impairment

Contraindicated in severe liver dysfunction.

Use in Renal Impairment

Use with caution in chronic renal failure.

Pediatric Use

Contraindicated for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

Use in lower doses in children – according to age and general condition.

Use with caution in children under 3 years of age.

Geriatric Use

Contraindicated in sick sinus syndrome in elderly patients.

Use in lower doses in elderly patients.

Special Precautions

Regional and local anesthesia should be performed by experienced specialists in an appropriately equipped room with readily available equipment and drugs necessary for monitoring cardiac activity and resuscitation.

The personnel performing anesthesia must be qualified and trained in anesthesia techniques, and must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

Lower doses should be used in elderly and debilitated patients, in acute diseases, as well as in children – according to age and general condition.

Avoid getting this agent into the eyes and respiratory tract (risk of aspiration). Special care is required when applying to the back of the throat.

Application to the buccal mucosa is associated with the risk of dysphagia and subsequent aspiration, especially in children. When the sensitivity of the tongue and buccal mucosa is impaired, the risk of biting them 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 the case of using this agent in the form of a spray during surgical operations in the pharynx or nasopharynx, it should be taken into account that Lidocaine, by suppressing the pharyngeal reflex, enters the larynx and trachea and suppresses the cough reflex, which can lead to bronchopneumonia.

This is especially important in children, since they more often have a pharyngeal reflex induced. In this regard, the spray is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

Care should be taken when applying this agent to damaged mucous membranes and/or infected areas.

Effect on the ability to drive vehicles and mechanisms

During the treatment period, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Cimetidine and propranolol reduce the hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation and decreased hepatic blood flow) and increase the risk of toxic effects (including stunned state, drowsiness, bradycardia, paresthesia), effectiveness (may require dose increase).

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

Concomitant use with beta-blockers increases the risk of bradycardia.

Cardiac glycosides weaken the cardiotonic effect, curare-like drugs enhance muscle relaxation.

Procainamide increases the risk of CNS excitation, hallucinations.

With simultaneous administration of lidocaine and hypnotics, sedative drugs, their depressant effect on the CNS may be enhanced. Under the influence of MAO inhibitors (furazolidone, procarbazine, selegiline), an increase in the local anesthetic effect of lidocaine is possible.

Incompatible with soap, as well as detergents containing an anionic group (saponins, sodium lauryl sulfate, sodium carboxymethylcellulose).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.