Lidocaine-Vial (Spray) Instructions for Use

Marketing Authorization Holder

Vial, LLC (Russia)

Manufactured By

Jewim Pharmaceutical (Shandong), Co. Ltd. (China)

Labeled By

OZON, LLC (Russia)

ATC Code

D04AB01 (Lidocaine)

Active Substance

Lidocaine (Rec.INN registered by WHO)

Dosage Forms

	Lidocaine-Vial	Dosed spray for topical application 10%: 38 g bottle
		Spray for topical and external application 10%: 38 g bottle

Dosage Form, Packaging, and Composition

38 g – polypropylene bottles (1) complete with a sprayer – cardboard packs.

Dosed spray for topical application 10% in the form of a transparent, colorless or yellowish liquid with a characteristic smell of ethanol and menthol.

Excipients : menthol, propylene glycol, rectified ethanol, sodium hydroxide, purified water.

25 g – aerosol cans with a mechanical dosing pump (1) complete with a sprayer for oral application and a dental nozzle – cardboard packs.
38 g – aerosol cans with a mechanical dosing pump (1) complete with a sprayer for oral application and a dental nozzle – cardboard packs.

Clinical-Pharmacological Group

Local anesthetic for superficial anesthesia

Pharmacotherapeutic Group

Local anesthetic agent

Pharmacological Action

The local anesthetic effect 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.

Pharmacokinetics

It is rapidly 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 mucous membrane, the total dose of the drug, 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. T_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 µg/ml (4.3-17.2 µmol/l).

It is distributed rapidly (distribution phase T_1/2 – 6-9 minutes), first entering well-perfused tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. It penetrates the blood-brain and placental barriers and is secreted with breast milk (40% of the concentration in 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), whose T_1/2 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 in 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.

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 mucous membrane; before fixing crowns and bridges; in the treatment of gum inflammation, periodontopathies; extraction of milk teeth; removal of tartar;
• In otorhinolaryngology: operations on the nasal septum and removal of nasal polyps; electrocoagulation in the treatment of nosebleeds; elimination of the pharyngeal reflex and anesthesia of the injection site before tonsil removal; opening of peritonsillar abscesses;
• In obstetrics and gynecology: episiotomy and treatment of the incision; suture removal; minor operations on the vagina and cervix; hymen rupture; treatment of suture suppuration;
• During instrumental and endoscopic examinations: before inserting a probe through the nose or mouth (duodenal intubation and fractional study of gastric secretion); during rectoscopy, intubation;
• During radiographic examination: elimination of nausea and pharyngeal reflex; as an analgesic for burns (including sunburns); bites; contact dermatitis (including that caused by irritating plants); minor wounds (including scratches);
• Superficial anesthesia of the skin during minor surgical interventions.

ICD codes

Dosage Regimen

Topically, externally. The required amount of the drug can vary widely depending on the size and nature of the treated surface.

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

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

Adverse Reactions

At the site of application of the drug mild burning, which stops after the onset of anesthesia (within 1 minute), erythema.

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

Systemic reactions from the central nervous system may be observed headache, dizziness, convulsions, tremor, visual impairment, tinnitus, agitation and/or depression, feeling of fear, euphoria, anxiety, fever, feeling of cold, respiratory depression.

From the cardiovascular system increased blood pressure, bradycardia.

Other urethritis (after topical application).

Contraindications

• Hypersensitivity.

With caution hemorrhoidal bleeding (during rectal examination), local infection in the application area, trauma to the mucous membrane or skin in the application area, concomitant acute diseases, debilitated patients, young children, elderly age, pregnancy, lactation period.

Use in Pregnancy and Lactation

With caution: pregnancy, lactation period.

Pediatric Use

With caution: young children.

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

Geriatric Use

With caution: elderly age.

Special Precautions

The bottle should be held in an upright position when in use. Avoid contact with eyes and respiratory tract (risk of aspiration). Particular care is required when applying the drug to the area of the posterior pharyngeal wall.

Influence on the ability to drive vehicles and mechanisms

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

Overdose

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

Treatment at the first signs of intoxication (dizziness, nausea, vomiting, euphoria), the patient is placed in a horizontal position and oxygen inhalation is prescribed; for psychomotor agitation – IV 10 mg of diazepam; for convulsions – IV 1% solution of hexobarbital or sodium thiopental; for bradycardia – IV 0.5-1 mg of atropine, sympathomimetic agents. Dialysis is ineffective.

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 stupor, drowsiness, bradycardia, paresthesia, etc.).

Barbiturates, phenytoin, rifampicin (inducers of hepatic microsomal enzymes) reduce effectiveness (a dose increase may be required).

When prescribed 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 central nervous system excitation, hallucinations.

With the simultaneous administration of lidocaine and hypnotic and sedative drugs, their depressant effect on the central nervous system may be enhanced. With intravenous administration of hexobarbital or sodium thiopental against the background of lidocaine action, respiratory depression is possible.

Under the influence of monoamine oxidase inhibitors, the local anesthetic effect of lidocaine may be enhanced. Patients taking monoamine oxidase inhibitors should not be prescribed Lidocaine parenterally. With the simultaneous use of lidocaine and polymyxin, the depressant effect on neuromuscular transmission may be enhanced, so in this case, it is necessary to monitor the patient’s respiratory function.

Storage Conditions

List B. Store in a light-protected place at a temperature not exceeding 30°C (86°F). Keep out of reach of children.

Shelf Life

Shelf life – 3 years.

Dispensing Status

By prescription.

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.