Lidocaine

INSTRUCTIONS for medical use of the medicinal product LIDOCAINE (LIDOCAINE)

Composition:

Active substance: lidocaine;

1 vial contains lidocaine 3.8 g; 1 dose contains lidocaine 4.6 mg;

Excipients: ethanol 96%, propylene glycol, peppermint oil.

Pharmaceutical form. Spray.

Main physicochemical properties: colorless or almost colorless alcoholic solution with a characteristic menthol odor.

Pharmacotherapeutic group.
Medicinal products for local anesthesia. ATC code D04AB01.

Pharmacological properties.

Pharmacodynamics.

Lidocaine is a membrane-stabilizing agent of the amide group used for local anesthesia. It inhibits sensitive nerve endings of the skin and mucous membranes, thereby causing reversible suppression of conduction in neural tissue elements (neuron, axon, synapses).

The mechanism of action of local anesthetics involves inhibition of ionic fluxes—essential for stimulus generation—across neuronal membranes.

Lidocaine suppresses the stimulus-activated transient increase in sodium ion permeability and, to a lesser extent, reduces passive permeability to potassium and sodium ions, thereby stabilizing neuronal membranes. Lidocaine reduces the degree of depolarization occurring in response to a physiological stimulus, as well as the amplitude of the action potential, and inhibits nerve conduction.

Among various sensory modalities, local anesthetics primarily suppress pain sensation, followed by suppression of warmth perception and tactile sensations. Lidocaine absorbed after local application may cause excitation or depression of the central nervous system. Its effects on the cardiovascular system may manifest as conduction disturbances and peripheral vasodilation.

Pharmacokinetics.

After local application, lidocaine penetrates tissues and exerts local analgesic action.

The effect of lidocaine develops within 1 minute and lasts from 5 to 6 minutes. Subjective symptoms of numbness gradually subside within 15 minutes.

Lidocaine is rapidly absorbed following application to mucous membranes and damaged skin, but poorly absorbed from intact skin. The rate of absorption and the amount of active substance entering the bloodstream depend on the dose, type, surface area, condition of the application site (skin or mucous membrane), and duration of exposure.

Transdermal administration of 500 mg of lidocaine achieves therapeutic blood levels of the drug. Maximum lidocaine concentration in plasma is reached within 1 hour after application. When this dose is used, plasma lidocaine concentration remains within the therapeutic range for 7–8 hours. The amount of active substance applied at any time should not exceed 300–350 mg.

Lidocaine is metabolized in the liver. It undergoes initial dealkylation, followed by hydrolysis. Both unchanged drug and its metabolites are primarily excreted by the kidneys. The elimination half-life of lidocaine is 1.6 hours.

Clinical characteristics.

Indications.

Dentistry and maxillofacial surgery

Anesthesia of the injection site prior to local anesthesia, anesthesia during incision of superficial abscesses, removal of loose deciduous teeth and bone fragments, suturing of mucous membranes. Gingival anesthesia for fixation of a dental crown or bridge prosthesis. The drug is used during manual or instrumental removal of dental calculus or trimming of enlarged interdental papillae to reduce or suppress a hypersensitive gag reflex. When taking impressions of the dental arch or placing X-ray film, the drug may be used only if elastic impression materials are employed.

Lidocaine spray may be used in children for frenectomy and removal of salivary gland stones.

Removal of superficial benign tumors of the mucous membrane.

Otolaryngology

In the treatment of nasal bleeding prior to electrocautery, septal resection, and nasal polypectomy. Also used prior to tonsillectomy to suppress the vomiting reflex and to anesthetize the injection site.

As an adjunctive anesthesia prior to incision of a peritonsillar abscess or prior to puncture of the maxillary sinus.

Anesthesia prior to irrigation of the maxillary sinus.

Endoscopic and instrumental examinations.

Pharyngeal anesthesia prior to insertion of various tubes through the nose or mouth (e.g., gastro-duodenal tube, Sengstaken tube).

Replacement of tracheostomy tube.

Obstetrics and gynecology.

Anesthesia of the perineum for episiotomy. Suture removal. Anesthesia of the surgical field during vaginal surgeries or cervical procedures.

Dermatology

Anesthesia of skin and mucous membranes during minor surgical procedures.

Contraindications.

Hypersensitivity to the components of the drug, as well as to other amide-type local anesthetics; in dentistry, the use of the drug is contraindicated prior to the use of plaster due to the risk of aspiration.

Special safety precautions.

Avoid entry of lidocaine into the respiratory tract (risk of aspiration).

When spraying, the bottle should be held as vertically as possible. Avoid contact of the spray with eyes.

Interaction with other medicinal products and other forms of interaction.

Caution is required when administering lidocaine to patients receiving antiarrhythmic agents of class IB (e.g., tocainide, mexiletine), due to the risk of cumulative toxic effects.

Concomitant use with antiarrhythmic agents of class IA (including quinidine, procainamide, disopyramide) may result in QT interval prolongation and, in very rare cases, development of AV block or ventricular fibrillation.

Phenytoin enhances the cardiodepressant effect of lidocaine.

Concomitant use with procainamide may lead to delirium and hallucinations.

Lidocaine may potentiate the effects of drugs causing neuromuscular blockade.

In the context of cardiac glycoside intoxication, lidocaine may exacerbate the severity of AV block.

Ethanol enhances the respiratory depressant effect of lidocaine.

Serum lidocaine concentration increases with concomitant use of the following drugs: chlorpromazine, cimetidine, propranolol, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline.

Specific studies on interactions between lidocaine and class III antiarrhythmic drugs (e.g., amiodarone) have not been conducted, but caution is recommended due to the potential for enhanced cardiac effects in patients with cardiovascular disorders.

Special precautions for use

The drug should be applied with caution to the posterior pharyngeal wall.

Transbuccal administration may lead to dysphagia and subsequent aspiration, especially in children. Due to numbness of the tongue and buccal mucosa, there is a risk of trauma from biting.

Lidocaine is rapidly absorbed through mucous membranes (especially the tracheal mucosa) as well as through damaged skin. This should be taken into account, particularly when the drug is applied over large areas or administered to children.

Caution should be exercised when applying the drug to injured mucous membranes and/or infected areas.

Caution is required when administering the drug to patients with epilepsy, as well as in cases of bradycardia, conduction disorders, heart failure, hepatic or renal dysfunction, and shock, especially when significant systemic absorption of the drug is possible, depending on the administered dose and the size of the treated area.

Weakened patients, elderly patients, critically ill patients, and children require reduced doses according to their age and general condition.

The drug contains propylene glycol, which may cause irritation of the skin or mucous membranes.

Lidocaine in spray form may have a porphyrinogenic effect in patients with acute porphyria; therefore, it should be prescribed only for life-threatening indications.

Use during pregnancy or breastfeeding

Well-controlled clinical studies on the safety of the drug during pregnancy have not been conducted. However, lidocaine has been used for a long time without causing harm to patient health.

Preclinical studies have not revealed any toxic effects of lidocaine on fetal development.

In the absence of a safer treatment method, lidocaine spray may also be used during pregnancy.

Lidocaine is excreted in breast milk; however, when usual therapeutic doses are applied, the amount excreted is so minimal that it does not cause harm to the breastfed infant.

Effect on ability to drive or operate machinery

Given that in sensitive patients, adverse reactions from the central nervous system (such as excitation, depression, nervousness, dizziness, somnolence, spasms, loss of consciousness, respiratory paralysis) may occur during drug use, patients should refrain from driving or operating machinery and from any other activities requiring concentration of attention during treatment.

Method of administration and dosage.

For external use.

Remove the cap, attach the dosing valve, and before the first use, prime the pump bottle with the solution (press the pump several times until aerosol appears in the air).

If the spray bottle has not been used for a prolonged period, the pump may need to be re-primed.

The dose of the drug depends on the indication and the size of the surface area requiring anesthesia.

Each spray delivers one dose, releasing 4.6 mg of lidocaine onto the surface.

To avoid high plasma concentrations of the drug, it is important to use the smallest dose that provides adequate effect.

Approximate dosages for various indications:

Usually 1–2 sprays are sufficient, although in obstetrics 15–20 sprays or more may be used (maximum dose 40 sprays/70 kg body weight).

The drug can be applied to large surfaces using a cotton swab soaked with Lidocaine 10% spray.

Use in children.

In dentistry or maxillofacial surgery, Lidocaine spray can be administered to children by means of a cotton swab, thus avoiding the risk of inhalation of the drug and the burning sensation usually associated with its use. The drug may be used in the same way in children under 2 years of age.

Children.

The drug is used in pediatric practice.

By suppressing the pharyngeal reflex and reaching the larynx and trachea (risk of aspiration), lidocaine suppresses the cough reflex, which may lead to the development of bronchopneumonia.

In children under 2 years of age, it is advisable to apply the drug using a cotton swab soaked with lidocaine.

Lidocaine spray is not recommended for local anesthesia prior to tonsillectomy and adenoidectomy in children under 8 years of age.

Overdose.

Symptoms: increased sweating, pallor, dizziness, headache, blurred vision, tinnitus, diplopia, decreased arterial pressure, bradycardia, arrhythmia, drowsiness, chills, numbness of extremities, anxiety, convulsions, shock, methemoglobinemia, cardiac arrest.

Treatment.

If necessary, ensure access to fresh air, oxygen supply, and/or artificial respiration.

Convulsions due to overdose should be managed with succinylcholine (1 mg/kg body weight) and/or diazepam (1 mg/kg body weight intravenously). Since succinylcholine may cause respiratory arrest, it should only be administered by experienced personnel capable of performing endotracheal intubation and managing patients with respiratory arrest.

Short-acting barbiturates such as thiopental may also be used.

In case of cardiovascular symptoms (bradycardia, conduction disturbances), atropine (0.5–1 mg intravenously) and sympathomimetics should be administered.

Ventricular fibrillation and cardiac arrest require immediate resuscitation measures.

Dosage in children must be adjusted according to age and body weight.

Side effects.

Local effects

When using Lidocaine, a burning sensation may occur, which disappears after the anesthetic effect develops (within 1 minute).

Transient erythema, swelling, and reduced sensitivity may be observed at the site of application.

Allergic reactions

Including: skin rash, itching, urticaria, angioneurotic edema, bronchospasm, and in extremely severe cases – shock.

If hypersensitivity reactions occur, the use of the drug should be discontinued.

Systemic effects

When Lidocaine spray is used according to the instructions, the incidence of systemic effects is extremely low, as the amount of active substance reaching the bloodstream is very small. However, when high doses are used, or in cases of rapid absorption of lidocaine, increased sensitivity, idiosyncrasy, or reduced tolerance, the following adverse effects may develop:

Central nervous system: excitation, depression, nervousness, dizziness, drowsiness, spasms, loss of consciousness, respiratory paralysis;

Cardiovascular system: arterial hypotension, myocardial infarction, bradycardia, cardiac arrest.

Shelf life. 5 years.

Storage conditions.

Store at a temperature not exceeding 25 °C in a place inaccessible to children.

Packaging.

38 g of spray in a bottle.

1 bottle + 1 plastic valve-dosing device in a cardboard box.

Prescription category. Prescription only.

Manufacturer.

EGIS Pharmaceuticals Ltd., Hungary.

Manufacturer's address and location of business operations.

65 Matyas kiraly str., Kermend, 9900, Hungary.