Instructions Lidocaine-Zdorovye spray for topical use 10% with spray nozzle bottle 38 g
Composition
active ingredient: lidocaine;
1 g of the drug contains 100 mg of lidocaine;
excipients: propylene glycol, peppermint oil, ethanol 96%. approx., Kharkiv city, Shevchenko street, building 22.
Dosage form
Spray for topical use.
Main physicochemical properties: transparent colorless solution with a specific odor.
Pharmacotherapeutic group
Local anesthetics. ATX code D04A B01.
Pharmacological properties
Pharmacodynamics
Pharmacodynamics. Lidocaine is a membrane-stabilizing agent of the amide group for local anesthesia. It inhibits sensitive nerve endings of the skin and mucous membranes, i.e. causes reversible inhibition of the conductivity of tissue elements of nerve cells (neuron, axon, synapses).
The mechanism of action of local anesthetics is to inhibit ion fluxes through neuronal membranes, which are essential for the generation of a stimulus.
Lidocaine inhibits the stimulus-activated transient increase in permeability for sodium ions and, to a lesser extent, reduces the passive permeability for potassium and sodium ions, thereby stabilizing neuronal membranes. Lidocaine reduces the degree of depolarization that occurs in response to a physiological stimulus, as well as the amplitude of the action potential, and inhibits nerve conduction.
Among the various sensory modes of action, local anesthetics primarily suppress pain sensitivity, which is accompanied by suppression of thermal and tactile sensations. Lidocaine absorbed after topical application can cause excitation or depression of the central nervous system. Its effects on the cardiovascular system can manifest as conduction disturbances and peripheral vasodilation.
Pharmacokinetics
After topical application, lidocaine penetrates the tissues and has a local anesthetic effect.
The effect of lidocaine develops within 1 minute and lasts from 5 to 6 minutes. Subjective symptoms of numbness disappear slowly, within 15 minutes.
Lidocaine is rapidly absorbed when applied to mucous membranes and damaged skin, but poorly absorbed when applied to healthy skin. The rate of absorption and the amount of active substance that enters the bloodstream depend on the dose, type, size and condition of the surface to which the drug is applied (skin or mucous membrane), as well as the duration of exposure.
Transdermal application of 500 mg of lidocaine provides therapeutic levels of the drug in the blood. The maximum concentration of lidocaine in the blood serum is reached within 1 hour after application of the drug. When using this dose, the concentration of lidocaine in the blood serum remains in the therapeutic range for 7-8 hours. The amount of active substance used in any case should not exceed 300-350 mg.
Lidocaine is metabolized in the liver. It is first dealkylated and then hydrolyzed. Both the unchanged drug and its metabolites are excreted mainly by the kidneys. The half-life of lidocaine is 1.6 hours.
Indication
Dentistry and maxillofacial surgery. Anesthesia of the injection site before local anesthesia; anesthesia during the opening of a superficial abscess, the removal of mobile deciduous teeth and bone fragments, and suturing of mucous membranes. Anesthesia of the gums for fixing a tooth crown or a dental bridge. The drug should be used during manual or instrumental removal of tartar or when cutting off enlarged interdental papillae to reduce or suppress the hypersensitive swallowing reflex. When taking an impression of the dentition or when placing an X-ray film, the drug can be used only when elastic impression materials are used.
The drug should be used in children for frenectomy and removal of salivary gland cysts.
Excision of superficial benign tumors of the mucous membrane.
Otolaryngology. In the treatment of nosebleeds before electrocautery, septal resection and nasal polyp resection. Also used before tonsillectomy to suppress the gag reflex and anesthetize the injection site.
As additional anesthesia before opening a peritonsillar abscess or before puncture of the maxillary sinus.
Anesthesia before sinus lavage.
Endoscopic and instrumental examinations. Pharyngeal anesthesia before insertion of various tubes through the nose or mouth (gastroduodenal tube, Sengstaken tube).
Tracheotomy tube replacement.
Obstetrics and gynecology. Perineal anesthesia for episiotomy. Suture removal. Anesthesia of the surgical field for vaginal or cervical surgeries.
Dermatology. Anesthesia of the skin and mucous membranes during minor surgical interventions.
Contraindication
Hypersensitivity to the components of the drug, as well as to other amide local anesthetic drugs; in dentistry, the use of the drug is contraindicated before using plaster due to the risk of aspiration.
Lidocaine should not be allowed to enter the respiratory tract (risk of aspiration). As far as possible, the bottle should be held in an upright position when spraying the aerosol. Avoid contact with the eyes.
Interaction with other medicinal products and other types of interactions
Caution should be exercised when using lidocaine in patients receiving IV-type antiarrhythmics (e.g., tocainide) due to the risk of additive toxicity.
When used simultaneously with class IA antiarrhythmic drugs (including quinidine, procainamide, disopyramide), the QT interval is prolonged and in very rare cases, AV block or ventricular fibrillation may develop.
Phenytoin enhances the cardiodepressive effect of lidocaine.
When used simultaneously with procainamide, delusions and hallucinations are possible.
Lidocaine may enhance the effect of drugs that cause neuromuscular blockade, as the latter reduce the conductivity of nerve impulses.
Against the background of digitalis glycoside intoxication, lidocaine may increase the severity of AV block.
Ethanol enhances the respiratory depressant effect of lidocaine.
Pharmaceutical interaction. When used simultaneously, the following drugs increase the concentration of lidocaine in the blood serum: aminazine, cimetidine, propranolol, peptidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline.
Application features
The drug should be applied with caution to the posterior wall of the pharynx.
With transbuccal use, there is a risk of dysphagia and subsequent aspiration, especially in children. Due to the insensitivity of the tongue and buccal mucosa, there is a risk of injury due to biting.
Lidocaine is rapidly absorbed through mucous membranes (especially the tracheal mucosa) and through damaged skin. This should be taken into account, especially when the drug is applied to large areas or used in children.
Caution should be exercised when applying the drug to affected mucous membranes and/or infected areas.
Caution should be exercised when using the drug in patients with epilepsy, as well as in bradycardia, conduction disorders, liver dysfunction, and shock, especially if absorption of a significant amount of the drug is expected based on the dose used and the area treated.
Debilitated patients, elderly patients, seriously ill patients, and children should use lower doses of the drug according to their age and general condition.
Propylene glycol may cause skin irritation.
Ability to influence reaction speed when driving vehicles or other mechanisms
Considering that sensitive patients may experience adverse reactions from the central nervous system (excitement, depression, nervousness, dizziness, drowsiness, spasms, loss of consciousness, respiratory paralysis) when using the drug, you should refrain from driving vehicles and performing other work that requires concentration of attention while taking the drug.
Use during pregnancy or breastfeeding
Strictly controlled clinical studies of the safety of the drug during pregnancy have not been conducted. However, lidocaine has been used for a long time and has not caused any harm to the patient's health.
Preclinical studies have not revealed any toxic effects of lidocaine on fetal development.
In the absence of a safer treatment method, the drug can also be used during pregnancy.
Lidocaine is excreted in breast milk, but at usual therapeutic doses the amount excreted is so small that it is unlikely to harm a breastfed infant.
Method of administration and doses
The dose of the drug depends on the indications and the size of the surface to be anesthetized.
With each spray of 1 portion of the spray, 4.8 mg of lidocaine (1 dose) is released onto the surface.
To avoid high plasma drug concentrations, it is important to use the lowest dose that provides a satisfactory effect.
Usually 1-2 sprays are sufficient, although in obstetrics 15-20 sprays or more are used (maximum dose – 40 sprays/70 kg of body weight).
Approximate doses for various indications.
Indication
| Dose (number of presses) | |
| Dentistry | 1-3 |
| Maxillofacial surgery | 1-4 |
| Otolaryngology | 1-4 |
| Endoscopy | 2-3 |
| Obstetrics | 15-20 |
| Gynecology | 4-5 |
| Dermatology | 1-3 |
The drug can be applied to large surfaces using a cotton swab soaked in the drug.
Children: In dentistry or maxillofacial surgery, the drug can be administered to children by applying it with a swab, which avoids the risk of inhalation of the drug, as well as the burning sensation that is usually a side effect of the drug. Children under 2 years of age can be administered the drug in the same way.
For children over 12 years of age, the maximum dose is 3 mg/kg.
Children
By suppressing the pharyngeal reflex and reaching the larynx and trachea (risk of aspiration), lidocaine suppresses the cough reflex, which can lead to bronchopneumonia.
For children under 2 years of age, it is advisable to apply the spray using a cotton swab soaked in Lidocaine.
The drug is not recommended for use for local anesthesia before tonsillectomy and adenoidectomy in children under 8 years of age.
Overdose
Symptoms: increased sweating, pale skin, dizziness, headache, blurred vision, tinnitus, diplopia, decreased blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness of the extremities, anxiety, convulsions, shock, methemoglobinemia.
Treatment: If necessary, provide access to fresh air, oxygen and/or artificial respiration.
Convulsions resulting from overdose should be treated with succinylcholine (1 mg/kg body weight) and/or diazepam (1 mg/kg body weight IV). Since succinylcholine may cause respiratory arrest, the drug should only be used by specialists experienced in endotracheal intubation and the management of patients with respiratory arrest.
Short-acting barbiturates, thiopental, can also be used.
If symptoms from the cardiovascular system appear (bradycardia, conduction disturbances), prescribe atropine (intravenously 0.5-1 mg) and sympathomimetics.
In case of ventricular fibrillation and cardiac arrest, immediate resuscitation measures are indicated.
Dosage for children should be based on the patient's age and body weight.
Adverse reactions
Local effects. When using the drug, a burning sensation may occur, which disappears after the anesthetic effect appears (within 1 minute).
Transient erythema, edema, and decreased sensitivity may occur at the site of application.
Allergic reactions. Including: skin rash, itching, urticaria, angioedema, bronchospasm, in extremely severe cases - shock.
If hypersensitivity reactions occur, the use of the drug should be discontinued.
Systemic effects. If the drug is used according to the instructions, the incidence of systemic effects is extremely low, since the amount of active substance that can reach the bloodstream is very small. When using high doses and in the case of rapid absorption of lidocaine or in case of hypersensitivity, idiosyncrasy or reduced tolerance, the following side effects may develop:
From the side of the central nervous system: excitement, depression, nervousness, dizziness, drowsiness, spasms, loss of consciousness, respiratory paralysis;
Cardiovascular system: hypotension, myocardial infarction, bradycardia.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 °C.
Keep out of reach of children. Incompatibility.
Incompatibility. Incompatibility of the drug in this dosage form is not described.
Packaging
Spray 10%, 38 g in a bottle equipped with a pump valve, a neck spray nozzle or a spray nozzle and a protective cap in a box.
Vacation category
According to the recipe.
Producer
Limited Liability Company "Pharmaceutical Company "Zdorovya".
Location of the manufacturer and its business address
Ukraine, 61013, Kharkiv region, Kharkiv city, Shevchenko street, building 22.
