Lidocaine, spray, 6 mg/dose 38 g

Lidocaine is a local anesthetic and antiarrhythmic drug.

The antiarrhythmic activity is due to inhibition of phase 4 (diastolic depolarization) in Purkinje fibers, reduction of automaticity, suppression of ectopic foci of excitation. The rate of rapid depolarization (phase 0) is not affected or slightly reduced. Increases membrane permeability to potassium ions, accelerates the process of repolarization and shortens the action potential. It does not change sinus-atrial node excitability and has little effect on myocardial conduction and contractility. When administered intravenously it works quickly and shortly (10-20 min)

The mechanism of local anesthetic effect consists in stabilization of neuronal membrane, reduction of its permeability for sodium ions which prevents initiation of action potential and impulse conduction. Antagonism with calcium ions is possible. It is quickly hydrolyzed in slightly alkaline environment of tissues and after a short latent period acts within 60-90 minutes.

In case of inflammation (tissue acidosis) anesthetic activity decreases. It is effective for all types of local anesthetization. It dilates blood vessels. It has no irritating effect on the tissues.

When using the drug in pharyngeal or nasopharyngeal surgery the pharyngeal reflex is suppressed. By reaching the larynx and trachea, the drug is good at slowing down the cough reflex, which can lead to bronchopneumonia.

The action of lidocaine in aerosol form develops within 1 min and lasts 5-6 min. The desensitization achieved slowly disappears within 15 min.

It is evenly distributed in the body. It penetrates through the placental barrier.

Indications

• prevention and treatment of ventricular rhythm disturbances (ventricular extrasystoles, ventricular paroxysmal tachycardia) associated with the acute phase of myocardial infarction, other forms of CHD, as well as caused by drugs (cardiac glycosides).

Local anesthesia: superficial, infiltration, conduction, epidural, spinal, intraligamentary in surgical procedures, painful manipulations, endoscopic and instrumental studies.

In dental practice, oral surgery:

• open superficial abscesses;
• removal of movable loose teeth;
• removal of bone fragments and suturing of mucosal wounds;
• anesthesia of gingiva for fixation of crown or bridge;
• Manual or instrumental removal (or excision) of enlarged papilla of tongue;
• to decrease or suppress elevated pharyngeal reflex in preparation for radiological examination;
• anesthesia in excision of superficial benign tumors of the oral mucosa;
• in children – for frenullectomy and opening of salivary gland cysts.

In ENT practice:

• before electrocoagulation (in the treatment of nasal bleeding), septectomy and resection of nasal polyps;
• before tonsillectomy to reduce pharyngeal 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.

In endoscopy and instrumental examinations:

• anesthesia before insertion through the nose or mouth of various probes (duodenal probe, before fractional food test);
• anesthesia before rectoscopy and in case of catheter replacement.

In obstetrics and gynecology:

• anesthesia of the perineum to treat and/or perform an episiotomy;
• anesthesia of the operating field in vaginal or cervical surgery;
• anesthesia for excision and treatment of ruptured hymen;
• anesthesia for suturing abscesses.

In dermatology:

• anesthesia of mucous membranes in minor surgical interventions.
  

Active ingredient

Lidocaine

Composition

Active ingredient:

Lidocaine;

Associates:

Ethanol (96%),

Pearmint oil,

Propylene glycol

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How to take, the dosage

In anesthesia of the mucous membrane of the esophagus, larynx, trachea, lubricate the outer surfaces of the instruments intended for examination; for surface anesthesia of the oral mucosa apply a sterile glass rod or a sterile cotton swab soaked in gel 0.2-2 g of gel; in case of insufficient anesthesia it is repeated after 2-3 min; maximum dose for adults in 12 hours is 300 mg (6 g of gel); In urology, 3-5 ml of 2% gel is used to lubricate the urethral mucosa before examination in women, 100-200 mg (5-10 ml of 2% gel) in men before catheterization, 600 mg (30 ml of 2% gel) in two instances at an interval of several minutes before cystoscopy for urethral filling and dilatation (the distal urethra is temporarily squeezed). The maximum dose is 600 mg (30 ml of 2% gel) for 12 hours. In children, up to 4.5 mg/kg.

TTC is applied to the painful surface for 12 hours, followed by a 12-hour break. No more than 3 TTCs can be applied at any one time. After applying the medication, the eyes should not be touched and the hands should be washed.

In dentistry, for anesthesia of the injection site, the gel is applied to the mucous membrane in the area of subsequent infiltration anesthesia at intervals of 2-3 min; for anesthesia in the removal of tartar the gel is rubbed into the gingival margin and the necks of teeth for 2-3 min, followed by the procedure; as a therapeutic dressing after removal of tartar or curettage gel is applied to the gingival margin and fixed; in the form of applications it is applied several times a day to the mucous membrane of the mouth on the sites of aphthas and erosions

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Interaction

It is undesirable to combine lidocaine with the following drugs:

With beta-adrenoblockers because of increased toxic properties of lidocaine, with digitoxin because of weakened cardiotonic effect, with curare-like drugs because muscle relaxation is increased.

Lidocaine should not be administered together with aymalin, amiodarone, verapamil or quinidine due to increased cardiodepressant effect.

The combined use of lidocaine and novocainamide may cause CNS agitation and hallucinations.

In intravenous administration of hexenal or thiopental sodium with lidocaine may cause respiratory depression.

MoA inhibitors may increase the local anesthetic effect of lidocaine. Patients taking MAO inhibitors should not administer lidocaine parenterally.

The simultaneous administration of lidocaine and polymyxin-B may increase inhibitory effects on neuromuscular transmission, so in this case the patient’s respiratory function should be monitored.

The simultaneous use of lidocaine with hypnotics or sedatives may increase their CNS depressant effect. When lidocaine is administered intravenously to patients taking cimetidine such unwanted effects as stunned state, somnolence, bradycardia, parasthesias, etc. are possible.

This is due to increased plasma levels of lidocaine, which is explained by the release of lidocaine from binding to blood proteins, as well as the slowing of its inactivation in the liver. If combined therapy with these drugs is necessary, the dose of lidocaine should be reduced.

Pharmaceutical interactions

When used concomitantly the following drugs increase the concentration of lidocaine in blood serum: aminazin, cimetidine, propranolol, pethidine, bupivacaine, quinidine, disopyramide, amitriptyline, imipramine, nortriptyline.

Special Instructions

With caution is used in patients with liver dysfunction, circulatory insufficiency, arterial hypotension, renal failure, epilepsy. In these cases, reduction of the dose of the drug is required.

In case of rapid intravenous administration there may be a sharp decrease in blood pressure and development of collapse.

In these cases, mesaton, ephedrine and other vasoconstrictors are used. Care should be used to inject lidocaine solutions into highly vascularized tissues to avoid entering the drug into the lumen (e.g., neck during thyroid surgery) (Lower doses of lidocaine are indicated in these cases).

Particular caution should be exercised when mucous membrane injuries are present, when mentally retarded, and in very old and/or weakened patients who are already receiving lidocaine type medications for cardiac problems.
In dentistry and orthopedics, the drug should only be used with elastic blinders.

Ingestion of the aerosol or contact with the eyes should be avoided and it is important to prevent aerosol from entering the respiratory tract (risk of aspiration). Particular caution is required when applying to the back of the throat. Remember that Lidocaine suppresses the pharyngeal reflex and inhibits the cough reflex, which can lead to aspiration and bronchopneumonia.

Pediatric use

Please note that the swallowing reflex is much more common in children than in adults.

Lidocaine in aerosol form is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

Influence on driving and operating machinery

If the side effects after using the drug do not cause discomfort, there are no restrictions on driving and operating machinery.

Contraindications

• Sinus node weakness syndrome.
• Developed bradycardia.
• Antrioventricular block of degree 2 and 3 (except when a ventricular simulation probe is inserted).
• Cardiogenic shock.
• Myasthenia gravis.
• High individual sensitivity to lidocaine.
• A history of lidocaine-induced epileptiform seizures.
• Developed impairment of liver function.

When plaster is used in dentistry as an impression material, aerosol is contraindicated because of the risk of aspiration.

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Side effects

CNS disorders: headaches, dizziness, somnolence, restlessness, euphoria, tinnitus, numbness of the tongue and mucous membrane of the mouth, speech and vision disorders are possible.

Cardiovascular system disorders: in high doses arterial hypotension, collapse, bradycardia, conduction disorders are possible.

Allergic reactions: rash, itching, exfoliative dermatitis, anaphylactic shock, hyperthermia are rare.

Local reactions: mild burning sensation, which disappears as the anesthetic effect develops (within 1 minute).

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Overdose

Symptoms: increased sweating, pale skin, nausea, vomiting, dizziness, headache, blurred vision, tinnitus, diplopia, decreased blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness, tremor, anxiety, agitation, seizures, methemoglobinemia, cardiac arrest.

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

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Pregnancy use

The use of Lidocaine in pregnancy should be excluded, because after I.V. injection the drug passes through the placenta after a few minutes.

Lidocaine aerosol can be used during pregnancy because it is safe in the recommended doses.
It is not known whether lidocaine is excreted with the breast milk.

Caution should be exercised when prescribing the drug to a nursing mother.

In lactation, the drug may be used after careful assessment of the expected benefit to the mother and the potential risk to the infant.

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Similarities

Lidocaine, Versatis, Lidocaine-Vial