Lidocaine, spray 10%, 38g

Composition

Active ingredient:

lidocaine;

Auxiliary substances:

ethanol (96%),

peppermint

oil

, propylene glycol Pharmacological action

Lidocaine is a local anesthetic and antiarrhythmic drug.

Antiarrhythmic activity is caused by inhibition of phase 4 (diastolic depolarization) in Purkinje fibers, a decrease in automatism, and suppression of ectopic foci of arousal. The rate of rapid depolarization (phase 0) is not affected or slightly reduced. Increases the permeability of membranes to potassium ions, accelerates the repolarization process, and shortens the action potential. It does not change the excitability of the sino-atrial node, has little effect on the conduction and contractility of the myocardium. When administered intravenously, it acts quickly and briefly (10-20 minutes).

The mechanism of the local anesthetic effect is to stabilize the neuronal membrane, reduce its permeability to sodium ions, which prevents the appearance of an action potential and the conduction of impulses. Antagonism with calcium ions is possible. It is rapidly hydrolyzed in a slightly alkaline tissue environment and acts for 60-90 minutes after a short latent period.

In case of inflammation (tissue acidosis), the anesthetic activity decreases. It is effective for all types of local anesthesia. Dilates blood vessels. It has no irritating effect on fabrics.

When the drug is used in pharyngeal or nasopharyngeal surgery, the pharyngeal reflex is suppressed. Reaching the larynx and trachea, the drug slows down the cough reflex well, which can lead to bronchopneumonia.

The action of lidocaine in the form of an aerosol develops within 1 min and lasts 5-6 minutes. The achieved decrease in sensitivity slowly disappears within 15 minutes.

It is distributed evenly in the body. Penetrates the placental barrier.

Indications

• prevention and treatment of ventricular arrhythmias (ventricular extrasystole, ventricular paroxysmal tachycardia) associated with the acute phase of myocardial infarction, other forms of CHD, as well as those caused by medications (cardiac glycosides).

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

In dental practice, oral surgery:

• the autopsy of superficial abscesses;
• removal of mobile lost teeth;
• removal of bone fragments and sutures the wounds of the mucous membranes;
• anesthesia gums to fix the crown or bridge;
• or a hand tool removal (or excision) of the enlarged papilla of the tongue;
• to reduce or suppress the increased gag reflex in preparation for x-ray examination;
• anesthesia for excision of superficial benign tumors of the mucous membrane of the oral cavity;
• from kids to frenulectomy and opening the cysts of the salivary glands.

In ENT practice:

• before electrocoagulation (in the treatment of nosebleeds), septectomy and resection of nasal polyps;
• before tonsillectomy to reduce the pharyngeal reflex and anesthetize the injection site;
• as an additional anesthesia before opening the peritonsilar abscess or before puncture of the maxillary sinus;
• anesthesia before washing the sinuses.

During endoscopy and instrumental examinations:

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

In obstetrics and gynecology:

• perineal anesthesia for the treatment and/or performance of episiotomy;
• surgical field anesthesia in vaginal or cervical surgery;
• anesthesia for excision and in the treatment of hymen rupture;
• anesthesia for suturing abscesses.

In dermatology:  

• anesthesia of the mucous membranes during minor surgical interventions.

Use during pregnancy and lactation

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

Lidocaine in an aerosol can be used during pregnancy, because in the recommended doses it does not pose a danger. It is not known whether lidocaine is excreted in breast milk.

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

During lactation, the use of the drug is possible after a preliminary careful assessment of the expected benefit of therapy for the mother and the potential risk for the infant.

Contraindications

• Sinus node weakness syndrome.
• Severe bradycardia.
• Grade 2 and 3 antrioventricular block (except when a ventricular simulation probe is inserted).
• Cardiogenic shock.
• Myasthenia gravis.
• Increased individual sensitivity to lidocaine.
• A history of lidocaine-induced epileptiform seizures.
• Severe liver dysfunction.

When using gypsum as an impression material in dentistry, aerosol is contraindicated due to the risk of aspiration.

Side effects

From the central nervous system:  possible headaches, dizziness, drowsiness, restlessness, euphoria, tinnitus, numbness of the tongue and oral mucosa, speech and vision disorders.

From the cardiovascular system:  at higher doses, hypotension, collapse, bradycardia, and conduction disturbances are possible.

Allergic reactions:  rarely-rash, pruritus, exfoliative dermatitis, anaphylactic shock, hyperthermia.

Local reactions:  a slight burning sensation that disappears as the anesthetic effect develops (within 1 min).

Interaction

It is undesirable to combine lidocaine with the following drugs:

With beta-blockers, due to the increased toxic properties of lidocaine, with digitoxin – due to the weakening of the cardiotonic effect, with curare-like drugs-muscle relaxation is enhanced.

It is not rational to prescribe lidocaine together with aimalin, amiodarone, verapamil or quinidine due to the increased cardiodepressive effect.

The combined use of lidocaine and novocainamide can cause excitement of the central nervous system, hallucinations.

With intravenous use of hexenal or thiopental sodium against the background of lidocaine, respiratory depression is possible.

Under the influence of MAO inhibitors, the local anesthetic effect of lidocaine is likely to increase. Patients taking MAO inhibitors should not be given lidocaine parenterally.

With the simultaneous use of lidocaine and polymyxin-B, it is possible to increase the depressing effect on neuromuscular transmission, so in this case it is necessary to monitor the patient’s respiratory function.

Concomitant use of lidocaine with sleeping pills or sedatives may increase their depressing effect on the central nervous system. When lidocaine is administered intravenously to patients taking cimetidine, undesirable effects such as a state of deafness, drowsiness, bradycardia, parastesias, etc. are possible.

This is due to an increase in the level of lidocaine in blood plasma, which is explained by the release of lidocaine from binding to blood proteins, as well as a slowdown in its inactivation in the liver. If it is necessary to conduct a combination therapy with these drugs, the dose of lidocaine should be reduced.

Pharmaceutical interaction

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

How to take, course of use and dosage

During anesthesia of the esophageal, laryngeal, tracheal mucosa, lubricate the outer surfaces of instruments intended for research; for surface anesthesia of the oral mucosa, apply 0.2-2 g of gel with a sterile glass stick or a sterile cotton swab soaked in gel; in case of insufficient anesthesia, repeat after 2-3 minutes; the maximum dose for adults for 12 hours is 300 mg (6 g of gel); in urology, women – 3-5 ml of 2% gel lubricate the urethral mucosa before the study, catheterization – 100-200 mg (5-10 ml of 2% gel), before cystoscopy for filling and dilating the urethra – 600 mg (30 ml of 2% gel) in 2 doses with an interval of several minutes (the distal part of the urethra is temporarily squeezed). The maximum dose is 600 mg (30 ml of 2% gel) for 12 hours. Children – up to 4.5 mg / kg.

TTS is applied to the painful surface for 12 hours, then a 12-hour break is taken. At the same time, you can nakldyvat no more than 3 TTS. After applying the drug, do not touch your eyes and wash your hands.

In dentistry, for anesthesia of injection site the gel is applied to the mucosa in the area the subsequent infiltration anesthesia at intervals of 2-3 min; for anesthesia during removal of Tartar gel is rubbed into the gingival margin and the neck of the teeth for 2-3 minutes, after which the procedure is carried out; as a therapeutic bandage after removing Tartar or curettage of the gel is applied to the gingival margin and fixed; in applied several times a day on the mucous membrane of the oral cavity in place of aft and erosions

Overdose

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

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

Special instructions

It is used with caution in patients with impaired liver function, circulatory insufficiency, arterial hypotension, renal failure, and epilepsy. In these cases, a reduction in the dose of the drug is required.

With rapid intravenous use, a sharp decrease in blood pressure and the development of collapse can occur.

In these cases, mezaton, ephedrine and other vasoconstrictors are used. Lidocaine solutions should be carefully introduced into highly vascularized tissues to avoid getting the drug into the lumen of the vessel (for example, in the neck during thyroid surgery). ( in such cases, lower doses of lidocaine are indicated.

With extreme caution, the drug should be used in the presence of injuries to the mucous membranes, with mental retardation, as well as in very old and / or weakened patients who are already receiving lidocaine-type drugs for cardiac problems. In dentistry and orthopedics, the drug should be used only with elastic impression materials.

Avoid ingestion of the aerosol or contact with the eyes, and it is important to prevent the aerosol from entering the respiratory tract (risk of aspiration). Applying the drug to the back of the pharynx requires special care. It should be remembered that Lidocaine suppresses the pharyngeal reflex and inhibits the cough reflex, which can lead to aspiration, bronchopneumonia.

Use in pediatrics

It should be borne in mind that in children, the swallowing reflex occurs much more often 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 the ability to drive motor vehicles and manage mechanisms

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

Form of production

spray

Storage conditions

At a temperature of 15-25 °C

Shelf

life is 4 years.

Active ingredient

Lidocaine

Conditions of release from pharmacies

By prescription

Dosage form

spray for external use