Lidocaine-ACOS, 6 mg/dose 38 g

Pharmacotherapeutic group

Local anesthetic agent

ATX code: N01BB

Pharmacodynamics:

Lidocaine is an amide type local anesthetic.

The local anesthetic action is due to reversible inhibition of nerve conduction by blockade of sodium channels in the nerve endings, thus preventing generation of impulses at the end of sensitive nerves and conducting of pain impulses along the nerve fibers.

Lidocaine has a rapid onset of action, high anesthetic activity and low toxicity.

In local application it dilates blood vessels and has no local irritant effect. It has analgesic effect.

The effect shall develop 1-5 minutes after application to the mucous membranes or skin and shall last for 10-15 minutes.

Pharmacokinetics:

It is quickly absorbed from mucous membranes (especially pharynx and respiratory tract) the degree of absorption of the drug is determined by the degree of blood supply to the mucous membrane by the total dose of the drug, location of site and duration of application. After application to the mucous membrane of the upper respiratory tract it is partially swallowed and inactivated in the gastrointestinal tract.

The time of reaching maximum concentration (ÒCmax) in plasma when applied to the mucous membrane of the oral cavity and upper respiratory tract is 10-20 minutes. Protein binding depends on the drug concentration and is 60-80% at drug concentration of 1-4 µg/ml (43-172 µmol/L). Fast drug distribution (half-life (T1/2) of distribution phase is 6-9 min) goes first to well supplied with blood tissues (heart, lungs, brain, liver, spleen) and then to fat and muscle tissues. It penetrates through the blood-brain barrier and the placental barrier and is secreted with the mother’s milk (40% of the concentration in the mother’s plasma).

Metabolized in the liver (90-95%) with microsomal enzymes by dealkylation of the amino group and breaking the amide bond to form less active compared to lidocaine metabolites (monoethylglycincylidine and glycincylidine) with a T1/2 of 2 h and 10 h respectively. In liver disease the metabolic rate is reduced and is 50% to 10% of the normal value. It is excreted with the bile and the kidneys (up to 10% unchanged).

In chronic renal failure cumulation of metabolites is possible. Urinary acidification contributes to increased excretion of lidocaine.

Indications

The drug may be used for local anesthesia in the following cases:

in dentistry – for terminal (superficial) anesthesia: anesthetization of the injection area before local anesthesia; opening of superficial abscesses; before mucosal sutures; before fixation of crowns and bridges; in the treatment of gum inflammation periodontopathies; extirpation of milk teeth; removal of tartar;

in otolaryngology – operations on the septum and removal of nasal polyps; conducting electrocoagulation in the treatment of nosebleeds elimination of pharyngeal reflex and anesthesia of the injection needle site before removal of tonsils; opening of peritonsillar abscesses; puncture of maxillary sinus;

In obstetrics and gynecology – egshiziotomy and incision handling; removal of sutures; minor operations on the vagina and cervix; rupture of the hymen; treatment of thread abscesses;

In instrumental and endoscopic examinations – before insertion of a probe through the nose or mouth (including duodenal tube.

In radiographic examination – to eliminate nausea and pharyngeal reflex;

as an analgesic (analgesic) medication for burns (including sunburns); bites; contact dermatitis (including those caused by irritants).

Surface skin anesthesia for minor surgical interventions.

Active ingredient

Composition

In 1 dose:

Active substance: lidocaine hydrochloride monohydrate (in terms of lidocaine hydrochloride) – 4.6 mg;

Auxiliary substances: 96% ethanol (rectified ethyl alcohol, grade “Extra”) – 18.4 mg, propylene glycol – 4.6 mg, sodium hydroxide (sodium hydroxide) – 0.23 mg, sodium saccharinate dihydrate (sodium saccharin) – 0.138 mg, racementol (menthol racemic) – 0.092 mg, purified water – up to 0.046 g.

How to take, the dosage

It is used topically and topically.

The dosage may vary depending on the indication and the size of the area to be anesthetized.

One dose of spray released by pressing the dispensing valve contains 46 mg of lidocaine.

Pressure recommendations for various applications:

Application area

Number of presses

Dentistry

1-4

Otorhinolaryngology

1-4

Endoscopic and instrumental examinations

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2-3

Obstetrics

15-20

Gynecology

4-5

Dermatology

1-3

Interaction

Vasoconstrictors (epinephrine phenylephrine methoxamine) prolong the local anesthetic effect of lidocaine.

Cimetidine and propranolol decrease 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 stun states sleepiness bradycardia paresthesia, etc.).

The barbiturates phenytoin rifampicin (inducers of microsomal liver enzymes) reduce the effectiveness of lidocaine (may require increasing the dose).

Phenytoin verapamil quinidine amiodarone may increase the negative inotropic effect.

The co-administration with beta-adrenoblockers increases the risk of bradycardia.

The cardiac glycosides attenuate the cardiotonic effect curare-like drugs increase muscle relaxation.

Procainamide increases the risk of central nervous system agitation of hallucinations.

The simultaneous administration of lidocaine and hypnotics and sedatives may increase their suppressive effects on the central nervous system.

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

Under the influence of monoamine oxidase inhibitors (furazolidone procarbazine selegiline) the local anesthetic effect of lidocaine may be enhanced. Patients taking monoamine oxidase inhibitors should not prescribe lidocaine parenterally.

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

Special Instructions

The bottle should be kept in an upright position when in use.

Avoid contact with the eyes and respiratory tract (risk of aspiration). Particular caution should be exercised when applying to the back of the throat.

Application to the cheek mucosa presents a risk of dysphagia and subsequent aspiration, particularly in children.

The sensitivity of the tongue and cheek mucosa increases the risk of biting.

Lidocaine is well absorbed through mucous membranes (especially in the trachea) and damaged skin. This should be taken into account especially when treating large areas of tissue in children.

If the spray is used for surgical procedures in the pharynx or nasopharynx, note that by suppressing the pharyngeal reflex, lidocaine enters the larynx and trachea and suppresses the cough reflex, which can lead to bronchopneumonia. This is especially important in children because they are more likely to have a pharyngeal reflex. Therefore, the spray is not recommended for local anesthesia before tonsillectomy and adenotomy in children under 8 years of age.

Caution should be exercised when applying lidocaine to damaged mucosa and/or infected areas.

The drug should be used with caution in patients with epilepsy as well as in patients with bradycardia, cardiac conduction abnormalities, hepatic dysfunction and severe shock especially when significant amounts of the drug can be expected to be absorbed when treating large tissue areas with high doses.

Lower doses should be used in frail and elderly patients with acute illnesses and in children, according to age and general condition.

In children under 2 years of age, Lidocaine Spray is recommended to be applied with a cotton swab moistened with the product.

We should be careful during treatment to drive vehicles and engage in other potentially hazardous activities that require increased concentration and quick psychomotor reactions.

Contraindications

– Hypersensitivity to lidocaine or any other component of the drug;

– Instrumental examination (rectoscopy) in patients with hemorrhoidal bleeding;

– Local infection in the area of application;

Side effects

In the place of application of the drug: a slight burning that stops after the onset of anesthesia (within 1 minute) erythema edema impaired sensitivity.

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

The use of the drug should be discontinued if any allergic reaction occurs.

The incidence of systemic reactions after using Lidocaine aerosol is extremely low because very small amounts of the active drug are applied and may enter the bloodstream.

If large doses are applied and if hypersensitivity and idiosyncrasy are quickly absorbed, the following side effects on the central nervous system and cardiovascular system may occur.

In the central nervous system, systemic reactions may be observed: headache dizziness cramps tremors visual disturbance tinnitus agitation and/or depression feeling of fear euphoria anxiety fever feeling of cold depressed breathing.

Cardiovascular system: increase in blood pressure decrease in blood pressure bradycardia arrhythmia suppression of myocardial function.

Others: urethritis (after local application).

Overdose

Symptoms: increased sweating pale skin nausea vomiting dizziness headache blurred vision tinnitus diplopia decreased blood pressure bradycardia arrhythmia sleepiness chills numbness tremors agitation convulsions methemoglobinemia cardiac arrest.

Treatment: At the first signs of intoxication (dizziness nausea vomiting euphoria) the patient is transferred to a horizontal position and oxygen inhalation is prescribed; for psychomotor agitation, intravenous 10 mg diazepam; for convulsions, IV 1% solution of hexobarbital or sodium thiopental; for bradycardia, IV 05-1 mg atropine sympathomimetic agents (norepinephrine phenylephrine). Dialysis is ineffective.

Pregnancy use

There are no results of controlled clinical trials in pregnant women.

If local anesthesia is required and if safer treatment is not available, the drug may be used during pregnancy.

Lidocaine is excreted in breast milk; however, after normal therapeutic doses, the amount excreted in milk is too small to cause any harm to the infant.

Similarities