Lidocaine-ACOS spray for local and external use 4.6mg/dose, 38g

Composition

Per 1 dose:

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

Auxiliary substances:  96% ethanol (ethyl alcohol rectified, the sort of “Extra”) is 18.4 mg, propylene glycol – 4,6 mg, sodium hydroxide (sodium hydroxide) – 0,23 mg, sodium saccharin dihydrate (sodium saccharin) – 0,138 mg, ramenta (menthol racemic) – 0,092 mg, purified water – up to 0,046 g.

Pharmacological properties

Pharmacotherapeutic group

Local anesthetic agent

ATX Code: N01BB

Pharmacodynamics :

Lidocaine is an amide-type local anesthetic.

The local anesthetic effect is caused by reversible inhibition of nerve conduction due to the blockade of sodium channels in the nerve endings, which prevents the generation of impulses in the endings of sensitive nerves and the conduct of pain impulses along nerve fibers.

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

When applied topically, dilates blood vessels does not have a local irritant effect. It has an analgesic effect.

The effect develops in 1-5 minutes after application to the mucous membranes or skin and persists for 10-15 minutes.

Pharmacokinetics:

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

The time to reach the maximum concentration (TMAX) in plasma when applied to the oral mucosa and upper respiratory tract is 10-20 minutes. Protein binding depends on the drug concentration and is 60-80% at a drug concentration of 1-4 mcg / ml (43-172 mmol / L). It is distributed quickly (half-life (T 1/2) of the distribution phase is 6-9 minutes), first enters well-supplied tissues (heart lungs brain liver spleen), then into adipose and muscle tissues. Penetrates through the blood-brain and placental barriers and is secreted in breast milk (40% of the maternal plasma concentration).

It is metabolized in the liver (by 90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and breaking the amide bond with the formation of metabolites less active than lidocaine (monoethylglycinxylidine and glycinxylidine) T 1/2 of which is 2 hours and 10 hours, respectively. In liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value. It is excreted in the bile and kidneys (up to 10% unchanged).

In chronic renal failure, accumulation of metabolites is possible. Acidification of urine increases the release of lidocaine.

Indications

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

in dentistry – for the terminal (surface) anesthesia: analgesia in the area before the injection of local anesthesia; opening of superficial abscesses; prior to suturing the mucous membrane; in front of crowns and bridges; in the treatment of inflammation of the gums parodontopatii; extirpation of milk teeth; removal of Tartar;

surgery – surgery on the nasal septum and removal of polyps of the nose; the holding of electrocoagulation in the treatment of nasal bleeding; the elimination of pharyngeal reflex and the epidural space of the injection needle before removing the tonsils; an autopsy peritonsillar abscesses; puncture of the maxillary sinus;

in obstetrics and gynecology – assitalia and treatment of the section; removal of seams; small operation on the vagina and cervix, break the hymen; processing thread suppuration;

instrumental and endoscopic studies before the introduction of the probe through the nose or mouth (including duodenal intubation and fractional study of gastric secretion); at rectoscopy intubation;

when radiographic examination is the elimination of nausea and gag reflex;

as analgesic (analgesic) drugs for burns (including solar); bites; contact dermatitis (including caused by irritating plants); small wounds (including scratches);

surface anesthesia of the skin with a small surgical interventions.

Use during pregnancy and lactation

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

If you need to use local anesthesia and there is no safer treatment, the drug can be used during pregnancy.

Lidocaine is excreted in breast milk, but after applying the usual therapeutic doses, the amount released in milk is too small to cause any harm to the infant.

Contraindications

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

– use of lidocaine in the form of a spray for tonsillectomy and adenotomy in children under 8 years of age.

With caution:

– Tests (rectoscopy) in patients with hemorrhoidal bleeding;

local infection in the application;

– the trauma of the mucous membrane or the skin in the application;

– severe somatic pathology;

– epilepsy;

– bradycardia is a violation of cardiac conduction;

– disorders of the liver;

– heavy shock

– associated acute diseases;

– weakened patients;

pregnancy breastfeeding;

the younger child age;

old age.

Side effects

At the site of application of the drug:  mild burning sensation that stops after the onset of anesthesia (within 1 minute) erythema edema sensitivity disorder.

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

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

The frequency of systemic reactions after applying Lidocaine aerosol is extremely low because a very small amount of the active drug is applied which can enter the bloodstream.

In the case of high doses and rapid absorption hypersensitivity idiosyncrasy poor tolerability of the drug, the following side effects may occur from the central nervous system and cardiovascular system.

From the central nervous system, systemic reactions may occur: headache dizziness convulsions tremor visual disturbances tinnitus agitation and / or depression feelings of fear euphoria anxiety fever cold sensation respiratory depression.

From the cardiovascular system:  increased blood pressure decreased blood pressure bradycardia arrhythmia inhibition of myocardial function.

Other services:  urethritis (after topical application).

Interaction

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

Cimetidine and propranolol reduce 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 dazed state, drowsiness, bradycardia, paresthesia, etc. ).

Barbiturates phenytoin rifampicin (inducers of microsomal liver enzymes) reduce the effectiveness of lidocaine (an increase in the dose may be required).

When administered with aimalin phenytoin verapamil quinidine amiodarone, it is possible to increase the negative inotropic effect.

Co-use with beta-blockers increases the risk of developing bradycardia.

Cardiac glycosides weaken the cardiotonic effect curare-like drugs enhance muscle relaxation.

Procainamide increases the risk of central nervous system arousal and hallucinations.

When lidocaine is administered simultaneously with sleeping pills and sedatives, it is possible to increase their depressing effect on the central nervous system.

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

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 be prescribed lidocaine parenterally.

With the simultaneous use of lidocaine and nolimixin, 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.

How to take it, course of use and dosage

Apply topically externally.

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

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

Recommendations for the number of clicks in different application areas:

The drug can also be applied with a cotton swab soaked in it.

To avoid absorption of the drug into the systemic circulation, a minimum dose should be used to ensure the effect. Usually 1-3 taps are sufficient; 15-20 taps or more can be used (the maximum dose is 40 taps per 70 kg of body weight).

In dental practice in children, it is preferable to apply in the form of lubrication (in order to avoid the child’s fright when spraying) by pre-impregnation with a cotton swab.

Overdose

Symptoms: increased sweating pallor of the skin nausea vomiting dizziness headache blurred vision tinnitus diplopia decreased blood pressure bradycardia arrhythmia drowsiness chills numbness tremor restlessness agitation seizures 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 05-1 mg of atropine sympathomimetic agents (norepinephrine phenylephrine). Dialysis is ineffective.

Special instructions

When using the bottle, keep it in an upright position.

Avoid contact with eyes and respiratory tract (risk of aspiration). Special care should be taken when applying the drug to the posterior pharyngeal wall.

Application to the cheek mucosa is associated with the risk of dysphagia and subsequent aspiration, especially in children.

If the sensitivity of the tongue and cheek mucosa is disturbed, the risk of biting them increases.

Lidocaine is well absorbed through the 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 operations in the pharynx or nasopharynx, it should be noted that lidocaine suppresses the pharyngeal reflex and 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 mucous membranes and / or infected areas.

The drug should be used with caution in patients with epilepsy as well as in patients with bradycardia impaired cardiac conduction impaired liver function and severe shock especially when a significant amount of the drug can be expected to be absorbed when treating large areas of tissue with high doses.

Lower doses should be used in debilitated and elderly patients with acute diseases, as well as in children-in accordance with age and general condition.

In children under 2 years of age, Lidocaine spray is recommended to be applied with a cotton swab soaked in the preparation.

Influence on the ability to drive vehicles and mechanisms:

During the treatment period, care should be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store in a dark place at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use after the expiration date indicated on the package.

Active ingredient

Lidocaine

Conditions of release from pharmacies

By prescription

Dosage form

spray for external use