Lidocaine - instructions for use, dose, side effects, contraindications

Excipients: ethanol (ethyl alcohol 95%) 15.36 g / 18.594 mg, propylene glycol 3.8 g (4.6 mg), levomenthol (L-Menthol) 0.076 g / 0.092 mg, sodium hydroxide (sodium hydroxide) 0.19 g / 0.23 mg, purified water 14.774 g / 17.884 mg.

Description:

Transparent colorless or yellowish tinged liquid with a characteristic smell of ethyl alcohol and menthol, located in a vial with a mechanical metering pump.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

N.01.B.B Amides

N.01.B.B.02 Lidocaine

C.01.B.B.01 Lidocaine

C.01.B.B Antiarrhythmic drugs Ib class

Pharmacodynamics:

The local anesthetic effect is due to the blockade of voltage-dependent sodium channels, which prevents the generation of pulses in the endings of the sensory nerves and pain impulses along nerve fibers. With topical application dilates blood vessels, does not have a locally irritating effect.

The effect develops after 1-5 min after application to the mucous membranes and lasts 10-15 minutes.

Pharmacokinetics:

Quickly 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 mucosa, the total dose of the drug, the localization of the site and the duration of the application. After application to the mucous membrane of the upper respiratory tract is partially swallowed and inactivated in the digestive tract. The period of reaching the maximum concentration (Tmax) when applied to the mucosa of the oral cavity and upper respiratory tract is 10-20 minutes. The connection with proteins depends on the concentration of the drug and is 60-80% at a drug concentration of 1-4 μg / ml (4.3-17.2 μmol / L).

The drug is quickly distributed, first enters the well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. Penetrates through the blood-brain and placental barrier, is secreted with the mother's milk (40% of the concentration in the mother's plasma). Metabolised in the liver (by 90-95%) with the participation of microsomal enzymes. With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value.It is excreted with bile and kidneys (up to 10% unchanged). With chronic renal failure, cumulation of metabolites is possible. Acidification increases the release of lidocaine.

Indications:Terminal (superficial) anesthesia of the mucous membranes: in stomatology (anesthesia of the injection site before local anesthesia, suturing of the mucosa, extirpation of milk teeth, removal of calculus), in otorhinolaryngology (nasal septum surgery, electrocoagulation, etc.), in obstetrics and gynecology (episiotomy and treatment of the incision, removal of sutures, vaginal and cervical interventions, etc.); with instrumental and endoscopic studies (probe insertion, rectoscopy, intubation, etc.), radiographic examination (elimination of nausea and pharyngeal reflex).

Contraindications:Hypersensitivity.

Carefully:Hemorrhoidal bleeding (for rectal examination), local infection in the field of application, trauma of the mucous membrane in the field of application, severe somatic pathology, younger children, elderly age, pregnancy, lactation.

Pregnancy and lactation:

The results of controlled clinical studies in pregnant women are absent. If it is necessary to use local anesthesia and there is no more safe treatment, lidocaine Spray can be used during pregnancy.

Lidocaine is excreted into breast milk, but after applying the usual therapeutic doses, its amount given off with milk is too small to harm any infant.

Dosing and Administration:

Locally, in dentistry, otolaryngology - 1-4 doses, with endoscopic and instrumental methods of research - 2-3 doses, in obstetrics - 15-20 doses, gynecology - 4-5 doses. The maximum dose is 40 doses with a body weight of 70 kg. In children, in dental practice, it is preferable to apply as a lubricant (to avoid the patient's fear of sprays) by pre-impregnating a cotton swab.

The severity of local anesthetic action depends on the individual characteristics of the patient.

Side effects:

Allergic reactions: allergic contact dermatitis (hyperemia at the site of application, skin rash, hives, itching), angioedema.

Overdose:

Symptoms: increased sweating, pale skin, dizziness, headache, blurred vision, ringing in the ears, diplopia, lowering blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness, tremor, anxiety, agitation, convulsions, methhemoglobinaemia, cardiac arrest.

Treatment: Further administration was stopped, the patient is transferred to a horizontal position when the first signs of intoxication (dizziness, nausea, euphoria); prescribe oxygen inhalation; with convulsions - intravenously 10 mg of diazepam; with bradycardia - M-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is ineffective.

Interaction:

Cimetidine and propranolol reduces hepatic clearance of lidocaine (decrease in metabolism by inhibiting microsomal oxidation and reduction of hepatic blood flow) and increase the risk of toxic effects (including stunned state, drowsiness, bradycardia, paresthesia et al.).

When administered with aymalin, phenytoin, verapamil, quinidine, amiodarone, an increase in the negative inotropic effect is possible.Co-administration with beta-blockers increases the risk of bradycardia.

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

Procainamide increases the risk of developing CNS excitement, hallucinations.

With the simultaneous administration of lidocaine, hypnotics and sedatives, it is possible to intensify their inhibitory effect on the central nervous system.

With intravenous injection of hexobarbital or thiopental sodium on the background of the action of lidocaine, respiratory depression is possible.

Under the influence of monoamine oxidase inhibitors, local anesthetic action of lidocaine is possible.

Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) reduce the effectiveness of the drug (an increase in dose may be required). With the simultaneous use of lidocaine and polymyxin, the oppressive effect on neuromuscular transmission may be increased, so in this case it is necessary to monitor the function of the patient's breathing.

Special instructions:

It is important not to let lidocaine enter the respiratory tract (risk of aspiration). Application to the throat requires special attention.

Application to the mucous membrane of the cheeks is accompanied by a risk of dysphagia and subsequent aspiration, especially in children. If the sensitivity of the tongue and the mucous membrane of the cheeks are impaired, the risk of their biting 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.

In cases of application of a spray during surgical operations in the pharynx or nasopharynx, it should be taken into account that lidocaine, suppressing the pharyngeal reflex, falls into the larynx and trachea and suppresses the cough reflex, which can lead to bronchopneumonia. This is especially important in children, because they often cause a swallowing reflex. In this regard, the spray is not recommended for local anesthesia before tonsillectomy and adenectomy in children under the age of 8 years.

Care should be taken when applying lidocaine to the damaged mucosa and / or infected areas.

The drug should be used with caution in patients with epilepsy, as well as with bradycardia, impaired conduction in the heart, impaired liver function and severe shock, especially when you can expect absorption of a significant amount of the drug when treating large areas of tissue with high doses.

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

In children under 2 years of age Lidocaine Spray is recommended to apply with a cotton swab dipped in the preparation.

During application, the vial should be kept as vertically as possible. The spray should not get into the eyes.

The bottle must not be opened or heated. Regional and local anesthesia should be carried out by experienced specialists in an appropriately equipped room with availability of ready-to-use equipment and preparations necessary for cardiac monitoring and resuscitation. Personnel performing anesthesia should be qualified and trained in the technique of performing anesthesia, should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Spray for topical use dosed, 4.6 mg / dose.

Packaging:

For 38 g (650 doses) in a polymer vial (high-density polyethylene) with a dosing pump and a protective cap. The bottle together with a spray for oral use or a dental nozzle and instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of 15 ° C to 25 ° C.

Keep out of the reach of children.

Shelf life:4 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002739 / 01

Date of registration:26.11.2007 / 09.01.2017

Expiration Date:Unlimited

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp27.02.2018

Illustrated instructions

Instructions

Lidocaine (Lidocaine)