Active substanceLidocaineLidocaine
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  • Dosage form: & nbsp
    Spray for local and external use.

    Composition:in one bottle contains: active substance - lidocaine 3.8 g; auxiliary substances - ethanol, xylitol, water for injections.
    Description:Transparent colorless or with a yellowish tinge solution.
    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 inhibition of nerve conduction by blocking the sodium channels in the nerve endings, 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 within 1-5 minutes after application to the mucous membranes or skin and persists for 10-15 minutes.
    Pharmacokinetics:
    Quickly absorbed from the mucous membranes (especially the pharynx and the 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 gastrointestinal tract. Time to reach the maximum concentration (TCmax) in the plasma when applied to the mucosa of the oral cavity and upper respiratory tract - 10-20 min. 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). It is distributed rapidly (half-life (T1 / 2) of the distribution phase is 6-9 minutes), first it enters the well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose and muscle tissue. Penetrates through the blood-brain and placental barriers, is secreted with the mother's milk (40% of the concentration in the mother's plasma).

    It is metabolized in the liver (by 90-95%) with participation of microsomal enzymes by dealkylation of the amino group and breaking of the amide bond with the formation of metabolites (monoethylglycinexldine and glycinexylidine) that are less active than lidocaine, T1 / 2 of which are 2 h and 10 h respectively. 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:

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

    in dentistry for terminal (superficial) anesthesia: anesthesia of the injection site before local anesthesia; opening of superficial abscesses; Before suturing the mucosa; before fixing the crowns and bridges; at treatment of an inflammation of gums, paradontopaty; extirpation of infant teeth; removal of tartar;

    in otorhinolaryngology: surgery on the nasal septum and removal of the polyps of the nose; electrocoagulation in the treatment of nasal bleeding; elimination of the pharyngeal reflex and anesthesia of the injection site of the injection needle before removal of the tonsils; opening of peritonsillar abscesses;

    in obstetrics and gynecology - episiotomy and cut treatment; removal of stitches; small surgery on the vagina and cervix; breakthrough of the hymen; treatment of filamentous suppuration;

    with instrumental and endoscopic studies - before inserting the probe through the nose or mouth (duodenal sounding and fractional examination of gastric secretion); with rectoscopy, intubation;

    when radiographic examination - elimination of nausea and pharyngeal reflex;

    as an analgesic drug for burns (including sunburn); bites; contact dermatitis (including caused by irritating plants); small wounds (including scratches);

    superficial anesthesia of the skin with small surgical interventions.

    Contraindications:Hypersensitivity.
    Carefully:
    hemorrhoidal bleeding (rectal examination), local infection in the field of application, trauma of the mucous membrane or skin in the field of application, concomitant acute diseases, weakened patients, younger children, elderly age, pregnancy, lactation.

    Dosing and Administration:Locally, externally. The required amount of the preparation can vary widely depending on the size and nature of the surface to be treated. Recommendations for the number of clicks in various applications:

    Application area

    Number of clicks

    Stomatology

    1-4

    Otolaryngology

    1-4

    Endoscopic and instrumental studies

    2-3

    Obstetrics

    15-20

    Gynecology

    4-5

    Dermatology

    1-3

    To avoid absorption of the drug in the systemic circulation, the minimum dose providing the effect should be applied. Usually enough 1-3 clicks; It is possible to apply 15-20 or more pressures (maximum 40 pressures per 70 kg of body weight).

    In dental practice, it is preferable to use children in the form of lubrication (in order to avoid the fright of the child during spraying) by pre-impregnating a cotton swab.

    Side effects:

    In the place of application: slight burning, which stops after anesthesia (within 1 minute), erythema.

    Possible allergic reactions, allergic contact dermatitis (hyperemia at the site of application, skin rash, hives, itching), angioedema, anaphylactic shock.

    From the central nervous system can there are systemic reactions: headache, dizziness, convulsions, tremor, visual impairment, tinnitus excitation and / or depression, a sense of fear, euphoria, anxiety, fever, a feeling of cold, respiratory depression.

    From the side of the cardiovascular system: increased blood pressure, bradycardia.

    Other: urethritis (after topical application).

    Overdose:
    Symptoms: increased sweating, pale skin, nausea, vomiting, dizziness, headache, blurred vision, ringing in the ears, diplopia, lowering blood pressure, bradycardia, arrhythmia, drowsiness, chills, numbness, tremor, anxiety, agitation, convulsions, methaemoglobinaemia, heart failure.

    Treatment: at the appearance of the first signs of intoxication (dizziness, nausea, vomiting, euphoria) the patient is transferred to a horizontal position and oxygen inhalation is prescribed; at psychomotor excitation - intravenously (iv) 10 mg of diazepam; with convulsions - in / in 1% solution of hexobarbital or thiopental sodium; at a bradycardia - in / in 0,5-1 mg atropine, sympathomimetic agents. Dialysis is ineffective.
    Interaction:
    Cimetidine and propranolol reduce liver lidocaine clearance (decrease in metabolism due to inhibition of microsomal oxidation and decrease in hepatic blood flow) and increase the risk of toxic effects (including stun, drowsiness, bradycardia, paresthesia, etc.).

    Barbiturates, phenytoin, rifampicin (inducers of microsomal liver enzymes) reduce efficacy (an increase in dose may be required).

    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 increase muscle relaxation.

    Procainamide increases the risk of excitation of the central nervous system, hallucinations.

    With the simultaneous administration of lidocaine and 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. Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine parenterally. With the simultaneous use of lidocaine and polymyxin, it is possible to intensify the inhibitory effect on neuromuscular transmission,therefore in this case it is necessary to monitor the function of the patient's breathing.
    Special instructions:When using the bottle, keep it in a vertical position. Avoid contact with eyes and respiratory tract (risk of aspiration). It requires special care application of the drug in the region of the posterior pharyngeal wall.
    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:
    Spray for local and external use 10%.


    Packaging:For 38 g is placed in a bottle of polypropylene or polyethylene with a protective cap complete with a spray nozzle. One bottle together with the instruction for use is placed in a cardboard pack.
    Storage conditions:
    List B.

    Store in a dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.
    Shelf life:
    3 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:LSR-000082/10
    Date of registration:15.01.2010/23.04.2010
    The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp12.04.2016
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