Active substanceLidocaineLidocaine
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  • Dosage form: & nbspInjection.
    Composition:
    Active substance: lidocaine hydrochloride monohydrate - 20 mg [in terms of lidocaine hydrochloride].

    Excipients: sodium chloride - 6 mg, 1 M sodium hydroxide solution to pH 5.0 - 7.0, water for injection up to 1 ml.
    Description:Transparent colorless or slightly colored liquid.
    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:It has a local anesthetic effect, blocks potential-dependent sodium channels, which prevents the generation of pulses in the endings of the sensory nerves and impulses along nerve fibers. It suppresses not only pain impulses, but also impulses of another modality. The anesthetic effect of lidocaine is 2-6 times stronger than procaine (it acts faster and longer - up to 75 minutes, and after the addition of epinephrine - more than 2 hours). When applied locally, it dilates the vessels, does not have a locally irritating effect on the tissue.
    Pharmacokinetics:
    For parenteral administration, the degree of absorption depends on the site of administration and the dose.At a concentration of 20 mg / ml is not administered intravenously. The time to reach maximum concentration (Tcmax) when administered epidurally - less than 30 minutes. The connection with plasma proteins is 50-80%. Rapidly distributed (distribution half-life phase 6-9 min), the drug comes first in well-perfused tissues (heart, lungs, brain, liver, spleen), and then in fat and muscle tissue. Penetrates through the blood-brain barrier (GEB), the placental barrier, is secreted with the mother's milk (40% of the concentration in the mother's plasma).

    It is metabolized in the liver (90-95%) with microsomal enzymes by dealkylation amino groups and cleavage of an amide bond to form active metabolites (monoetilglitsinsilidin and glitsinsilidin), half life (T1 / 2) which was 2 hours and 10 hours, respectively. If the liver function is disturbed, the intensity of the metabolism decreases and ranges from 50% to 10% of the normal value. It is excreted with bile (part of the dose is reabsorbed in the gastrointestinal tract) and kidneys (up to 10% unchanged). With chronic renal failure, cumulation of metabolites is possible.Acidification increases the excretion of lidocaine.
    Indications:
    - local infiltration anesthesia;

    - conductor anesthesia (including retrobulbar, parabulbar);

    - spinal anesthesia;

    - epidural anesthesia.
    Contraindications:
    - hypersensitivity to any of the components of the drug;

    - hypersensitivity to other amide local anesthetics in history;

    - infection of the site of the proposed injection;

    - syndrome of weakness of the sinus node;

    - atrioventricular blockade of II-III degree (except when an artificial pacemaker is installed);

    - sinoauric blockade;

    - Wolff-Parkinson-White syndrome (WPW syndrome);

    - cardiogenic shock;

    - violations of intraventricular conduction;

    - closed angle glaucoma (with retrobulbar injection);

    - pregnancy, breastfeeding (penetrates the placental barrier, excreted in breast milk).

    It is also necessary to take into account the general contraindications to the conduct of a particular type of anesthesia.
    Carefully:
    Chronic heart failure II-III functional class according to the classification of the New York Heart Association (NYHA), severe hepatic insufficiency,severe kidney failure, hypovolemia, atrioventricular blockade of the 1st degree, sinus bradycardia, arterial hypotension, severe myasthenia gravis, the presence of epileptiform seizures (including those caused by lidocaine) in history, children under 12 years of age (due to delayed metabolism, possibly accumulation of the drug), seriously ill, weakened patients, elderly age (over 65 years), local anesthesia of blood-rich regions.

    For spinal (subarachnoid) and epidural anesthesia - diseases of the central nervous system (CNS) (including infection, tumors), presence of blood impurities in the cerebrospinal fluid, parasthesia, psychosis, spinal deformity, peripheral neuropathy, aortic stenosis, antiplatelet therapy (including acetylsalicylic acid).
    Pregnancy and lactation:Data on the safety of lidocaine when it is used in pregnant women are not available. During pregnancy and breastfeeding, the drug is contraindicated. If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.
    Dosing and Administration:

    The amount of solution and the total dose of lidocaine depends on the type of anesthesia, the nature and duration of the surgery.

    The method of diluting 20 mg / ml (2%) of lidocaine solution to obtain a solution of the required concentration:

    To prepare 10 mg / ml (1%) solution of lidocaine it is necessary to take 1 part of 20 mg / ml lidocaine solution and 1 part water for injection, i.e. mix 2 ml of 20 mg / ml lidocaine solution with 2 ml water for injection (for a 2 ml ampoule) or mix 5 ml of 20 mg / ml lidocaine solution with 5 ml water for injection (for a 5 ml ampoule).

    To prepare 5 mg / ml (0.5%) solution of lidocaine it is necessary to take 1 part of 20 mg / ml lidocaine solution and 3 part water for injection, i.e. mix 2 ml of 20 mg / ml lidocaine solution with 6 ml of water for injection (for a 2 ml ampoule) or mix 5 ml of 20 mg / ml lidocaine solution with 15 ml of water for injection (for a 5 ml ampoule).

    To prepare a 2.5 mg / ml (0.25%) solution of lidocaine it is necessary to take 1 part of 20 mg / ml lidocaine solution and 7 parts water for injection, i.e. mix 2 ml of 20 mg / ml lidocaine solution with 14 ml of water for injection (for a 2 ml ampoule) or mix 5 ml of 20 mg / ml lidocaine solution with 35 ml of water for injection (for a 5 ml ampoule).

    To prepare 1.25 mg / ml (0.125%) solution of lidocaine it is necessary to take 1 part 20 mg / ml lidocaine solution and 15 parts water for injection, i.e. mix 2 ml of 20 mg / ml lidocaine solution with 30 ml of water for injection (for a 2 ml ampoule) or mix 5 ml of 20 mg / ml lidocaine solution with 75 ml of water for injection (for a 5 ml ampoule).

    For infiltration anesthesia (intradermally, subcutaneously) 0.125%, 0.25%, 0.5% solutions are used; To achieve infiltration anesthesia, up to 60 ml (5-300 mg) of a 0.5% solution or up to 30 ml of a 1% solution is used.

    For conductive anesthesia (anesthesia of peripheral nerves, including blockade of nerve plexuses) 1 and 2% solutions are used; the maximum total dose is up to 400 mg (40 ml of a 1% solution or 20 ml of a 2% solution). For blockade of nerve plexuses, 10-20 ml of a 1% solution or 5-10 ml of a 2% solution.

    For conductive anesthesia of peripheral nerves: humerus - 15-20 ml (225-300 mg) of 1.5% solution; in dental practice - 1-5 ml (20-100 mg) of 2% solution; blockade of intercostal nerves - 3 ml (30 mg) of 1% solution.

    For paracervical anesthesia: 10 ml (100 mg) of 1% solution in each direction, if necessary, repeated administration is possible after at least 1.5 hours.

    For paravertebral anesthesia: from 3 to 5 ml (30-50 mg) of 1% solution.

    Retrobulbaria Anesthesia - 3,0-4,0 ml (60-80 mg) of 2% solution.

    Parabulbar anesthesia 1.0-2.0 ml (20-40 mg) of a 2% solution.

    Vagosimpathetic blockade: cervical (stellate) node - 5 ml (50 mg) of 1% solution, lumbar - 5-10 ml (50-100 mg) of 1% solution.

    Spinal Anesthesia - 3.0-4.0 ml (60-80 mg) of a 2% solution.

    Epidural anesthesia - for the preparation of analgesia 25-30 ml (250-300 mg) of 1% solution is used; to obtain anesthesia 15-20 ml (225-300 mg) of a 1.5% solution or 10-15 ml (200-300 mg) of a 2% solution; for thoracic epidural anesthesia - 20-30 (200-300 mg) of 1% solution. It is not recommended to use continuous administration of anesthetic with a catheter; the maximum dose should not be repeated more than 90 minutes later.

    When using caudal anesthesia: in surgical practice, 15-20 ml (225-300 mg) of a 1.5% solution. It is not recommended to use continuous administration of anesthetic with a catheter; the maximum dose should not be repeated more than 90 minutes later.

    Recommended doses for children with neuromuscular blockade - up to 4.5 mg / kg 0.25-1.0% solution.

    The maximum dose for children is 4.5 mg / kg, but not more than 100 mg; the maximum dose for adults is not more than 4.5 mg / kg or 300 mg. These doses should not be repeated within 24 hours.

    The effect of lidocaine can be prolonged by the addition of a 0.1% solution of epinephrine (0.1 ml per 20 ml of lidocaine).In this case, with regional anesthesia, the dose of lidocaine can be increased to 600 mg.

    The procedure for working with a polymer ampoule: see the diagram on the package.

    1. Take an ampoule and shake it, holding it by the neck.

    2. Press the ampoule with your hand, while the drug should not be isolated, and rotate and separate the valve with rotating movements.

    3. Through the formed hole, immediately connect the syringe with the ampoule.

    4. Turn the ampoule over and slowly put the contents into the syringe.

    5. Put the needle on the syringe.

    Side effects:

    The frequency of adverse events is presented by the World Health Organization (WHO) classification: often 1-10%; infrequently - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.001%, including individual cases.

    From the nervous system and sensory organs: often - dizziness, headache, weakness, infrequent - motor anxiety, rarely - nystagmus, unconsciousness, drowsiness, visual and auditory disorders, tremors, trimester, convulsions (the risk of their development rises against hypercapnia and acidosis), very rarely paralysis of respiratory muscle, respiratory arrest, motor and sensory block, respiratory paralysis (often develops with subarachnoid anesthesia).

    From the cardiovascular system: often - increase or decrease in blood pressure, rarely - bradycardia, arrhythmia, tachycardia - when administered with a vasoconstrictor, very rarely - peripheral vasodilation, collapse, pain in the chest.

    Allergic reactions: often - skin rash, urticaria (on the skin and mucous membranes), itching of the skin, very rarely - angioedema, anaphylactic shock.

    On the part of the organs of the gastrointestinal tract: often - nausea, vomiting, involuntary defecation.

    From the side of the blood: infrequently - methemoglobinemia.

    Local reactions: often - with spinal anesthesia - back pain, with epidural anesthesia - accidental entry into the subarachnoid space.

    Other: infrequent - persistent anesthesia, very rarely - respiratory depression, up to a stop, hypothermia.

    Overdose:
    Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria, drowsiness, headache, paresthesia, disorientation, visual impairment; then - convulsions of mimic muscles of the face with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, asthenia, apnea, bradycardia, lowering of arterial pressure, collapse, methemoglobinemia; when used in childbirth in a newborn - bradycardia, oppression of the respiratory center, apnea.

    Treatment: when the first signs of intoxication appear, the drug is discontinued, the patient is transferred to a horizontal position and oxygenotherapy is performed. When convulsions are administered intravenously 10 mg of diazepam, with bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). If necessary, an artificial ventilation, resuscitation measures. Dialysis is ineffective.
    Interaction:
    Vase-converters (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

    Cimetidine reduces hepatic clearance of lidocaine (decreased metabolism due to inhibition of microsomal oxidation) and increases the risk of toxic effects.

    Reduces the effect of antimiasthenic drugs.

    When treating the site of injection of a local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of tenderness and swelling increases.

    When using local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine,trimethofan with camsilate increases the risk of severe hypotension and bradycardia.

    Beta-adrenoblockers slow down the metabolism of lidocaine, increasing its toxicity

    (decrease in hepatic blood flow).

    Cardiac glycosides weaken the cardiotonic effect.

    Strengthens and lengthens the effect of myorelaxing drugs.

    With the simultaneous administration of lidocaine and hypnotics and sedatives

    means may increase their oppressive effect on the central nervous system.

    When combined with narcotic analgesics, additive

    effect, which is used in epidural anesthesia, but is enhanced

    respiratory depression.

    Use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegi-lin) increases the risk of lowering blood pressure.

    Anticoagulants (including ardeparin sodium, dalteparin sodium, sodium danaparoid, sodium enoxa-parin, heparin sodium, warfarin and others) increase the risk of bleeding.

    Does not reduce the antimicrobial activity of sulfonamides (metabolism does not generate PABA (para-aminobenzoic acid)).
    Special instructions:
    Prophylactic administration to all patients without acute myocardial infarction is not recommended (routine prophylactic administration of lidocaine may increase the risk of death due to an increase in the incidence of asystole). When the inefficiency of lidocaine as an antiarrhythmic drug, it is first necessary to exclude hypokalemia. In urgent situations, a cautious increase in the dose is possible before the occurrence of side effects from the central nervous system (sluggishness, difficulty speaking); or application, sometimes joint, drugs of class AI (procainamide), transition to preparations of III class (amiodarone, brethil tosylate).

    Particular caution should be exercised when carrying out local anesthesia of vascular-rich organs; Avoid intravascular injection during administration. When administered to a vascularized tissue, an aspiration test is recommended. It is necessary to abolish monoamine oxidase (MAO) inhibitors no less than 10 days before planning a subarachnoid anesthetic with lidocaine.

    With rapid intravenous administration, there may be a sharp drop in blood pressure and collapse.In these cases, phenylephrine, ephedrine and other vasoconstrictors.
    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:
    Solution for injection 20 mg / ml.


    Packaging:
    By 2 or 5 ml in polymer ampoules, produced by the technology of "blow-fill-seal" "blow-fill-seal".

    For 5 or 10 polymer ampoules, along with the instructions for medical use, put in a pack of cardboard.
    Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:
    3 years.

    Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LP-002574
    Date of registration:11.08.2014/29.07.2015
    Date of cancellation:2019-08-11
    The owner of the registration certificate:SLAVYANSKAYA APTEKA, LLC SLAVYANSKAYA APTEKA, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp13.04.2016
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