Active substanceLidocaineLidocaine
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  • Dosage form: & nbspinjection
    Composition:


    10 mg / ml

    20 mg / ml

    100 mg / ml

    Active substance:


    Lidocaine hydrochloride monohydrate (in terms of lidocaine hydrochloride)

    - 10 mg

    - 20 mg

    - 100 mg

    Excipients:


    sodium chloride

    - 6 mg

    - 6 mg

    -

    1 M sodium hydroxide solution

    to pH 5.0-7.0

    water for injections

    - up to 1 ml

    Description:
    Transparent colorless or slightly yellowish liquid.
    Pharmacotherapeutic group:Local anesthetic, antiarrhythmic agent
    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:

    Lidocaine in chemical structure refers to acetanilide derivatives. Has a pronounced local anesthetic and antiarrhythmic (IB class) action. The local anesthetic effect is due to the inhibition of nerve conduction by blocking the sodium channels in nerve endings and nerve fibers. By its anesthetic action lidocaine significantly (2-6 times) exceeds procaine; the action of lidocaine develops faster and lasts longer - up to 75 minutes, while with simultaneous application with epinephrine - more than 2 hours.With topical application dilates blood vessels, does not have a locally irritating effect.

    Antiarrhythmic properties of lidocaine are due to its ability to stabilize the cell membrane, block sodium channels. Virtually without affecting the electrophysiological state of the atria, lidocaine accelerates repolarization in the ventricles, depresses the IV depolarization phase in Purkinje fibers (diastolic depolarization phase), reducing their automatism and duration of action potential, increases the minimal potential difference at which myofibrils react to premature stimulation. The speed of rapid depolarization (phase 0) does not affect or slightly reduces. Has no significant effect on conduction and contractility of the myocardium (inhibits conductivity only in large, close to toxic doses). Intervals PQ, QRS and QT under its influence on ECG do not change. Negative inotropic effect is also expressed slightly and manifests itself briefly only with the rapid administration of the drug in large doses.

    Pharmacokinetics:Time to reach the maximum concentration in the blood plasma after intramuscular injection - 5-15 minutes,with slow intravenous infusion without the initial saturating dose - after 5-6 hours (in patients with acute myocardial infarction - up to 10 hours). With proteins of blood plasma, 50-80% of lidocaine is bound. Rapidly distributed (half-life of the distribution phase - 6-9 minutes) in organs and tissues with good perfusion, including in the heart, lungs, liver, kidneys, then in muscle and adipose tissue. Penetrates through the blood-brain and placental barriers, is secreted with the mother's milk (up to 40% of the concentration in the mother's plasma). Metabolized mainly in the liver (90-95% of the dose) with the participation of microsomal enzymes with the formation of active metabolites - monoethylglycinexylidide and glycinexylidide, having a half-life of 2 hours and 10 hours, respectively. The intensity of metabolism decreases with liver diseases (can be from 50 to 10% of the normal value); if there is a violation of liver perfusion in patients after myocardial infarction and / or with chronic heart failure. Half-life with continuous infusion for 24-48 hours - about 3 hours; if the kidney function is impaired - can increase 2 or more times.It is excreted with bile and urine (up to 10% unchanged). Acidification increases the excretion of lidocaine.
    Indications:Infiltration (including subconjunctival), conductive (including retro-bulbar, parabulbar anesthesia), spinal and epidural anesthesia. Coping of resistant paroxysms of ventricular tachycardia (including myocardial infarction and cardiosurgical interventions), prevention of recurrent ventricular fibrillation in acute coronary syndrome and repeated paroxysms of ventricular tachycardia (usually within 12-24 hours), ventricular arrhythmias due to glycoside intoxication (use a solution with concentration of 100 mg / ml).
    Contraindications:

    Syndrome of weakness of the sinus node, pronounced bradycardia, atrioventricular blockade of II-III degree (except when the probe is inserted for stimulation of the ventricles), sinoatrial block, Wolff-Parkinson-White syndrome, acute and chronic heart failure (III-IV functional class), cardiogenic shock, Morgagni-Adams-Stokes syndrome, intraventricular conduction disorders; hypersensitivity to any of the components of the drug;pregnancy, lactation (penetrates through 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 functional class), arterial hypotension, hypovolemia, atrioventricular blockade of the 1st degree, sinus bradycardia, severe hepatic and / or renal insufficiency, severe myasthenia gravis, epileptiform convulsions (including in the anamnesis), decreased hepatic blood flow, weakened or elderly patients (over 65 years of age), children under 18 years of age (due to delayed metabolism, lidocaine accumulation is possible), hypersensitivity to other amide local anesthetics in the anamnesis.
    Pregnancy and lactation:The drug is contraindicated in pregnancy and during lactation.
    Dosing and Administration:

    For infiltration anesthesia: intramuscularly, intradermally, subcutaneously. Apply a solution of lidocaine 5 mg / ml (maximum dose of 400 mg).

    For blockade of peripheral nerves and nerve plexuses: perineural, 10-20 ml of a solution of 10 mg / ml or 5-10 ml of a solution of 20 mg / ml (not more than 400 mg).

    For conductive anesthesia: perineurally apply solutions of 10 mg / ml and 20 mg / ml (not more than 400 mg).

    For epidural anesthesia: epidurally, solutions of 10 mg / ml or 20 mg / ml (not more than 300 mg).

    For spinal anesthesia: subarachnoid, 3-4 ml of a solution of 20 mg / ml (60-80 mg). Parabulbar anesthesia: parabulbar, 1-2 ml of lidocaine 20 mg / ml. Retrobulbaric anesthesia: retrobulbarno, 3-4 ml of a solution of lidocaine 20 mg / ml. Subconjunctival anesthesia: injection under the conjunctiva, 0.5-1 ml of lidocaine solution 20 mg / ml.

    To lengthen the action of lidocaine, it is possible to add ex tempore 0.1% solution of epinephrine (adrenaline) (1 drop per 5-10 ml of lidocaine solution, but not more than 5 drops for the entire volume of the solution).

    It is recommended to reduce the dose of lidocaine in elderly patients and patients with liver diseases (cirrhosis, hepatitis) or with reduced hepatic blood flow (chronic heart failure) by 40-50%.

    With chronic renal failure, dose adjustment is not required.

    For children with local anesthesia, the maximum dose in newborns is 4 mg / kg, in children over 1 year - 5-7 mg / kg.

    Lidocaine solution with a concentration of 100 mg / ml can be used only after dilution.

    As an antiarrhythmic drug: intravenously, 25 ml of a solution of 100 mg / ml, 100 ml of 0.9% sodium chloride solution should be diluted to a lidocaine concentration of 20 mg / ml. This diluted solution is used to administer a loading dose. The administration begins with a loading dose of 1 mg / kg (for 2-4 minutes at a rate of 25-50 mg / min) with immediate connection of a constant infusion at a rate of 1-4 mg / min. Due to the rapid distribution (half-life of about 8 minutes), 10-20 minutes after the first dose, the drug concentration in the blood plasma decreases, which may require a repeated bolus administration (against a background of constant infusion) at a dose of 1 / 2-1 / 3 loading dose, with an interval of 8-10 minutes. The maximum dose at 1 hour is 300 mg, per day 2000 mg.

    Intravenous infusion is usually performed for 12-24 hours with constant ECG monitoring, after which the infusion is stopped to assess the need for changing antiarrhythmic therapy in the patient.

    Intravenously sprayed children - 1 mg / kg (usually 50-100 mg) as a loading dose at a rate of 25-50 mg / min (ie within 3-4 minutes); if necessary, the dose is repeated after 5 minutes, after which a continuous infusion is prescribed.Intravenously in the form of continuous infusion (usually after a loading dose): the maximum dose for children is 30 mcg / kg / min.

    Side effects:

    From the nervous system, the senses and the psyche: oppression or excitation of the central nervous system, nervousness, euphoria, headache, dizziness, drowsiness, general weakness, neurotic reactions, confusion or loss of consciousness, oppression or stopping of breathing, disorientation, convulsions (the risk of developing is increased by background of hypercapnia and acidosis), noise in the ears, paresthesia, diplopia, nystagmus, photophobia, tremor, trichism of facial muscles, anxiety.

    From the cardiovascular system: decreased or increased blood pressure, impaired conduction of the heart, arrhythmia, sinus bradycardia, peripheral vasodilation, collapse, chest pain, cardiac arrest.

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

    From the digestive system: nausea, vomiting.

    Other: feeling of "heat", "cold" or numbness of limbs, persistent anesthesia,erectile dysfunction, malignant hyperthermia, methemoglobinemia, flickering before the eyes and tachycardia with simultaneous administration with a vasoconstrictor.

    Overdose:

    Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria, lowering blood pressure, asthenia; then - convulsions of mimic muscles with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, bradycardia, asystole, collapse; when used during childbirth, a newborn may have bradycardia, respiratory depression, apnea.

    Treatment - discontinuation of the drug, pulmonary ventilation, inhalation with oxygen. Symptomatic therapy. With convulsions intravenously administered 10 mg of diazepam. With bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). It is possible to carry out intubation, artificial ventilation, resuscitation. Hemodialysis is ineffective.

    Interaction:

    Beta-blockers and cimetidine increase the risk of toxic effects. Aymalin, amiodarone, verapamil and quinidine increase the negative inotropic effect.

    Inducers of microsomal liver enzymes (barbiturates, phenytoin, rifampicin) reduce the effectiveness of lidocaine.

    Vasoconstrictors (epinephrine, methoxamine, phenylephrine) lengthen the local anesthetic effect of lidocaine and can cause an increase in blood pressure and tachycardia.

    Lidocaine reduces the effect of antimiasthenic drugs.

    Co-administration with procainamide can cause excitation of the central nervous system, hallucinations.

    Guanadrel, guanethidine, mecamylamine, trimetaphane camsylate increase the risk of pronounced reduction in blood pressure and bradycardia. Strengthens and prolongs the action of muscle relaxants.

    The combined use of lidocaine and phenytoin should be used with caution, since it is possible to reduce the resorptive action of lidocaine, as well as the development of an undesirable cardiodepressant effect.

    Under the influence of monoamine oxidase inhibitors, it is likely that local anesthetic action of lidocaine is enhanced and blood pressure is lowered. Patients taking monoamine oxidase inhibitors, lidocaine should not be appointed.

    With the simultaneous administration of lidocaine and polymyxin B, an increase in the inhibitory effect on the neuromusculartransmission. In this case, it is necessary to monitor the function of the patient's breathing.

    With the combined use of lidocaine with hypnotics or sedatives, narcotic analgesics, hexenal or thiopental sodium, it is possible to intensify the inhibitory effect on the central nervous system and respiration. When intravenous lidocaine is administered to patients receiving cimetidine, such undesirable effects as stunnedness, drowsiness, bradycardia, paresthesia, etc. are possible. This is due to the increase in lidocaine concentration in the blood plasma, which is explained by liberation of lidocaine from the connection with blood proteins, as well as slowing its inactivation in the liver. If the need for combined therapy with these drugs should reduce the dose of lidocaine.

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

    Special instructions:

    It is not recommended to prevent the prescription of the drug to all patients without exception with acute myocardial infarction (routine preventive administration of lidocaine may increase the risk of death due to an increase in the incidence of asystole).When lidocaine is ineffective, hypokalemia should be first and foremost eliminated, in urgent situations there are several options for further action: cautious dose increase until the occurrence of side effects from the central nervous system (sluggishness, difficulty speaking); appointment, sometimes co-medication, IA class medications (procainamide), transition to preparations of III class (amioaron, brethil tosylate).

    It is necessary to abolish monoamine oxidase inhibitors in at least 10 days, in case of planned use of lidocaine.

    Care should be taken when carrying out local anesthesia of tissues with high vascularity, an aspiration test is recommended to avoid intravascular injection.

    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 10 mg / ml, 20 mg / ml, 100 mg / ml.
    Packaging:

    5 ml or 10 ml (for solutions of 10 mg / ml or 20 mg / ml) and 2 ml (for solutions of 20 mg / ml or 100 mg / ml) in ampoules.

    For 10 ampoules of 2 ml or 10 ml are placed in cartons of cardboard with corrugated septa.

    For 5 ampoules of 2 ml, 5 ml or 10 ml in a contiguous cell pack of a polyvinyl chloride film. For 1, 2 contour squares are placed in a pack of cardboard. In each pack, the box is enclosed with the instruction for use, the ampoule knife or the scarifier (when packing ampoules with a break ring, a point and an incision, an ampoule knife or a scarifier do not invest).

    Storage conditions:In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.
    Shelf life:2 years. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N001276 / 01-2002
    Date of registration:09.02.2009 / 01.12.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia
    Manufacturer: & nbsp
    Information update date: & nbsp27.02.2018
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