Active substanceLidocaineLidocaine
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  • Dosage form: & nbspInjection.
    Composition:
    active substance: 20 mg / ml 100 mg / ml

    lidocaine hydrochloride monohydrate

    (in terms of lidocaine hydrochloride) 20.0 mg, 100.0 mg;

    Excipients:

    sodium chloride 6.0 mg;

    sodium hydroxide solution 1M to a pH of 5.0-7.0;

    water for injections up to 1.0 ml.
    Description:
    Transparent, colorless or slightly colored liquid.

    Pharmacotherapeutic group:Local anesthetic and 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:It has a local anesthetic effect, it blocks the potential-dependent sodium channels, which prevents the generation of pulses in the endings of the sensory nerves and the impulses in the endings of the sensory nerves and impulses along nerve fibers. It suppresses not only pain impulses, but also impulses of another modality. It is used for all types of local anesthesia: infiltration, conduction and surface. Anesthetic action of lidocaine lasts up to 75 minutes, and after the addition of epinephrine - more than 2 hours.With topical application dilates blood vessels, does not have a locally irritating effect. Has antiarrhythmic (lb class) properties. Stabilizes cell membranes, blocks sodium channels, increases membrane permeability for potassium ions. Almost without affecting the electrophysiological state of the atria, accelerates repolarization in the ventricles, depresses the depolarization phase IV in Purkinje fibers (especially the ischemic myocardium), reducing their automatism and the duration of the action potential. Practically does not affect the conductance and contractility of the myocardium (conduction inhibition is noted when administered only in large, close to toxic doses) - the duration of the intervals PQ, QT (duration of the ventricular complex, reflecting the duration of the electric systole of the ventricles) and width of the QRS complex (the first phase of the ventricular complex, reflecting the process of depolarization of the ventricles) on the ECG (electrocardiogram) does 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:
    With parenteral absorption, the absorption is complete (the rate of absorption depends on the site of administration and the dose). Time to reach the maximum concentration (Tshah) with intravenous administration - 3-5 minutes. The connection with plasma proteins is 50-80%. It is distributed rapidly (the distribution phase of the distribution phase is 6-9 min), first it enters the well-blood-supplying tissues (heart, lungs, liver, spleen), then into adipose and muscle tissue. Penetrates through the blood-brain barrier and placental barrier, sek-retitsya with breast milk (40% of the concentration in the plasma of the mother). The half-life (T1 / 2) (after intravenous bolus administration) -1.5-2 h; in newborns - 3 hours. With prolonged infusion of lidocaine within 24-48 hours significantly increases (up to 3 hours). If there is a violation of liver function, T1 / 2 increases 2 times or more. With constant infusion (without the introduction of the initial saturating dose), the therapeutically effective concentration (2-6 μg / ml) is reached after 5-9 hours.

    Metabolised in the liver (by 90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and breaking of the amide bond to form active metabolites (monoethylglycinexylidine and glycinexylidin) having T1 / 2 - 2 hours and 10 hours, respectively.With liver diseases, the intensity of metabolism decreases and ranges from 50% to 10% of the normal value.

    It is excreted in the bile (part of the dose is reabsorbed in the gastrointestinal tract and kidneys (up to 10% in unchanged form.) In chronic renal failure, cumulation of metabolites is possible. Acidification increases the release of lidocaine.
    Indications:
    For the concentration of the drug 20 mg / ml:
    - local anesthesia (terminal, conductor) in surgery, dentistry, otolaryngology; blockade of peripheral nerves and nerve plexuses in various pain syndromes.

    For the concentration of the drug 100 mg / ml:

    - treatment and prevention of mono- and polytopic ventricular extrasystole and tachycardia of various genesis, especially in the acute phase of myocardial infarction.
    Contraindications:
    - syndrome of weakness of the sinus node;

    - severe bradycardia;

    - atrioventricular blockade of 2 and 3 degrees (with the exception of cases when a probe is inserted to stimulate the ventricles);

    - severe forms of chronic heart failure;

    - cardiogenic shock;

    - severe arterial hypotension, a collapoid state;

    - liver failure;

    - hypersensitivity;

    - the presence in the anamnesis of epileptiform seizures caused by lidocaine;

    - for paracervical introduction in obstetric practice - fetoplacental insufficiency, prematurity, endurance, toxicosis of pregnancy;

    - for epidural anesthesia - neurological diseases, deformation of the spine;

    - for subarachnoid anesthesia - back pain, diseases of the central nervous system (including infection, tumors), coagulopathy (caused by anticoagulants or blood clotting disorder), headache (including migraine in the anamnesis), the presence of a blood impurity in the cerebrospinal fluid, arterial hypertension, arterial hypotension, paresthesia, psychosis, hysteria, non-contact patient, deformation of the spine;
    Carefully:Heart failure of II-III degree, cardiovascular insufficiency, hepatic insufficiency, renal failure, hypovolemia, atrioventricular blockade of I degree, Wolff-Parkinson-White syndrome, sinus bradycardia, arterial hypotension, severe myasthenia gravis, children under 6 years, pregnancy, period lactation.
    Pregnancy and lactation:During pregnancy and lactation, use only for life indications. Lidocaine excreted in breast milk.
    Dosing and Administration:

    Before applying Lidocaine 20 mg / ml, it is mandatory to carry out a skin test for increased individual sensitivity to the drug, which is indicated by edema and redness of the injection site.

    For local anesthesia apply injectively (subcutaneously, intramuscularly) and topically on mucous membranes. Avoid intravascular drug administration.

    For conductive anesthesia (including for pain relief of the brachial and sacral plexus), the usual dose for adults is 5-10 ml of the solution (100-200 mg of lidocaine).

    For anesthesia of fingers limbs, nose, and ear are injected with 2-3 ml of solution (40-60 mg of lidocaine).

    The maximum dose of a solution of lidocaine for adults when used for conductive anesthesia is 10 ml (200 mg of lidocaine).

    For terminal anesthesia, mucous membranes lubricate with a solution of Lidocaine in a volume of not more than 20 ml for adults in a dose of up to 2 mg / kg of body weight, the duration of anesthesia is 15-30 minutes. For superficial anesthesia of the mucous membranes of the nasal cavity, nasopharynx, larynx, oral cavity, esophagus, rectum, respiratory and urinary tract, the vagina is prescribed lubrication adult solution in dosage up to 2 mg / kg body weight; duration of anesthesia is 15-30 minutes. The maximum dose of the solution to adults is 20 ml. Intravenous 25 ml of 100 mg / ml solution diluted in 100 ml 0.9% sodium chloride solution to a concentration of lidocaine 20 mg / ml, which was used as a loading dose of 1-1.5 mg / kg (within 2-4 min at a rate of 25-50 mg / min) with immediate connection of a constant infusion at a rate of 1-4 mg / min. Because of the rapid distribution (T1/2 approximately 8 minutes), 10-20 minutes after the first dose, the concentration of the drug 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 min. The maximum dose per hour is 300 mg, per day 2000 mg. Intravenous infusion is carried out for 12-24 hours with constant elektrokardiogramnym-monitoring, after which the infusion was stopped, to evaluate the need to change antiarrhythmic therapy in a patient. The elimination rate of the drug is reduced in chronic heart failure and liver dysfunction (cirrhosis, hepatitis), which requires reducing the dose and rate of administration of the drug to 25- 50%.Intravenously sprayed: children - 1 mg / kg (usually 50-100 mg) as a loading dose at a rate of 25-50 mg / min (that is, within 3-4 minutes); if necessary, the dose is repeated after 5 minutes, after which a continuous intravenous infusion is prescribed. Intravenously, as a continuous infusion (usually after a loading dose): the maximum dose for children is 30 μg / kg / min (20-50 μg / kg / min).

    Side effects:- From the side of the nervous system and sensory organs: dizziness, headache, mood reduction, euphoria, neurotic reactions, confusion, drowsiness, tinnitus, paresthesia, diplopia, tremor, facial muscles facial trimesus, seizures, loss of consciousness.

    - From the cardiovascular system: lowering blood pressure, bradycardia, vasodilation, arrhythmia, collapse, chest pain, cardiac arrest.

    Allergic reactions: skin rash, hives, itching, angioedema, anaphylactic shock.

    - Local reactions: with spinal anesthesia - pain in the back, with epidural anesthesia - accidental entry into the subarachnoid space. Other: nausea, involuntary urination and defecation, decreased libido, impotence, respiratory depression until the stop.
    Overdose:
    Symptoms: the first signs of intoxication - dizziness, nausea, vomiting, euphoria; then - convulsions of facial muscles of the face with transition to tonic-clonic convulsions of skeletal muscles, psychomotor agitation, general weakness, apnea, bradycardia, lowering of arterial pressure, collapse, methemoglobinemia; when used in childbirth in a newborn - bradycardia, oppression of the respiratory center, apnea.

    Treatment: the patient should be in a horizontal position; prescribe oxygen inhalation and injected intravenously 10 mg of diazepam. In cases of manifestations of skeletal muscle cramps, the latter are stopped by a slow intravenous injection of 1% hexobarbital or thiopental sodium solution. With bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). Dialysis is not effective.
    Interaction:
    With the simultaneous use of lidocaine and beta-blockers, it is possible to intensify the toxic effects of lidocaine.

    It is irrational to appoint lidocaine together with aymalin, amiodarone, verapamil or quinidine in connection with the intensification of cardiodepressive action.

    The joint use of lidocaine and procainamide can cause excitation of the central nervous system, hallucinations.

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

    Combined use of lidocaine and phenytoin should be used with caution, since it leads to increased cardiodepressive effect. Under the influence of monoamine oxidase inhibitors, the local anesthetic action of lidocaine is likely to increase. Patients taking monoamine oxidase inhibitors should not be prescribed lidocaine parenterally. With simultaneous application of lidocaine and polymyxin B may increase inhibitory effect on neuromuscular transmission, is used as an antiarrhythmic, so in this case it is necessary to monitor the patient's respiratory function.

    With the combined use of lidocaine with hypnotics or sedatives, it is possible to intensify the inhibitory effect on the central nervous system.

    Under the influence of cimetidine intravenous administration of lidocaine causes unwanted effects (stunning, drowsiness, bradycardia, etc.).If necessary, combination therapy should reduce the dose of lidocaine.

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

    Reduces the effect of antimiasthenic drugs. When administered with aymalin, phenytoin, quinidine, amiodarone, an increase in the negative inotropic effect is possible. 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 intravenous injection of hexobarbital or thiopental sodium on the background of the action of lidocaine, respiratory depression is possible.

    Anticoagulants (including heparin, 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, of IA class medications (procainamide), transition to preparations of III class (amiodarone, brethil tosylate). Caution should be given with local anesthesia of organs rich in blood vessels; Avoid intravascular injection during administration. When diluted, the toxicity decreases. During the treatment period it is necessary to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

    With rapid intravenous administration, there may be a sharp drop in blood pressure and collapse. In these cases, phenylephrine, ephedrine and other vasoconstrictors.
    Form release / dosage:
    Solution for injection 20 mg / ml, 100 mg / ml.
    Packaging:
    2 ml of the drug into neutral glass ampoules.

    Each label is labeled with label paper or writing paper, or self-adhesive, or the label text is applied to the ampoule by gravure printing with a fast-fixing ink.

    5 ampoules are placed in a contour mesh package from a polyvinyl chloride film without coating.

    1 or 2 contour mesh packages are placed in a pack of cardboard for consumer containers.

    5.10 ampoules are placed in a pack of cardboard for consumer containers with partitions or grilles, or a paperboard separator for consumer packaging or sack paper.

    10 ampoules are placed in a box of cardboard for consumer containers and with a loose leaf of paper paste. The box is pasted with a label-parcel of paper label or coated.

    Each instruction pack or box is supplied with instructions for use, an ampoule knife or ampoule scarifier.

    When using ampoules with incisions, break rings or break points, the ampoule knife or the ampoule scapegrator is not inserted. Packs and boxes are placed in a group package.
    Storage conditions:In a place protected from light and inaccessible to children at a temperature of no higher than 30 ° C.
    Shelf life:2 of the year. Do not use after the expiry date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:LS-001516
    Date of registration:04.10.2011/12.08.2015
    The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia
    Manufacturer: & nbsp
    Information update date: & nbsp11.04.2016
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