Active substanceLidocaineLidocaine
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  • Dosage form: & nbspInjection.
    Composition:
    Active substance: lidocaine hydrochloride (in terms of anhydrous substance) - 40 mg;

    Excipients: sodium chloride - 12 mg, 1 M sodium hydroxide solution - up to pH 5.0 - 7.0, water for injection - up to 2 ml.
    Description:Transparent colorless or slightly yellowish liquid.
    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 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 min, and after the addition of epinephrine, more than 2 h). With topical application dilates blood 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 the maximum concentration (Tcmax) with epidural administration is less than 30 minutes.

    The connection with plasma proteins is 50-80%.Distributed quickly (the half-life of the distribution phase - 6-9 minutes), first the drug enters the well-blood-supplying tissues (heart, lungs, brain, liver, spleen), then into adipose 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). Metabolised 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 active metabolites (monoethylglycinexylidine and glycinexylidine), the half-life (T1 / 2) of which is 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 classification of New York Heart Association (NYHA), severe hepatic failure, severe renal insufficiency, hypovolemia, atrioventricular block I degree, sinus bradycardia, hypotension, myasthenia gravis, history of epileptiform convulsions (in including those caused by lidocaine),children under 12 years of age (due to delayed metabolism, possibly accumulation of the drug), seriously ill, weakened patients, advanced age (over 65 years), local anesthesia of blood-rich regions.

    For spinal (subarachnoid) and epidural anesthesia, central nervous system (CNS) disease (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 parts 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 must take 1 part 20 mg / ml of lidocaine and 7 parts of water for injection, t. e. mixing 2 ml of 20 mg / ml lidocaine solution with 14 ml of water for injections (to ampoules of 2 ml) or mixed with 5 ml of 20 mg / ml lidocaine solution with 35 ml water for injection (for a 5 ml ampoule).

    To prepare 1.25 mg / ml (0.125%) solution of lidocaine must take 1 part 20 mg / ml of lidocaine and 15 parts of water for injection, t. e. mixing 2 ml of 20 mg / ml lidocaine solution with 30 ml of water for injections (to ampoules of 2 ml) or mixed with 5 ml of 20 mg / ml lidocaine solution with 75 ml 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 the peripheral nerves, including when blocking the nerve plexuses) apply 1 and 2% solutions; 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: 3 to 5 ml (30-50 mg) of 1% solution. Retrobulbar anesthesia - 3.0-4.0 (60-80 mg) of a 2% solution.

    Parabulbar anesthesia 1.0-2.0 (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 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 ml (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 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 to 4.5 mg / ml 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 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:

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

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

    3.After the opening, immediately connect the syringe with the ampoule.

    4. Turn over the ampoule and slowly fill the syringe with its contents.

    5. Put the needle on the syringe.

    Side effects:

    The frequency of side effects is given in accordance with the classification of the World Health Organization: very often - not less than 10%; often - not less than 1% and less than 10%; not often - not less than 0.1% and less than 1%; rarely - not less than 0.01% and less than 0.1%; very rarely - less than 0.01%, including isolated cases.

    From the central nervous system and sensory organs: often - dizziness, headache, weakness, infrequently - motor anxiety, rarely - nystagmus, loss of consciousness, drowsiness, visual and auditory disorders, tremor, trismus, convulsions (the risk of their development increases against hypercapnia and acidosis), rarely - paralysis of the respiratory muscles, respiratory arrest, motor and sensory block, respiratory paralysis (often develops with subarachnoid anesthesia).

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

    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 - pain in the back, with epidural anesthesia - accidental entry into the subarachnoid space.

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

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

    Overdose:
    Symptoms: initial signs of intoxication - dizziness, nausea, vomiting, euphoria, drowsiness, headache, paresthesia, disorientation, impaired vision; 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, a newborn has bradycardia, depression of the respiratory center, apnea.

    Treatment: when the first signs of intoxication appear, the administration is stopped, the patient is transferred to a horizontal position and oxygenation is performed.When convulsions are administered intravenously 10 mg of diazepam, with bradycardia - m-holinoblokatory (atropine), vasoconstrictors (norepinephrine, phenylephrine). If necessary, intubation, mechanical ventilation, resuscitation. Dialysis is ineffective.
    Interaction:
    Vasoconstrictors (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.

    With the use of local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimethofan camzilate, the risk of severe hypotension and bradycardia increases.

    Beta-andrenoblokatory slows the metabolism of lidocaine, increasing its toxicity (decrease in the value of 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, it is possible to intensify their inhibitory effect on the central nervous system.

    When combined with narcotic analgesics, an additive effect develops, which is used in epidural anesthesia, but respiratory depression is increased.

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

    Anticoagulants (including ardeparin sodium, dalteparin sodium, sodium danaparoid, sodium enoxaparin, 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:
    It is inadmissible to use lidocaine, a solution for injection (2%), as an antiarrhythmic agent.

    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 the planning of subarachnoid anesthesia with lidocaine.

    With rapid intravenous injection, there may be a sharp decrease

    blood pressure and develop 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 2%.
    Packaging:
    2 ml per ampoule of glass.

    For 10 ampoules, together with a knife or scarifier for opening ampoules and instructions for medical use are placed in a box of cardboard with a corrugated liner of corrugating paper. 10 ampoules are placed in a blister pack of a polyvinyl chloride film. 1 blister pack together with a knife or scarifier for opening ampoules and instructions for medical use are placed in a pack of cardboard.

    For 10 ampoules, together with a knife or scarifier for opening ampoules and instructions for medical use, put in a pack of cardboard with a cardboard insert to fix the ampoules.

    In the case of using ampoules with a kink ring or with a notch and a break point, the insertion of a knife or scarifier for opening ampoules is not provided.
    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:П N015364 / 01
    Date of registration:03.11.2009/18.07.2014
    The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus
    Manufacturer: & nbsp
    Information update date: & nbsp12.04.2016
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