Active substanceAtracuria bezylateAtracuria bezylate
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  • Dosage form: & nbspsolution for intravenous administration
    Composition:

    1 ml of the drug contains

    active substance: atrakuria besilata 10 mg

    Excipients: benzenesulfonic acid, water for injection.

    Description:Colorless or light yellow transparent solution.
    Pharmacotherapeutic group:Non-depolarizing muscle relaxant peripheral action
    ATX: & nbsp

    M.03.A.C   Other quaternary ammonium compounds

    M.03.A.C.04   Atracuria bezylate

    Pharmacodynamics:Highly selective competitive nondepolarizing muscle relaxant of peripheral action. Reduces the sensitivity of synaptic n-cholinergic receptors to acetylcholine, which blocks the excitation of muscle fibers and their contraction. Promotes the release of histamine. At a dose of 0.3-0.6 mg / kg (depending on the required duration of neuromuscular blockade) provides adequate myoplegia within 15-35 minutes.A dose of 0.5 to 0.6 mg / kg allows intubation of the trachea in the first 90 seconds from the time of administration. Spontaneous recovery of conduction after complete neuromuscular blockade occurs after approximately 35 minutes (determined by restoring the tetanic contraction to 95% of the baseline).
    Pharmacokinetics:

    Metabolized by elimination of Hofmann (non-enzymatic process, occurring at physiological values ​​of blood pH and body temperature) and by ether hydrolysis with the participation of nonspecific esterases. Metabolites pharmacologically inactive. Do not cumulate, do not penetrate the placental barrier in clinically significant concentrations. Physiological changes in blood pH and body temperature have little effect on the duration of the action. The duration of neuromuscular blockade does not change because of the deficiency of liver and kidney functions, as well as the level of plasma pseudocholinesterase. Under hypothermia conditions (up to 25-26 ° C) there is a decrease in the rate of inactivation. Hemofiltration and hemodiafiltration have a minimal effect on the concentration of atracurium besylate and its metabolites in blood plasma.

    Indications:

    Miorelaxation for carrying out artificial ventilation (IVL), intubation of the trachea, surgical interventions.

    Contraindications:Hypersensitivity to any of the components of the drug, age up to 1 month.
    Carefully:

    Myasthenia gravis, hypersensitivity to histamine, bronchial cancer, dysfunction of the respiratory system (including respiratory depression), dehydration, severe disturbances of the acid-base state and electrolyte balance, arterial hypotension, hypothermia.

    Pregnancy and lactation:

    When carrying out studies on animals, a teratogenic and embryotoxic effect was detected. Studies in humans have not been conducted. Atrakurium-Medargo can be used during pregnancy only if the potential benefit to the mother exceeds the possible negative effects on the fetus.

    It is possible to use it to create muscle relaxation during caesarean section, since when administered the drug at recommended doses, a clinically insignificant quantity penetrates the placenta.

    There are no data on the isolation of the drug with breast milk.

    Dosing and Administration:

    Intravenously, infusion.

    The dose is set individually and depends on the necessary duration and depth of the neuromuscular blockade.

    Adults

    - Bolus administration.

    To provide muscular relaxation within 15-35 minutes 0.3-0.6 mg / kg is administered. The dose for intubation of the trachea is 0.5-0.6 mg / kg. The duration of complete neuromuscular blockade can be increased by introducing additional doses at the rate of 0.1-0.2 mg / kg.

    - Infusion introduction.

    After bolus administration, it is possible to administer the drug as a continuous infusion at a rate of about,3-0.6 mg / kg / hour to maintain neuromuscular blockade during long-term surgical interventions. This method of administration can be recommended for operations on the lungs and the heart. To maintain complete myoplegia with artificial hypothermia, the infusion rate should be reduced by a factor of 2.

    Atrakurium-Medargo is compatible with the following infusion solutions:

    Infusion solution

    Stability period

    A solution of sodium chloride 0.9%

    24 hours

    A solution of dextrose 5%

    8 ocloc'k

    Ringer's solution

    8 ocloc'k

    A solution of sodium chloride 0.18% + dextrose 4%

    8 ocloc'k

    Hartmann's solution

    4 hours

    Children.

    Children over 1 month are prescribed in the same dosages (based on body weight) as adults.

    The elderly.

    Dose adjustment is not required, however, it is recommended to use the lower level of the dose range.

    Impaired liver and / or kidney function.

    A dose adjustment is not required.

    Diseases of the cardiovascular system.

    In patients with severe cardiovascular pathology, the initial dose should be administered at least 60 seconds.

    Application in intensive care units.

    After initial bolus administration at a dose of 0.3-0.6 mg / kg, administered by continuous infusion at a rate of 0.65-0.78 mg / kg / h, however, in different patients, a dose variation of 0.27 mg / kg / hour up to 1.77 mg / kg / hour.

    After the initial bolus dose, drip continuous infusion can be used to maintain the required degree of neuromuscular blockade at a rate of 6-10 μg / kg / min. The exact dosage during infusion is provided by the use of a special metered micropump. When the body is hypothermic, complete neuromuscular blockade is maintained at doses equal to half the usual dose.

    The dose in children 1-24 months - 0.3-0.4 mg / kg, over 2 years - as in adults.

    Doses for children younger than 1 month - doses not established. For elderly patients, they recommend use the lowest recommended dose with reduced injection rate - 60 sec.

    Side effects:

    From the cardiovascular system:

    decrease and increase of blood pressure; moderate tachycardia; vasodilation, sometimes arrhythmia.

    Allergic reactions:

    bronchospasm, laryngospasm, edema, erythema, skin rash, hives, itchy skin, anaphylactoid reactions.

    Other:

    increased intraocular pressure, drooling, rhabdomyolysis, manifested by myoglobinemia and myoglobinuria, malignant hyperthermia.

    Local reactions:

    Usually Atrakurium-Medargo is well tolerated, sometimes in the place of administration, redness of the skin is possible.

    Overdose:

    Overdose can cause depression of the cardiovascular and respiratory systems. In case of oppression of the respiratory system, artificial ventilation of the lungs with oxygen should be performed until spontaneous breathing is restored. When signs of spontaneous recovery of respiration appear, it can be accelerated by the administration of anticholinesterase agents in combination with atropine. When oppression of cardiovascular activity, it is necessary to change the position of the patient - the head should be lowered and the legs lifted, if these disorders are serious, vasopressor and plasma-substituting agents should be used.

    Interaction:

    The use of the drug together with inhalation anesthetics (enflurane, isoflurane) can enhance the effect, so the dose of Atrakurium-Medargo should be reduced to 1 / 2-1 / 3 of the usually recommended.

    Neuromuscular blockade may be strengthened by the joint use of the drug following medicines: antibiotics, including aminoglycosides and polypeptide antibiotics (polymexin), lincomycin, clindamycin, tetracyclines, spectinomycin, capreomycin; antiarrhythmic drugs (propranolol, slow calcium channel blockers, lidocaine, procainamide, quinidine); diuretics (furosemide, perhaps - mannitol, thiazide, acetazolamide); magnesium sulfate; ketamine; lithium salts; ganglion blockers (trimetafan kamsilata, hexamethonium); citrates.

    Sometimes certain drugs can enhance or unmask a latent myasthenia gravis or cause a myasthenic syndrome. As a result of this effect, hypersensitivity to the drug Atrakurium-Medargo may develop. To drugs with this effect are: antibiotics, beta2-adrenoblockers (propranolol, oxprenolol), antiarrhythmic drugs (procainamide, quinidine), antirheumatic drugs (chloroquine, D-penicillamine), trimethofan camsilate, chlorpromazine, steroids, phenytoin, lithium preparations.

    Reduces the effect of anticholinesterase drugs.

    Compatible with the following infusion solutions for the time indicated below:

    - 0.9% solution of sodium chloride for intravenous administration - 24 hours;

    - 5% glucose solution for intravenous administration - 8h;

    - Ringer's injection solution is 8 hours;

    - solution for intravenous administration containing 0.18% sodium chloride solution and 4% glucose solution - 8h;

    - sodium lactate solution for intravenous administration (Hartman solution) - 4h.

    After diluting the drug in these solutions and adjusting the concentration of atracurium besilate to 0.5-0.9 mg / ml, the resulting solutions can be stored in daylight for the indicated time at ambient temperatures up to + 30 ° C.

    Special instructions:

    Atrakurium-Medargo does not affect consciousness, therefore the drug should be used only in combination with adequate general anesthesia, under the supervision of an experienced anesthesiologist.This should not be done by a doctor performing surgical or diagnostic procedures. The patient must be constantly monitored. In the presence there should be an equipment of artificial ventilation, oxygen enrichment, and also other reanimation means.

    When the drug is administered for general anesthesia through the same needle or catheter, a vein rinse with a 0.9% sodium chloride solution is necessary after the injection of each drug.

    Atrakurium-Medargo is inactivated in a medium with a high pH, ​​so the drug should not be administered in the same syringe with thiopental and other alkaline preparations.

    When used in recommended doses, Atrakurium-Medargo does not have a pronounced ganglion-blocking effect and does not suppress vagal innervation. Therefore Atrakurium-Medarga at recommended doses does not have a clinically significant effect on the rhythm of heartbeats and the administration of this drug does not eliminate bradycardia, which develops with many means for anesthesia or with vagal stimulation during surgical interventions.

    During the introduction of the drug, there is a risk of increased release of histamine in patients who are predisposed to it. Precautions should be taken with the use of the drug in patients who are suspected to have or have had a history of episodes of hypersensitivity to the action of histamine.

    In patients with bronchial asthma, receiving high doses of corticosteroids, it is necessary to evaluate the level of serum creatinine phosphokinase.

    When using the drug in a caesarean section, one should keep in mind the potential for respiratory depression and decreased muscle activity in newborns.

    Form release / dosage:Solution for intravenous administration 10 mg / ml.
    Packaging:

    By 2.5 ml into ampoules of colorless hydrolytic glass I type with a yellow dot on the top of the ampoule.

    5, 10 ampoules are placed in a plastic tray sealed with foil.

    1 plastic tray with 5 ampoules, sealed with foil, along with instructions for use in a cardboard box.

    1 or 5 plastic pallets with 10 ampoules sealed with foil, along with instructions for use in a cardboard box.

    Storage conditions:

    List A.

    In the dark place at a temperature of 2 to 8 ° C.Do not freeze.

    Keep out of the reach of children.

    Shelf life:

    2 years. The drug should be used before the date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-006974/08
    Date of registration:01.09.2008 / 18.05.2012
    Expiration Date:Unlimited
    The owner of the registration certificate:Hana Pharmaceutical Co., Ltd. Hana Pharmaceutical Co., Ltd. The Republic of Korea
    Manufacturer: & nbsp
    HANA PHARMACEUTICAL, Co. Ltd. The Republic of Korea
    Representation: & nbspPULMOMED CJSC PULMOMED CJSC Russia
    Information update date: & nbsp20.09.2017
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