Arduan (Arduan)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substancePiperecuronium bromidePiperecuronium bromide
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    • Dosage form: & nbsplyophilizate for the preparation of a solution for intravenous administration
    Composition:

    Lyophilizate

    Active substance: pipecuronium bromide 4 mg in each vial.

    Excipients: mannitol.

    Solvent:

    Sodium chloride, water for injection.

    Description:

    Lyophilizate: white or almost white lyophilizate.

    Solvent: colorless and clear solution.

    Pharmacotherapeutic group:Muscle relaxant nondepolarizing peripheral action
    ATX: & nbsp

    M.03.A.C.06   Piperecuronium bromide

    Pharmacodynamics:

    It is a non-depolarizing long-acting muscle relaxant. Due to the competitive connection with n-holinoretseptorami, located on the end plate of the neuromuscular synapse of skeletal muscles, blocks the transmission of the signal from the nerve endings to the muscle fibers. Does not cause muscle fasciculation, does not have a hormonal effect.

    Even at doses several times greater than its effective dose,necessary for 90% reduction in muscle contractility (ED90), does not have ganglion blocking, m-cholinoblocking and sympathomimetic activity.

    According to studies, with balanced anesthesia, ED50 and ED90 doses of pipecuronium bromide are 0.03 and 0.05 mg / kg body weight, respectively.

    A dose of 0.05 mg / kg of body weight provides 40-50 minutes of muscle relaxation during various operations.

    The maximum effect of pipecuronium bromide depends on the dose and occurs after 1.5-5 minutes. The effect develops most rapidly at doses equal to 0.07-0.08 mg / kg. A further increase in the dose reduces the time required for the development of the effect, and significantly prolongs the effect of the drug.

    Pharmacokinetics:

    When administered intravenously, the initial volume of distribution (Vdc) is 110 ml / kg body weight, the volume distribution in the saturation phase (Vdss) reaches 300 (± 78) ml / kg, the plasma clearance (CI) is approximately 2.4 (± 0.5) ml / min / kg, the mean half-life (T1/2β) is 121 (± 45) min, the average time in the blood plasma (MRT) is 140 min.

    With repeated administration of maintenance doses, the cumulative effect is insignificant if doses of 0.01-0.02 mg / kg were used at the time of 25% recovery of the initial muscle contractility.

    It is excreted mainly by the kidneys, with 56% of the drug in the first 24 hours. One third is unchanged, and the rest is in the form of 3-deacetyl-pipecuronon bromide.

    According to preclinical research, the liver is also involved in the elimination of pipecuronium bromide.

    Penetrates through the placental barrier.

    Indications:Endotracheal intubation and relaxation of skeletal muscles with general anesthesia during various surgical operations requiring more than 20-30-minute muscle relaxation and under conditions of mechanical ventilation.
    Contraindications:

    - Hypersensitivity to pipecuronium bromide and / or bromide.

    - Children up to 3 months.

    - Severe hepatic insufficiency.

    Carefully:Biliary tract obstruction, edematous syndrome, increased circulating blood volume or dehydration, diuretics, acid-base disorder (acidosis, hypercapnia) and water-electrolyte metabolism (hypokalemia, hypermagnesia, hypocalcemia), hypothermia, digitalisation, hypoproteinemia, cachexia, myasthenia gravis number of myasthenia gravis, Eaton-Lambert's syndrome) because of the possible in such cases as strengthening, and weakening the effect of the drug.Small doses of Arduan with severe myasthenia gravis or Eaton-Lambert's syndrome can cause a pronounced effect. Such patients are prescribed at very low doses after careful assessment of potential risk, respiratory depression, renal failure (prolongs the effect of the drug and post-nasal depression), decompensated chronic heart failure, children under 14 years of age, malignant hyperthermia, anaphylactic reaction caused by some muscle relaxant in a patient's anamnesis (because of possible cross-allergy).
    Pregnancy and lactation:

    Clinical studies to prove the safety of the use of Arduan in pregnant women and the fetus is not enough. The use of the drug during pregnancy is not recommended.

    Clinical data on the safe use of Arduan during lactation is not enough. The use of the drug during breastfeeding is not recommended.

    Dosing and Administration:

    As with other non-depolarizing muscle relaxants, Arduan's dose is selected for each patient individually, taking into account the type of anesthesia, the estimated duration of the surgery,possible interactions with other medications used before or during anesthesia, concomitant diseases and the general condition of the patient.

    It is recommended to use a peripheral nerve fiber stimulator to control the neuromuscular block.

    Use only intravenously. Immediately prior to administration 4 mg of dry substance is diluted with the applied solvent.

    Recommended doses for adults and children over 14 years of age:

    - initial dose for intubation and subsequent surgical intervention: 0.06-0.08 mg / kg body weight, provides good / excellent conditions for intubation for 150-180 sec, while the duration of muscle relaxation is 60-90 min;

    - The initial dose for miorelaxation with intubation using suxamethonium: 0.05 mg / kg, provides 30-60-minute muscle relaxation;
    - maintenance dose: 0.01-0.02 mg / kg, provides 30-60-minute muscle relaxation during surgery;

    - In chronic renal failure, doses exceeding 0.04 mg / kg are not recommended (in large doses, an increase in the duration of muscle relaxation may be possible);

    - with excess weight and obesity, it is possible to prolong the action of Arduan, therefore, a dose calculated for ideal weight should be used.

    Doses in children: from 3 to 12 months. - 0.04 mg / kg (which provides muscle relaxation lasting from 10 to 44 minutes).

    From 1 year to 14 years - 0,05-0,06 mg / kg (muscular relaxation - from 18 to 52 minutes).

    Termination of the effect: at the time of 80-85% of the blockade, measured with a stimulant of peripheral nerve fibers, or at the time of partial blockade, determined by clinical signs, the use of atropine (0.5-1.25 mg) in combination with neostigmine methylsulfate (1-3 mg) or galantamine (10-30 mg) stops the muscle relaxant effect of Arduan.

    Side effects:

    From the nervous system: rarely (less than 1%): depression of the central nervous system (CNS), drowsiness, hypoesthesia, paralysis of skeletal muscles.

    From the musculoskeletal system: rarely (less than 1%): weakness of skeletal muscles after cessation of muscle relaxation, muscle atrophy.

    From the respiratory system: rarely (less than 1%): apnea, lung atelectasis, respiratory depression, laryngospasm as a result of an allergic reaction, bronchospasm, cough.

    From the cardiovascular system: rarely (less than 1%): myocardial ischemia (up to myocardial infarction) and the brain, arrhythmias, tachycardia, bradycardia, decreased or increased blood pressure, atrial fibrillation, ventricular extrasystole, ventricular tachycardia.

    On the part of the organs of hematopoiesis and the system of hemostasis: rarely (less than 1%): thrombosis, reduced activated partial thromboplastin and prothrombin time.

    From the urinary tract of the system: rarely (less than 1%): anuria.

    Allergic reactions: rarely (less than 1%): skin rash, allergic reactions, edema Quincke.

    Laboratory indicators: rarely (less than 1%): hypercreatininaemia, hyperglycemia, hypokalemia, hypomagnesemia, hypocalcemia.

    Other: blepharitis, ptosis.

    Overdose:

    Symptoms: prolonged paralysis of skeletal musculature and apnea, marked decrease in blood pressure (BP), shock.

    In case of an overdose or a prolonged neuromuscular block, the artificial ventilation of the lungs continues until the recovery of spontaneous breathing. At the beginning of the recovery of spontaneous breathing, an acetylcholinesterase inhibitor (for example, neostigmine methylsulfate, pyridostigmine bromide, eudrophonia chloride): atropine 0.5-1.25 mg in combination with neostigmine methylsulfate (1-3 mg) or galantamine (10-30 mg). Before the restoration of satisfactory spontaneous breathing, careful monitoring of the respiratory function should be carried out.

    Interaction:

    Inhalational anesthetics (halothane, methoxyflurane, diethyl ether, enflurane, isoflurane, cyclopropane), anesthetics for intravenous administration (ketamine, propanidide, barbiturates, etomidate, γ-hydroxybutyric acid), depolarizing and nondepolarizing muscle relaxants, some antibiotics (aminoglycosides, nitroimidazole derivatives, including. metronidazole, tetracyclines, bacitracin, capreomycin, clindamycin, polymyxins, incl. colistin, lincomycin, amphotericin B), nitrate anticoagulants, mineralocorticoids and glucocorticosteroids, diuretics, incl. bumetanide, inhibitors of carbonic anhydrase, ethacrynic acid, corticotropin, α- and β-adrenoblockers, thiamine, monoamine oxidase (MAO) inhibitors, guanidine, Protamine sulfate, phenytoin, blockers of "slow" calcium channels, magnesium salts, procainamide, quinidine, lidocaine and procaine for intravenous administration, enhance and / or prolong the effect.

    Drugs that reduce the concentration of potassium in the blood, aggravate respiratory depression (until it stops).

    Opioid analgesics increase respiratory depression.High doses of sufentanil reduce the need for high initial doses of nondepolarizing muscle relaxants. Non-depolarizing muscle relaxants prevent or reduce the rigidity of muscles caused by high doses of opiod analgesics (including alfentanil, fentanyl, sufentanil). Does not reduce the risk of bradycardia and arterial hypotension caused by opioid analgesics (especially against vasodilators and / or beta-adrenoblockers).

    During intubation with suxamethonium, Arduan is administered after the disappearance of clinical signs of suxamethonium. As with other nondepolarizing muscle relaxants, the administration of Arduan can shorten the time required for the onset of muscle relaxation and increase the duration of the maximum effect; With long-term preliminary use of glucocorticosteroids, neostigmine methyl sulfate, edrophonium chloride, pyridostigmine bromide, norepinephrine, azathioprine, epinephrine, theophylline, potassium chloride, sodium chloride, calcium chloride, possibly weakening the effect.

    Depolarizing muscle relaxants can both enhance and weaken the action of pipecuronium bromide (depending on the dose,time of application and individual sensitivity).

    Doxapram temporarily masks the residual effects of muscle relaxants.

    Special instructions:

    To be used exclusively in the conditions of a specialized hospital with the availability of appropriate equipment for artificial respiration and in the presence of an artificial respiration specialist due to the effect of the drug on the respiratory musculature.

    Careful monitoring is necessary during the operation and in the early postoperative period to maintain vital functions until the restoration of muscle contractility is complete.

    When calculating the dose, one should take into account the technique of anesthesia used, possible interactions with drugs administered before or during anesthesia, the condition and sensitivity of the patient to the drug.

    In the medical literature, cases of anaphylactic and anaphylactoid reactions are described with the use of muscle relaxants. Despite the absence of reports of such an action of Arduan, the drug can be used exclusively in conditions that allow immediate treatment of such conditions.

    Caution must be especially careful in the application Arduana with a history of the patient anaphylactic reaction caused by any relaxant due to possible cross-allergies.

    Arduana doses, causing muscle relaxation, do not possess significant cardiovascular effects and virtually no cause bradycardia.

    The use and dose of m-holinoblokatorov for the purpose of premedication is subject to a thorough preliminary assessment; should also take into account the stimulating effect on n. vagus of other, simultaneously used drugs and the type of operation.

    In order to avoid a relative overdose of the drug and to provide adequate control over the restoration of muscle activity, it is recommended to use a peripheral nerve fiber stimulant.

    Patients with disorders of neuromuscular transmission, obesity, renal insufficiency, liver and biliary tract, with indications of a history of polio transferred, should be administered the drug in smaller doses.

    In case of liver disease, Arduan's use is possible only in cases where the risk is justified. The dose should be minimal.

    Some conditions (hypokalemia, digitalisation, hypermagnesemia, diuretic administration, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may contribute to lengthening or intensifying the effect.

    As in the case of other muscle relaxants, before applying Arduan should normalize the electrolyte balance and acid-base state, eliminate dehydration.

    Like other muscle relaxants, Arduan can reduce activated partial thromboplastin and prothrombin time.

    Children aged 1 to 14 years are less sensitive to pipecuronium bromide and the duration of their miorelaxing effect is shorter in them than in adults and children under 1 year of age.

    Efficacy and safety of use in the neonatal period have not been studied. The miorelaxing effect in infants from 3 months. up to 1 year practically does not differ from that in adults.

    Use only a freshly prepared solution.

    Effect on the ability to drive transp. cf. and fur:In the first 24 hours after the termination of the muscle relaxant action of Arduan it is not recommended to drive and engage in potentially dangerous activities,requiring increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:

    Liofilizate for the preparation of a solution for intravenous administration of 4 mg / complete with a solvent - sodium chloride solution 0.9%.

    Packaging:

    10 mg of lyophilizate in a vial of colorless glass (1 hydrolytic class) contain 4 mg of pipecuronium bromide; 2 ml of solvent in a colorless glass ampoule (1 hydrolytic class).

    5 bottles and 5 ampoules in a plastic pallet, 5 plastic pallets in a cardboard box with instructions for use.

    Storage conditions:

    At a temperature of 2 to 8 ° C, in a dark place.

    Keep out of the reach of children!

    Shelf life:

    3 years.

    Do not use after the expiration date stated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N011430 / 01
    Date of registration:24.03.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp11.09.2017
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