28.02.2012 6464

Arduan. Description, instruction.

Relaxation of skeletal muscles and facilitation of endotracheal intubation during operations and diagnostic procedures under mechanical ventilation.

International name:
Pipecuronium bromide (Pipecuronium bromide)

Description of the active substance (INN):
Pipecuronium bromide

Dosage form:
lyophilisate for solution for intravenous administration

Pharmachologic effect:
Long-acting non-depolarizing muscle relaxant. Competitively blocks skeletal muscle n-cholinergic receptors, preventing acetylcholine-induced depolarization of the end plate and excitation of the muscle fiber. Muscle paralysis develops gradually in the following sequence: the muscles that raise the eyelid, the muscles of mastication, the muscles of the limbs, the muscles of the abdomen, the muscles of the glottis, the intercostal muscles and the diaphragm. Neuromuscular blockade is achieved 5.5-6 minutes after a single dose of 50 µg/kg and 3-5 minutes after 70-85 µg/kg. Carrying out tracheal intubation is possible already 2.5-3 minutes after the introduction of 70-100 mcg / kg; when using a lower dose, the time to achieve muscle relaxation sufficient for intubation is lengthened. The duration of the effect (recovery time of 25% of muscle activity) after the introduction of the initial dose depends on the size of the dose and the type of anesthesia performed: in adults at a dose of 70 mcg / kg, the duration of the effect is 30-175 minutes, 80-85 mcg / kg - 40- 211 min; against the background of neuroleptic anesthesia (nitrous oxide, fentanyl, droperidol) at a dose of 50 mcg / kg - 30 min; against the background of balanced anesthesia (against the background of short-acting barbiturates or propofol (as an introductory drug), opioid and inhalation (nitrous oxide) anesthetics) at a dose of 70-85 mcg / kg - 1-2 hours. The recovery time of spontaneous muscle activity is from 25% up to 50% of the control level - 24 minutes, up to 75% - 33 minutes. When used after depolarizing muscle relaxants, the duration of effect at a dose of 50 mcg / kg is 45 minutes (a similar duration of effect can be achieved at a dose of 70-85 mcg / kg without the use of depolarizing muscle relaxants). In children, the duration of the effect (recovery time of 25% of muscle activity) with the introduction of an effective dose depends on age: children under 3 months old - 13 minutes, from 3 months to 1 g - 10-44 minutes, 1-14 years old - 18-52 minutes. The recovery time of spontaneous muscle activity from 25% to 75% of the control level is 25-30 minutes. The duration of the effect on the background of maintenance therapy (additional administration in doses of 10-15 mcg/kg) is 50 minutes; increases against the background of enflurane and isoflurane, practically does not change against the background of halothane. In medium doses does not cause significant changes in the activity of the CCC; in large doses, it has a weak ganglioblocking, m-anticholinergic activity. Unlike pancuronium, bromide has practically no vagolytic activity; unlike other non-depolarizing muscle relaxants, it does not release histamine and does not cause hemodynamic disturbances.

Indications:
Relaxation of skeletal muscles and facilitation of endotracheal intubation during operations and diagnostic procedures under mechanical ventilation.

Contraindications:
Hypersensitivity. With caution. Obstruction of the biliary tract, edematous syndrome, increased BCC or dehydration, impaired acid-base balance and water-electrolyte metabolism, hypothermia, myasthenia gravis (including myasthenia gravis, Eaton-Lambert syndrome), respiratory depression, renal / liver failure, decompensated CHF, pregnancy , caesarean section (strictly controlled studies have not been conducted), lactation, children's age (up to 14 years).

Side effects:
From the musculoskeletal system: rarely (less than 1%) - muscle weakness after the cessation of muscle relaxation, muscle atrophy. From the nervous system: rarely (less than 1%) - CNS depression, hypesthesia, stroke. From the respiratory system: rarely (less than 1%) - hypopnea, apnea, lung atelectasis, laryngospasm, respiratory depression. From the CCC: less often - bradycardia (1.4%), lowering blood pressure (2.5%); rarely (less than 1%) - increased blood pressure, myocardial ischemia (up to myocardial infarction) and the brain, atrial fibrillation, ventricular extrasystole. On the part of the hematopoietic organs and the hemostasis system: rarely (less than 1%) - a decrease in partial thromboplastin and prothrombin time, thrombosis. From the urinary system: rarely (less than 1%) - anuria. Laboratory indicators: rarely (less than 1%) - hypercreatininemia, hypoglycemia, hyperkalemia. Allergic reactions: rarely (less than 1%) - skin rash, urticaria. Overdose. Symptoms: prolonged paralysis of skeletal muscles and apnea, marked decrease in blood pressure, shock. Treatment: mechanical ventilation, to eliminate the muscle relaxant effect - cholinesterase inhibitors (neostigmine, pyridostigmine, galantamine) in combination with m-cholinergic blockers (atropine); symptomatic therapy.

Dosage and administration:
Only in / in. Immediately before administration, 4 mg of dry matter is diluted with the supplied solvent. Adults and children from 14 years of age and older for complete muscle relaxation are administered 70-80 mcg / kg. The maximum single dose is 100 mcg / kg. For obesity, the dose is calculated based on the "ideal" body weight. To maintain muscle relaxation for a long time, it should be repeated at doses that are 15% of the original (10-15 mcg / kg). When carrying out intubation against the background of suxamethonium, the initial dose is 40-50 mcg / kg. With chronic renal failure, the amount of administered dose is determined by the values ​​​​of CC: with CC more than 100 ml / min - up to 100 μg / kg, CC 100 ml / min - 85 μg / kg, CC 80 ml / min - 70 μg / kg, CC 60 ml / min - 55 mcg / kg, CC less than 40 ml / min - 50 mcg / kg. Doses in children under 3 months of age have not been determined; from 3 to 12 months - 40 mcg / kg (provides muscle relaxation lasting from 10 to 44 minutes); from 1 year to 14 years - 57 mcg / kg (muscle relaxation - from 18 to 52 minutes).

Special instructions:
Apply only under the supervision of an experienced anesthesiologist, if there are conditions for intubation, mechanical ventilation, oxygen therapy. Careful monitoring of vital functions is required during surgery and in the early postoperative period. When calculating the dose, one should take into account the anesthesia technique used, possible interactions with drugs administered before or during anesthesia, the condition and sensitivity of the patient. Patients with neuromuscular transmission disorders, obesity, renal failure, diseases of the liver and biliary tract, with indications of a history of poliomyelitis, it is necessary to prescribe the drug in smaller doses. Some conditions (hypokalemia, digitalization, hypermagnesemia, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may prolong or enhance the effect. Before starting anesthesia, electrolyte balance, CBS should be normalized and dehydration should be eliminated. For pregnant women who have taken Mg2+ salts (which can increase neuromuscular blockade) for the treatment of toxicosis, pipecuronium bromide is prescribed in reduced doses. It is not known whether the drug passes into breast milk. Efficacy and safety of use in the neonatal period have not been studied. The therapeutic effect in infants from 3 to 12 months is practically the same as in adults. Children aged 1 to 14 years are less sensitive to pipecuronium bromide, and the duration of the therapeutic effect is shorter than in adults and infants (under 1 year). Within 24 hours after the complete restoration of neuromuscular conduction, it is not recommended to drive and engage in potentially hazardous activities in terms of injury.

Interaction:
Means for inhalation (halothane, methoxyflurane, enflurane, isoflurane, diethyl ether) and intravenous general anesthesia (ketamine, fentanyl, propanidide, barbiturates), depolarizing and non-depolarizing muscle relaxants, antibiotics (aminoglycosides, tetracyclines, bacitracin, capreomycin, clindamycin, colistin, lincomycin, polymexin), citrate anticoagulants, imidazole and metronidazole, antifungal drugs (amphotericin B), diuretics, mineralocorticoids and corticosteroids, bumetanide, carbonic anhydrase inhibitors, corticotropin, ethacrynic acid, beta-blockers, thiamine, MAO inhibitors, guanidine, protamine, phenytoin, alpha-blockers, BMCK, Mg2+ preparations, procainamide, quinidine, lidocaine and procaine, when administered intravenously, enhance and / or prolong the effect. Drugs that reduce the concentration of K + in the blood aggravate respiratory depression (up to its stop). Opioid analgesics increase respiratory depression. High doses of sufentanil reduce the need for high initial doses of non-depolarizing muscle relaxants. Non-polarizing muscle relaxants prevent or reduce muscle stiffness caused by high doses of opioid analgesics (including alfentanil, fentanyl, sufentanil). Does not reduce the risk of bradycardia and arterial hypotension caused by opioid analgesics (especially against the background of vasodilators and / or beta-blockers). When used before surgery, corticosteroids, anticholinesterase drugs (neostigmine, pyridostigmine), edrophonium, epinephrine, theophylline, KCl, NaCl, CaCl2 may weaken the effect. Depolarizing muscle relaxants can either enhance or weaken the effect of pipecuronium bromide (depending on dose, time of use and individual sensitivity). Doxapram temporarily masks the residual effects of muscle relaxants.

Name: Arduan (Arduan)

Release form, composition and pack

Lyophilizate for the preparation of a solution for intravenous administration of white or almost white color; the applied solvent is colorless, transparent.

1 vial pipecuronium bromide 4 mg.

Excipients: mannitol. Solvent: sodium chloride solution 0.9% - 2 ml.

Clinical and pharmacological group: Peripheral muscle relaxant of non-depolarizing competitive type.

pharmachologic effect

Long-acting peripheral muscle relaxant. Due to competitive binding to n-cholinergic receptors located in the motor endings of striated muscle fibers, it blocks signal transmission from nerve endings to muscle fibers.

Does not cause muscle twitches, does not have a hormonal effect, does not stimulate the release of histamine. In medium doses does not cause significant hemodynamic changes. A dose of 5 µg/kg of body weight provides 40-50 minutes of muscle relaxation during surgery. The maximum effect develops after 2.5-5 minutes, the effect occurs most quickly at doses equal to 70-80 mcg / kg. A further increase in the dose of the product shortens the time required for the manifestation of the action, and significantly lengthens the duration of the product.

Pharmacokinetics

Distribution

With intravenous administration, the initial Vd is 110 ml / kg. Vd in the equilibrium state reaches 300±78 ml/kg. The cumulative effect is insignificant or absent with repeated administration at doses of 10-20 mcg/kg at the time of restoration of the initial contractility by 25%. Penetrates through the placental barrier.

Metabolism and excretion

Plasma clearance is approximately 2.4±0.5 ml/min/kg. T1 / 2 pipecuronium is approximately 121 ± 45 minutes. It is excreted mainly in the urine, while 56% of the active substance is excreted in the first 24 hours, 1/3 of the active substance is excreted unchanged, the rest is in the form of 3-deacetyl-pipecuronium.

Indications

endotracheal intubation and relaxation of skeletal muscles during general anesthesia in surgical interventions requiring more than 20-30 minutes of muscle relaxation.

Dosing regimen

The drug should be used only in / in. Immediately before administration, 4 mg of dry matter is diluted with the supplied solvent.

Under balanced anesthesia, the ED50 and ED90 of Arduan are 30 µg/kg and 50 µg/kg body weight, respectively. The minimum time required for the onset of the effect is observed at doses of 70-80 mcg / kg. The dose should be selected individually for each patient, taking into account the type of anesthesia, the expected duration of the surgical intervention, possible interactions with other medicinal products used before or during anesthesia, concomitant diseases and the general condition of the patient. To control neuromuscular blockade, the use of a peripheral nerve stimulator is recommended.

The drug should be used under the supervision of a qualified physician with clinical experience in the use of peripheral muscle relaxants.

The initial dose for intubation and subsequent surgical intervention - 80-100 mcg / kg of body weight - provides good or excellent conditions for intubation for 150-180 seconds, while the duration of muscle relaxation is 60-90 minutes;

The initial dose for muscle relaxation during surgery after intubation with succinylcholine - 50 μg / kg of body weight provides 30-60 minutes of muscle relaxation;

The maintenance dose - 10-20 mcg / kg - provides 30-60 minutes of muscle relaxation. In chronic renal failure, the dose of the product should be calculated depending on the CC.

Children aged 3 months to 1 year the product should be prescribed at the rate of 40 mcg/kg of body weight (which provides muscle relaxation lasting from 10 to 44 minutes), from 1 to 14 years - 57 mcg/kg (muscle relaxation is provided lasting from 18 to 52 minutes).

Eliminate product action

In the event of neuromuscular blockade at 80-85%, determined using a peripheral nerve fiber stimulator, or at the time of partial blockade, determined by clinical signs, the use of atropine (0.5-1.25 mg) in combination with neostigmine (1-3 mg) or galantamine (10-30 mg) stops the neuromuscular action of Arduan.

Side effect

From the side of the central nervous system and peripheral nervous system: infrequently (less than 1%) - CNS depression, hypoesthesia.

From the musculoskeletal system: infrequently - weakness of the skeletal muscles after the cessation of muscle relaxation, muscle atrophy.

On the part of the respiratory system: infrequently - hypnoea, apnea, lung atelectasis, respiratory depression, laryngospasm as a result of an allergic reaction.

From the side of the cardiovascular system: infrequently - myocardial ischemia (up to myocardial infarction) and the brain, atrial fibrillation, ventricular premature beats, bradycardia, lowering blood pressure.

From the blood coagulation system: infrequently - thrombosis, a decrease in APTT and prothrombin time.

From the urinary system: infrequently - hypercreatininemia, anuria.

From the side of metabolism: infrequently - hypoglycemia, hyperkalemia.

Allergic reactions: infrequently - skin rash, hypersensitivity reactions, Quincke's edema.

Contraindications

children's age up to 3 months;

high susceptibility to pipecuronium and/or bromine.

It should be used with caution in obstruction of the biliary tract, edematous syndrome, dehydration, impaired water and electrolyte metabolism, hypothermia, myasthenia gravis, respiratory failure, heart failure in the stage of decompensation, renal and / or liver failure, pregnancy, during breastfeeding.

Pregnancy and lactation

The use of the product during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. Pipecuronium bromide crosses the placental barrier. For pregnant women who, with toxicosis, took magnesium salts as palliative therapy (which can enhance neuromuscular blockade), pipecuronium bromide is prescribed in reduced doses. The product should be used with caution during breastfeeding.

special instructions

The drug should be used exclusively in a specialized hospital with appropriate equipment for artificial respiration and in the presence of a specialist in artificial respiration. It is necessary to carefully monitor the maintenance of vital functions during surgery and in the early postoperative period until full restoration of adequate vitality.

When calculating the dose, it is necessary to take into account the anesthesia technique used, possible interactions with other drugs administered before or during anesthesia, the condition and individual susceptibility of the patient to the product. Doses that cause muscle relaxation do not have a significant cardiovascular effect and in the vast majority of cases do not cause bradycardia.

The need to prescribe and dosing regimen of vagolytic products for the purpose of premedication should be carefully analyzed in advance (the stimulating effect on n. vagus of other drugs used simultaneously, as well as the type of operation, should also be taken into account).

The use of a peripheral nerve stimulator is recommended to prevent relative overdose of the product and to ensure adequate control of muscle recovery. Patients with neuromuscular transmission disorders, obesity, renal insufficiency, with impaired liver and / or biliary tract function, and if there is a history of poliomyelitis, it is necessary to prescribe the product in smaller doses.

In case of impaired liver function, the use of Arduan is possible only in cases where the intended benefit to the patient outweighs the potential risk.

In this case, the product should be used in the minimum effective dose. With overweight and obesity, an increase in the duration of action of Arduan is possible, therefore, a dose calculated for ideal weight should be used. Some conditions (hypokalemia, digitalization, hypermagnesemia, diuretics, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may contribute to a change in the duration of the effect. Before starting anesthesia, it is necessary to normalize the electrolyte balance, acid-base balance and eliminate dehydration. Greater caution should be exercised when using Arduan in the presence of a history of anaphylactic reactions caused by muscle relaxants, due to the possible development of cross-hypersensitivity.

Pediatric use

Children aged 1 to 14 years are less sensitive to pipecuronium bromide and the duration of the therapeutic effect is shorter than in adults and infants (under 1 year). Efficacy and safety of use in the neonatal period have not been studied. The therapeutic effect in infants from 3 months to 1 year is not significantly different from that in adults.

Influence on the ability to drive vehicles and control mechanisms

In the first 24 hours after the termination of the muscle relaxant action of Arduan, it is forbidden to drive a car and other mechanisms, work with which is associated with an increased risk of injury.

Overdose

Symptoms: prolonged paralysis of skeletal muscles, apnea, marked decrease in blood pressure.

Treatment: in case of overdose or prolonged neuromuscular blockade, mechanical ventilation is performed until spontaneous breathing is restored. At the beginning of the restoration of spontaneous breathing, an acetylcholinesterase inhibitor (neostigmine, pyridostigmine, endrophonium) is administered as an antidote: atropine 0.5–1.25 mg in combination with neostigmine (1–3 mg) or galantamine (10–30 mg). Careful monitoring of respiratory function should be carried out until satisfactory spontaneous breathing is restored.

Attention!
Before using the medication "Arduan (Arduan)" you need to consult a doctor.
The instructions are provided solely for familiarization with " Arduan (Arduan)».

Arduan, lyophilizate for solution for intravenous administration 4 mg - vial (vial) with a solvent in ampoules, carton pack 25 - EAN code: 5997001392980 - No. P N011430/01, 2009-03-24 from Gedeon Richter (Hungary)

Latin name

Arduan

Active substance

Pipecuronium bromide * (Pipecuronium bromide *)

ATX

M03AC06 Pipecuronium bromide

Pharmacological group

n-Cholinolytics (muscle relaxants)

Nosological classification (ICD-10)

Z100.0* Anesthesiology and premedication

Composition

Lyophilisate for solution for intravenous administration 1 vial. active substance: pipecuronium bromide 4 mg excipients lyophilisate: mannitol - 6 mg solvent: sodium chloride - 18 mg;

Description of the dosage form

Lyophilisate: white or almost white.

Solvent: colorless and transparent solution.

pharmachologic effect

Pharmacological action - muscle relaxant.

Pharmacodynamics

It is a long-acting non-depolarizing muscle relaxant. Due to the competitive connection with n-cholinergic receptors located on the end plate of the neuromuscular synapse of skeletal muscles, it blocks signal transmission from nerve endings to muscle fibers. Does not cause muscle fasciculations.

Even at doses several times greater than its effective dose required for a 90% decrease in muscle contractility (ED90), it does not exhibit ganglioblocking, m-anticholinergic and sympathomimetic activity.

According to studies, with balanced anesthesia, the effective dose required for a 50% reduction in muscle contractility (ED50) and ED90 of pipecuronium bromide is 0.03 and 0.05 mg/kg, respectively.

A dose of 0.05 mg/kg 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 of 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

With intravenous administration, the initial Vd (Vdc) is 110 ml / kg, Vss reaches (300 ± 78) ml / kg, plasma clearance is approximately equal to (2.4 ± 0.5) ml / min / kg, average T1 / 2 (T1 / 2% 26beta-) is (121 ± 45) minutes, the average residence time in blood plasma (MRT) is 140 minutes.

With repeated administration of maintenance doses, the cumulative effect is insignificant if doses of 0.01-0.02 mg/kg are 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. 1/3 is excreted unchanged, and the rest is in the form of 3-deacetylpipecuronium bromide.

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

Penetrates through the placental barrier.

Indications for Arduan

Endotracheal intubation and relaxation of skeletal muscles under general anesthesia during various surgical operations requiring more than 20-30 minutes of muscle relaxation, subject to mechanical ventilation.

Contraindications

hypersensitivity to pipecuronium bromide and / or bromine

severe liver failure

children's age up to 3 months.

With caution: obstruction of the biliary tract - edematous syndrome - increased BCC or dehydration - taking diuretics - violation of the acid-base state (acidosis, hypercapnia) and water and electrolyte metabolism (hypokalemia, hypermagnesemia, hypocalcemia) - hypothermia - digitalization - hypoproteinemia - cachexia - myasthenia gravis (including myasthenia gravis, Eaton-Lambert syndrome) due to the possible in such cases both strengthening and weakening of the effect of the drug - respiratory depression - renal failure (prolongs the effect of the drug and the time of post-anesthetic depression) - decompensated chronic heart failure - malignant hyperthermia - an anaphylactic reaction caused by any muscle relaxant in history (due to possible cross-allergy) - children under 14 years of age.

Use during pregnancy and lactation

Clinical studies to prove the safety of the use of Arduan in pregnant women and the fetus are 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.

Side effects

From the side of the nervous system: rarely (

From the musculoskeletal system: rarely (

From the respiratory system: rarely (

From the side of the CCC: rarely (

On the part of the hematopoietic organs and the hemostasis system: rarely (

From the urinary system: rarely (

Allergic reactions: rare (

Laboratory indicators: rarely (

Others: blepharitis, ptosis.

Interaction

Inhalation anesthetics (halothane, methoxyflurane, diethyl ether, enflurane, isoflurane, cyclopropane), intravenous anesthetics (ketamine, propanidide, barbiturates, etomidate, %26gamma-hydroxybutyric acid), depolarizing and non-depolarizing muscle relaxants, some antibiotics (aminoglycosides , nitroimidazole derivatives, including metronidazole, tetracyclines, bacitracin, capreomycin, clindamycin, polymyxins, including colistin, lincomycin, amphotericin B), citrate anticoagulants, mineralocorticoids and corticosteroids, diuretics, incl. bumetanide, carbonic anhydrase inhibitors, ethacrynic acid, corticotropin, %26alpha- and %26beta-adrenergic blockers, thiamine, MAO inhibitors, guanidine, protamine sulfate, phenytoin, CCA, magnesium salts, procainamide, quinidine, lidocaine and procaine for intravenous administration enhance and/or prolong the action.

Drugs that reduce the concentration of potassium in the blood aggravate respiratory depression (up to its stop).

Opioid analgesics increase respiratory depression. High doses of sufentanil reduce the need for high initial doses of non-depolarizing muscle relaxants. Non-depolarizing muscle relaxants prevent or reduce muscle stiffness caused by high doses of opioid analgesics (including alfentanil, fentanyl, sufentanil). Does not reduce the risk of bradycardia and arterial hypotension caused by opioid analgesics (especially against the background of vasodilators and / or% 26beta-blockers).

During intubation with suxamethonium, Arduan is administered after the disappearance of clinical signs of the action of suxamethonium. As with other non-depolarizing muscle relaxants, the administration of Arduan may shorten the time required for muscle relaxation to occur and increase the duration of the maximum effect.

With prolonged preliminary use of GCS, neostigmine methyl sulfate, edrophonium chloride, pyridostigmine bromide, norepinephrine, azathioprine, epinephrine, theophylline, potassium chloride, sodium chloride, calcium chloride, the effect may be weakened.

Depolarizing muscle relaxants can either enhance or weaken the effect of pipecuronium bromide (depending on dose, time of use and individual sensitivity).

Doxapram temporarily masks the residual effects of muscle relaxants.

Dosage and administration

In / in. As with other non-depolarizing muscle relaxants, the dose of Arduan is selected for each patient individually, taking into account the type of anesthesia, the expected duration of the surgical intervention, possible interactions with other drugs used before or during anesthesia, concomitant diseases and the general condition of the patient. The use of a peripheral nerve stimulator is recommended to control the neuromuscular block.

Immediately before administration, 4 mg of dry matter is diluted with the supplied solvent.

The initial dose for intubation and subsequent surgical intervention - 0.06-0.08 mg / kg, provides good / excellent conditions for intubation for 150-180 s, while the duration of muscle relaxation is 60-90 minutes -

The initial dose for muscle relaxation during intubation using suxamethonium - 0.05 mg / kg, provides 30-60 minutes of muscle relaxation -

Maintenance dose - 0.01-0.02 mg / kg, provides 30-60 minutes of muscle relaxation during surgery -

In chronic renal failure, it is not recommended to use doses exceeding 0.04 mg / kg (in large doses, an increase in the duration of muscle relaxation is possible) -

Overweight and obesity may prolong the action of Arduan, so you should use a dose calculated for ideal weight.

Doses in children: from 1 year to 14 years - 0.05-0.06 mg / kg (muscle relaxation - from 18 to 52 minutes) - from 3 to 12 months - 0.04 mg / kg (which provides muscle relaxation for a duration from 10 to 44 minutes).

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

Overdose

Symptoms: prolonged paralysis of skeletal muscles and apnea, marked decrease in blood pressure, shock.

Treatment: in case of overdose or prolonged neuromuscular block, IVL is continued until spontaneous breathing is restored. At the beginning of the restoration of spontaneous breathing, an acetylcholinesterase inhibitor (for example, neostigmine methyl sulfate, pyridostigmine bromide, edrophonium chloride) is administered as an antidote - atropine 0.5-1.25 mg in combination with neostigmine methyl sulfate (1-3 mg) or galantamine (10-30 mg ). Careful monitoring of respiratory function should be carried out until satisfactory spontaneous breathing is restored.

Precautionary measures

Small doses of Arduan in severe myasthenia gravis or Eaton-Lambert syndrome can cause a pronounced effect; in such patients, the drug is prescribed in very low doses after a thorough assessment of the potential risk.

special instructions

Use only in a specialized hospital with appropriate equipment for artificial respiration and in the presence of a specialist in artificial respiration due to the effect of the drug on the respiratory muscles.

Careful monitoring during surgery and in the early postoperative period is necessary to maintain vital functions until full recovery of muscle contractility.

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

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

Increased caution should be exercised in the use of Arduan in the presence of a patient's history of an anaphylactic reaction caused by any muscle relaxant, due to a possible cross-allergy.

Doses of Arduan that cause muscle relaxation do not have a significant cardiovascular effect and practically do not cause bradycardia.

The use and dose of m-anticholinergics for the purpose of premedication is subject to careful preliminary evaluation; the stimulating effect on n should also be taken into account. vagus other concomitant medications and type of surgery.

In order to prevent a relative overdose of the drug and ensure appropriate control over the restoration of muscle activity, it is recommended to use a peripheral nerve fiber stimulator.

Patients with neuromuscular transmission disorders, obesity, renal failure, diseases of the liver and biliary tract, with indications of a history of poliomyelitis, should be prescribed the drug in lower doses. In the case of liver disease, the use of Arduan is possible only in cases where the risk is justified. In this case, the dose should be minimal.

Some conditions (hypokalemia, digitalization, hypermagnesemia, diuretics, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may prolong or enhance the effect.

As in the case of other muscle relaxants, before using Arduan, the electrolyte balance and acid-base state should be normalized, dehydration should be eliminated.

Like other muscle relaxants, Arduan may reduce aPTT and PT.

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

Efficacy and safety of use in the neonatal period have not been studied. The muscle relaxant effect in infants from 3 months to 1 year is practically the same as in adults.

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PIPECURONIUM BROMIDE(pharmacological analogues: arduan, pipecurium bromide) is a muscle relaxant of the antidepolarizing type of action. Pipecuronium bromide does not cause changes in the activity of the cardiovascular system, does not contribute to the release of histamine. Pipecuronium bromide is used to relax muscles during various operations, including those on the heart. Pipecuronium bromide is administered intravenously at the rate of 0.04-0.06 mg/kg of body weight, achieving complete muscle relaxation for 30-40 minutes. Repeated injections of pipecuronium bromide (0.02-0.03 mg/kg body weight) prolong the action. The drug can be used with various drugs for anesthesia (halothane, ether, nitrous oxide, etc.). Pipecuronium bromide is contraindicated in: myasthenia gravis, pregnancy, severe kidney disease. Release form pipecuronium bromide: ampoules with 4 mg of the drug, the solvent is attached. List A.

Recipe for pipecuronium bromide in Latin:

Rp.: Arduani 0.004

D.t. d. N. 5 in amp.

S. Dissolve the contents of the ampoule in the supplied solvent (4 ml), inject 3-4 ml intravenously.

SUXAMETHONIUM(pharmacological analogues: dithylin, myorelaxin, listenone etc.) - a drug of a depolarizing type of action. Suxamethonium gives a quick but short-term effect. For prolonged action, repeated injections of the drug are necessary, which provides controlled muscle relaxation. After the cessation of the introduction of suxamethonium, a rapid restoration of skeletal muscle tone occurs. Suxamethonium is used for tracheal intubation; endoscopic procedures (bronchoscopy, etc.), short-term surgical interventions. Suxamethonium is administered intravenously at a dose of 0.5-1 mg/kg of body weight, fractionally - for prolonged muscle relaxation throughout the operation; at a dose of 1.5-2 mg / kg of body weight - for tracheal intubation and complete relaxation of the skeletal and respiratory muscles. Side effects of suxamethonium: muscle pain, respiratory depression. cholinesterase is an antidote of the drug).If muscle relaxation and breathing are not fully restored within 30 minutes (one can think of the so-called double block, when an antidepolarizing effect develops after depolarization), then anticholinesterase drugs (prozerin, etc.) should be administered. : glaucoma, pregnancy, severe liver diseases.Myasthenia gravis is not a contraindication.It should be borne in mind that suxamethonium solutions should not be mixed with barbiturate solutions and donor blood! containing 0.25 g and 0.1 g of dry matter (with the addition of a solvent) List A.

DIOXONIUM- a muscle relaxant of a mixed type of action. After the depolarization phase, dioxonium exerts an anti-depolarizing effect. Dioxonium is used to relax skeletal muscles. Dioxonium is administered intravenously, mechanical ventilation is used. The average dose of dioxonium is 0.04-0.05 mg/kg of the patient's body weight. Dioxonium release form: 5 ml ampoules of 0.1% solution. List A.

An example of a dioxonium recipe in Latin:

Rp.: Sol. Dioxonii 0.1% 5 ml

D.t. d. N. 10 ampull.

S. Administer intravenously at the rate of 0.04-0.05 mg/kg of the patient's body weight.

Instructions for the medical use of the drug

Description of the pharmacological action

It blocks n-cholinergic receptors of skeletal muscles, prevents their contact with the mediator (acetylcholine), inhibits the depolarization of the end plate and disrupts neuromuscular transmission.

Indications for use

Relaxation of striated muscles during operations and diagnostic procedures under mechanical ventilation.

Release form

lyophilisate for solution for intravenous administration 4 mg; vial (flacon) with solvent in ampoules, cardboard pack 25;

Lyophilisate for solution for intravenous administration 4 mg; bottle (flacon) with solvent in ampoules, contour plastic packaging (pallets) 5, cardboard pack 5;

Lyophilisate for solution for intravenous administration 4 mg; bottle (flacon) with solvent in ampoules, contour plastic packaging (pallets) 5, cardboard pack 1;

Lyophilisate for solution for intravenous administration 4 mg; vial (vial), cardboard pack 1;

Pharmacodynamics

Competes with acetylcholine for n-cholinergic endplate receptors, causing blockade of neuromuscular transmission. In average therapeutic doses does not affect hemodynamics; in large doses, it has a weak ganglioblocking activity.

The average effective dose, causing muscle relaxation by 95%, is 0.041 mg/kg under balanced anesthesia. After a single intravenous injection of 0.07-0.085 mg/kg, intubation is possible after 2-3 minutes, the maximum effect develops after 5 minutes, the duration of muscle relaxation is 50-70 minutes. When administered at a dose of 40–50 μg/kg (after intubation with succinylcholine), it causes muscle relaxation for 15–25 minutes, depending on individual sensitivity. In children, the duration of action is shorter than in adults: 10–44 minutes for children aged 3 months to 1 year, 18–52 minutes for children aged 1 to 14 years. Children from 1 to 14 years of age are less sensitive to the action of pipecuronium than adults and children under 1 year of age.

Acetylcholinesterase inhibitors, contributing to the accumulation of acetylcholine, remove the effect of pipecuronium bromide.

Pharmacokinetics

Clearance - 0.12 l / h / kg, volume of distribution - 0.25 l / kg, half-life - 6.2 minutes, T1 / 2 - 1.7 (0.9–2.7) hours. kidney clearance - 0.08 l / kg / h, volume of distribution - 0.37 l / kg, T1 / 2 - 4 hours.

It is metabolized to form an active 3-deacetyl metabolite (40-50% of pipecuronium activity) and a number of inactive derivatives. Excreted mainly by the kidneys unchanged (75%) and 15% as metabolites. T1 / 2 lengthens with impaired renal function.

After the introduction of repeated doses, a small cumulation is possible.

Use during pregnancy

Contraindicated in early pregnancy. To a small extent passes through the placenta.

Application during caesarean section does not change the Apgar score, muscle tone and cardiovascular adaptation of the fetus.

It is not known whether pipecuronium bromide passes into breast milk.

Contraindications for use

Hypersensitivity, myasthenia.

Side effects

Bradycardia, arterial hypotension; rarely - anaphylactic reactions.

Dosage and administration

Immediately before administration, 4 mg of dry matter is diluted with the supplied solvent.

Under balanced anesthesia, the ED50 and ED90 of Arduan are 0.03 and 0.05 mg/kg body weight, respectively. The minimum time required for the onset of the effect is observed at doses of 0.07-0.08 mg / kg.

The dose is selected for each patient individually, taking into account the type of anesthesia, the expected duration of the surgical intervention, possible interactions with other drugs used before or during anesthesia, concomitant diseases and the patient's condition. To control the neuromuscular block, the use of a peripheral nerve stimulator is recommended.

The drug should be used under the supervision of an experienced clinician familiar with the action and use of such drugs.

The initial dose for intubation and subsequent surgical intervention - 0.08-0.1 mg / kg provides good / excellent conditions for intubation for 150-180 s, while the duration of muscle relaxation is 60-90 minutes;

The initial dose for muscle relaxation during surgery after intubation with succinylcholine - 0.05 mg / kg provides 30-60 minutes of muscle relaxation;

Maintenance dose - 0.01-0.02 mg / kg provides 30-60 minutes of muscle relaxation.

In chronic renal failure, the dose is calculated depending on creatinine clearance: with Cl> 100 ml / min - up to 100 μg / kg, with Cl 100 ml / min - 85 μg / kg, with Cl 80 ml / min - 70 μg / kg, at Cl 60 ml/min - 55 mcg/kg, at Cl
Doses in children under 3 months of age have not been determined: from 3 to 12 months - 40 mcg / kg (which provides muscle relaxation lasting from 10 to 44 minutes), from 1 year to 14 years - 57 mcg / kg (muscle relaxation - from 18 to 52 min).

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

Overdose

Symptoms: muscle weakness, apnea, prolonged paralysis, hypotension.

Treatment: mechanical ventilation, the introduction of neostigmine methyl sulfate at a dose of 1–3 mg or galanthamine at a dose of 10–30 mg against the background of intravenous administration of 1.25 mg of atropine.

Interactions with other drugs

The effects of Arduan are enhanced and / or prolonged by inhaled (halothane, diethyl ether) and non-inhaled (ketamine, fentanyl, propanidide, barbiturates) drugs for anesthesia, antibiotics (aminoglycosides, tetracyclines, polypeptides, metronidazole), diuretics, beta-adrenergic blockers, thiamine, inhibitors MAO, protamine, phenytoin, alpha-adrenergic blockers, calcium antagonists, lidocaine (with intravenous administration); reduce - glucocorticoids, neostigmine, norepinephrine, theophylline, calcium chloride, sodium chloride.

Storage conditions

In a place protected from light, at a temperature of 2-8 ° C.

Keep out of the reach of children.

Best before date

Belonging to ATX-classification:

** The Medication Guide is for informational purposes only. For more information, please refer to the manufacturer's annotation. Do not self-medicate; Before you start using Arduan, you should consult a doctor. EUROLAB is not responsible for the consequences caused by the use of the information posted on the portal. Any information on the site does not replace the advice of a doctor and cannot serve as a guarantee of the positive effect of the drug.

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