Composition, structure and packing
Lyophilisates for solution for i / in the introduction of white or nearly white; attached solvent is colorless and transparent.
1 vial. pipekuroniya bromide 4 mg.
Excipients: mannitol. Solvent: sodium chloride, p-p 0.9% - 2 ml.
Clinico-pharmacological group: peripheral actions of nondepolarizing muscle relaxant competitive type.
Pharmacological action
Peripheral long-acting muscle relaxant. Due to the competitive binding with N-cholinergic receptors located in the motor endings of the cross-striped muscle fibers, blocks the transmission of signals from nerve endings to the muscle fibers.
There is no twitches, has no hormonal action, does not stimulate the release of histamine. In medium doses, no significant hemodynamic changes. Dose of 5 mg / kg of body weight for 40-50-minute miorelaxation during surgery. The maximal effect develops after 2.5-5 min, the fastest effect occurs at doses equal to 70-80 mg / kg. Further increase in dose shortens the time required for the manifestation of action and significantly prolongs the duration of the drug.
Pharmacokinetics
Distribution
When i / in the introduction of the initial Vd of 110 ml / kg. Vd in the equilibrium state is 300 ± 78 ml / kg. The cumulative effect is negligible or absent in the re-introduction to the doses of 10-20 mg / kg at the time of the initial contractile recovery of 25%. Penetrates through the placental barrier.
Metabolism and excretion
Plasma clearance is approximately 2.4 ± 0.5 ml / min / kg. T1 / 2 pipekuroniya an average of 121 ± 45 min. Write mainly in the urine, while 56% of the active substance - in the first 24 h, 1 / 3 of the active substance appears unchanged, the remainder - in the form of 3-dezatsetil-pipekuroniya.
Statement
endotracheal intubation and skeletal muscle relaxation during general anesthesia in surgical interventions that require more than 20-30-minute miorelaxation.
Dosage regimen
The drug should be used only in /. Immediately before the introduction of 4 mg dry weight throw came with solvent.
With a balanced anesthetic ED50 and ED90 Arduana amount to 30 mcg / kg and 50 mg / kg body weight. The minimum time required for the onset of the effect observed at doses of 70-80 mg / kg. The dose should be selected individually for each patient according to the type of anesthesia, the expected duration of surgery, possible interactions with other drugs used before or during anesthesia, concomitant diseases and patient's general condition. For the control of neuromuscular blockade is recommended to use peripheral nerve stimulator.
The drug should be used under the supervision of a qualified doctor who has clinical experience of peripheral muscle relaxants.
Recommended doses
The initial dose for intubation and subsequent surgery - 80-100 mg / kg of body weight - provides good or excellent conditions for intubation within 150-180 seconds, with a duration miorelaxation is 60-90 minutes;
The initial dose for miorelaxation during surgery after intubation with succinylcholine - 50 mg / kg body weight provides 30-60-minute miorelaxation;
Maintenance dose - 10-20 mg / kg - provides 30-60-minute miorelaxation. In chronic renal failure dose should be calculated depending on the spacecraft.
Children aged 3 months to 1 year of drug should be administered per 40 mg / kg body weight (which provides miorelaxation ranging from 10 to 44 minutes), from 1 year to 14 years - 57 mg / kg (provided miorelaxation duration of 18 to 52 min).
Removal of the drug
In the implementation of neuromuscular blockade at 80-85%, determined by stimulating the peripheral nerve fibers, or when a partial blockade, as 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 neuromuscular action Arduana.
Side effect
From the central nervous system and peripheral nervous system: rare (less than 1%) - inhibition of the CNS, hypoesthesia.
On the part of the musculoskeletal system: rarely - the weakness of skeletal muscles after the cessation miorelaxation, muscular atrophy.
On the part of the respiratory system: rarely - gipnoe, apnea, pulmonary atelectasis, respiratory depression, laryngism by an allergic reaction.
Since the cardiovascular system: rarely - myocardial ischemia (up to a myocardial infarction) and brain, atrial fibrillation, ventricular extrasystoles, bradycardia, blood pressure reduction.
From the blood coagulation system: rarely - thrombosis, a decrease APTT and prothrombin time.
From the urinary system: rarely - hypercreatininemia, anuria.
On the part of metabolism: the rare-hypoglycemia, hyperkalemia.
Allergic reactions: seldom - skin rashes, hypersensitivity reactions, Quincke's edema.
Contraindications
Children aged 3 months;
Hypersensitivity to pipekuroniyu and / or bromine.
Precautions should be used with biliary tract obstruction, edema, dehydration, disruption of water and electrolyte metabolism, hypothermia, myasthenia gravis, respiratory failure, cardiac insufficiency in the stage of decompensation, renal and / or hepatic insufficiency, pregnancy, during breastfeeding.
Pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. Pipekuroniya bromide penetrates the placental barrier. Pregnant women who are at toxicosis as a palliative treatment received magnesium salts (which can enhance neuromuscular blockade), pipekuroniya bromide administered in small doses. Precautions should use the drug during breastfeeding.
Cautions
The drug should be used only in a specialized hospital with appropriate equipment for artificial respiration and in the presence of a specialist to carry out artificial respiration. Must be carefully monitored to maintain vital functions during surgery and in the early postoperative period until full restoration of adequate vitality.
When calculating the dose should be taken into account of the technique of anesthesia, possible interactions with other drugs, introduced before or during anesthesia, the state and the individual patient's sensitivity to the drug. Doses causing miorelaxation do not have a significant cardiovascular effect and in most cases do not cause bradycardia.
The need for supplies and dosing regimen vagolytic drugs for sedation should first carefully analyze (it should also take into account the stimulating effect on the n. vagus others used both drugs, as well as the type of operation).
To prevent relative overdose of the drug and to ensure appropriate monitoring recovery of muscle activity is recommended to use peripheral nerve stimulator. Patients with disorders of neuromuscular transmission, obesity, renal insufficiency, disorders of liver function and / or biliary tract, and if history is indication transferred polio, should be prescribed the drug in smaller doses.
When violations of liver function application Arduana possible only in cases where the intended benefits to the patient outweighs the potential risk.
This medication should be used in the lowest effective dose. When overweight and obesity may increase the duration of the Arduana, so you should apply a dose, calculated on ideal weight. Some states (hypokalemia, digitalization, gipermagniemiya, diuretics, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may help to change the duration of effect. Before anesthesia should be to normalize the electrolyte balance, AAR and eliminate dehydration. It should be especially careful applying Arduan in the presence of a history of anaphylactic reactions caused by muscle relaxants, because of the possible development of cross-hypersensitivity.
Use in Pediatrics
Children aged from 1 year to 14 years are less sensitive to pipekuroniyu bromide and duration of therapeutic effect, they are shorter than in adults and infants (under 1 year). Efficacy and safety of 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.
Effects on ability to drive vehicles and management mechanisms
In the first 24 h after the cessation of miorelaksiruyuschego Arduana prohibited from driving and other mechanisms, work with which is associated with increased risk of injury.
Overdose
Symptoms: prolonged paralysis of skeletal muscles, sleep apnea, marked reduction of BP.
Treatment: In case of overdose or prolonged neuromuscular blockade spend ventilator to restore spontaneous breathing. In the beginning recovery of spontaneous breathing as an antidote to introduce an inhibitor of acetylcholinesterase (neostigmine, pyridostigmine, endrofony): atropine 0.5 - 1.25 mg in combination with neostigmine (1-3 mg) or galantamine (10-30 mg). Until the restoration of a satisfactory spontaneous respiration should conduct a careful control of respiratory function.
Drug Interactions
Acetylcholinesterase inhibitors (neostigmine, pyridostigmine, edrofony) are antagonists Arduana. Increased intensity and / or duration of action Ardurana occurs when:
simultaneous use of inhaled anesthetics (halothane, Methoxyflurane, ether, enflurana, izoflurana, cyclopropane);
usually requires a reduction in dose Arduana.
simultaneous use with other nedepolyariziruyuschie muscle relaxants, anesthetics for in / injection (ketamine, fentanyl, propanididom, barbiturates, etomidatom, γ-gidroksimaslyanoy acid).
simultaneous use of some antibiotics and chemotherapeutic drugs (drugs aminoglycoside, tetracyclines, polypeptides, imidazole, and metronidazole and antifungal agents (amphotericin B).
simultaneous use of diuretics, alpha-and beta-blockers, thiamine, MAO inhibitors, guanidine, protamine, phenytoin, calcium channel blockers slow, salts of magnesium, lidocaine for in / in the introduction.
Provisional application of succinylcholine is accompanied by a reduction of time required for the onset of miorelaxation and increase the duration of effect. Arduan should be introduced after the disappearance of clinical signs of succinylcholine. In this case the effect depends on dose and individual sensitivity.
Reduces the intensity and / or duration of the preceding introduction Ardurana Arduana prolonged use of GCS, neostigmine, pyridostigmine, azathioprine, theophylline, epinephrine, potassium chloride, sodium chloride. Strengthening or weakening action is a preliminary (before surgery) application depolyariziruyuschih muscle relaxants (playing the role of dose, time of use and individual sensitivity).
In case of simultaneous appointment with chinidin, magnesium salts, procainamide may gain miorelaxation. In cases of simultaneous use of halothane or fentanyl for sedation may reduce blood pressure and the development of bradycardia.
Terms and Conditions of storage
The drug should be stored out of reach of children, protected from light at 2-8 ° C.
Lyophilisates for solution for i / in the introduction of white or nearly white; attached solvent is colorless and transparent.
1 vial. pipekuroniya bromide 4 mg.
Excipients: mannitol. Solvent: sodium chloride, p-p 0.9% - 2 ml.
Clinico-pharmacological group: peripheral actions of nondepolarizing muscle relaxant competitive type.
Pharmacological action
Peripheral long-acting muscle relaxant. Due to the competitive binding with N-cholinergic receptors located in the motor endings of the cross-striped muscle fibers, blocks the transmission of signals from nerve endings to the muscle fibers.
There is no twitches, has no hormonal action, does not stimulate the release of histamine. In medium doses, no significant hemodynamic changes. Dose of 5 mg / kg of body weight for 40-50-minute miorelaxation during surgery. The maximal effect develops after 2.5-5 min, the fastest effect occurs at doses equal to 70-80 mg / kg. Further increase in dose shortens the time required for the manifestation of action and significantly prolongs the duration of the drug.
Pharmacokinetics
Distribution
When i / in the introduction of the initial Vd of 110 ml / kg. Vd in the equilibrium state is 300 ± 78 ml / kg. The cumulative effect is negligible or absent in the re-introduction to the doses of 10-20 mg / kg at the time of the initial contractile recovery of 25%. Penetrates through the placental barrier.
Metabolism and excretion
Plasma clearance is approximately 2.4 ± 0.5 ml / min / kg. T1 / 2 pipekuroniya an average of 121 ± 45 min. Write mainly in the urine, while 56% of the active substance - in the first 24 h, 1 / 3 of the active substance appears unchanged, the remainder - in the form of 3-dezatsetil-pipekuroniya.
Statement
endotracheal intubation and skeletal muscle relaxation during general anesthesia in surgical interventions that require more than 20-30-minute miorelaxation.
Dosage regimen
The drug should be used only in /. Immediately before the introduction of 4 mg dry weight throw came with solvent.
With a balanced anesthetic ED50 and ED90 Arduana amount to 30 mcg / kg and 50 mg / kg body weight. The minimum time required for the onset of the effect observed at doses of 70-80 mg / kg. The dose should be selected individually for each patient according to the type of anesthesia, the expected duration of surgery, possible interactions with other drugs used before or during anesthesia, concomitant diseases and patient's general condition. For the control of neuromuscular blockade is recommended to use peripheral nerve stimulator.
The drug should be used under the supervision of a qualified doctor who has clinical experience of peripheral muscle relaxants.
Recommended doses
The initial dose for intubation and subsequent surgery - 80-100 mg / kg of body weight - provides good or excellent conditions for intubation within 150-180 seconds, with a duration miorelaxation is 60-90 minutes;
The initial dose for miorelaxation during surgery after intubation with succinylcholine - 50 mg / kg body weight provides 30-60-minute miorelaxation;
Maintenance dose - 10-20 mg / kg - provides 30-60-minute miorelaxation. In chronic renal failure dose should be calculated depending on the spacecraft.
Children aged 3 months to 1 year of drug should be administered per 40 mg / kg body weight (which provides miorelaxation ranging from 10 to 44 minutes), from 1 year to 14 years - 57 mg / kg (provided miorelaxation duration of 18 to 52 min).
Removal of the drug
In the implementation of neuromuscular blockade at 80-85%, determined by stimulating the peripheral nerve fibers, or when a partial blockade, as 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 neuromuscular action Arduana.
Side effect
From the central nervous system and peripheral nervous system: rare (less than 1%) - inhibition of the CNS, hypoesthesia.
On the part of the musculoskeletal system: rarely - the weakness of skeletal muscles after the cessation miorelaxation, muscular atrophy.
On the part of the respiratory system: rarely - gipnoe, apnea, pulmonary atelectasis, respiratory depression, laryngism by an allergic reaction.
Since the cardiovascular system: rarely - myocardial ischemia (up to a myocardial infarction) and brain, atrial fibrillation, ventricular extrasystoles, bradycardia, blood pressure reduction.
From the blood coagulation system: rarely - thrombosis, a decrease APTT and prothrombin time.
From the urinary system: rarely - hypercreatininemia, anuria.
On the part of metabolism: the rare-hypoglycemia, hyperkalemia.
Allergic reactions: seldom - skin rashes, hypersensitivity reactions, Quincke's edema.
Contraindications
Children aged 3 months;
Hypersensitivity to pipekuroniyu and / or bromine.
Precautions should be used with biliary tract obstruction, edema, dehydration, disruption of water and electrolyte metabolism, hypothermia, myasthenia gravis, respiratory failure, cardiac insufficiency in the stage of decompensation, renal and / or hepatic insufficiency, pregnancy, during breastfeeding.
Pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. Pipekuroniya bromide penetrates the placental barrier. Pregnant women who are at toxicosis as a palliative treatment received magnesium salts (which can enhance neuromuscular blockade), pipekuroniya bromide administered in small doses. Precautions should use the drug during breastfeeding.
Cautions
The drug should be used only in a specialized hospital with appropriate equipment for artificial respiration and in the presence of a specialist to carry out artificial respiration. Must be carefully monitored to maintain vital functions during surgery and in the early postoperative period until full restoration of adequate vitality.
When calculating the dose should be taken into account of the technique of anesthesia, possible interactions with other drugs, introduced before or during anesthesia, the state and the individual patient's sensitivity to the drug. Doses causing miorelaxation do not have a significant cardiovascular effect and in most cases do not cause bradycardia.
The need for supplies and dosing regimen vagolytic drugs for sedation should first carefully analyze (it should also take into account the stimulating effect on the n. vagus others used both drugs, as well as the type of operation).
To prevent relative overdose of the drug and to ensure appropriate monitoring recovery of muscle activity is recommended to use peripheral nerve stimulator. Patients with disorders of neuromuscular transmission, obesity, renal insufficiency, disorders of liver function and / or biliary tract, and if history is indication transferred polio, should be prescribed the drug in smaller doses.
When violations of liver function application Arduana possible only in cases where the intended benefits to the patient outweighs the potential risk.
This medication should be used in the lowest effective dose. When overweight and obesity may increase the duration of the Arduana, so you should apply a dose, calculated on ideal weight. Some states (hypokalemia, digitalization, gipermagniemiya, diuretics, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may help to change the duration of effect. Before anesthesia should be to normalize the electrolyte balance, AAR and eliminate dehydration. It should be especially careful applying Arduan in the presence of a history of anaphylactic reactions caused by muscle relaxants, because of the possible development of cross-hypersensitivity.
Use in Pediatrics
Children aged from 1 year to 14 years are less sensitive to pipekuroniyu bromide and duration of therapeutic effect, they are shorter than in adults and infants (under 1 year). Efficacy and safety of 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.
Effects on ability to drive vehicles and management mechanisms
In the first 24 h after the cessation of miorelaksiruyuschego Arduana prohibited from driving and other mechanisms, work with which is associated with increased risk of injury.
Overdose
Symptoms: prolonged paralysis of skeletal muscles, sleep apnea, marked reduction of BP.
Treatment: In case of overdose or prolonged neuromuscular blockade spend ventilator to restore spontaneous breathing. In the beginning recovery of spontaneous breathing as an antidote to introduce an inhibitor of acetylcholinesterase (neostigmine, pyridostigmine, endrofony): atropine 0.5 - 1.25 mg in combination with neostigmine (1-3 mg) or galantamine (10-30 mg). Until the restoration of a satisfactory spontaneous respiration should conduct a careful control of respiratory function.
Drug Interactions
Acetylcholinesterase inhibitors (neostigmine, pyridostigmine, edrofony) are antagonists Arduana. Increased intensity and / or duration of action Ardurana occurs when:
simultaneous use of inhaled anesthetics (halothane, Methoxyflurane, ether, enflurana, izoflurana, cyclopropane);
usually requires a reduction in dose Arduana.
simultaneous use with other nedepolyariziruyuschie muscle relaxants, anesthetics for in / injection (ketamine, fentanyl, propanididom, barbiturates, etomidatom, γ-gidroksimaslyanoy acid).
simultaneous use of some antibiotics and chemotherapeutic drugs (drugs aminoglycoside, tetracyclines, polypeptides, imidazole, and metronidazole and antifungal agents (amphotericin B).
simultaneous use of diuretics, alpha-and beta-blockers, thiamine, MAO inhibitors, guanidine, protamine, phenytoin, calcium channel blockers slow, salts of magnesium, lidocaine for in / in the introduction.
Provisional application of succinylcholine is accompanied by a reduction of time required for the onset of miorelaxation and increase the duration of effect. Arduan should be introduced after the disappearance of clinical signs of succinylcholine. In this case the effect depends on dose and individual sensitivity.
Reduces the intensity and / or duration of the preceding introduction Ardurana Arduana prolonged use of GCS, neostigmine, pyridostigmine, azathioprine, theophylline, epinephrine, potassium chloride, sodium chloride. Strengthening or weakening action is a preliminary (before surgery) application depolyariziruyuschih muscle relaxants (playing the role of dose, time of use and individual sensitivity).
In case of simultaneous appointment with chinidin, magnesium salts, procainamide may gain miorelaxation. In cases of simultaneous use of halothane or fentanyl for sedation may reduce blood pressure and the development of bradycardia.
Terms and Conditions of storage
The drug should be stored out of reach of children, protected from light at 2-8 ° C.
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