Arduan synonyms analogues. Arduan is a means for relaxation of skeletal muscles. Doses and method of application

Active substance

Pipecuronium bromide (pipecuronium bromide)

Release form, composition and packaging

Lyophilisate for solution for intravenous administration white or almost white; the applied solvent is a colorless transparent solution.

Excipients: mannitol 6.0 mg.

Solvent: sodium chloride 18.0 mg, up to 2 ml.

10 mg - colorless glass bottles (5) - plastic trays (5) complete with a solvent (amp. 25 pcs.) - cardboard packs.

pharmachologic effect

Long-acting non-depolarizing peripheral muscle relaxant. Due to competitive binding to 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 fasciculation, does not have a hormonal effect.

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

According to studies, with balanced anesthesia, the doses of ED 50 and ED 90 of pipecuronium bromide are 30-50 μg / kg of body weight, respectively.

A dose of 50 mcg/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 develops after 1.5-5 minutes. The effect develops most rapidly at doses of 70-80 mcg/kg. A further increase in the dose of the drug reduces the time required for the development of the effect, and significantly increases the duration of the drug.

Pharmacokinetics

Distribution

With a / in the introduction of the initial V d is 110 ml / kg of body weight. V d in the equilibrium state reaches 300±78 ml/kg. Average time spent in (MRT) - 140 min.

With repeated administration of maintenance doses, the cumulative effect is insignificant if doses of 10-20 mcg/kg are used at the time of 25% recovery of the initial muscle contractility.

Penetrates through the placental barrier.

Metabolism and excretion

Plasma clearance is approximately 2.4±0.5 ml/min/kg. Average T 1/2β is 121±45 min.

It is excreted mainly by the kidneys, with 56% of the active substance in the first 24 hours, 1/3 of the active substance is excreted unchanged, the rest is in the form of 3-deacetyl-pipecuronium bromide. According to preclinical studies, the liver is also involved in the elimination of pipecuronium bromide.

Indications

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

Contraindications

• severe liver failure;
• children's age up to 3 months;
• hypersensitivity to pipecuronium and / or bromine.

Carefully: biliary tract obstruction, edematous syndrome, increased BCC or dehydration, diuretics, acid-base imbalance (acidosis, hypercapnia) and water-electrolyte metabolism (hypokalemia, hypermagnesemia, hypocalcemia), hypothermia, digitalization, hypoproteinemia, cachexia, myasthenia gravis (including .h. myasthenia gravis, Eaton-Lambert syndrome) due to the possible increase or weakening of the drug in such cases (small doses of Arduan in severe myasthenia gravis or Eaton-Lambert syndrome can cause a pronounced effect; such patients should be given the drug in very low doses after a careful assessment of the potential risk), respiratory depression, renal failure (increased duration of action of the drug and the time of post-anesthesia depression), in chronic heart failure in the stage of decompensation, malignant hyperthermia, with a history of an anaphylactic reaction to any muscle relaxant ( due to possible crosstalk lergy), children under the age of 14 years.

Dosage

As with other non-depolarizing myorelaxants, 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. To control neuromuscular blockade, the use of a peripheral nerve stimulator is recommended.

Apply only in / in. Immediately before administration, the contents of the vial (4 mg of dry matter) are diluted with the supplied solvent. Only freshly prepared solution should be used.

Initial dose for intubation and subsequent surgery: 60-80 mcg/kg of body weight - provides good/excellent conditions for intubation within 150-180 seconds, while the duration of muscle relaxation is 60-90 minutes.

Initial dose for muscle relaxation during intubation using suxamethonium: 50 mcg/kg of body weight - provides 30-60 minutes of muscle relaxation.

Maintenance dose: is 10-20 mcg / kg - provides 30-60 minutes of muscle relaxation during surgery.

With Arduan, it is not recommended to use in doses of more than 40 mcg / kg (in high doses, an increase in the duration of muscle relaxation is possible).

At overweight and obese patients it is possible to increase the duration of action of Arduan, so the drug should be used at a dose calculated for ideal weight.

Children aged 3 to 12 months

The dose is 40 mcg / kg (which provides muscle relaxation lasting from 10 to 44 minutes).

The dose is 50-60 mcg / kg (which provides muscle relaxation lasting from 18 to 52 minutes).

End 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.

Side effects

From the nervous system: rarely (<1%) - угнетение ЦНС, сонливость, гипестезия, паралич скелетной мускулатуры.

From the musculoskeletal system: rarely (<1%) - слабость скелетной мускулатуры после прекращения миорелаксации, мышечная атрофия.

From the respiratory system: rarely (<1%) - апноэ, ателектаз легкого, угнетение дыхания, ларингоспазм в результате аллергической реакции, бронхоспазм, кашель.

From the side of the cardiovascular system: rarely (<1%) - ишемия миокарда (вплоть до инфаркта миокарда) и мозга, тахикардия, брадикардия, аритмии (в т.ч. фибрилляция предсердий, желудочковая экстрасистолия, желудочковая тахикардия), снижение или повышение АД.

From the blood coagulation system: rarely (<1%) - тромбоз, уменьшение АЧТВ и протромбинового времени.

From the urinary system: rarely (<1%) - анурия.

From the side of the organ of vision: blepharitis, ptosis.

Allergic reactions: rarely (<1%) - кожная сыпь, реакции гиперчувствительности, отек Квинке.

Laboratory indicators: rarely (<1%) - гиперкреатининемия, гипергликемия, гипокалиемия, гипомагниемия, гипокальциемия.

Overdose

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

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 (for example, neostigmine methyl sulfate, edrophonium chloride) is administered as an antidote: atropine 0.5-1.25 mg in combination with neostigmine methyl sulfate (1-3 mg) or galanthamine (10-30 mg). Careful monitoring of respiratory function should be carried out until satisfactory spontaneous breathing is restored.

drug interaction

Inhalation anesthetics (halothane, methoxyflurane, diethyl ether, enflurane, isoflurane, cyclopropane), intravenous anesthetics (ketamine, propanidide, barbiturates, etomidate, gamma-hydroxybutyric acid), depolarizing and non-depolarizing muscle relaxants, some antibiotics (aminoglycosides, derivatives nitroimidazole, including metronidazole, tetracyclines, bacitracin, capreomycin, clindamycin, polymyxins, including colistin, lincomycin, ), citrate anticoagulants, mineralocorticoids and glucocorticoids, diuretics, incl. bumetanide, carbonic anhydrase inhibitors, ethacrynic acid, corticotropin, alpha- and beta-blockers, thiamine, MAO inhibitors, guanidine, phenytoin, slow calcium channel blockers, magnesium salts, procainamide, quinidine, lidocaine and procaine for intravenous administration increase the intensity and / or the duration of Arduan's action.

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

Opioid analgesics increase respiratory depression. Sufentanil at high doses reduces 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). Arduan does not reduce the risk of bradycardia and arterial hypotension caused by opioid analgesics (especially against the background of vasodilators and / or beta-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 the onset of muscle relaxation 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, sodium chloride, calcium chloride, the effect may be weakened.

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

Doxapram temporarily masks the residual effects of muscle relaxants.

special instructions

The drug should be used 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.

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

When calculating the dose, one should take into account the anesthesia technique used, possible interactions with other drugs administered before or during anesthesia, the condition and individual 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.

Greater caution should be exercised when using Arduan in patients with a history of anaphylactic reactions caused by muscle relaxants, due to the possible development of cross-allergy.

Arduan in doses that cause muscle relaxation does not have a significant cardiovascular effect and in the vast majority of cases does not cause bradycardia.

The use and dose of m-anticholinergics for the purpose of premedication is subject to careful preliminary evaluation; one should also take into account the stimulating effect on n. vagus of other concomitantly used drugs, as well as the type of operation.

To prevent a relative overdose of the drug and to ensure adequate control of the recovery of muscle activity, it is recommended to use a peripheral nerve stimulator.

Patients with neuromuscular transmission disorders, obesity, renal insufficiency, diseases of the liver and / or biliary tract, with indications of a history of poliomyelitis, it is necessary to prescribe the drug in lower doses.

In the case of liver disease, the use of Arduan is possible only in cases where the intended benefit to the patient outweighs the potential risk. In this case, the drug should be used in the minimum effective dose.

Some conditions (hypokalemia, digitalization, hypermagnesemia, diuretics, hypocalcemia, hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia, hypothermia) may increase the intensity or duration of the effect. As in the case of other muscle relaxants, before using Arduan, electrolyte balance, acid-base balance should be normalized and dehydration should be eliminated.

Like other muscle relaxants, Arduan may reduce aPTT and prothrombin time.

Pediatric use

Children aged 1 to 14 years 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.

muscle relaxant effect infants from 3 months to 1 year not significantly different from that in adults.

Influence on the ability to drive vehicles and mechanisms

In the first 24 hours after the cessation of the muscle relaxant action of Arduan, it is not recommended to drive vehicles and engage in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Pregnancy and lactation

Clinical studies to prove the safety of the use of Arduan during pregnancy for the mother and fetus are not enough. The use of the drug during pregnancy is not recommended.

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

Application in childhood

Contraindicated in children under 3 months of age.

FROM caution the drug should be used in children under the age of 14 years.

For impaired renal function

At chronic renal failure Arduan is not recommended for use in doses greater than 0.04 mg/kg (high doses may increase the duration of muscle relaxation).

For impaired liver function

FROM caution should be used in liver failure.

Use is contraindicated in severe liver failure.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

The drug should be stored out of the reach of children, protected from light at a temperature of 2° to 8°C. Shelf life - 3 years.

International name

Group affiliation

Dosage form

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 μg / kg, the duration of the effect is 30-175 minutes, 80-85 μg / 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

Contraindications

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 side of 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.

Application and dosage

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 value of the 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

Medications 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.

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pharmachologic effect

Peripheral muscle relaxant of non-depolarizing competitive type. It is a bis-quaternary ammonium compound with a steroid structure. It blocks n-cholinergic receptors of skeletal muscles and prevents the depolarizing action of acetylcholine. Muscle-relaxing effect after intravenous administration of pipecuronium bromide develops after 2-3 minutes and lasts 30-120 minutes, depending on the dose.

Muscle relaxation is not accompanied by fasciculations and muscle pain after surgery. Pipecuronium bromide does not cause the release of histamine from mast cells, in therapeutic doses it has little effect on the cardiovascular system, and in high doses it has some ganglioblocking activity.

Pharmacokinetics

After intravenous administration, a fast initial distribution phase and a slow elimination phase are noted. Does not undergo metabolism. T 1/2 is 60-120 min. More than 75% of the administered dose is excreted in the urine, the rest, apparently, in the bile.

Indications

For relaxation of skeletal muscles during general anesthesia during surgical interventions and mechanical ventilation.

Dosing regimen

The dose is set individually, depending on the type of anesthesia, the expected duration of surgery, the patient's condition. Enter / in doses of 20-85 mcg / kg, if necessary, increase the duration of action is administered 1/4 of the initial dose.

Side effect

From the side of the cardiovascular system: moderate bradycardia, some decrease in blood pressure are possible.

From the blood coagulation system: a decrease in partial thromboplastin and prothrombin time has been described.

Allergic reactions: rarely - anaphylactoid reactions.

Contraindications for use

Severe form of myasthenia gravis, hypersensitivity to pipecuronium bromide.

Use during pregnancy and lactation

In pregnant women who received magnesium salts (which can potentiate neuromuscular blockade) for the treatment of toxicosis, pipecuronium bromide should be used in reduced doses. There are no data on the excretion of pipecuronium bromide in breast milk.

Use in children

Contraindicated in children under 3 months of age.

FROM caution the drug should be used in children under the age of 14 years.

Overdose

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

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 (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.

drug interaction

Strengthening and / or prolonging the action of pipecuronium bromide is possible with simultaneous use with inhalation anesthesia agents (halothane, methoxyflurane, diethyl ether), intravenous anesthesia agents (ketamine, propanidide, barbiturates), other non-depolarizing muscle relaxants, aminoglycoside antibiotics, tetracyclines, imidazole , metronidazole, diuretics, beta-blockers, thiamine, MAO inhibitors, guanidine, protamine, phenytoin, alpha-blockers, calcium channel blockers, lidocaine (with intravenous administration).

When used before surgery, corticosteroids, neostigmine, norepinephrine, theophylline, potassium chloride, sodium chloride, calcium chloride may weaken the effect of pipecuronium bromide.

Depolarizing muscle relaxants can both enhance and weaken the effect of pipecuronium bromide; it depends on the dose, time of application and individual sensitivity to drugs.

Terms of dispensing from pharmacies

The drug is dispensed by prescription.

Terms and conditions of storage

The drug should be stored out of the reach of children, protected from light at a temperature of 2° to 8°C. Shelf life - 3 years.

Application for violations of liver function

In patients with liver disease, pipecuronium bromide should be used at lower doses.

Application for violations of kidney function

In patients with renal insufficiency, pipecuronium bromide should be used at lower doses.

Use in elderly patients

Use with caution in elderly patients.

special instructions

Pipecuronium bromide should be used only in a specialized hospital with the availability of equipment for mechanical ventilation by anesthesiologists.

Before starting anesthesia, electrolyte balance, acid-base balance should be normalized and dehydration should be eliminated.

In patients with neuromuscular transmission disorders, obesity, renal insufficiency, diseases of the liver and biliary tract, with indications of a history of poliomyelitis, pipecuronium bromide should be used in lower doses.

Use with caution in patients with chronic heart failure, in the elderly.

With extreme caution, pipecuronium bromide, like other neuromuscular blockers, should be used in patients with myasthenia gravis or myasthenic syndrome.

The effect of pipecuronium bromide is enhanced by hypokalemia, hypocalcemia, hypermagnesemia, hypoproteinemia, dehydration, in conditions of acidosis, hypercapnia, cachexia.

The drug is a non-depolarizing muscle relaxant. Arduan is a medicine presented in the form of a white powder, which is perfectly soluble in both water and alcohol. That is why the form of its release is not a solution, but a lyophilisate for its preparation.

Release form

One package of medicine includes:

• 25 colorless vials directly with the medicine (4 mg), which is a dry powder of a white or yellowish tint
• 25 ampoules with solvent (clear colorless liquid)

Compound

The solution for injection is prepared immediately before it is carried out. Therefore, for one vial of powder, which contains the active ingredient, there is one ampoule with a solvent. In this way:

• One vial of Arduan contains 4 mg pipecuronium bromide (active substance) and mannitol (excipient)
• One ampoule with a solvent contains a solution of sodium chloride 0.9% (saline) with a volume of 2 ml

pharmachologic effect

Arduan is a long-acting non-depolarizing competitive muscle relaxant.

Pharmacodynamics

• Carries out a competitive connection with n-cholinergic receptors located in the neuromuscular synapse of skeletal muscles and, thus, blocks the signal from nerve endings to muscle fibers
• Does not have a hormonal effect and does not cause involuntary muscle contraction
• Does not contribute to m-anticholinergic, sympathomimetic and ganglion blocking activity, even at a dosage that is several times higher than the effective
• Studies have shown that 0.05 mg of the active ingredient per kilogram of body weight is sufficient to provide the patient with muscle relaxation during surgery for 40-50 minutes.
• The active substance begins to act in the body 1.5-5 minutes after administration
• The maximum effect depends on the dose

Pharmacokinetics

• Clearance is 0.12 l/h/kg
• Distribution volume - 0.25 l / kg
• Half-life - 6.2 minutes
• Half-life - from one hour to three hours
• With impaired renal function, the half-life increases to 4 hours
• Metabolized in the liver, forming a pharmacologically active metabolite (3-deacetyl-pipecuronium bromide) and a number of inactive derivatives
• 25% is excreted by the kidneys unchanged, the rest is in the form of a metabolite.
• Penetrates through the placental barrier

Indications

The use of Arduan is indicated in the following cases:

1. 1. For endotracheal intubation before general anesthesia during surgical operations, the condition of which is muscle relaxation for more than 20-30 minutes

1. For relaxation of skeletal muscles
2. During mechanical ventilation

Contraindications

Absolute:

1. Children's age up to 3 months
2. The period of pregnancy and breastfeeding
3. Severe liver failure
4. Hypersensitivity to any of the components of the drug

Relative (with caution):

• • Patients with dehydration
  • With increased blood circulation
  • With a tendency to edema
  • With severe renal failure
  • With acid-base balance disorders
  • With disorders of water and electrolyte metabolism

• Increased levels of magnesium in the body
• Decreased levels of potassium and calcium
• Simultaneous reception of Arduan with diuretics is unacceptable
• For malignant hyperthermia during or after general anesthesia
• With a low amount of protein in the blood plasma
• With digitalization
• Patients with chronic heart failure, in the stage of decompensation
• With cachexia
• With respiratory depression
• If you have a history of an anaphylactic reaction to any muscle relaxant
• Age up to 14 years
• Myasthenia gravis (there is a risk that even from a small dose of Arduan the effect will be too strong, or, conversely, insufficient)

Side effects

1. Nervous system: hyperesthesia, skeletal muscle paralysis, depression of the central nervous system, drowsiness
2. Respiratory system: bronchospasm, laryngospasm, lung atelectasis, apnea, cough, respiratory depression
3. Blood coagulation system: thrombosis, decreased partial thromboplastin and prothrombin time
4. Cardiovascular system: bradycardia, tachycardia, ventricular extrasystole, atrial fibrillation, arrhythmia, myocardial infarction, myocardial and cerebral ischemia, increased or decreased blood pressure
5. Musculoskeletal system: muscle atrophy, skeletal muscle weakness after muscle relaxation
6. Metabolism: blood sugar may increase significantly, while the content of potassium, calcium and magnesium, on the contrary, may decrease
7. Urinary system: increased blood creatinine in men, anuria
8. Organs of vision: blepharitis, ptosis
9. Allergic reactions: angioedema, skin rash

Instructions for use

Important! The use of Arduan is possible only in a hospital, in an operating room, which is equipped with the necessary equipment for artificial ventilation and relief of anaphylactic shock in case of its occurrence.

The drug has a strong effect on the respiratory system, so a specialist in artificial lung ventilation must be present during the operation.

Instructions for the use of Arduan have differences when using the drug in adult patients and in children.

For adults and children over 14 years old

• The initial dose for intubation during subsequent surgery is 0.06-0.08 mg per kg of body weight. Duration of action - from an hour to an hour and a half
• Maintenance dose - 0.01-0.02 mg / kg. Time of action - from half an hour to an hour
• If the patient has a history of chronic renal failure, it is not recommended to use a dose of more than 0.04 mg / kg, since due to the long half-life, the effect of the muscle relaxant may be increased
• With overweight and obesity of the patient, a longer action of Arduan is also possible, therefore the dosage is calculated based on the ideal weight of the patient

Children

• From 3 to 12 months: 0.04 mg/kg. Action time - 10-45 minutes
• From one year to 14 years: 0.05-0.06 mg / kg, Duration of action - 18-52 minutes

To stop the action of Arduan during the period of blockade (80% -85%), which is controlled by a peripheral nerve fiber stimulator, or during partial blockade (it can be determined by clinical signs), Atropine is administered to the patient in combination with Galantamine or neostigmine methyl sulfate.

Overdose

Symptoms:

1. Severe reduction in blood pressure
2. Apnea
3. Prolonged skeletal muscle paralysis

Treatment:

• Artificial lung ventilation
• To restore spontaneous breathing, an antidote is administered - an acetylcholinesterase inhibitor (Atropine with Galantomin or neostigmine methyl sulfate)
• Respiratory function is carefully monitored until normal breathing is restored.

Analogues

Arduan has analogues - preparations with an identical active ingredient:

• Aperomide
• Vero-Pipecuronium
• Pipecuronium bromide
• Arkuron

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