ARDUAN

Active material: Pipekuroniya bromide
When ATH: M03AC06
CCF: Muscle relaxants peripherally acting non-depolarizing competitive type
ICD-10 codes (testimony): Z51.4
When CSF: 21.03.01.01
Manufacturer: GEDEON RICHTER Ltd. (Hungary)

DOSAGE FORM, COMPOSITION AND PACKAGING

Valium for drug of a solution for / in white or nearly white; attached colorless solvent, clear.

1 fl.
pipekuroniya bromide4 mg

Excipients: mannitol.

Solvent: sodium chloride rr 0.9% – 2 ml.

Bottles (25) together with the solvent (amp. 25 PC.) – packs cardboard.

 

Pharmacological action

Non-depolarizing muscle relaxant peripheral long-acting. Due to the competitive binding with n-holinoretseptorami, motor terminals disposed in striated muscle fibers, blocks the signal transmission from nerve to muscle fibers.

It does not cause muscle twitches, It does not have a hormonal action, It does not stimulate histamine release. In moderate doses does not cause significant hemodynamic changes.

Dose, equal 5 ug / kg body weight, It provides a 40-50-minute muscle relaxation during surgery. The maximum effect is developed through 2.5-5 m, the fastest effect occurs at doses, equal 70-80 mg / kg. Further increase of the dose shortens time, required to develop action, and significantly extends the duration of drug action.

 

Pharmacokinetics

Distribution

The on / in the introduction of the initial Vd is 110 ml / kg. Vd in an equilibrium state is 300 ± 78 mL / kg.

The cumulative effect is insignificant or absent upon repeated administration at doses 10-20 ug / kg in the time of recovery of the initial contractility at 25%.

It penetrates through the placental barrier.

Metabolism and excretion

Plasma clearance is about 2.4 ± 0.5 ml / min / kg. T1/2 pipekuroniya averaged 121 ± 45 min. Write mainly in the urine, wherein 56% active substance – first 24 no, 1/3 active substance appears unchanged, remainder – a 3-desacetyl-pipekuroniya.

 

INDICATIONS

- Endotracheal intubation and relaxation of skeletal muscles in the course of general anesthesia during surgery, requiring more than 20-30 minutes of muscle relaxation.

 

DOSAGE

The drug should be used only in /.

Immediately before administration 4 mg of dry matter bred enclosed solvent. With a balanced anesthesia ED50 и AND90 Arduana are respectively 30 mg / kg 50 ug / kg body weight. Minimal, necessary for the onset of effect, observed at doses 70-80 mg / kg.

The dose should be individualized for each patient based on the type of anesthesia, the expected duration of surgery, possible interactions with other drugs, applied before or during anesthesia, comorbidities, and general condition of the patient. For monitoring of neuromuscular blockade is recommended that the use of peripheral nerve stimulator.

The drug should be used under the supervision of a qualified physician, having clinical experience of peripheral muscle relaxants.

Recommended dose

The initial dose intubation and subsequent surgery - 80-100 ug / kg body weight - provides good or excellent conditions for intubation 150-180 sec, The duration of neuromuscular blockade 60-90 m.

The initial dose for muscle relaxation during surgery after intubation with succinylcholine - 50 ug / kg of body weight provides the 30-60 minute miorelaxation.

Maintenance dose - 10-20 ug / kg - provides 30-60 minute miorelaxation.

At chronic renal failure the dose should be calculated according to the QC.

CC (ml / min)Dose (ug / kg body weight)
>100to 100
10085
8070
6055
4050

Children aged 3 months before 1 year the drug should be used in the calculation 40 ug / kg body weight (providing muscle relaxation duration from 10 to 44 m), from 1 Year to 14 years - 57 mg / kg (muscle relaxation provided by the duration 18 to 52 m).

Elimination of the drug

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

 

SIDE EFFECT

From the central and peripheral nervous system: rarely (less 1%) - CNS depression, gipesteziya.

On the part of the musculoskeletal system: rarely - weakness of the skeletal muscles after the cessation of muscle relaxation, muscular atrophy.

The respiratory system: rarely - gipnoe, apnea, pulmonary atelectasis, respiratory depression, laryngospasm due to an allergic reaction.

Cardio-vascular system: rarely – myocardial ischemia (until myocardial infarction) and brain, Atrial fibrillation, ventricular premature beats, bradycardia, decrease in blood pressure.

From the blood coagulation system: rarely - thrombosis, decrease in aPTT and prothrombin time.

From the urinary system: rarely - hypercreatininemia, anurija.

Metabolism: rarely - hypoglycemia, hyperkalemia.

Allergic reactions: seldom - skin rash, hypersensitivity reactions, angioedema.

 

CONTRAINDICATIONS

- Children up to age 3 Months;

- Hypersensitivity to pipekuroniyu and / or bromine.

FROM caution should be applied in biliary tract obstruction, Edema syndrome, degidratacii, violation of water-electrolyte metabolism, gipotermii, myasthenia, respiratory failure, heart failure decompensation, kidney and / or liver failure, pregnancy, during breastfeeding.

 

Pregnancy and lactation

Use of the drug during pregnancy is possible only in case, when the intended benefits to the mother outweighs the potential risk to the fetus. Pipekuroniyu bromide crosses the placental barrier.

Pregnant women, that when toxemia as palliative therapy took magnesium salts (can enhance neuromuscular blockade), pipekuroniya bromide is administered in small doses.

Precautions should use the drug during breastfeeding.

 

Cautions

The drug should be used only in a specialized hospital with the appropriate equipment for artificial respiration and in the presence of a specialist to conduct artificial respiration.

Careful monitoring of the maintenance of vital functions during surgery and in the early postoperative period until the full restoration of adequate vitality.

When calculating the dose should be considered to apply the technique of anesthesia, the possible interaction with other drugs, administered before or during anesthesia, the state and the individual patient's sensitivity to the drug.

Doses, causing muscle relaxation, not have a significant cardiovascular effect and in most cases do not cause bradycardia.

The need for the appointment and dosing regimen vagolytic preparations for premedication should first carefully consider (It should also take into account the stimulating effect of the n. vagus others, used both drugs, as well as the type of operation).

To prevent relative overdose and to ensure appropriate monitoring recovery of muscle activity is recommended to use a peripheral nerve stimulator.

Patients with disorders of neuromuscular transmission, obesity, renal failure, for violations of the liver and / or biliary tract, or if a history of myocardial indicate polio, the drug should be prescribed in smaller doses.

If abnormal liver function Arduana application is possible only in cases, when the intended benefits to the patient outweighs the potential risk. When this drug should be used in the minimum effective dose.

When overweight and obesity may increase the duration of Arduana, therefore the dose should be used, designed for ideal weight.

Some state (kaliopenia, digitization, gipermagniemiya, diuretics, hypocalcemia, hypoproteinemia, degidratatsiya, Acidosis, giperkapniя, kaxeksija, gipotermiя) may contribute to a change in the duration of effect. Before the start of anesthesia should normalize the electrolyte balance, AAR and eliminate dehydration.

Observe extreme caution, applying Arduan with a history of anaphylactic reactions, caused by muscle relaxants, because of the possible development of cross-hypersensitivity.

Use in Pediatrics

Children ages 1 Year to 14 years pipekuroniyu less sensitive to bromide and duration of the therapeutic effect they have short, than in adults and infants (younger 1 year).

Efficacy and safety of use in the neonatal period have not been studied.

The therapeutic effect in infants from 3 Months before 1 the year is not significantly different from that of adults.

Effects on ability to drive vehicles and management mechanisms

First 24 hours after the termination of the action miorelaksiruyuschego Arduana prohibited to drive a car and other mechanisms, the work that is associated with an increased risk of injury.

 

OVERDOSE

Symptoms: prolonged paralysis of skeletal muscle, apnea, marked reduction in blood pressure.

Treatment: In case of overdose or prolonged neuromuscular blockade mechanical ventilation until recovery of spontaneous breathing. Early recovery of spontaneous breathing as an antidote is administered acetylcholinesterase inhibitor (neostigmine, pyridostigmine, endrofonii): atropyn 0.5 – 1.25 mg in combination with neostigmine (1-3 mg) or galantamine (10-30 mg). Before restoring a satisfactory spontaneous respiration should be careful monitoring of respiratory function.

 

Drug Interactions

Acetylcholinesterase inhibitors (neostigmine, pyridostigmine, эdrofonyy) antagonize Arduana.

Increasing the intensity and / or duration of action Ardurana It occurs at:

– concomitant use of inhaled anesthetics (halothane, metoksiflurana, ether, enflurane, isoflurane, cyclopropane); usually require a dose reduction Arduana;

– concomitant use of other muscle relaxants nedepolyariziruyuschie, anesthetics for / in the (Ketamine, fentanilom, propanidid, ʙarʙituratami, etomidate, γ-hydroxybutyric acid);

– the simultaneous use of certain antibiotics and chemotherapy drugs (aminoglycoside drugs, tetracyclines, polypeptides, imidazole, and metronidazole and antifungals (amphotericin B);

– the simultaneous use of diuretics, alpha- and beta-blockers, tiaminom, MAO inhibitors, guanidine, protamine, phenytoin, blockers of slow calcium channels, magnesium salts, lidocaine for the on / in the.

Provisional application is accompanied by a reduction in the time of succinylcholine, necessary for the onset of muscle relaxation and increased duration of effect. Arduan should be administered after the disappearance of clinical signs of the action of succinylcholine. In this case, the effect is dose-dependent and individual sensitivity.

It reduces the intensity and / or duration of action Ardurana preceded by an introduction Arduana prolonged use of corticosteroids, neostigmine, pyridostigmine, azathioprine, teofillina, epinephrine, potassium chloride, sodium chloride.

Strengthening or weakening of the action is preliminary (prior to surgery) the use of muscle relaxants depolyariziruyuschih (play a role dose, time of application and individual sensitivity).

When concomitant administration with quinidine, magnesium salts, procainamide may increase muscle relaxation. In the case of simultaneous use of halothane or fentanyl for sedation may reduce blood pressure and bradycardia.

 

Conditions of supply of pharmacies

The drug is released under the prescription.

 

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dark place at a temperature of 2-8 ° C.