TRAKRIUM

Active material: Atrakuriya besilate
When ATH: M03AC04
CCF: Muscle relaxants peripherally acting non-depolarizing competitive type
ICD-10 codes (testimony): Z51.4
When CSF: 21.03.01.01
Manufacturer: GlaxoSmithKline Trading Company (Russia)

Pharmaceutical form, composition and packaging

The solution for the on / in the clear, colorless to pale yellow.

Excipients: r-r benzolsul′fonovoj acid 32%, water d / and.

2.5 ml – Ampoules with ceramic stain blue and two colored rings on top vials (5) – trays, plastic (1) – packs cardboard.

The solution for the on / in the clear, colorless to pale yellow.

Excipients: r-r benzolsul′fonovoj acid 32%, water d / and.

5 ml – Ampoules with ceramic stain blue and two colored rings on top vials (5) – trays, plastic (1) – packs cardboard.

Pharmacological action

Muscle relaxants peripherally acting non-depolarizing competitive type. Atracurium besilate reduces sensitivity n-holinoretseptorov synaptic area for acetylcholine, as a result of which it becomes impossible to initiation of muscle fiber and its reduction. Contributes to the release of histamine.

Atracurium BESYLATE has no direct influence on intraocular pressure. Thus, Atracurium besilate apply ophthalmic surgical practice.

Pharmacokinetics

Metabolism

Atracurium besilate inaguiruetsa off by Hoffmann (process, which occurs when the physiological pH and temperature without the participation of enzymes) and by hydrolysis broadcasting with the participation of nonspecific esterases. Study of plasma in patients with low pseudocholinesterasis revealed, the products of metabolism of Atracurium bezilata do not change.

Modify the values of the pH of the blood and body temperature within physiological limits would not significantly affect the duration of Atracurium bezilata.

Deduction

Duration of neuromuscular blockade, caused by the introduction of Atracurium bezilata, does not depend on its metabolism in the liver or kidneys, or from its excretion. Therefore it is unlikely, that the duration of the drug changes when violations of the kidneys, liver and circulatory disorders.

Pharmacokinetics in special clinical situations

Hemofiltration and hemodiafiltration have minimal effect on the concentration of Atracurium and its metabolites bezilata (including laudanozin) plasma. On the influence of hemodialysis and hemoperfusion on concentration of Atracurium bezilata and its metabolites in blood plasma is unknown.

Intensive care unit patients (BITS) with the human kidney and/or liver were observed higher concentrations of metabolites of Atracurium bezilata. Metabolites do not affect neuromuscular conductivity.

Testimony

as a component of general anesthesia to ensure tracheal intubations and relaxation skeletal muscles in surgical interventions, or controlled ventilation, and to facilitate mechanical ventilation (IVL) patients in intensive care unit (BITS).

Dosage regimen

Trakrium^® misleading in/in in the form of injections. To Adult range of doses is 300-600 mg / kg (Depending on the required duration of full closures), that provides adequate mioplegiû for 15-35 m.

After the on / in the doses 500-600 mg/kg endotracheal intubation can be performed, usually, After 90 sec.

At need rollover complete neuromuscular blockade Optionally, enter Trakrium^® dose 100-200 mg / kg. Correct introduction of additional doses of the drug does not lead to the cumulation of miorelaksiruûŝego effect.

Spontaneous recovery of conductivity after complete neuromuscular blockade occurs in approximately 35 m, determined to restore tetaničeskogo reduction 95% from normal neuromuscular function. Neuromuscular blockade, called atrakuriem, can be quickly eliminated by the use of a standard dose antiholinesteraznah funds, such as neostigmine and èdrofonij, combined with the simultaneous or prior to the introduction of atropine (without signs of rekurarizacii).

After the initial dose bolusna 300-600 mg/kg Trakrium^® You can apply for maintenance of neuromuscular blockade during long surgery by continuous infusion with speed 300-600 mcg/kg/h. Trakrium^® You can enter through the infusions for operation kardiopul′monarnogo bypass surgery with speed, recommended for infusion. When induced hypothermia with body temperature from 25° to 26° c decreases speed of inactivation of Trakriuma^®, thus, to maintain full miorelaxation speed infusion at low temperatures reduce the approximately 2 times.

For children 2 and older Trakrium^® designate the same doses, as adults, based on the weight of the body.

Initial dose Trakriuma^®, applied at the children aged 1 Months before 2 years When galotanovoj anesthesia, is 300-400 mg / kg. Children may need more frequent application doses, than in adults.

Trakrium^® You can apply a standard dose at elderly patients. However, the recommended initial dose, that the lower dose range values, and enter the drug slowly.

Trakrium^® You can apply a standard dose at any level abnormal liver function or kidney, including insufficient final stage.

In patients with cardiovascular disease with asymptomatic initial dose Trakriuma^® be administered during 60 sec.

Use in patients a BIT

After the introduction of Trakriuma if necessary^® primary bolusna dose 300-600 mg/kg of the drug can be used to maintain neuromuscular blockade by carrying out continuous infusion with speed 11-13 ug / kg / min (650-780 mcg/kg/h). However, there are wide differences in dosing mode mežindividual′nye. The dosage may vary in time. Some patients may require both low speed infusion – 4.5 ug / kg / min (0.27 mg / kg / hr), and high – 29.5 ug / kg / min (1.77 mg / kg / hr).

Speed the spontaneous recovery from neuromuscular blockade when infusion Trakriuma^® patients a BIT does not depend on the length of the introduction. Spontaneous recovery nervous conductivity (ratio of height to the first quarter of podergivaniû in the test train-of-four T₄/T₁>0.75) usually occurs in approximately 60 m. In clinical studies this period ranged from 32 to 108 minutes after infusion Trakriuma^®, and its speed does not depend on the duration of drug administration.

Monitoring

Like other muscle relaxants, during the entire period of use of Trakriuma^® It is recommended that monitoring of neuromuscular function to determine the dosage in each case.

Side effect

Below lists the adverse reactions, organs and systems monitored frequency. Frequency of adverse reactions is defined as follows:: Often (≥1/10), often (≥1 / 100 and <1/10), sometimes (≥1 / 1000 <1/100), rarely (≥1/10 000 less 1/1000), rarely (<1/10 000) and individual messages (when, When the data to determine the incidence of adverse reactions is not enough).

Data from clinical studies

Cardio-vascular system: often – transient reduction in blood pressure, dermahemia.

The respiratory system: sometimes – bronchospasm.

Data from unwanted phenomena are associated with histamine release.

Post-marketing data

On the part of the immune system: rarely – anaphylactic and anaphylactoid reactions. Very rarely reported severe anaphylactic or anaphylactoidnykh reactions when combined with the application of Trakriuma^® with anaesthetics.

From the nervous system: in some cases – convulsions. There were reports of cases of convulsions in patients, located on the intensive therapy, receiving other drugs, In addition to Trakriuma^®. Usually these patients were preconditions for the emergence of convulsing, such as head injury, cephaledema, viral encephalitis, hypoxic encephalopathy, uremia. Relationship between the occurrence of seizures and the use of laudanozine is not installed. As a result of clinical studies correlation between plasma laudanozine concentration and the incidence of stroke is missing.

On the part of the musculoskeletal system: in some cases – myopathy, muscular weakness. It was reported on several cases of myopathy and/or muscle weakness caused by prolonged use of muscle relaxant from seriously ill patients, located in a block of intensive therapy. Most of them at the same time receive the GCS. This adverse reaction is regarded as abnormal for Trakriuma^®, connection with the use of the drug is not installed.

Contraindications

is a known hypersensitivity to atrakuriû, cisatrakuriû or benzolsul′fonovoj acid, any other components of the drug;

is a known sensitivity to gistaminu.

Prone patients Trakrium^® can cause reactions, associated with the release of gistamina. Observe caution with the introduction of Trakriuma^® patients with a history of sensitivity to the effects of histamine.

Caution is also required when the introduction Trakriuma^® patients, have experienced hypersensitivity reactions to other miorelaksantam, tk. There was revealed high incidence of cross sensitivity between miorelaxanthami (more 50%).

Like other nedepoliarizuth miorelaksantov, hypersensitivity to Trakriumu^® may occur in patients with severe myasthenia, other neuromuscular diseases and severe violations elektrolitnogo balance.

Pregnancy and lactation

Study of the impact on fertility has not been.

Trakrium^® should be used during pregnancy only in cases of, When the potential benefit to the mother is greater than any possible risk to the fetus.

Trakrium^® can be applied with a view to miorelaxation in Cesarean section, tk. When you assign in the recommended doses, Atracurium besilate penetrates through the placental barrier in clinically insignificant quantities.

Unknown, whether Atracurium besilate stands out with breast milk in humans.

Cautions

Like other muscle relaxants, Trakrium^® causes paralysis of skeletal muscle, including the respiratory muscles, but does not affect consciousness.

Trakrium^® should only be entered during general anesthesia under the close supervision of a qualified anesthesiologist if there is equipment for tracheal intubations and IVL.

When used in recommended doses range Trakrium^® does not cause significant blockade of the vagus nerve and the nerve ganglia. Hence, Trakrium^® in the recommended range of doses has no clinically significant effects on HEART RATE and a does not prevent bradycardia, caused by anaesthetics or stimulation wandering nerve during surgery.

Patients with a penchant for sharp decline in HELL, eg, with gipovolemiei, Trakrium^® We recommend that you enter for more 60 sec.

Trakrium^® inaguiruetsa in alkaline Wednesday, and it should not be confused in one sprite with tiopentonom or any alkaline solutions.

Introduction of Trakriuma^® produced in small-calibre vein, After the injection, it should be rinsed with saline solution. With the introduction of other anesthetics through the same injecting the needle or cannula is important, to each drug smyvalsâ the appropriate number of physiological solution.

Solution Trakriuma^® hypotonic, and it cannot be entered simultaneously through a single system with gemotransfuziej.

Clinical studies in patients, susceptible to malignant hyperthermia, show, that Trakrium^® does not cause this syndrome.

In patients with severe burns can develop resistance to nedepolârizuûŝim miorelaksantam. In such cases, you may need to increase doses, the value of which depends on the time, Since the burn, and of the surface area of the burn.

Patients a BIT, receiving Trakrium^®, There were cramps, However, the causal link their development with laudanozinom (metabolite of Atracurium bezilata) not installed.

Effects on ability to drive vehicles and management mechanisms

Data not available.

Overdose

Symptoms: prolonged muscle paralysis and its impact are the main symptoms of overdose.

Treatment: the most important is to maintain patency of the Airways, in conjunction with the use of positive pressure VENTILATION to adequate recovery of spontaneous breathing. You must use sedation, because consciousness of patients is not disturbed. As soon as there are signs of spontaneous recovery, It can be enhanced through antiholinesteraznah drugs in combination with atropinom or glikopirrolatom.

Drug Interactions

Induced Trakriumom^® neuromuscular blockade can be reinforced when applying means of inhalation narcosis, such as halothane, izofluran, enfluran.

Like other nedepoliarizuth miorelaksantov, the increase in the intensity and/or duration of neuromuscular blockade by the interaction with: antibiotics (aminoglikozidy, Polymyxin, spectinomycin, tetracikliny, lincomycin and clindamycin); antiarrhythmics (propranolol, Calcium channel blockers, lidokain, procainamide and quinidine); Diuretic (furosemide and, perhaps, mannitol, tiazidnye dioretiki and acetazolamide); magnesium sulfate; ketamine; lithium salt; ganglioblokatorы (trimetafan, geksametonïy).

In rare cases, certain drugs cause worsening of myasthenia, contribute to the development of myasthenia of latent forms, as well as the myasthenic syndrome, where possible increased sensitivity to Trakriumu^®. They include different antibiotics, beta-blockers (propranolol, oxprenolol), antiarrhythmic (prokaynamyd, quinidine) and antirheumatic products (chloroquine, D-Penicillamine), trimetafan, chlorpromazine, steroids, phenytoin, lithium salts.

Development of neuromuscular blockade, caused by non-depolarizing muscle relaxants, probably, slows down, and its duration is reduced in patients, receiving protivosudorojnuu therapy for a long time.

Combined application of nedepoliarizuth neuromuscular blocker and Trakriuma^® may cause excessive blockade, compared with the expected from the introduction of the single Trakriuma^® in èkvipotencial′noj total dose. Any effect, due to synergism, may vary with different combinations of drugs.

Depolarizing muscle relaxant suksametonia chloride should not be used to prolong neuromuscular blockade, caused by non-depolarizing muscle relaxants, such as Trakrium^®, because it can cause extended and difficult siege, which is difficult to abolish antiholinesteraznami means.

Therapy antiholinesteraznami drugs, often used for the treatment of Alzheimer's disease, eg, donepezil, can shorten the duration of neuromuscular blocking effect and weaken Trakriuma^®.

Pharmaceutically compatible

Trakrium^® compatible with the following infusion solutions within the specified time:

Solution Trakriuma^® When breeding compatible infusion solutions to obtain a concentration of Atracurium bezilata 500 µg/ml and more is stable in daylight for a set period at a temperature up to 30° c.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in the dark, inaccessible to children at 2 ° to 8 ° C; Do not freeze. Shelf life – 2 year.