Trakrium - Instructions For Use, Price, Analogues, Dose, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Trakrium

Trakrium: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Tracrium

ATX code: M03AC04

Active ingredient: atracuria besilat (Atracurii Besilas)

Manufacturer: GlaxoSmithKline Manufacturing S.p. A. (GlaxoSmithKline Manufacturing SpA) (Italy)

Description and photo update: 2018-11-09

Prices in pharmacies: from 1055 rubles.

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Trakrium is a highly selective non-depolarizing muscle relaxant of peripheral action.

Release form and composition

Dosage form of the drug - solution for intravenous (iv) administration: clear liquid, light yellow or colorless (2.5 ml or 5 ml each in ampoules with a blue ceramic spot and two colored rings on the top; 5 ampoules each in a plastic pallet, in a cardboard box 1 pallet and instructions for the use of Trakrium).

1 ml of solution contains:

• active ingredient: atracuria besylate - 10 mg;
• additional components: benzenesulfonic acid solution, water for injection.

Pharmacological properties

Pharmacodynamics

The active component of Trakrium, atracuria besylate, is a highly selective muscle relaxant of peripheral action of a non-depolarizing competitive type. Its mechanism of action is to reduce the sensitivity of the H-cholinergic receptors of the synaptic region to acetylcholine, due to which the excitation of the muscle fiber and its contraction become impossible.

Atracuria besylate promotes the release of histamine.

The substance does not directly affect the intraocular pressure, therefore it can be used in ophthalmic surgical practice.

Pharmacokinetics

Atracuria besylate is inactivated by a process that occurs at physiological pH and temperature without the participation of enzymes (Hoffman elimination), and by ether hydrolysis with the participation of nonspecific esterases. Plasma studies carried out in patients with a low level of pseudocholinesterase showed that the metabolic products of atracurium besylate remain unchanged.

Changes in blood pH and body temperature within physiological limits have little effect on the duration of the active substance.

The dependence of the duration of the neuromuscular blockade caused by the administration of Tracrium on the metabolism of atracurium besylate in the liver or kidneys, or its excretion was not observed. Therefore, the likelihood that the duration of action of the drug may change in case of circulatory disorders, impaired renal or hepatic functions is extremely small.

Hemodiafiltration and hemofiltration have a minimal effect on the concentration of atracurium besylate and its metabolites (including laudanosine, the main metabolite) in blood plasma. It is not known whether hemoperfusion and hemodialysis affect the concentration of atracurium besylate and its metabolites in blood plasma.

Higher concentrations of atracurium besylate metabolites were observed in intensive care unit (ICU) patients with impaired renal and / or hepatic function. Metabolites do not affect neuromuscular conductivity.

Indications for use

Trakrium is used as a component of general anesthesia in the following cases:

• providing tracheal intubation and relaxation of skeletal muscles during surgical interventions or with controlled ventilation;
• facilitation of mechanical ventilation (artificial lung ventilation) in patients with BIT.

Contraindications

Absolute:

• children's age up to 1 month;
• known hypersensitivity to histamine;
• known hypersensitivity to the components of Trakrium: atracuria (cisatracuria), benzenesulfonic acid.

Relative contraindications (the drug is prescribed with caution):

• a history of indication of hypersensitivity to the action of histamine (in this group of patients, due to a predisposition, the administration of Trakrium can cause the development of reactions associated with the release of histamine);
• known hypersensitivity to other muscle relaxants [since a high (over 50%) incidence of cross-sensitization between muscle relaxants has been identified];
• severe myasthenia gravis, other neuromuscular diseases and severe electrolyte imbalance (as with the use of other non-depolarizing muscle relaxants, this category of patients may have hypersensitivity to Trakrium).

Trakrium, instructions for use: method and dosage

Bolus administration

When Tracrium is administered as an intravenous injection to adult patients, the dose range is 0.3–0.6 mg / kg (depending on how long the complete block is required), which ensures adequate myoplegia for 15–35 minutes.

After intravenous administration in doses of 0.5–0.6 mg / kg, endotracheal intubation can be performed, as a rule, after 1.5 minutes.

If prolongation of complete neuromuscular blockade is necessary, additional administration of the drug is carried out at a dose of 0.1–0.2 mg / kg. Provided that additional doses of Trakrium are correctly administered, the muscle relaxant effect is not cumulative.

Approximately 35 minutes after complete neuromuscular blockade, spontaneous restoration of conduction is observed, which is determined by the restoration of tetanic contraction to 95% of normal neuromuscular function.

The neuromuscular blockade caused by atracuria besylate can be quickly eliminated by the use of anticholinesterase agents in standard doses (for example, edrophonium and neostigmine) in combination with preliminary or simultaneous administration of atropine (provided that there are no signs of recurarization).

Infusion administration

After the introduction of the initial bolus dose (0.3-0.6 mg / kg), the use of Trakrium can be continued by long-term intravenous infusion at a rate of 0.3-0.6 mg / kg / h in order to maintain the neuromuscular blockade during long-term surgical intervention.

The drug can be administered by intravenous infusion during cardiopulmonary bypass surgery at the rate recommended for infusion. In case of induced hypothermia with a body temperature of 25–26 ° C, the rate of inactivation of Trakrium decreases, and therefore, in order to maintain complete muscle relaxation at low temperatures, the infusion rate should be approximately halved.

Special categories of patients

• children: children aged 2 years and older are prescribed Trakrium in doses similar to those for adult patients, in terms of body weight. With halothane anesthesia, the initial dose of atracurium besylate for children aged 1 month to 2 years is 0.3–0.4 mg / kg. Children require more frequent maintenance doses of Trakrium than adults;
• elderly patients: this category of patients is allowed to use the drug in standard doses. In this case, the solution should be injected slowly, using an initial dose that is less than the lower value of the dose range;
• BIT patients: after administration of the solution at an initial bolus dose of 0.3–0.6 mg / kg, if necessary, it can be used to maintain neuromuscular blockade through a continuous infusion, the rate of which is 11–13 μg / kg / min (0, 65–0.78 mg / kg / h). At the same time, in the dosage regimen, it is important to take into account the existence of wide interindividual differences (it can change over time). Some patients require infusion at a lower rate of 4.5 μg / kg / min (0.27 mg / kg / h), others at a higher rate of 29.5 μg / kg / min (1.77 mg / kg / h). In intensive care patients, at the end of the infusion of Trakrium, there is no dependence of the rate of spontaneous recovery after neuromuscular blockade on the duration of administration. Spontaneous restoration of neuromuscular conduction (ratio of quarter height to first twitch in the train-of-four T test₄ / T ₁ > 0.75), as a rule, is noted after about 60 minutes. In clinical studies, this period varied from 32 to 108 minutes after infusion (the dependence of the rate of spontaneous recovery on the duration of Trakrium administration was not observed);
• patients with cardiovascular diseases: in the presence of cardiovascular diseases with severe clinical symptoms, the initial dose of the drug should be administered within 1 minute;
• patients with impaired renal / hepatic function: this category of patients is allowed to use Trakrium in standard doses for any degree of impairment of renal / hepatic function, including end stage failure.

Throughout the entire period of treatment with Trakrium, as in the case of the use of other muscle relaxants, it is necessary to monitor neuromuscular function in order to determine the dosage regimen in each individual case.

Side effects

The frequency of adverse reactions is classified by organ systems and is defined as follows: very often (≥ 1/10), often (≥ 1/100 and <1/10), sometimes (≥ 1/1000 and <1/100), rarely (≥ 1/10 000 and <1/1000), very rarely (<1/10 000), including individual messages, with an unknown frequency - in cases where there is insufficient data to determine the frequency of occurrence of an adverse reaction.

Adverse reactions associated with the release of histamine, data on which were obtained in clinical trials:

• cardiovascular system: often - skin hyperemia, transient decrease in blood pressure (BP);
• respiratory system: sometimes - bronchospasm.

Adverse reactions, data on which were obtained during post-registration observation:

• nervous system: with an unknown frequency - seizures (there are reports of seizures in patients in intensive care and taking atracuria besylate concurrently with certain other drugs. As a rule, these patients had one or more conditions that predispose to seizures (edema of the head brain injury, head trauma, hypoxic encephalopathy, viral encephalitis, uremia) A causal relationship between the occurrence of seizures and laudanosine (the main metabolite of atracurium besylate) has not been established. According to the results of clinical studies, the correlation between plasma concentrations of laudanosine and the occurrence of seizures was not noted;
• immune system: very rarely - anaphylactoid and anaphylactic reactions, including shock, circulatory failure and cardiac arrest (with the combined use of Trakrium with anesthetics, in very rare cases, the development of severe anaphylactoid or anaphylactic reactions was reported);
• musculoskeletal system and connective tissue: with unknown frequency - muscle weakness, myopathy (there are reports of muscle weakness and / or myopathy with prolonged use of muscle relaxants in critically ill patients in intensive care. Most of them simultaneously received glucocorticosteroids (GCS) This adverse reaction is not typical for atracurium besylate, its connection with the use of Trakrium has not been established;
• skin and subcutaneous tissue: rarely - urticaria.

Overdose

Symptoms: prolonged muscle paralysis, including the consequences of this condition.

Therapy: maintaining the patency of the airways with simultaneous artificial ventilation of the lungs under positive pressure until adequate spontaneous breathing is restored (in this case, it is necessary to use sedative drugs, since the patient's consciousness is not disturbed). If signs of spontaneous recovery appear, it is accelerated with the help of anticholinesterase drugs, combining their intake with glycopyrrolate or atropine.

special instructions

Trakrium, similar to other muscle relaxants, causes paralysis of skeletal muscles, including respiratory, but does not affect consciousness. It should be administered only under general anesthesia, subject to close supervision by a qualified anesthesiologist and equipment for tracheal intubation and mechanical ventilation.

In patients with hypersensitivity to other muscle relaxants, the administration of Tracrium should be carried out with caution, since a high frequency of cross-sensitivity between muscle relaxants has been revealed (over 50%).

The use of Trakrium in patients with a predisposition can provoke the appearance of reactions associated with the release of histamine. If the patient has a history of hypersensitivity to the effects of histamine, the drug should be administered with caution. In particular, patients with a history of allergies or bronchial asthma may experience bronchospasm.

Patients with bronchial asthma receiving high doses of corticosteroids and muscle relaxants in the BIT should consider the possibility of multiple monitoring of the CPK (creatine phosphokinase) content.

During therapy with Trakrium, as in the case of the use of other non-depolarizing muscle relaxants:

• hypophosphatemia can slow down recovery (it can be accelerated by correcting this condition);
• disturbances in the balance of serum electrolytes and / or severe disturbances in acid-base balance may decrease or, conversely, increase the sensitivity of patients to the drug;
• hypersensitivity to the drug may occur in patients with severe myasthenia gravis, other neuromuscular diseases and severe electrolyte imbalance;
• the development of resistance can be observed in patients with burns (it may be necessary to increase the dose of Trakrium, the value of which depends on the surface area of the burn and on the time elapsed after the burn).

The use of Trakrium in the recommended dose range does not cause significant blockade of the nerve ganglia and the vagus nerve. Consequently, it does not have a clinically significant effect on the heart rate and does not prevent bradycardia caused by many anesthetics or stimulation of the vagus nerve during surgery.

Patients who have a tendency to a sharp decrease in blood pressure (for example, patients with hypovolemia) are advised to administer the drug for more than 1 minute.

Trakrium loses its activity in an alkaline environment, therefore, it is prohibited to mix the drug in the same syringe with thiopental or any alkaline solutions.

The solution of the drug is hypotonic, for this reason, it is prohibited to enter it through the same system simultaneously with blood transfusion.

After the injection of Trakrium into a small-caliber vein, it is washed with saline. When administering other anesthetics through the same injection needle or cannula, it is important to flush each drug with the appropriate amount of saline.

In the course of clinical studies in which patients sensitive to malignant hyperthermia took part, as well as studies of this disease in predisposed animals, namely pigs, it was proved that Trakrium does not cause this syndrome.

When laudanosine was administered to laboratory animals in large doses, a transient decrease in blood pressure was noted, and in some animal species, with cerebral stimulating effects. In patients in the intensive care unit who received Trakrium, the appearance of seizures was noted, but the causal relationship of their development with the use of laudanosine has not been established.

Application during pregnancy and lactation

The effect of the drug on fertility has not been studied.

Studies carried out on animals have shown that the use of Trakrium does not affect the development of the fetus. However, as is the case with other muscle relaxants, it is recommended to use it during gestation only in cases where the potential benefit to the mother is higher than any possible risk to the fetus.

For the purpose of muscle relaxation, the solution is approved for use during cesarean section operations, since atracuria besylate, used in recommended doses, penetrates the placental barrier in quantities that have no clinical significance.

There are no data on the excretion of atracurium besilate in breast milk.

Pediatric use

• children aged 1 month to 2 years: the initial dose of Trakrium with halothane anesthesia is 0.3–0.4 mg / kg;
• children aged 2 years and older: the drug is prescribed in doses similar to those for adult patients, based on the child's body weight.

Children require more frequent maintenance doses than adults.

With impaired renal function

In standard doses, Trakrium is approved for use for any degree of impairment of renal function, including end-stage failure.

For violations of liver function

In standard doses, Trakrium is approved for use for any degree of impairment of hepatic function, including end-stage failure.

Use in the elderly

In standard doses, Trakrium is approved for use in elderly patients.

Elderly patients should be administered slowly and given an initial dose that is less than the lower value of the recommended dose range.

Drug interactions

The neuromuscular blockade caused by the administration of Tracrium can be enhanced by the use of drugs for inhalation anesthesia, such as enflurane, halothane, isoflurane.

When taking beta-blockers (oxprenolol, propranolol), various antibiotics, antirheumatic (D-penicillamine, chloroquine) and antiarrhythmic (quinidine, procainamide) drugs, chlorpromazine, trimetaphan, steroids, lithium and phenytoin salts, exacerbation of myasthenia gravis, in rare cases, may occur develop myasthenia gravis from a latent form or myasthenic syndrome, in which an increase in sensitivity to atracuria besilate is possible.

The simultaneous administration of the drug with non-depolarizing blockers of neuromuscular conduction can lead to excessive blockade in comparison with that expected from the introduction of one Trakrium in an equipotential total dose. Any synergistic effect may change with different drug combinations.

Anticholinesterase drugs, which are often used to treat patients with Alzheimer's disease (for example, donepezil), when taken together with atracuria besylate, can weaken its blocking effect and shorten the duration of neuromuscular blockade.

When interacting with antibiotics (aminoglycosides, polymyxins, tetracyclines, lincomycin, spectinomycin, clindamycin), diuretics (furosemide and, possibly, mannitol, acetazolamide, thiazide diuretics), antiarrhythmics (calcium channel blockers, propranamidinetamine, procainamidinomine), magnesium sulfate, lithium salts, ganglion blockers (hexamethonium, trimetaphan), as in the case of the use of other non-depolarizing muscle relaxants, an increase in the duration and / or intensity of neuromuscular blockade is possible.

In patients who receive anticonvulsant therapy for a long time, the development of neuromuscular blockade caused by non-depolarizing muscle relaxants is likely to slow down, and its duration is reduced.

In order to prolong the neuromuscular blockade caused by the use of Trakrium, it is not recommended to use the depolarizing muscle relaxant suxamethonium chloride, as this can cause a prolonged and complex blockade, which is difficult to stop with anticholinesterase agents.

The following infusion solutions are compatible with Trakrium for the time indicated:

• sodium chloride solution for infusion 0.9% - 1 day;
• Ringer solution for injections - ¹ / ₃ days;
• glucose solution infusion of 5% - ¹ / ₃ days;
• sodium chloride solution, 0.18% glucose and 4% for infusion - ¹ / ₃ days;
• sodium lactate solution complex for infusion (Hartman injection) - ¹ / ₆ days.

For a specified period, diluted with compatible infusion solutions to obtain a concentration of atracurium besylate of 0.5 mg / ml or more, the Trakrium solution remains stable under daylight and a temperature not exceeding 30 ° C.

Analogs

The analogues of Trakrium are Atracurium-Medargo, Atracuria besilat, Ridelat-S, Atracurium-Novo, Notrixum, etc.

Terms and conditions of storage

Store out of the reach of children, protected from light, at a temperature of 2 to 8 ° C (do not freeze).

The shelf life is 24 months.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Trakrium

Due to the specifics of the use of the drug, there are no reviews about Trakrium on the network.

Price for Trakrium in pharmacies

The price of Trakrium for a package of 5 ampoules of 2.5 ml is from 498 to 690 rubles, for 5 ml - from 969 to 1080 rubles.

Trakrium: prices in online pharmacies

Drug name Price Pharmacy

Trakrium 10 mg / ml solution for intravenous administration 5 ml 5 pcs. 1055 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!