Tracrium, 10 mg/ml, solution for intravenous administration, 2.5 ml, 5 pcs.

Tracrium, 10 mg/ml, solution for intravenous administration, 2.5 ml, 5 pcs.

IV.

Adults and children over 1 month.

Bolus administration

Recommended doses for adults are 0.3–0.6 mg/kg (depending on the required duration of neuromuscular blockade), which provides adequate myoplegia within 15–35 minutes.

Tracheal intubation can be performed within 90 s after intravenous administration of Trakrium at a dose of 0.5–0.6 mg/kg.

The duration of complete neuromuscular blockade can be increased by introducing additional doses at the rate of 0.1–0.2 mg/kg, which is not accompanied by cumulation of the effect of the drug. Spontaneous restoration of conduction after complete neuromuscular blockade is observed after approximately 35 minutes (determined by the restoration of tetanic contraction to 95% of the original). Neuromuscular conduction can be quickly restored with the administration of anticholinesterase drugs (neostigmine, etc.) in combination with atropine without the appearance of signs of recurarization.

Infusion administration

After an initial bolus of 0.3–0.6 mg/kg Tracrium can be administered by continuous infusion at a rate of 0.3–0.6 mg/kg/hour to maintain neuromuscular blockade during prolonged surgical procedures. This method of administration can be recommended for operations on the heart and lungs.

With artificial hypothermia, accompanied by a decrease in body temperature to 25–26 °C, the rate of inactivation of atracurium decreases, therefore, to maintain complete myoplegia, the infusion rate should be reduced by approximately 2 times.

Elderly patients

Tracrium is prescribed in standard doses, but it is preferable to use the lower end of the recommended dosage range and administer the drug slowly.

If liver and/or kidney function is impaired,

incl. for end-stage liver or kidney failure, Tracrium is prescribed in standard doses.

Use for diseases of the cardiovascular system.

In patients with severe cardiovascular pathology, the initial dose should be administered over at least 60 seconds.

Use in intensive care units.

To maintain myoplegia after an initial bolus dose of 0.3–0.6 mg/kg, Tracrium can be administered by continuous infusion at a rate of 11–13 mcg/kg/min (0.65–0.78 mg/kg/h). The dose is not the same for different patients and may change over time. Some patients may require doses as low as 4.5 mcg/kg/min (0.27 mg/kg/hour) and doses as high as 29.5 mcg/kg/min (1.77 mg/kg /h). Spontaneous recovery of neuromuscular conduction (T4/T1>0.75) usually occurs approximately 60 minutes (in clinical trials, this period ranged from 32 to 108 minutes) after Tracrium infusion and its rate does not depend on the duration of drug administration.

Instructions for use

Tracrium is compatible with the following infusion solutions.

Tracrium solution, when diluted with compatible infusion solutions to obtain an atracurium besylate concentration of at least 0.5 mg/ml, remains stable for a specified period of time under normal lighting and temperatures up to 30 °C.

Pharmacological properties of the drug Tracrium

A peripherally acting muscle relaxant of the non-depolarizing competitive type. Blocks H-cholinergic receptors in the terminal plates of skeletal muscle fibers and prevents the depolarizing effect of acetylcholine, resulting in inhibition of neuromuscular transmission at the level of the postsynaptic membrane. After intravenous administration, it is spontaneously metabolized by Hoffman elimination (a non-enzymatic process that occurs at physiological values ​​of blood pH and body temperature of the patient), as well as by ether hydrolysis with the participation of nonspecific esterases in blood plasma. This leads to the formation of laudanosine and other metabolites. Metabolites do not have muscle relaxant properties. The binding of atracurium besylate to plasma proteins is about 80%, the half-life is 20 minutes. Excreted in urine and bile, mainly in the form of metabolites.

Special instructions for the use of the drug Tracrium

Like all other neuromuscular blockers, atracurium besilate causes paralysis of the respiratory muscles in the same way as other skeletal muscles, without affecting consciousness. Therefore, the use of the drug is possible only against the background of adequate general anesthesia under the supervision of an experienced anesthesiologist and in the presence of equipment for endotracheal intubation and mechanical ventilation. In sensitive patients, there is a potential for histamine release during the use of atracurium besylate, so caution should be exercised when administering it to patients with allergic diseases and hypersensitivity to histamine. Because there are reports of cross-sensitivity between various neuromuscular blocking agents, atracurium besylate should be administered with caution to patients with hypersensitivity to other drugs in this group. When used in recommended doses, Tracrium does not have a significant vagal or ganglion-blocking effect and is not contraindicated in bradycardia associated with the use of many anesthetics or vagal stimulation during surgery. As with other non-depolarizing muscle relaxants, patients with myasthenia gravis, neuromuscular diseases and severe electrolyte disturbances may experience increased sensitivity to Tracrium. In patients at risk of a significant decrease in blood pressure, for example with hypovolemia, Tracrium should be administered over 60 s. Atracurium besylate is inactivated at a high pH value of the solution, so it cannot be mixed in the same syringe with sodium thiopental or any other alkaline solution. After introducing Tracrium into a peripheral vein or when introducing other drugs into the same needle or cannula, the infusion system should be flushed with an adequate amount of isotonic sodium chloride solution. Tracrium is a hypotonic solution and cannot be used in the same infusion system with blood products or during blood transfusion. In patients sensitive to malignant hyperthermia, it was found that the drug does not contribute to the appearance of this hyperthermia syndrome. As with the use of other non-depolarizing muscle relaxants, patients with burns may develop resistance to Tracrium, which may require increasing its dose depending on the period that has passed since the burn and the area of ​​the burn surface. The results of experimental and clinical studies conducted on animals indicate that when atracurium besylate is used in high doses, its metabolite laudanasine can cause arterial hypotension, and sometimes the effect of cerebral excitation. A reliable reason for the relationship between the seizures observed in patients receiving Tracrium and the action of the laudanasine metabolite has not been established. During pregnancy and breastfeeding. During pregnancy, Tracrium should be used with caution and only if the expected benefit to the mother outweighs the potential risk to the fetus. In obstetric practice, Tracrium can be used as a muscle relaxant during cesarean section, since when used in recommended doses it does not cross the placenta in a clinically significant concentration. It is not known whether atracurium besylate and its metabolites are excreted in breast milk. Ability to drive vehicles and operate other machinery . No data.

Side effects of the drug Tracrium

The following side effects are classified by organ, system and frequency of occurrence. Classification of the frequency of side effects: very often (1/10); often (1/10, but ≤1/100); uncommon (1/100, but ≤1/1000); rare (1/1000, but ≤1/10,000); very rare (≤1/10,000). The definition of “ unknown ” refers to those side effects when it is impossible to determine the frequency of their occurrence from available sources. Data obtained from clinical studies Vascular disorders Often: skin hyperemia*, arterial hypotension (moderate, transient)*. Respiratory and thoracic disorders Uncommon : bronchospasm *. *These symptoms may be due to an increase in histamine release. Data obtained from post-licensing use Immune system Very rare: anaphylactic, anaphylactoid reactions. When Tracrium is used in combination with other anesthetic drugs, there are isolated reports of severe anaphylactoid or anaphylactic reactions. CNS Convulsions (frequency unknown ). There are isolated reports of the occurrence of seizures in patients undergoing intensive treatment when using Trakrium in combination with other drugs. These patients, as a rule, had one or more factors causing convulsive syndrome (head injury, cerebral edema, viral encephalitis, hypoxic encephalopathy, uremia). A causal relationship with the action of laudanosine has not been established. According to clinical studies, a correlation between the level of laudanosine in the blood plasma and the occurrence of seizures has not been established. Musculoskeletal system and connective tissue Myopathy, muscle weakness (the frequency of their occurrence is unknown ). With long-term use of muscle relaxants in critically ill patients in intensive care units, cases of muscle weakness and/or myopathy have been reported. The majority of these patients received concomitant treatment with corticosteroids. Such reports were infrequent, and a causal relationship with the use of Tracrium has not been established.

Interactions of the drug Tracrium

The neuromuscular blockade caused by Tracrium can be enhanced by the use of inhaled anesthetics such as halothane, isoflurane, and enflurane. When Tracrium is administered, the intensity of neuromuscular blockade and/or its duration may increase when used in combination with:

• antibiotics, including aminoglycosides, polymyxins, spectinomycins, tetracyclines, lincomycin and clindamycin;
• antiarrhythmic drugs: propranolol, calcium channel blockers, lidocaine, procainamide, quinidine;
• diuretics: furosemide, possibly with mannitol, thiazide diuretics, acetazolamine;
• magnesium sulfate;
• ketamine;
• lithium salts;
• ganglion blockers (trimethorphan, hexamethonium).

Rarely, when administered simultaneously with certain drugs that increase the manifestations of myasthenia gravis (including during its latent course) and provoke the development of myasthenic syndrome, increased sensitivity to atracurium besilate is possible. These drugs include various antibiotics, β-adrenergic blockers (propranolol, oxprenolol), antiarrhythmics (procainamide, quinidine), antirheumatic drugs (chloroquine, D-penicillamine), trimetaphan, chlorpromazine, steroids, phenytoin and lithium. In patients receiving long-term anticonvulsants, a later onset and shorter duration of neuromuscular blockade caused by Trakrium are possible. Administration of non-depolarizing neuromuscular blocking agents in combination with atracurium besylate may cause greater neuromuscular blockade than would be expected with an equivalent total dose of atracurium besylate. The synergistic effect may vary depending on the combination of drugs. Depolarizing muscle relaxants should not be administered to increase the duration of neuromuscular blockade caused by non-depolarizing muscle relaxants, as this may lead to the development of prolonged and deep relaxation, which is difficult to eliminate with anticholinesterase drugs.

Tracrium drug overdose, symptoms and treatment

Symptoms : prolonged paralysis of skeletal muscles and its consequences are the main signs of overdose. Treatment : maintain unobstructed air access along with positive pressure ventilation until spontaneous breathing is restored. At this time, it is necessary to ensure complete sedation of the patient. When the first signs of spontaneous respiratory recovery appear, it can be accelerated by the administration of anticholinesterase drugs in combination with atropine.