Esmeron - instructions for use, dose, side effects, contraindications

Active substanceRokuronium bromideRokuronium bromide

Similar drugsTo uncover

Croaron

solution in / in

LENS-PHARM, LLC Russia

Roqueronius Kabi

solution in / in

Fresenius Kabi Deutschland GmbH Germany

Roelax

solution in / in

KE G Laboratories (Yu Kay) Limited United Kingdom

Esmeron®

solution in / in

Organon, N.V. Netherlands

Dosage form: & nbspsolution for intravenous administration

Composition:

Active substance: rocuronium bromide 10 mg / ml.

Excipients: sodium acetate, sodium chloride, acetic acid, ice, water for injection.

Description:Transparent solution from colorless to light brown in color.

Pharmacotherapeutic group:Nondepolarizing muscle relaxant of peripheral action.

ATX: & nbsp

M.03.A.C Other quaternary ammonium compounds

M.03.A.C.09 Rokuronium bromide

Pharmacodynamics:

Mechanism of action

Esmeron® (rocuronium bromide) is a high-speed, nondepolarizing muscle relaxant of medium duration, with all the pharmacological effects (curare-like) characteristic of this class of drugs. It blocks n-cholinergic receptors of skeletal muscle and prevents the depolarizing effect of acetylcholine. Antagonists of this action are acetylcholinesterase inhibitors such as neostigmine methylsulfonate, edrophonium chloride and pyridostigmine bromide.

Pharmacodynamic effects

ED90 (the dose necessary to inhibit the contractile response of the thumb muscle in response to stimulation of the ulnar nerve by 90%) with intravenous general anesthesia is about 0.3 mg / kg rocuronium bromide. ED95 Infants are lower than in adults and children (0.25, 0.35 and 0.40 mg / kg, respectively).

Clinical duration of action (time to spontaneous recovery of contractile ability of skeletal muscles to 25% of the control level) at a dose of 0.6 mg / kg of rocuronium bromide is 30-40 minutes. The total duration (time to spontaneous recovery of the contractile ability of skeletal muscles to 90% of the reference level) is 50 minutes. The average time of spontaneous recovery of the contractility of skeletal muscles from 25% to 75% of the reference level (recovery index) after a bolus dose of 0.6 mg / kg of rocuronium bromide is 14 minutes. At lower doses, 0.3-0.45 mg / kg of rocuronium bromide (1-1_1/2 x ED90) The beginning of the action comes later and the duration of the action is shorter. At high doses of 2 mg / kg rocuronium bromide, the clinical duration is 110 minutes.

Intubation of the trachea during routine anesthesia

During 60 seconds after intravenous administration 0,6 mg / kg rocuronium bromide (2 x ED90 with intravenous general anesthesia), practically all patients have adequate conditions for intubation, and in 80% of them, the conditions for intubation are regarded as excellent. General relaxation of skeletal muscles, adequate for any surgical interventions, develops within 2 minutes. After administration of 0.45 mg / kg rocuronium bromide, acceptable conditions for intubation are created after 90 seconds.

Fast sequential induction of anesthesia

With rapid sequential induction of anesthesia with propofol or fentanyl / thiopental sodium, adequate conditions for intubation are achieved after 60 seconds in 93% and 96% of patients, respectively, after administration of 1.0 mg / kg of rocuronium bromide. Of these, in 70% of patients they are assessed as excellent. The clinical duration of action of rocuronium bromide at this dose is about 1 hour, after which the neuromuscular conduction can be restored. After administering a dose of 0.6 mg / kg rocuronium bromide, adequate conditions for intubation are achieved after 60 seconds in 81% and 75% of patients with rapid sequential induction of anesthesia with propofol or fentanyl / thiopental sodium, respectively.

Special patient groups

The average time of onset of action in infants and children with an intubation dose of 0.6 mg / kg rocuronium bromide is slightly shorter than in adults. The duration of action and the recovery time of neuromuscular conduction may be shorter in children than in infants and adults.

The duration of action of maintenance doses (0.15 mg / kg) of rocuronium bromide may be somewhat greater in patients of senile age and in patients with liver and / or kidney disease (approximately 20 minutes) with enflurane and isoflurane anesthesia than in patients without functional impairment excretory organs with intravenous anesthesia (approximately 13 minutes). With repeated introduction of supporting doses at the recommended level, the cumulative effect (progressive increase in the duration of action) was not observed.

Intensive Care Unit

After continuous infusion of rocuronium bromide in the intensive care unit, the recovery time train-of-the four (TOF) - Relations (the ratio of the values of the fourth and the first muscle responses to a four-digit (TOF) stimulation) to 0.7 depends on the level of blockade at the end of the infusion.After a continuous infusion for 20 hours or more, the average time (range) between the reappearance of T₂ (the second muscle response) in response to TOF stimulation and recovery TOFratio up to 0.7 is approximately 1.5 (1-5) hours in patients without multiple organ failure and 4 (1-25) hours in patients with multiple organ failure.

Cardiovascular Surgery

In patients who are scheduled to undergo heart surgery, the most frequent cardiovascular effects observed during the development of the maximal block after the administration of 0.6-0.9 mg / kg of the Esmeron® drug are a mild and clinically not pronounced increase in frequency cardiac contractions - up to 9% and an increase in mean arterial pressure - up to 16% of the control levels.

Restoration of neuromuscular conduction

The introduction of inhibitors of acetylcholinesterase (neostigmine, pyridostigmine or eudrophonia) with the reappearance of T₂ or at the first signs of clinical recovery leads to a recovery of neuromuscular conduction after the block caused by the action of the drug Esmeron®.

Pharmacokinetics:After intravenous administration of a single bolus dose of rocuronium bromide, the change in its concentration in the blood plasma passes through three exponential phases. In healthy adults, the mean half-life (95% confidence interval) is 73 (66-80) minutes, (apparent) volume of distribution under equilibrium conditions is 203 (193-214) ml / kg. The plasma clearance is 3.7 (3.5-3.9) ml / kg / min. In controlled studies it was shown that plasma clearance in patients of senile age and in patients with impaired renal function is slowed down, but in most studies the observed differences did not reach statistical significance. Half-life in patients with liver disease increases on average by 30 minutes, the clearance decreases by 1 ml / kg / min.

In infants (from 3 months to 1 year), the apparent volume of distribution under equilibrium conditions is increased in comparison with adults and children (1-8 years). In children 3-8 years, there is a tendency to increase in clearance and shortening of the half-life (approximately 20 minutes) compared with adults, children (1-3 years) and infants. When rocuronium bromide is introduced as a continuous infusion to facilitate artificial ventilation for 20 hours or more,the average half-life and the average (apparent) volume of distribution in the equilibrium state of rocuronium bromide increase. In controlled clinical trials, a pronounced interindividual variability of indices was established, associated with different genesis and severity (poly) organ failure and individual characteristics of the patient. In patients with multiple organ dysfunction, the mean (± SD) half-life was 21.5 (± 3.3) hours, the (apparent) volume of distribution in the equilibrium state was 1.5 (± 0.8) l / kg and the plasma clearance was 2 , 1 (± 0.8) ml / kg / min.

Rokuronium bromide is excreted in the urine and bile. Urinary excretion reaches 40% within 12-24 hours. After the injection of radiolabeled radicuronium bromide, its excretion averaged 47% with urine and 43% with feces for 9 days. Approximately 50% of the drug is excreted unchanged.

Indications:

Esmeron® is indicated for:

- facilitating intubation of the trachea during planned surgical interventions and rapid sequential induction of anesthesia and to ensure the relaxation of skeletal muscles during surgical interventions of a different nature in adults;

- facilitating intubation of the trachea during planned surgical interventions and to ensure the relaxation of skeletal muscles during surgical interventions of various types in children from 1 month;

- facilitating intubation of the trachea during artificial ventilation in intensive care units in adults (except children and elderly patients).

Contraindications:

Hypersensitivity to rocuronium or to bromide ion or to any auxiliary substance;

Children up to 1 month of age (due to insufficient data);

Pregnancy, with the exception of caesarean section (due to insufficient data);

Lactation period (due to insufficient data).

Carefully:Hepatic and / or renal failure, cardiovascular diseases, accompanied by severe circulatory insufficiency (heart diseases, pulmonary hypertension), neuromuscular system diseases (including myasthenia gravis), obesity, acid-base balance, burns, cachexia, old age, miorelaxation with caesarean section. When conducting a caesarean section, the recommended dose of rocuronium bromide is 0.6 mg / kg body weight, since the use of higher doses (1.0 mg / kg body weight) has not been investigated.

Pregnancy and lactation:

Pregnancy

With respect to rocuronium bromide there are no clinical data on the effect of the drug during pregnancy (with the exception of caesarean section). The use of Esmeron in pregnant women due to the inadequacy of these clinical trials is not recommended (with the exception of caesarean section).

Cesarean section

When conducting a caesarean section, Esmeron® can be used as part of the rapid sequential induction of anesthesia, unless difficulties are expected with intubation of the trachea and a sufficient dose of anesthetic is administered, or after intubation with suksamethonium. It was shown that the use of Esmeron ® at a dose of 0.6 mg / kg is safe in women undergoing cesarean section. The preparation of Esmeron® does not affect the Apgar score, the muscle tone of the fetus, or its cardiorespiratory adaptation. Analyzes of blood samples from the umbilical cord indicate that only very small amounts of rocuronium bromide penetrate the placental barrier, which does not lead to clinically significant undesirable effects in the newborn.

Note 1: doses of 1.0 mg / kg have been investigated in the rapid sequential induction of anesthesia, but not in patients undergoing cesarean delivery. Therefore, in this group of patients only a dose of 0.6 kg / kg is recommended. Note 2: Restoration of neuromuscular conduction after the administration of muscle relaxants may be delayed or incomplete in patients receiving magnesium salts for the treatment of pregnancy toxicosis, as magnesium salts strengthen the neuromuscular block. Therefore, in such patients, doses of Esmeron® should be reduced and titrated, depending on the muscle response.

Lactation

At present, it remains unknown whether Esmeron® is excreted in a person with breast milk. The appointment of Esmeron® during lactation due to the inadequacy of these clinical trials is not recommended.

Dosing and Administration:

Esmeron® is administered intravenously both as a bolus injection and as a continuous infusion (see "Compatibility when mixed with other medicinal products").

As with other muscle relaxants, Esmeron® should be administered only by experienced clinicians who are familiar with the action of muscle relaxants, or under their supervision.

The dose of Esmeron®, as in the case of the use of other muscle relaxants, must be selected individually for each patient. When choosing a dose, one should take into account the method of anesthesia and the estimated duration of the operation, the method of sedation and the expected duration of mechanical ventilation, possible interaction with other, jointly prescribed, drugs, as well as the general condition of the patient.

To assess the degree of neuromuscular block and restore neuromuscular conduction it is recommended to use the appropriate methods of neuromuscular monitoring.

Inhalational anesthetics increase the neuromuscular block caused by the Esmeron® preparation. This enhancement, however, becomes clinically significant only when, during general anesthesia, the concentration of volatile substances in the tissues reaches a level sufficient for such interaction. Therefore, the dosage of Esmeron® should be adjusted by administering lower maintenance doses at longer intervals or using lower rates of Esmeron® infusion during long (more than 1 hour) procedures,conducted with the use of inhalation anesthesia (see "Interaction with other drugs and other forms of interaction").

In adult patients, the following doses may be recommended as the general scheme for endotracheal intubation and for providing muscle relaxation in operations of varying duration and for use in the intensive care unit.

In surgical interventions

Endotracheal intubation

The standard dose of rocuronium bromide for endotracheal intubation during normal anesthesia is 0.6 mg / kg, after which adequate conditions for intubation of the trachea develop in about 60 seconds in most patients. In the rapid sequential induction of anesthesia to facilitate intubation of the trachea, the recommended dose is 1.0 mg / kg rocuronium bromide. In this case, adequate conditions for intubation of the trachea develop in 60 seconds in almost all patients. When a dose of 0.6 mg / kg of rocuronium bromide is used to perform a rapid sequential induction of anesthesia, it is recommended that the trachea of the patient be intubated 90 seconds after the administration of the drug.

Information regarding the use of rocuronium bromide during rapid sequential induction of anesthesia in patients undergoing Cesarean section is indicated in the section on "Application in pregnancy and lactation".

High doses

The choice of a higher dose should be justified in each individual patient. It was noted that the administration of initial doses up to 2 mg / kg of rocuronium bromide during surgical operations proceeded without side effects from the cardiovascular system. The use of these doses of rocuronium bromide shortens the time of its onset and increases the duration of action (see the section "Pharmacodynamics").

Maintenance doses

The recommended maintenance dose is 0.15 mg / kg rocuronium bromide; in the case of prolonged inhalation anesthesia, it should be reduced to 0.075-0.1 mg / kg. Supportive doses are best administered at the time when the amplitude of muscle contractions is restored to 25% of the control level or when there are 2-3 responses when monitoring in the four-digit stimulation mode (TOF).

Continuous infusion

If rocuronium bromide is administered by continuous infusion,it is recommended to start with a loading dose of 0.6 mg / kg rocuronium bromide, and when the neuromuscular conduction begins to recover, begin infusion. The rate of infusion should be selected in such a way that the contractile response of skeletal muscles is at the level of 10% of the control level or maintenance of 1-2 responses when monitoring in the four-digit stimulation mode (TOF). In adults with intravenous general anesthesia, the infusion rate required to maintain the neuromuscular block at this level is 0.3-0.6 mg / kg / h, and with inhalational anesthesia 0.3-0.4 mg / kg / h. It is recommended to carry out continuous monitoring of neuromuscular conduction, since the necessary infusion rate can vary depending on the individual patient's characteristics and on the various methods of anesthesia.

Children

For children from 1 month, the recommended dose for intubation with conventional anesthesia (0.6 mg / kg rocuronium bromide) and maintenance dose (0.15 mg / kg rocuronium bromide) are the same as for adults.

With continuous infusion in pediatrics, the infusion rate is the same as for adults (0.3-0.6 mg / kg / h), except for children (2-11 years old) who may require higher infusion rates.The initial infusion rate for children is recommended the same as for adults (0.3-0.6 mg / kg / h). Already during the procedure, the speed should be adjusted in order to maintain the amplitude of muscle contractions at the level of 10% of the reference amplitude or the presence of 1-2 responses when monitoring in the four-digit stimulation mode(TOF).

At the moment, there is insufficient data on the use of rocuronium bromide in neonates (0-1 months).

The experience with rocuronium bromide during the rapid sequential induction of anesthesia in children is limited. therefore rocuronium bromide It is not recommended to facilitate intubation of the trachea during the rapid sequential induction of anesthesia in children.

Elderly patients and patients with liver and / or biliary tract disease and / or renal insufficiency

The standard intubation dose for elderly patients and patients with liver and / or bile duct disease and / or with renal failure with conventional anesthesia is 0.6 mg / kg rocuronium bromide. In the procedure of fast sequential induction in patients withit is recommended that a dose of 0.6 mg / kg of rocuronium bromide be used in the proposed prolonged duration of the muscle relaxant.

Regardless of the technique of administration, the recommended maintenance dose for these patients is 0.075-0.1 mg / kg rocuronium bromide, the recommended infusion rate is 0.3-0.4 mg / kg / h (See also "Continuous infusion").

Patients with overweight and obesity

When using the drug in patients with excessive body weight or obesity (such are considered patients whose body mass index value is more than 30), the dose of rocuronium bromide should be reduced, based on the normal for a given age and sex indices of the body mass index.

Use in the intensive care unit

Intubation of the trachea

Doses are similar to those for surgical interventions. Maintenance doses

It is recommended to start with a dose of 0.6 mg / kg of rocuronium bromide, followed by a transfer to continuous infusion of the drug while restoring neuromuscular conduction to 10% of the baseline level or receiving 1-2 responses with stimulation in the regimen TOF. Dosages of rocuronium bromide should be selected individually depending on the effect.The recommended initial infusion rate to maintain the neuromuscular block at 80-90% (1-2 responses with stimulation in the mode TOF) in adult patients is 0.3-0.6 mg / kg^;h during the first hour of administration, after which, during 6-12 hours, it is necessary to reduce the infusion rate, in accordance with the individual reaction of the patient. After that, individual needs for a certain dose of the drug remain relatively constant.

In controlled clinical trials, a significant interindividual variability was detected with respect to the hourly infusion rate, with an average value of 0.2-0.5 mg / kg / h, depending on the cause and extent of the organ failure (s), concomitant drug treatment and individual characteristics of the patient. To ensure optimal control over each patient, it is highly recommended to carry out continuous monitoring of neuromuscular conduction. The administration of the drug lasting up to 7 days was investigated.

Special patient groups

Esmeron® is not recommended for ease of artificial ventilation in the Intensive Care Unitchildren and elderly patients due to the lack of safety and efficacy data for these groups of patients.

Side effects:

The most common adverse reactions include pain at the injection site, changes in the basic indicators of the state of the body (tachycardia, hypotension) and an increase in the duration of the neuromuscular block. The most frequently reported serious adverse drug reactions at the post-marketing follow-up period are anaphylactic and anaphylactoid reactions and associated symptoms (see also the information in the table below).

System-	Frequency of occurrence^a
organ	Infrequently/	Rarely
grade	rarely^b	(<1/10 000)
MedDRA	(<1/100, >
	1/10 000)
Immune violations		Increased sensitivity Anaphylaxis the reaction Anaphylactoid reaction Anaphylaxis shock Anaphylactoid shock
Violations from nervous systems		Sluggish paralysis
Violations from cardiac active ti	Tachycardia
Vascular disorders	Arterial hypotension	Vascular collapse and shock Hyperemia dermal integument
Violations from systems bodies breathing		Bronchospasm
Disturbances from the skin and subcutaneous tissue		Angioedema swelling Hives Rash Erythematous rash
Disturbances from skeletal muscles and connective tissue		Muscle weakness^from Steroid myopathy^from
General disorders and reactions at the site of administration	Ineffectiveness of the drug Reduced drug effect / therapeutic response Increased drug effect / therapeutic response Pain at the injection site	Facial edema Malignant hyperthermia
Injuries, poisoning and procedural th complicated and I	Prolongiro the nervously- muscular bloc Slowdown restore of the neuro- muscular the ongoing after anesthesia	Breathing complications after anesthesia
Injuries, poisonings and procedural complications	Prolongation of the neuromuscular block Delay in conduction of neuromuscular conduction after anesthesia	Respiratory complications after anesthesia

MedDRA version 8.1
^a Frequency of occurrence		is estimated
on the basis of the data obtained in
period	post-registration
observation	for the drug and
literary data.
^b Observations of the drug in
postgistratsionny period is not
can determine the exact frequency
occurrence. For this reason
The reported frequency was divided into
two, not five categories
^from After long-term use in
intensive care unit. Anaphylaxis On the occurrence of severe anaphylactic reactions as a result of the use of muscle relaxants, including Esmeron®, reported very rarely. Anaphylactic / anaphylactoid reactions: bronchospasm, changes from the side cardiovascular system (for example, hypotension, tachycardia, vascular collapse - shock) and changes from the skin (eg, angioedema, urticaria). In some cases these reactions were fatal. Because of the possible severity of these reactions, it is always necessary to keep in mind the possibility of their occurrence and observe the appropriate precautions. Since it is known that muscle relaxants are able to cause the release of histamine as locally at the injection site, and systemically, then with the introduction of these drugs it is always necessary to take into account Possible occurrence of pruritus and erythematous reactions at the injection site and / or generalized histamine-like (anaphylactoid) reactions (see Fig.also the anaphylactic reactions described higher). In clinical studies, only a slight increase in the mean plasma concentration of histamine after rapid bolus administration of 0.3-0.9 mg / kg rocuronium bromide. Prolongation of the neuromuscular block The most common adverse reaction of nondepolarizing muscle relaxants as a class of drugs drugs is lengthening the period of their pharmacological action beyond the required period of time. The degree of severity of this reaction can vary from skeletal-muscle weakness to deep and prolonged paralysis of skeletal muscles, leading to respiratory failure or apnea. Myopathy Myopathy was noted after the use of various muscle relaxants in the intensive care unit in combination with glucocorticosteroids (see section "Special instructions"). Local reactions at the injection site During the rapid sequential induction of anesthesia, painful sensations were reported during injection, especially when the patient was still conscious, and also using propofol as a means to induce anesthesia.In clinical trials, injection pain was noted in 16% of patients undergoing rapid sequential induction of anesthesia with propofol and less than 0.5% of patients undergoing rapid sequential induction of anesthesia with fentanyl and thiopental sodium. Children and teens Meta-analysis of 11 clinical studies of rocuronium bromide (up to 1 mg / kg) with participation children and adolescents (n = 704) showed that a side effect was a tachycardia with a frequency of 1.4%.

Overdose:In the case of an overdose and the development of a prolonged neuromuscular block, the patient must continue to use artificial ventilation and sedation. When the spontaneous recovery of neuromuscular conduction begins, it is necessary to administer an appropriate dose of an acetylcholinesterase inhibitor (for example, neostigmine methylsulfonate, edrophonium chloride, pyridostigmine bromide). If administration of an acetylcholinesterase inhibitor does not remove the blocking effect of Esmeron®, ventilation should continue until self-respiration regains.Repeated administration of an acetylcholinesterase inhibitor can be dangerous.

Interaction:

It is shown that the medicines listed below influence the strength and / or duration of action of nondepolarizing muscle relaxants.

The effect of other drugs on Esmeron®

Enhance the effect

- - Halogenated volatile anesthetics increase the neuromuscular block caused by the Esmeron® preparation. This effect becomes noticeable only with the administration of maintenance doses (see "Method of administration and dose"). Restoration of neuromuscular conduction with inhibitors of acetylcholinesterase can be slowed down.

- - Prior administration of suxamethonium (see "Specific guidance");

- - Prolonged concomitant administration of glucocorticosteroids and Esmeron® in the intensive care unit can lead to an increase in the duration of the neuromuscular block or to myopathy (see "Special instructions" and "Side effect").

- - Preparations of other groups: antibiotics (aminoglycosides, lincosamides and polypeptide antibiotics, antibiotics of acylamino-penicillin series); diuretics, chiidine and its quinine isomer, magnesium salts, slow calcium channel blockers, lithium salts, local anesthetics (lidocaine intravenously, bupivacaine epidural) and acute administration of phenytoin or β-blockers. The recovery was noted after the postoperative administration: aminoglycoside, lincosamide, polypeptide and acylaminopenicillin antibiotics, quinidine, quinine and magnesium salts (see "Special instructions").

Decreased effect

- Previous long-term administration of phenytoin or carbamazepine;

- Inhibitors of proteases (gabexate, vernastatin).

Changing effect

The introduction of other non-depolarizing muscle relaxants in combination with the Esmeron® preparation may cause a weakening or strengthening of the neuromuscular block, depending on the order of administration and the muscle relaxant used.

Suxamethonium, which is administered after the Esmeron® preparation, may enhance or weaken

neuromuscular block caused by the preparation Esmeron®.

The effect of Esmeron® on other drugs

The combination of Esmeron with lidocaine may lead to a faster onset

action of lidocaine.

Pharmaceutical interaction

Incompatibility

It was found that the preparation Esmeron® is incompatible for administration in a single syringe with solutions containing the following drugs: amphotericin B, amoxicillin, azathioprine, cefazolin, cloxacillin, dexamethasone, diazepam, enoximone, erythromycin, famotidine, furosemide, hydrocortisone sodium succinate, insulin, metohexital, methylprednisolone, prednisolone sodium succinate, sodium thiopental, trimethoprim and vancomycin. Esmeron® is also incompatible with the preparation Intralipid (fat emulsions for parenteral administration).

Esmeron® should not be mixed with other medicines, except as indicated below.

Compatibility when mixed with other medicinal products

It was shown that, at nominal concentrations of 0.5 mg / ml and 2.0 mg / ml, Esmeron ® is compatible with 0.9% sodium chloride, 5% dextrose, 5% dextrose in 0.9% sodium chloride solution, sterile water for injections, Ringer's solution and Gemazzel (polygelin). The introduction should be started immediately after mixing and finished within 24 hours. Unused solutions should be poured out.

Special instructions:

Since the preparation Esmeron® does not contain a preservative, the solution should be used immediately after opening the vial.

After dilution with infusion liquids, the drug remains chemically and physically stable for 72 hours at a temperature of 30 ° C. From a microbiological point of view, a divorced the drug should be applied immediately. If the drug is not applied immediately, the patient / physician is responsible for the time and storage conditions prior to use, which usually should not exceed 24 hours at a temperature of 2 to 8 ° C. except for the case when dilution is carried out in controlled and validated aseptic conditions. If the Esmeron® drug is administered through a single infusion system with other medicinal products (0.9% solution of NaCl) between the administration of Esmeron® and preparations with incompatibility with it, and if compatibility is not established, it is necessary to thoroughly wash the system. Since the Esmeron® preparation causes paralysis of the respiratory muscles, it is absolutely necessary for patients receiving this preparation to perform artificial ventilation of the lungs until adequate self-breathing recovery is achieved. As with other muscle relaxants, it is important to foresee possible difficulties in intubation of the trachea, especially if the drug is used as part of rapid sequential induction of anesthesia. As with the use of other muscle relaxants, after the use of Esmeron®, cases of development of the residual block were noted.To prevent complications resulting from the development of the residual block, it is recommended to extubate the trachea only after neuromuscular conduction has recovered sufficiently. In elderly patients (65 years and older), the risk of developing residual neuromuscular block may be increased. Other factors that can cause the development of the residual block after extubation in the postoperative period (for example, drug interaction or the patient's condition) should also be considered. It is necessary to consider the possibility of introducing drugs that restore neuromuscular conduction (such as sugammadex or inhibitors of acetylcholinesterase), especially in those cases in which the emergence of a residual block is most likely. After the administration of muscle relaxants, anaphylactic reactions may develop, so always take the necessary precautions to treat such reactions. In particular, in the presence of anaphylactic reactions to muscle relaxants in a history, precautionary measures should be taken, since cases of cross-allergic reactivity to muscle relaxants are known.

After lasting the introduction of muscle relaxants to patients in the intensive care unit, there may be a development of a prolonged neuromuscular block and / or muscle weakness. To prevent the possible prolongation of the neuromuscular block and / or overdose, it is necessary that during the entire period of the use of muscle relaxants, monitoring neuromuscular conductivity, and that patients receive adequate analgesia and sedatives. Moreover, muscle relaxants should be administered in carefully selected doses in accordance with the patient's individual response, and the administration should be performed by an experienced physician who is familiar with the actions of muscle relaxants or under his supervision, as well as using appropriate neuromuscular monitoring techniques. After prolonged administration of nondepolarizing muscle relaxants in combination from therapy with glucocorticosteroids in the intensive care unit is possible the development of myopathy: therefore, patients receiving both muscle relaxants and glucocorticosperoids. the period of the muscle relaxant should be as limited as possible.If suksamethonium is used for intubation, the administration of Esmeron® should be postponed until the clinical recovery of neuromuscular conduction after the block caused by suxamethonium. The following factors may affect the pharmacokinetics and / or pharmacodynamic drugs of Esmeron®:

Diseases of the liver and / or bile duct and kidney failure

Since rocuropium bromide is excreted in the urine and bile, it should be used with caution in patients with clinically expressed liver disease and / or

biliary tract and / or renal failure. In these groups of patients, prolongation of the action of rocuronium bromide at doses of 0.6 mg / kg was observed.

Increasing the circulation time

Conditions associated with increased circulation of the drug in the blood, such as cardiovascular diseases, advanced age and swelling, leading to an increase in the volume of distribution, may contribute to the later onset of the drug. The duration of action can also be increased due to reduced plasma clearance.

Diseases of the neuromuscular system

Like other muscle relaxants, the drug Esmeron® should be used with extreme caution in patients with neuromuscular or poliomyelitis diseases, since the response to muscle relaxants can be significantly altered in these cases. The severity and direction of these changes can be different. In patients with severe myasthenia gravis or myasthenic syndrome (Eaton-Lambert syndrome), small doses of Esmeron® can cause a pronounced neuromuscular block, so the dose of Esmeron® should be selected according to the individual patient's response.

Hypothermia

In the conduct of surgical interventions against the background of hypothermia, the blocking effect of Esmeron® on the neuromuscular system is enhanced, and the duration of action is increased.

Obesity

Like other muscle relaxants, the Esmeron® preparation may be characterized by an increase in the duration and time of spontaneous recovery of neuromuscular conduction when used in obese patients (when the dose is calculated based on actual body weight).

Burns

In patients with burns, resistance to non-depolarizing muscle relaxants may develop.Follow the wire, the selection of the effective dose by titration.

Conditions that may enhance the effect of Esmeron®

Hypokalemia (for example, after severe vomiting, diarrhea, or diuretic treatment), hypermagnesia, hypocalcemia (after massive transfusions), hypoprogesinemia. dehydration, acidosis, hypercapia. cachexia. In this regard, severe disturbances in the balance of electrolytes, changes pi 1 blood or dehydration should, if possible, be adjusted.

Effect on the ability to drive transp. cf. and fur:As the preparation Esmeron® is used as an aid in general anesthesia; follow the usual precautions recommended after general anesthesia for outpatients. It is not recommended to manage potentially dangerous mechanisms or drive a car within 24 hours after the complete recovery of neuromuscular conduction caused by Esmeron®.

Form release / dosage:Solution for intravenous administration 10 mg / ml.

Packaging:Solution for intravenous administration of 10 mg / ml, 5 ml in bottles of colorless glass type 1 (EF), clogged with rubber stoppers type 1 (EF) and crimp caps.For 10 bottles of 5 ml in cardboard packs together with instructions for use.

Storage conditions:

List A.

At a temperature of 2-8 ° C.

Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:For hospitals

Registration number:П N012646 / 01

Date of registration:29.09.2011/15.01.2016

The owner of the registration certificate:Organon, N.V.Organon, N.V. Netherlands

Manufacturer: & nbsp

ORGANON, N.V. Netherlands

HAMELN PHARMACEUTICALS, GmbH Germany

Representation: & nbspMSD Pharmaceuticals Ltd.MSD Pharmaceuticals Ltd.

Information update date: & nbsp13.06.2016

Illustrated instructions

Instructions

Esmeron® (Esmeron®)