Active substanceSuxamethonium chlorideSuxamethonium chloride
Similar drugsTo uncover
  • Listenon®
    solution w / m in / in 
    Takeda Austria GmbH     Austria
  • Suxamethonium chloride
    solution w / m in / in 
    SYNTHESIS, OJSC     Russia
  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    5 ml of solution contains:

    Active substance: suxamethonium chloride dihydrate 110.0 mg (including an excess of 3%, the amount is 113.30 mg), equivalent to 100 mg of suxamethonium chloride.

    Excipients: sodium chloride 22.50 mg, leading for injection up to 5.0 ml.

    Description:A clear, colorless solution.
    Pharmacotherapeutic group:Muscle relaxant depolarizing the peripheral action
    ATX: & nbsp

    M.03.A.B   Derived choline

    Pharmacodynamics:

    Listenon® is a depolarizing muscle relaxant and causes reversible short-term paralysis of skeletal muscles by blocking the impulse conduction to the end postsynaptic plates of the motor nerves. As an analogue of acetylcholine, suxamethonium binds to n-cholinergic receptors; however, unlike acetylcholine, the result of its action is a longer depolarization (depolarizing unit, or phase I block of the action potential).As long as suxamethonium remains bound to the receptor, stimulation is not possible. Depolarization of the membrane becomes possible only after separation of the suxamethonium and the receptor. From non-depolarizing long-acting muscle relaxants, Listenon® is characterized by the rapid development of the effect (within 1 minute) and its short duration, from 2 to 6 minutes. This allows for high controllability of muscle relaxation in accordance with the requirements of surgery, and also to avoid unnecessary duration of its action.

    Relaxation of the muscles occurs in the following sequence: ocular muscle of the eye, chewing muscles, muscles of the limbs, abdominal wall, pharynx, diaphragm.

    Pharmacokinetics:

    Suction

    After intravenous administration, Listenon® has an effect in 30-60 seconds; the duration of the effect is approximately 2-6 minutes.

    With intramuscular injection, the action of the Listenon® drug begins in 75 seconds. The duration of the effect is 3 minutes in adults, 3.5 minutes in children and 4 minutes in newborns.

    Metabolism

    The short duration of action of the drug Listenon® is due to rapid inactivation of suxamethonium by cholinesterase plasma: most of the suxamethonium is inactivated immediately after administration,until the end plates of the motor nerves are reached. Suxamethonium hydrolyses with the formation of choline and succinyl monocholine (plasma half-life is less than 1 minute). Succinyl monocholine is a non-depolarizing muscle relaxant whose activity is 20-50 times lower than the original substance. Subsequently, the metabolic rate slows down, and succinyl monocholine decomposes into succinic acid (inactive metabolite) and choline (active metabolite).

    Excretion

    The rate of excretion is determined by the hydrolysis of suxamethonium by plasma cholinesterase. About 10% is excreted by the kidneys unchanged.

    Indications:Listenon ® is used only in conditions of general anesthesia for relaxation of skeletal muscles for intubation of the trachea, for surgical interventions with a high risk of regurgitation: for example, with intestinal obstruction, "acute abdomen", emergency cesarean section, in urgent operations in patients with a non-liberated stomach, and also to reduce the severity of seizures in electropulse therapy.
    Contraindications:

    - Hypersensitivity to suxamethonium chloride or to any of the excipients;

    - propensity to malignant hyperthermia;

    - hyperkalemia and conditions increasing its risk (severe renal failure, intake of potassium preparations), because of possible hyperkalemic cardiac arrest;

    - severe burns, multiple trauma;

    - severe infections of the abdominal cavity, sepsis;

    - long-term immobilization;

    - penetrating wounds of the eye with increased intraocular pressure;

    - increased intracranial pressure;

    - disorders of neuromuscular conduction at, myotonia, poliomyelitis, amyotrophic lateral sclerosis, multiple sclerosis, all forms of muscular dystrophy, severe myasthenia;

    - impairment of innervation, leading to secondary muscular atrophy (transverse syndrome);

    - congenital insufficiency of cholinesterase;

    - lactation period.

    Carefully:

    - Diseases of the heart;

    - lung diseases;

    - states, accompanied by a decrease in the activity of cholinesterase;

    - hypothermia;

    - hypermagnesia;

    - hypocalcemia;

    - hypokalemia;

    - pregnancy.

    Pregnancy and lactation:

    During pregnancy, Listenon® is used provided that the intended benefit to the mother exceeds the potential risk to the fetus.

    Due to the reduced level of cholinesterase of blood plasma during pregnancy, the duration of action of the drug Listenon® can increase. The cholinesterase activity in the blood plasma reaches normal values ​​approximately 6-8 weeks after birth (see section "Special instructions"). Listenon® does not penetrate the placenta.

    If necessary, in the use of Lystenon ® during lactation, women should stop breastfeeding, as there is no data on the isolation of suxamethonium with human milk.

    Dosing and Administration:

    Intravenously

    During general anesthesia, Listenon® is administered intravenously as a single slow jet injection (10-30 seconds).

    Dosage regimen in children over 12 years of age and adults:

    A single dose for intubation of the trachea: 1-1.5 mg / kg body weight (maximum 150 mg); for prevention of complications during electropulse therapy (convulsions, muscle and tendon rupture): 0.5-0.7 mg / kg body weight.

    Dosing regimen in children from 1 year to 12 years: 1 mg / kg body weight.

    Dosage regimen in newborns and children under 1 year: 1 -2 mg / kg body weight. Newborns require a large dose of suxamethonium in mg / kg (greater volume of distribution).Equivalent therapeutic doses of suxamethonium have a similar duration of action in all age groups, despite the fact that the cholinesterase activity of plasma before the age of 6 months is only 40-50% compared to adults (see "Interaction with Other Drugs").

    Dosing regimen in obese patients:

    The dosage regimen for such patients should be calculated based on the ideal, not the actual body weight.

    The dosage regimen for violations of the liver, kidneys and diseases of the heart:

    There is no need for special dosing regimens, but the information contained in the "Contraindications" and "Special instructions" sections should be taken into account.

    Listenon® should not be administered as a continuous infusion (see section "Special instructions").

    Intramuscularly

    In case of poor access to the superficial veins (for example, in children) or in emergency cases, when rapid endotracheal intubation is required, Listenon® can be administered intramuscularly.

    Children over 12 years and adults: 3-4 mg / kg body weight (maximum 150 mg).

    Children from 1 year to 12 years: 3-4 mg / kg body weight (maximum 150 mg).

    Newborns and children under 1 year of age: 3-4 mg / kg body weight (maximum 150 mg).

    Listenon® is compatible with blood, 0.9% sodium chloride solution, Ringer's solution, 5% fructose solution, 5% dextrose solution, 6% dextran solution. Listenon® is not recommended for mixing with any substances other than those listed above.

    Side effects:

    Undesirable effects are listed by category in order of decreasing severity. Very frequent (>1/10); frequent (>1/100, <1/10); infrequent (>1/1000, <1/100); rare (>1/10000, <1/1000); very rare (<1/10000, including isolated cases).

    Immune system disorders

    Frequent: allergic reactions (sharp reddening of the skin, urticaria).

    Rare: bronchospasm.

    Very rare: anaphylactic shock with sudden reddening of the skin, with / without bronchospasm and lowering blood pressure.

    Violations of the blood and lymphatic system

    Very frequent: increased potassium concentration in the serum (most often a slight increase of 0.05 mmol / l). Myoglobinemia (found in 20% of children, less often in adults). This effect is dose independent and can develop with or without muscular fasciculation.

    Very rare: ventricular fibrillation and cardiac arrest due to hyperkalemia.

    Disorders from the metabolism and nutrition

    Very rare: life-threatening hyperkalemia, porphyria, malignant hyperthermia with / without muscle rigidity (spasm of masticatory muscles), cardiovascular complications (tachyarrhythmias, unstable blood pressure), elevated CO concentration2 at the end of exhalation (with capnometry), elevated body temperature, severe acidosis, hemoglobinuria.

    Disturbances on the part of the organ of sight

    Frequent: increased intraocular pressure.

    Disturbances from the respiratory system, chest and mediastinal organs

    Rare: prolonged apnea in patients with impaired cholinesterase activity of blood plasma, laryngoepasms.

    Very rare: late respiratory failure in cases of neuromuscular transmission, laryngeal edema, pulmonary edema.

    Disorders from the gastrointestinal tract

    Frequent: increased intragastric pressure (risk of regurgitation in pregnant patients, patients with hernia of the esophagus of the diaphragm, atony of the stomach and intestines, ascites, as well as tumors of the abdominal cavity), increased salivation.

    Disturbances from musculoskeletal and connective tissue

    Very frequent: muscular fasciculation (90%), myalgia as a result of muscular fasciculations (approximately 60% of all patients), most often develops in the neck, shoulder girdle, chest and back, especially in middle-aged patients (20 to 50 years).

    Infrequent: minor trisus (up to 60 seconds), which can be reduced with propofol or a small dose of nondepolarizing muscle relaxant.

    Rare: muscle contraction instead of relaxation (often against a background of dystrophic myotonia or congenital myotonia). Prolonged paralysis as a result of the development of a double block and the violation of neuromuscular transmission, which can also be a consequence of idiosyncrasy (a hereditary cholinesterase variant, see the "Special instructions" section), an overdose or a decrease in cholinesterase activity in plasma.

    Very rare: acute rhabdomyolysis with established and unsettled disorders of neuromuscular conduction.

    Cardiovascular disorders

    Very frequent: arrhythmias (found in 50% of children and 20% of adults after the first intravenous injection, most often in young children) (see section "Special instructions"), mild bradycardia (especially in children, less often in adults).

    Frequent: increase or decrease in blood pressure.

    Infrequent: tachycardia.

    Very rare: ventricular arrhythmias, ventricular fibrillation, cardiac arrest, (due to hyperkalemia), hypercalcemia, especially in children with unsettled skeletal muscle diseases (Duchenne myopathy); heart failure as a result of anaphylactoid reactions.

    Disturbances from the skin and subcutaneous tissues

    Frequent: redness of the skin due to the release of histamine.

    Disorders from the kidneys and urinary tract

    Rare: myoglobinuria and increased activity of creatine phosphokinase, mainly in children who received Listenon ® in combination with halothane.

    Very rare: myoglobinuria leading to renal failure, mainly in patients with diagnosed or concealed muscular dystrophy.

    Disturbances from the nervous system

    Frequent: increased intracranial pressure.

    Overdose:An overdose of Lystenon® can lead to a prolonged blockade of neuromuscular transmission, which continues after the operation and anesthesia is complete. It is manifested by muscle weakness, decreased respiratory reserves, volume of inspiration or apnea.Treatment consists in maintaining the patency of the airways and adequate breathing to complete recovery of muscle tone.
    Interaction:

    The effect of suxamethonium is enhanced or prolonged:

    - Means for inhalation anesthesia (enflurane, desflurane, isoflurane, sevoflurane).

    - Cholinesterase inhibitors (neostigmine methylsulfate), including eye drops containing cholinesterase inhibitors (ecothiopath chloride, eudrophonia chloride, pyridostigmine iodide).

    - Antibiotics, especially aminoglycosides (gentamicin, neomycin, streptomycin).

    - Local anesthetics (procaine, lidocaine), as a result of reduced permeability of the membrane for sodium ions.

    - Metoclopramide, as a result of decreased cholinesterase activity.

    - Magnesium sulfate: Infusion of magnesium salts should be stopped 20-30 minutes before the administration of Lystenon® (see section "Special instructions").

    - Antiarrhythmic drugs (class I substances) due to a decrease in the permeability of membranes for sodium ions.

    - Blockers of "slow" calcium channels and "loop" diuretics - due to blockade of calcium channels.

    - Beta-blockers.

    - Lithium salts.

    - Hormonal contraceptives and estrogens - as a result of decreased cholinesterase activity.

    - Corticosteroids.

    - Oxytocin, cimetidine.

    - Inhibitors of monoamine oxidase (phenelzine) and some neuroleptics (perphenazine) - as a result of a decrease in cholinesterase activity.

    - Sympathomimetics - as a result of a decrease in cholinesterase activity.

    - Antiepileptic drugs reduce the effect of nondepolarizing muscle relaxants, however, for suxamethonium, cases of elongation of the effect are described.

    - Alcohol and drugs that depress the central nervous system.

    The effect of suxamethonium is reduced:

    - Parasympathetic effects of suxamethonium can be reduced by atropine (see section "Special instructions")

    - Concomitant transfusions of whole blood or plasma.

    The effect of suxamethonium on other drugs:

    - Suxamethonium potentiates the effect of cardiac glycosides, which can lead to arrhythmia.

    Incompatibility with sodium thiopental:

    - Listanon® and thiopental sodium should not be administered simultaneously or mixed, because sodium thiopental is chemically incompatible with solutions that have low pH and oxidizing agents.

    Special instructions:

    Being a depolarizing muscle relaxant, Listenon® causes paralysis of the respiratory muscles without affecting the patient's consciousness. Therefore, during general anesthesia, Listenon® should only be administered by an experienced anesthesiologist with access to the means for intubation of the trachea, artificial ventilation, and, if necessary, resuscitation.

    - Parasympathetic effects, ranging from bradycardia to asystole, hypotension and hypersalivation, can often be prevented or weakened by the administration of atropine.

    Side effect on the heart is more common in children (first bradycardia, then tachycardia, possible replacement nodal rhythm, ventricular extrasystole). Registered cases of death in children and adolescents were the result of immunity to resuscitative therapy. In some of these cases, the patients had unrecognized neuromuscular transmission disorders.

    Depending on the age of the patient, the incidence of arrhythmias increased with the administration of a second dose within 15 minutes after the first (see "Side effect" section). In this regard, as well as for the reasons described below, Listenon® should not be administered as a continuous infusion.

    - Suxamethonium chloride is inactivated during hydrolysis under the action of cholinesterase or pseudocholinesterase of plasma blood, so the duration of the effect of the drug Listenon ®, in the first place, depends on the activity of these enzymes.

    Insufficiency of cholinesterase or pseudocholinesterase can significantly prolong the effect of the drug Listenon ®. Insufficiency of cholinesterase can be congenital, develop against a background severe liver function disorders, terminal renal failure, hypothyroidism or severe diseases of various etiologies (malignant tumors, cachexia), burns or medication (see the section "Interaction from other medicinal means ").

    Physiological inhibition of cholinesterase activity note in newborns, in women in late pregnancy and in elderly people. Essential longer duration The action of suxamethonium chloride is of clinical importance, primarily for patients with genetic insufficiency cholinesterase of blood plasma. Under certain circumstances, such patients should continue to be on the ventilator for several hours.

    - Repeated administration of Lystenon®, as well as its prolonged infusion, may alter the ability of suxamethonium to induce a neuromuscular block (the required aggregate dose of 5-10 mg / kg body weight). The initial long-term depolarizing unit (Phase 1 block) goes into a long non-depolarizing unit (phase II block, or double block). Double block develops if suxamethonium can not be hydrolyzed by atypical cholinesterase and therefore accumulates in the synaptic cleft. Based on clinical data, it is impossible to distinguish two types of block; Relaxography is used for this. In contrast to the depolarization block, cholinesterase inhibitors have partial antagonism with respect to the double block.

    - The introduction of the drug Listenon may be accompanied by admission a significant number potassium inside the cell. An increase in potassium concentration in the serum can lead to life-threatening hyperkalemia with the development of ventricular fibrillation and asystole. Particular risk is for patients with renal insufficiency, with severe burns or multiple injuries.

    - After the administration of Lystenon®, temporary muscle fasciculations may result, leading to myalgia or muscle pain.Prekurarisation (the introduction of low doses of nondepolarizing muscle relaxants) makes it possible to reduce primary muscular fasciculation and myalgia.

    - Hypothermia can potentiate and prolong the effects of suxamethonium by slowing down physical and biochemical membrane processes.

    - The effect of suxamethonium can be enhanced and prolonged hypermagnesemia and hypocalcemia in connection with the inhibition of the presynaptic release of acetylcholine and hypokalemia, by decreasing the membrane resting potential.

    Effect on the ability to drive transp. cf. and fur:
    Patients should not drive vehicles or mechanisms for at least 24 hours after the administration of Lystenon®.
    Form release / dosage:
    A solution for intravenous and intramuscular administration of 20 mg / ml.
    Packaging:

    5 ml in colorless ampoules of hydrolytic glass (type 1, Hebrew farm.) With a break point.

    5 ampoules per plastic contour mesh package. 1 contour pack with instructions for use in a cardboard box.

    Storage conditions:In the dark place at a temperature of 2-8 ° C. Keep out of the reach of children!
    Shelf life:
    2 years.Do not use after the expiration date printed on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:П N012564 / 01
    Date of registration:13.09.2011 / 01.12.2016
    Expiration Date:Unlimited
    The owner of the registration certificate:Takeda Austria GmbHTakeda Austria GmbH Austria
    Manufacturer: & nbsp
    Representation: & nbspTakeda Pharmaceuticals Ltd.Takeda Pharmaceuticals Ltd.
    Information update date: & nbsp11.04.2018
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