Suxamethonium chloride (Suxamethonium chloride)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceSuxamethonium chlorideSuxamethonium chloride
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    SYNTHESIS, OJSC     Russia
    • Dosage form: & nbspSolution for intravenous and intramuscular injection.
    Composition:
    Composition for 1 ml.
    Active substance: suxamethonium chloride - 20 mg.
    Excipients: disodium edetate (ethylenediaminetetraacetic acid disodium salt [Trilon B]), sodium chloride, water for injection.
    Description:
    Transparent or slightly opalescent colorless, or slightly yellowish tinge solution.

    Pharmacotherapeutic group:Miorelaxant depolarizing the peripheral action.
    ATX: & nbsp

    M.03.A.B   Derived choline

    Pharmacodynamics:
    Depolarizing short-acting muscle relaxant. It causes a blockade of the neuromuscular transmission. Stimulating n-holinoretseptory, causes depolarization of the terminal plate. The process extends to the adjacent membranes, a generalized disorganized contraction of myofibrils (ie, the blockade is preceded by muscle twitching - the result of a short-term relief of neuromuscular transmission).Membranes, remaining depolarized, do not respond to additional impulses, since the maintenance of muscle tone requires the arrival of repeated pulses, associated with repolarization of the terminal plate, spastic paralysis occurs. After intravenous injection, muscle relaxation occurs in the following sequence: eyelids, chewing muscles, muscles of the fingers, eyes, limbs, neck, back and abdomen, vocal cords; then intercostal muscles and diaphragm.
    Increases cerebral blood flow and intracranial pressure in conditions of general anesthesia.
    After intramuscular injection, the effect develops in 2-4 minutes; after intravenous administration - after 54-60 seconds, after 2-3 min the relaxation of muscles reaches a maximum and remains in full for 3 minutes. The duration of action is 5-10 minutes.
    The severity of the action depends on the amount of the administered dose: 0.1 mg / kg - relaxation of the skeletal muscles without a significant effect on the respiratory musculature, 0.2-1 mg / kg - complete relaxation of the musculature of the abdominal wall and respiratory muscles (there is a significant restriction or complete stopping of spontaneous breathing).For a long relaxation of the muscles, a second injection is necessary. The rapid onset of the effect and the subsequent rapid restoration of muscle tone allow the creation of a controlled and controlled relaxation of the muscles.
    Pharmacokinetics:After intravenous administration, it is distributed in plasma and extracellular fluid. More than 90% is hydrolyzed by cholinesterase of blood to succinic acid and holim. The half-life is 90 seconds with normal cholinesterase concentration. It is excreted by the kidneys (10% unchanged). It does not penetrate the intact blood-brain barrier. Do not cumulate.
    Indications:Interventions requiring miorelaxation (usually short-term): disabling of spontaneous breathing (intratracheal intubation, bronchoscopy); complete miorelaxation (endoscopy, reversal of dislocations, reposition of fractures, gynecological, thoracic, abdominal operations); prevention of convulsions in electropulse therapy; poisoning with strychnine, tetanus (symptomatic therapy).
    Contraindications:Hypersensitivity, malignant hyperthermia (including in the anamnesis), myasthenia gravis, congenital and dystrophic myotonia, Duchenne muscular dystrophy,closed angle glaucoma, acute liver failure, pulmonary edema, penetrating eye trauma, cholinesterase deficiency, bronchial asthma, hyperkalemia, children under 1 year of age, pregnancy and lactation.
    Carefully:Emergency surgery in patients with a "full stomach", decreased serum cholinesterase activity (terminal stage of liver failure), anemia, cachexia, prolonged fasting, chronic infections, widespread burns, trauma, postpartum period, tetanus, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, systemic connective tissue diseases, conditions after a plasma transfusion, plasmapheresis, operations under conditions of artificial circulation, acute or chronic infection oksikatsiya insecticide inhibitor of cholinesterase (by ingestion) or anticholinesterase agents (neostigmine methylsulfate, physostigmine, distigmine bromide, ecotiopathic iodide), simultaneous administration of drugs competing with suxamethonium chloride for cholinesterase (for example, procaine in / in).
    Dosing and Administration:
    Intravenous (jet, drip), intramuscularly.
    Adults: intravenously slow, jet or drip (for long-term drop infusion use 0.1% solution). Depending on the clinical situation with intravenous administration, a single dose varies from 0.1 to 1.5-2 mg / kg. Intramuscular - 3-4 mg / kg, but not more than 150 mg.
    Intramuscularly used in children in doses up to 2.5 mg / kg, but not more than 150 mg, intravenously 1-2 mg / kg.
    For intubation of the trachea - 0.2-0.8 mg / kg; for miorelaxation and disabling of spontaneous breathing - 0.2-1 mg / kg; for the relaxation of skeletal musculature when sprains are dislocated and reposition of bone fragments at fractures - 0.1-0.2 mg / kg; for endoscopy and electroencephalography - 0.2 mg / kg; for the prevention of complications during electropulse therapy (seizures, muscle and tendon rupture) - 0.1-1 mg / kg intravenously and up to 2.5 mg / kg intramuscularly, but not more than 150 mg.
    For a long relaxation of the musculature during the whole operation, it is possible to inject fractionally, at 5-7 mim, at 0.5-1 mg / kg. Repeated doses last longer.
    Side effects:Allergic reactions (anaphylactic shock, bronchospasm); hyperkalaemia, lowering of arterial pressure, arrhythmias, bradycardia (more often in children, repeated injection in children and adults), conduction disorders,cardiogenic shock; increased intraocular pressure, hypersalivation, fever; myalgia (in the postoperative period); long paralysis of the respiratory muscles (associated with a genetically determined violation of the formation of serum cholinesterase); rarely - rhabdomyolysis with the development of myoglobinemia and myoglobinuria.
    Overdose:
    Symptoms: stop breathing.
    Treatment: artificial ventilation of the lungs, in case of a decrease in cholinesterase in the blood serum - a transfusion of fresh blood.
    Interaction:
    Enhances the effects of cardiac glycosides.
    Reduces the effectiveness of antimiasthenic drugs.
    Pharmaceutically incompatible with donor blood (hydrolysis occurs), blood preservatives, whey preservatives, with blood products, with solutions of barbiturates (a precipitate is formed) and alkaline solutions. Compatible with 0.9% sodium chloride solution, Ringer's solution, 5% fructose solution and 6% dextran solution.
    Anticholinesterase drugs, procaine, procainamide, lidocaine, verapamil, beta-adrenoblockers, aminoglycoside antibiotics, amphotericin B, clindamycin, cyclopropane, propanidide, organophosphorus insecticides, magnesium and lithium salts, quinidine, quinine, chloroquine, pancuronium bromide, enhances and prolongs the muscle relaxant action. Compatible with other muscle relaxants, narcotic analgesics.
    Halogen-containing agents for general anesthesia are enhanced, and thiopental sodium and atropine reduce the undesirable effect on the cardiovascular system. Drugs that have the potential to reduce the cholinesterase activity of blood (aprotipin, diphenhydramine, promethazine, estrogens, oxytocin, glucocorticosteroids in high doses, oral contraceptives), enhance and prolong the muscle relaxant effect of suxamethonium.
    Special instructions:
    Introduction 1 min before suxamethonium chloride of nondepolarizing muscle relaxants almost completely prevents muscle twitching and subsequent myalgia. With the appropriate dose and repeated administration may be used for longer operations, but for a prolonged muscle relaxation commonly used non-depolarizing muscle relaxants are administered after pre-tracheal intubation on a background suxamethonium chloride. Applied only in the conditions of a specialized department with the availability of equipment for artificial ventilation and personnel who own this technique, and against a background of general anesthesia.
    To prevent bradycardia, increased bronchial secretion, and others. Effects associated with the m-holinostimuliruyuschim action recommended to introduce before administration suxamethonium chloride atropine. Patients with renal failure (without signs of hyperkalemia and neuropathy) administered once in moderate doses, but not used for multiple injections or in high doses because of the risk of hyperkalemia.
    The prolonged muscle relaxation with possible apnea may be caused by several reasons: "atypical" cholinesterase serum hereditary deficiency of serum cholinesterase or temporary decrease in its concentration in severe liver disease, severe anemia after prolonged fasting, in cachexia, dehydration, fever, after acute poisoning or chronic effects of insecticides - cholinesterase inhibitors (if ingested) or anticholinesterase agents (neostigmine methylsulfate, physostigmine, distigmine bromide), as well as the simultaneous use of drugs that compete with suxamethonium chloride for holnesteazu (for example, procaine in / in).
    With prolonged administration at doses of 3-5 mg / kg, a so-called "double block" may develop - a prolonged curare-like action that can be eliminated by neostigmine methylsulfate.
    Effect on the ability to drive transp. cf. and fur:In the first 24 hours after the cessation of the muscle relaxant effect of the drug, it is not recommended to drive and engage in potentially dangerous activities requiring increased concentrated attention and speed of psychomotor reactions.
    Form release / dosage:
    A solution for intravenous and intramuscular administration of 20 mg / ml.
    Packaging:
    5 ml in ampoules of colorless or light-protective neutral glass. 10 ampoules are placed in a box of cardboard.
    5 or 10 ampoules are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered or foil-free.
    I contour cell package with 10 ampoules or 1, 2 contoured cells with 5 ampoules are placed in a pack of cardboard.
    In each pack, the box is attached instructions for use, the ampullar scarifier.
    Ampoule scapper does not invest in case of using ampoules with a kink ring or with an incision and a point.
    Storage conditions:List A.In the dark place at a temperature of 2 to 8 ° C. Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiration date.
    Terms of leave from pharmacies:On prescription
    Registration number:P N003409 / 01
    Date of registration:12.12.2008
    The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp25.08.2015
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