Suxamethonium chloride (Suxamethonii iodidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

"N-holinoblokatory (muscle relaxants, curare-like remedies)"

Included in the formulation
  • Listenon®
    solution w / m in / in 
    Takeda Austria GmbH     Austria
  • Suxamethonium chloride
    solution w / m in / in 
    SYNTHESIS, OJSC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    M.03.A.B   Derived choline

    Pharmacodynamics:

    Noncompetitive binding to H-holinoretseptora nervously-muscle synapses: the discovery of potential-dependent ion channels, mediator of which is acetylcholine, persistent depolarization of the postsynaptic membrane. Because of the resistance to acetylcholinesterase, acetylcholine is longer in the synaptic cleft. The emergence of temporary fasciculations - the onset of action, then the blockade of neuromuscular conduction and flaccid paralysis (complete refractoriness to the action of acetylcholine - desensitization) is an action typical for the depolarizing muscle relaxant.

    Pharmacokinetics:After administration, biotransformation takes place in the blood: rapid hydrolysis with pseudocholinesterase plasma to succinyl monocholine (mild muscle relaxant effect), then to choline and succinic acid. There is no connection with plasma proteins.The half-life is 90 seconds (in persons with normal pseudocholinesterase activity). Elimination by the kidneys (10% unchanged).
    Indications:

    Interventions requiring miorelaxation (usually short-term):

    - disabling of spontaneous breathing (intratracheal intubation, bronchoscopy);

    - complete miorelaxation (endoscopy, correction of dislocations, repositioning of fractures, gynecological, thoracic, abdominal operations);

    - prevention of seizures in electropulse therapy;

    - Strychnine poisoning;

    - tetanus (symptomatic therapy).

    ICD-10

    I.A30-A49.A35   Other forms of tetanus

    XIX.T51-T65.T65.1   The toxic effect of strychnine and its salts

    XXI.Z40-Z54.Z51.4   Preparatory procedures for subsequent treatment, not elsewhere classified

    Contraindications:

    Hypersensitivity, malignant hyperthermia (including anamnesis), myasthenia gravis, congenital and dystrophic myotonia, Duchenne muscular dystrophy, angle-closure glaucoma, acute liver failure, pulmonary edema, penetrating eye traumas, bronchial asthma, hyperkalemia, breast age (under 1 year), pregnancy.

    Carefully:

    Emergency surgery in patients with a "full stomach", a decrease in cholinesterase activity (terminal stage of hepatic insufficiency, anemia, cachexia, prolonged fasting, chronic infections, widespread burns, trauma, postpartum period, tetanus, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, collagen diseases , after plasma transfusion, plasmapheresis, artificial circulation, acute or chronic intoxication with insecticides - cholinesterase inhibitors (if ingested), or anticholines with various drugs (neostigmine methylsulfate, physostigmine, distigmine bromide, phospholin), simultaneous administration of drugs that compete with suxamethonium for cholinesterase (for example, procaine in / in).

    Pregnancy and lactation:

    Studies in humans have not been conducted. Studies in animals have revealed a delay in fetal development of the fetus, deformation of the limbs. There is no information on the penetration into breast milk. Do not apply!


    Category of recommendations FDA C.

    Dosing and Administration:

    The drug is administered intravenously (spray, drip), in / m.

    Adults are injected iv slowly, spray or drip.Depending on the clinical situation, with iv introduction, a single dose varies from 100 μg / kg to 1.5-2 mg / kg.

    In / m injected in a dose of 3-4 mg / kg, but not more than 150 mg.

    For children, the drug is given in / m in doses up to 2.5 mg / kg, but not more than 150 mg, iv in a dose of 1-2 mg / kg.

    Side effects:

    Allergic reactions: anaphylactic shock, bronchospasm.

    From the side of water-electrolyte balance: hyperkalemia.

    From the cardiovascular system: arrhythmias, lowering blood pressure, bradycardia (more often in children, with repeated administration - in children and adults), conduction disorders, cardiogenic shock.

    From the side of the organ of vision: increased intraocular pressure.

    From the musculoskeletal system: myalgia (in the postoperative period), rhabdomyolysis with the development of myoglobinemia and myoglobinuria.

    On the part of the respiratory system: prolonged paralysis of the respiratory muscles (associated with a genetically determined disruption of pseudocholinesterase production).

    Other: hypersalivation, fever.

    Overdose:

    Acute respiratory arrest, severe hypotension, prolonged paralysis, shock.

    Treatment symptomatic - ventilation, transfusion of freshly frozen plasma (replenishment of pseudocholinesterase deficiency),However, with the long-term administration of suxamethonium, when signs of a non-depolarizing action appear, low doses of anticholinesterase agents and atropine may be prescribed.

    Interaction:

    Aminoglycosides, vancomycin, capreomycin, lincomycin, massive infusions of citrated blood, local (including procaine and lidocaine) and general anesthetics, polymyxins, tetracyclines, trimetafan, ureidopenicillins - additive muscle relaxant effect.

    Anesthetics common (halothane, isoflurane, methoxyflurane, trichloroethylene, chloroform, cyclopropane, enflurane, diethyl ether) - increased risk of malignant hyperthermia.

    Anticholinesterase drugs, neurotoxic insecticides, cyclophosphamide, phenelzine, thiotepa, estrogens - inhibition of serum pseudocholinesterase activity and reduced clearance of suxamethonium.

    Aprotinin - the risk of apnea.

    Anticonvulsants (carbamazepine, phenytoin), lithium, metoclopramide - increase in the duration of action of suxamethonium.

    Verapamil, magnesium salts, procainamide, quinidine - strengthening neuromuscular blockade.

    Muscle relaxants nedepoljarizujushchie - amplification miorelaksatsii if appoint or nominated after introduction suksametonija.

    Opioid analgesics are an additive depressive effect on respiratory function, a reduction in muscle rigidity caused by fentanyl and its derivatives, an additive depressive effect on hemodynamics, an additive effect on the release of histamine.

    Cardiac glycosides - additive cardiotropic action.

    Physostigmine - increased risk of myofascing and increased depolarization block.

    Special instructions:

    The sequence of muscle relaxation: small fast muscles (eye, jaw, larynx), then the muscles of the trunk and extremities, the latter - intercostal muscles and diaphragm, restoration in reverse order.

    They are used mainly during large operations to relax the muscles (especially the abdomen), facilitating surgical manipulation. Short-acting drugs in combination with general anesthetics are used to facilitate intubation of the trachea, laryngo-, broncho- and esophagoscopy.

    Monitoring serum potassium, ECG, body temperature, oxygen saturation.

    Distinctive characteristics.

    Depolarizing muscle relaxant of ultrashort action, used for rapid achievement of muscle relaxation.Derivative diacetylcholine - structurally similar to acetylcholine, as a result of which it manifests its tropicity to the H-holinoretseptoru. Quaternary ammonium base, as a result of which it does not penetrate the BBB. The only depolarizing muscle relaxant applied today.

    To achieve muscle relaxation with the aim of intubation of the trachea, suxamethonium is superior to rocuronium and is equivalent to a combination of rocuronium and propofol.

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