Suksamethonium iodide - instructions for use, dose, side effects, contraindications

Pharmacodynamics:Depolarizing muscle relaxant of peripheral action. 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 significant effect on the respiratory musculature, 0.2-1 mg / kg - complete relaxation of the musculature of the abdominal wall and respiratory musculature (there is a significant restriction or complete stop of the spontaneous respiration).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 choline. The half-life (T1 / 2) is 90 seconds. at a normal concentration of cholinesterase. It is excreted by the kidneys. 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 to the drug components, malignant hyperthermia (including in the anamnesis), myasthenia gravis, congenital and dystrophic myotonia, Duchenne muscular dystrophy,closed angle glaucoma, acute hepatic insufficiency, pulmonary edema, penetrating eye trauma, bronchial asthma, hyperkalemia, breast age (up to 1 year), pregnancy, 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 - cholinesterase inhibitors (by ingestion) or anticholinesterase drugs (neostigmine methylsulfate, physostigmine, distigmine bromide, ecotiopathic iodide), simultaneous administration of drugs competing with suxamethonium iodide for cholinesterase (for example, procaine intravenously).

Dosing and Administration:

Adults: intravenously slow, jet or drip (for long-term drip 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 W doses up to 2.5 mg / kg, but not more than 150 mg, intravenously 1-2 mg / kg.

To carry out 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 in the direction of dislocation and reposition of bone fragments in 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 laceration) - 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 entire operation, the drug can be injected fractionally after 5-7 minutes at 0.5-1 mg / kg. Repeated doses of suxamethonium iodide last longer.

Side effects:Allergic reactions (anaphylactic shock, bronchospasm); hyperkalemia, lowering of arterial pressure, arrhythmias, bradycardia (more often in children, with repeated administration - 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% solution of sodium chloride, Ringer's solution, 5% solution of fructose and 6% solution of dextran. 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 effect. Compatible with other muscle relaxants, narcotic analgesics.

Halogen-containing drugs 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 cholinesterase activity (aprotinin, diphenhydramine, promethazine, estrogens, oxytocin, glucocorticoid agents in high doses, oral contraceptives), enhance and prolong the muscle relaxant effect of suxamethonium iodide.

Special instructions:

Introduction 1 min before suxamethonium iodide 3-4 mg of nondepolarizing muscle relaxants almost completely prevents muscle twitching and subsequent myalgia. With the appropriate dose and repeated administration can be used for longer operations, however, for long-term relaxation of the muscles, nondepolarizing muscle relaxants are usually used, which are administered after a pre-intubation of the trachea against a background of suxamethonium iodide.

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 pronounced bradycardia, increase of bronchial secretion and other effects associated with m-cholinostimulating action, it is recommended to enter, before the administration of suxamethonium iodide atropine. Patients with renal insufficiency (without signs of hyperkalemia and neuropathy) are injected once in medium doses, but do not use for multiple administrations or at elevated doses because of the risk of developing hyperkalemia.

Prolonged muscle relaxation with possible apnea can be caused by several reasons: "atypical" cholinesterase of blood serum, hereditary deficiency of serum cholinesterase or temporary decrease in its concentration in case of severe liver disease, severe anemia, after prolonged fasting, with cachexia, dehydration, fever, after acute poisoning or chronic effects of insecticides - cholinesterase inhibitors (if ingested) or an-tiloline-esterase drugs (neostigmine methylsulfate, fizostig-mines, distigmine bromide, ecotiopathic iodide), simultaneous administration of drugs competing with suxamethonium iodide for cholinesterase (for example, procaine intravenously).

With prolonged administration at doses of 3-5 mg / kg, a so-called "double block" may develop - a prolonged curare similar action that can be eliminated by neostigmine methylsulfate.

Effect on the ability to drive transp. cf. and fur:

Form release / dosage:

A solution for intravenous and intramuscular administration of 20 mg / ml.

Packaging:

5 ml of the drug into neutral glass ampoules.

For 10 ampoules, together with instructions for medical use and scarifier in a cardboard box with cardboard partitions, or 5 or 10 ampoules in a contiguous cell pack of a polyvinyl chloride film.

When using ampoules with a notch or a fracture ring, the scarifier is not inserted. For 1 or 2 contour acupule packs, together with instructions for medical use, are placed in a cardboard box.

Storage conditions:List A. Store in a dark place at a temperature of no higher than 5 ° C. Freezing is not allowed. Keep out of the reach of children.

Shelf life:1 year 6 months.Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-010036/09

Date of registration:09.12.2009

The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia

Manufacturer: & nbsp

ESKOM NPK, OAO Russia

Information update date: & nbsp25.08.2015

Illustrated instructions

Instructions

Suxamethonium iodide (Suxamethonium iodide)