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

Excipients: sodium chloride -7 mg; disodium edetate (disodium ethylenediaminetetraacetic salt acids; Trilon B) - 0.05 mg; ascorbic acid - 0.05 mg; hydrochloric acid 0.1 M solution to pH 3.3-3.6; water for injection - up to 1 ml.

Description:Transparent colorless liquid.

Pharmacotherapeutic group:Muscle relaxant depolarizing the peripheral action

ATX: & nbsp

M.03.A.B Derived choline

Pharmacodynamics:

Depolarizing short-acting muscle relaxant. It causes blockade of the neuromuscular transmission. Interacting with n-holinoretseptorami, causes depolarization of the end plate of motor nerves. The process extends to adjacent membranes, there is a generalized disorganized contraction of myofibrils (i.e.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: the muscles of the eyelids, chewing musculature, the muscles of the fingers, eyes, extremities, neck, back and abdomen, vocal cords, then intercostal muscles and diaphragm.

Causes an increase in cerebral blood flow and increased intracranial pressure. Duration of action 5-10 minutes.

The severity of the action depends on the amount of the dose administered:

0.1 mg / kg - relaxation of skeletal muscles without significant effect on the respiratory system;

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 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:

Suction: After intravenous administration, the action begins after 54-60 seconds, after 2-3 min the muscle relaxation reaches its maximum and remains in full for 3 minutes. After intravenous administration, it is distributed in plasma and extracellular fluid. The short duration of action of suxamethonium iodide is due to the rapid inactivation of blood plasma by cholinesterase with the formation of choline and succinyl monocholine. The half-life (T1 / 2) is 90 seconds with a normal plasma cholinesterase level. The succinyl monocholine is a non-depolarizing muscle relaxant whose activity is 20-50 times lower in comparison with the initial substance. Subsequently, the metabolic rate slows down and succinyl monocholine decomposes into succinic acid and choline. It is excreted by the kidneys. It does not penetrate the intact blood-brain barrier. Do not cumulate.

Indications:

The drug is used only in conditions of general anesthesia for relaxation of skeletal muscles with the purpose of intubation of the trachea,at 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, to reduce the severity of convulsions in electropulse therapy. Strychnine poisoning, tetanus (symptomatic therapy).

Contraindications:

Suxamethonium iodide (dithiline) does not affect the level of consciousness and should not be administered to patients without anesthesia.

- hypersensitivity to suxamethonium iodide or to any of the auxiliary components of the drug;

- predisposition to malignant hyperthermia;

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

- severe burns, multiple trauma;

- severe infections of the abdominal cavity, sepsis;

- long-term immobilization;

- penetrating trauma of the eye with increased intraocular pressure;

- increased intracranial pressure;

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

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

- congenital insufficiency of cholinesterase;

- children under 1 year;

- pregnancy;

- the period of breastfeeding.

Carefully:

- Diseases of the heart;

- lung diseases;

- states, accompanied by a decrease in the activity of cholinesterase (except congenital insufficiency of cholinesterase);

- hypothermia;

- hypermagnesia;

- hypokalemia;

- hypocalcemia;

- children age over 1 year;

- renal failure of mild to moderate severity (without signs of hyperkalemia and neuropathy).

Pregnancy and lactation:The drug is contraindicated in pregnancy and during breastfeeding.

Dosing and Administration:

The administration of the drug is allowed only in the specialized department of the hospital if there are all conditions for carrying out artificial ventilation (IVL) or after transferring the patient to controlled breathing.

The dose is set individually, taking into account the required degree of relaxation, body weight and patient response.

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 mg / kg to 1.5-2 mg / kg body weight.

With intubation of the trachea, the dose is 0.2-0.8 mg / kg.

For miorelaxation and switching off spontaneous breathing 0.2-1 mg / kg.

For relaxation of skeletal muscles in orthopedic and traumatic interventions (fractures, reposition of bone fragments, directing of dislocations and others), a dose of 0.1-0.2 mg / kg.

For endoscopy - 0.2 mg / kg.

To prevent complications of electropulse therapy (seizures, muscle and tendon lacerations) 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 is introduced fractionally, after 5-7 minutes at 0.5-1 mg / kg. Repeated doses last longer.

Children over 1 year old:

Intravenously 1-2 mg / kg or intramuscularly at doses up to 2.5 mg / kg, but not more than 150 mg.

Older patients:

Dose adjustments in elderly patients are not required. However, elderly patients are more prone to heart rhythm disturbances, especially when using cardiac glycosides.

Side effects:

From the immune system: allergic reactions (sharp reddening of the skin, urticaria); anaphylactic shock with or without bronchospasm and lowering blood pressure; anaphylactoid reactions; bronchospasm as a result of anaphylactoid reactions; insufficiency of blood circulation as a result of anaphylactoid reactions.

From the side of metabolism and nutrition: hyperglycemia, transient increase in potassium levels, life-threatening hyperkalemia. porphyria, malignant hyperthermia with or without muscle stiffness (spasm of masticatory muscles), severe acidosis, hypercalcemia, especially in children with unsettled skeletal muscle diseases (Duchenne's myopathy).

From the nervous system: increased intracranial pressure.

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

From the cardiovascular system: increase or decrease in blood pressure, blood flow, short-term bradycardia (more often in children, with repeated administration in children and adults), asystole, tachycardia, arrhythmia (including ventricular arrhythmias), cardiovascular complications (tachyarrhythmias, unstable blood pressure); ventricular fibrillation,cardiac conduction disorder, cardiogenic shock, collapse.

From the respiratory system of the chest and mediastinum: apnea, bronchospasm, prolonged paralysis of respiratory muscles (associated with genetically determined violation products pseudocholinesterase), laryngospasm, tardive respiratory failure in disorders of neuromuscular transmission, laryngeal edema, pulmonary edema, increased concentration of carbon dioxide at the end of exhalation (when capnometry).

From the gastrointestinal tract: hypersalivation, 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, and tumors of the abdominal cavity).

From the liver and bile ducts: abnormal liver function.

From the side of the musculoskeletal and connective tissue: occurrence of musculoskeletal pain in 10-12 hours after injection, muscle fasciculations, with subsequent development of rhabdomyolysis mioglobinemii and myoglobinuria, myalgia as a result of muscle fasciculations, most often develops in the neck.(up to 60 seconds), which can be reduced with propofol or a small dose of nondepolarizing muscle relaxant, muscle contraction instead of relaxation (often against the background of dystrophic myotonia or congenital myotonia); prolonged paralysis as a result of the development of the "double block" and the violation of the neuromuscular transmission, which can also be a consequence of idiosyncrasy (a hereditary cholinesterase variant), an overdose or a decrease in the asset cholinesterase in the blood plasma, myoglobinemia (this effect does not depend on the dose and can develop with or without muscle fascination), myoglobinuria and increased activity of creatine phosphokinase, the main in children who received suxamethonium in combination with halothane.

From the skin and subcutaneous tissue: redness of the skin.

From the side of the kidneys and urinary tract: Myoglobinuria leading to renal diseaseinsufficiency, mainly in patients with diagnosed or concealed muscular dystrophy, hemoglobinuria.

General disorders: hyperthermia.

Overdose:

Symptoms: increased severity of dose-dependent side effects, respiratory arrest, prolonged blockade of neuromuscular transmission.

Treatment: artificial lung ventilation, in case of a decrease in the content of cholinesterase in the blood serum - direct blood transfusion.

Interaction:

Pharmaceutically incompatible with donor blood and blood products (hydrolysis occurs), blood and serum preservatives, with barbiturate solutions and alkaline solutions (a precipitate is formed). Compatible with 0.9% (isotonic) sodium chloride solution, Ringer's solution, 5% fructose solution and 6% dextran solution.

The effect of suxamethonium is enhanced and prolonged: anticholinesterase drugs, procaine, procainamide, lidocaine, verapamil, beta-adrenoblockers, aminoglycoside antibiotics, amphotericin B, clindamycin, cyclopropane, propanidide, organophosphate insecticides, magnesium sulfate (infusion of magnesium salts should be stopped 20-30 minutes before the drug) and lithium salts, quinidine, quinine, chloroquine, pancuronium, antiarrhythmic drugs of the first class, blockers of "slow" calcium channels, looped diuretics,antiepileptic drugs, alcohol and CNS suppressants - enhance and prolong the muscle relaxant effect of suxamethonium iodide.

Drugs that have the potential to reduce cholinesterase activity (atropine, diphenhydramine, promethazine, estrogens, oxytocin, glucocorticosteroids in high doses, oral contraceptives, cimetidine, metoclopramide), as well as cytostatics (cyclophosphamide, thiophosphamide), monoamine oxidase (MAO) inhibitors and some neuroleptics (for example, perphenazine), sympathomimetics enhance and prolong the miorelaksiruyuschee action of suxamethonium iodide.

The effect of suxamethonium reduces concomitant transfusion of whole blood or plasma.

Effect of suxamethonium on other drugs. Suxamethonium iodide compatible with other muscle relaxants, narcotic analgesics. Enhances cardiac effects of cardiac glycosides (bradycardia).

Suxamethonium iodide reduces the effectiveness of antimiasthenic drugs. Halogen-containing agents for general anesthesia are enhanced, and thiopental sodium and atropine reduce the undesirable effect of suxamethonium on the cardiovascular system.

Special instructions:

They are used only in the conditions of a specialized department of a hospital by decision and under the supervision of an experienced anesthesiologist with the presence of equipment for urgent intubation of the trachea and artificial ventilation (IVL). inhalation with oxygen. Neostigmine methyl sulfate (proserin) or other anticholinesterase agents are not antagonists of suxamethonium iodide, on the contrary, by suppressing cholinesterase activity, they can enhance and prolong the action of suxamethonium. Undesirable reactions from the heart are more common in children (first bradycardia, then tachycardia, possible replacement nodal rhythm, ventricular extrasystole). Cases of death in children and adolescents as a result of immunity to resuscitation therapy have been reported. In some of these cases, there were unrecognized disorders of the neuromuscular transmission.

Slow administration of suxamethonium. as well as a preliminary intravenous injection of atropine at a dose of 1-1.5 mg significantly prevent bradycardia and an increase in bronchial secretion.

Preliminary (for 1 min) administration of 3-4 mg tubocurarine chloride or 10-15 mg of diplatcin chloride almost completely prevents the fasciculation of muscles and subsequent myalgia.For prolonged operations, nondepolarizing muscle relaxants are usually used. which are administered after a pre-intubation of the trachea against a background of suxamethonium iodide. Prolonged muscle relaxation with possible apnea can be caused by several reasons: "atypical" cholinesterase of blood serum, hereditary insufficiency of serum cholinesterase or a temporary decrease in its concentration in the blood plasma.

If the drug is injected repeatedly and 25-30 minutes after the end of the injection, the muscle tone is not restored in the patient, the breath remains superficial, one can think of the transition of the depolarizing unit to an antidepolarizing (so-called "double block"). To remove this effect, intravenously injected atropine in a dose of 0.5-0.7 mg (0.5-0.7 ml of a 0.1% solution), after increasing the heart rate after 1 to 2 minutes, you enter prozerin at a dose of 1.5 mg (3 ml of 0.05% solution ).

The introduction of suxamethonium may be accompanied by the receipt of a significant amount potassium inside the cell. Increase in potassium concentration in 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. Patients with renal insufficiency (without signs of hyperkalemia and neuropathy) are given a single dose of the drug in moderate doses, but do not apply for multiple injections or at elevated doses because of the risk of developing hyperkalemia.

Insufficiency of cholinesterase or pseudocholinesterase may significantly prolong the action of suxamethonium. Cholinesterase deficiency can be congenital, develop against a background of severe liver function disorders, terminal renal failure, hypothyroidism or severe diseases of various etiologies (malignant tumors, cachexia), burns or medication (see section "Interaction with other medicines"). Physiological inhibition of cholinesterase activity is noted in newborns, at a young age and in women at late pregnancy.

Under certain circumstances, patients with hereditary failure of serum cholinesterase should continue to be on the ventilator for several hours.

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 by hypermagnesemia and hypocalcemia in connection with the inhibition of presynaptic release of acetylcholine and hypokalemia, by decreasing the membrane resting potential.

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

The drug is used only in a hospital. Patients should not drive vehicles or mechanisms for at least 24 hours after the administration of suxamethonium iodide.

Form release / dosage:

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

Packaging:

But 5 ml into neutral glass ampoules.

For 10 ampoules with instructions for use and a knife ampoule or scarifier ampoule placed in a box of cardboard.

By 5 or 10 ampoules are placed in a contour cell box from the film polyvinyl chloride or polyethylene terephthalate tape and aluminum foil, or paper with a polyethylene coating, or without a foil, or without paper.

1 or 2 contour packs with instructions on application and a knife ampoule or scarifier ampullum is placed in a pack of cardboard.

When you pack the ampoules with a break ring or break point, the ampoule knife or ampoule scapegrator is not inserted.

Storage conditions:

In the dark place at a temperature of 2 to 8 ° C.

Do not freeze.

Keep out of the reach of children.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-004086

Date of registration:19.01.2017

Expiration Date:19.01.2022

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Suxamethonium iodide (Suxamethonium iodide)