Gross formula
C 14 H 30 Cl 2 N 2 O 4Pharmacological group of the substance Suxamethonium chloride
Nosological classification (ICD-10)
CAS code
71-27-2Characteristics of the substance Suxamethonium chloride
White fine crystalline powder. Easily soluble in water, very little in alcohol.
Pharmacology
pharmachologic effect- muscle relaxant.Depolarizes the postsynaptic myoneural membrane. Resistant to the effects of synaptic cholinesterase, therefore, causes prolonged depolarization of the muscle fiber and blockade of neuromuscular transmission, which is prolonged by anticholinesterase agents. With repeated or prolonged use, there is a transition to a non-polarization block with the development of prolonged respiratory depression and apnea. Promotes the release of histamine from the depot. The effect develops in 0.5-1 min (in / in) or 3 minutes (in / m). The duration of the effect with intravenous administration is 4-10 minutes (maximum after 1-2 minutes), with intramuscular injection - 10-30 minutes. Destroyed by plasma pseudocholinesterase. Excreted by the kidneys (10% unchanged).
Application of the substance Suxamethonium chloride
Muscle relaxation during surgical interventions: reduction of dislocations, reposition of bone fragments; electropulse therapy.
International name
Suxamethonium chloride (Suxamethonium chloride)Group affiliation
Muscle relaxant depolarizing peripheral actionDosage form
Solution for intravenous and intramuscular administrationpharmachologic effect
Short acting depolarizing muscle relaxant. Causes blockade of neuromuscular transmission. Interacting with n-cholinergic receptors, causes depolarization of the end plate. The process extends to the adjacent membranes, a generalized disorganized contraction of myofibrils occurs (i.e., the development of the blockade is preceded by muscle twitches - the result of a short-term relief of neuromuscular transmission). The membranes, remaining depolarized, do not respond to additional impulses, since in order to maintain muscle tone the arrival of repeated impulses associated with repolarization of the end plate is required, spastic paralysis occurs. After intravenous administration, muscle relaxation occurs in the following sequence: eyelid muscles, 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 under general anesthesia.
After the / m administration, the action develops after 2-4 minutes; after intravenous administration - after 54-60 s, after 2-3 minutes, muscle relaxation reaches a maximum and remains in full for 3 minutes. Duration of action - 5-10 minutes.
The severity of the action depends on the size of the administered dose: 0.1 mg / kg - relaxation of the skeletal muscles without a significant effect on the respiratory system, 0.2-1 mg / kg - complete relaxation of the muscles of the abdominal wall and respiratory muscles (there is a significant limitation or complete cessation of spontaneous breathing). For prolonged muscle relaxation, repeated administration is necessary. The rapid onset of the effect and the subsequent rapid recovery of muscle tone allow you to create controlled and controlled muscle relaxation.
Indications
Interventions requiring muscle relaxation (usually short-term): turning off spontaneous breathing (intratracheal intubation, bronchoscopy); complete muscle relaxation (endoscopy, reduction of dislocations, reduction of fractures, gynecological, thoracic, abdominal operations); prevention of seizures during electropulse therapy; strychnine poisoning, tetanus (symptomatic therapy).Contraindications
Hypersensitivity, malignant hyperthermia (including history), myasthenia gravis, congenital and dystrophic myotonia, Duchenne muscular dystrophy, angle-closure glaucoma, acute liver failure, pulmonary edema, penetrating eye injury, bronchial asthma, hyperkalemia, infancy(up to 1 year), pregnancy. With caution. Emergency surgery in patients with a "full stomach", decreased serum cholinesterase activity (end-stage liver failure), anemia, cachexia, prolonged fasting, chronic infections, widespread burns, trauma, postpartum period, tetanus, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, collagen diseases, conditions after plasma transfusion, plasmapheresis, cardiopulmonary bypass, acute or chronic intoxication with insecticides - cholinesterase inhibitors (when ingested) or anticholinesterase drugs (neostigmine, physostigmine, distigmine, phospholine), simultaneous use of drugs that compete with suxamethonium for cholinesterase (for example procaine IV).Side effects
Allergic reactions (anaphylactic shock, bronchospasm); hyperkalemia, decreased blood pressure, arrhythmias, bradycardia (more often in children, with repeated administration - in children and adults), conduction disturbance, cardiogenic shock; increased intraocular pressure, hypersalivation, fever; myalgia (in the postoperative period); prolonged 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.Application and dosage
In / in (stream, drip), in / m.
Adults: in / in slowly, by stream or drip (for long-term drip infusion, a 0.1% solution is used). Depending on the clinical situation with intravenous administration, a single dose varies from 0.1 to 1.5-2 mg / kg.
V / m - 3-4 mg / kg, but not more than 150 mg. V / m is used in children in doses up to 2.5 mg / kg, but not more than 150 mg, in / in - 1-2 mg / kg.
For tracheal intubation - 0.2-0.8 mg / kg; for muscle relaxation and switching off spontaneous breathing - 0.2-1 mg / kg; for relaxation of skeletal muscles during reduction of dislocations and reposition of bone fragments in fractures - 0.1-0.2 mg / kg; for endoscopy and EEG - 0.2 mg / kg; for the prevention of complications during electrical impulse therapy (convulsions, avulsion of muscles and tendons) - 0.1-1 mg / kg IV and up to 2.5 mg / kg IV, but not more than 150 mg.
For long-term relaxation of the muscles during the entire operation, it can be administered fractionally, after 5-7 minutes, at a dose of 0.5-1 mg/kg. Repeated doses last longer.
special instructions
Introduction 1 min before suxamethonium chloride 3-4 mg of d-tubocurarine or 10-15 mg of diplacin almost completely prevents muscle twitching and subsequent myalgia.
With an appropriate dose and repeated administration, it can also be used for longer operations, however, for prolonged muscle relaxation, non-depolarizing muscle relaxants are usually used, which are administered after preliminary tracheal intubation against the background of suxamethonium.
They are used only in the conditions of a specialized department in the presence of equipment for artificial ventilation of the lungs and personnel who own this equipment, and against the background of general anesthesia.
To prevent severe bradycardia, increase bronchial secretion, and other effects associated with m-anticholinergic action, it is recommended to administer atropine before the administration of suxamethonium.
Patients with renal insufficiency (without signs of hyperkalemia and neuropathy) are administered once at medium doses, but are not used for multiple injections or at higher doses due to the risk of developing hyperkalemia.
Protracted muscle relaxation with possible apnea can be caused by several reasons: "atypical" serum cholinesterase, hereditary deficiency of serum cholinesterase or a temporary decrease in its concentration in severe liver diseases, severe anemia, after prolonged fasting, with cachexia, dehydration, febrile conditions, after acute poisoning or chronic exposure to insecticides - cholinesterase inhibitors (when ingested) or anticholinesterase drugs (neostigmine, physostigmine, distigmine, phospholine), as well as with the simultaneous use of drugs that compete with suxamethonium for cholinesterase (for example, procaine in / in).
With prolonged administration at doses of 3-5 mg / kg, the so-called "double block" may develop - prolonged curariform action, which can be eliminated by neostigmine.
Interaction
Enhances the effects of cardiac glycosides.
Reduces the effectiveness of antimyasthenic drugs.
Pharmaceutically incompatible with donor blood (hydrolysis occurs), blood preservatives, serum preservatives, blood products, barbiturate solutions (precipitation) and alkaline solutions. Compatible with 0.9% NaCl solution, Ringer's solution, 5% fructose solution and 6% dextran solution.
Anticholinesterase drugs, procaine, procainamide, lidocaine, verapamil, beta-blockers, aminoglycoside antibiotics, amphotericin B, clindamycin, cyclopropane, propanidide, organophosphorus insecticides, Mg2+ and Li+ salts, quinidine, quinine, chloroquine, pancuronium, enhance and lengthen the muscle relaxant effect. Compatible with other muscle relaxants, narcotic analgesics.
Drugs with the potential ability to reduce the activity of blood cholinesterase (aprotinin, diphenhydramine, promethazine, estrogens, oxytocin, corticosteroids in high doses, oral contraceptives) increase and prolong the muscle relaxant effect of suxamethonium.
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Do you use Suxamethonium chloride as an analogue or vice versa?Release form, composition and packaging
Solution for intravenous and intramuscular administration transparent, colorless or slightly yellowish.
Excipients: sodium chloride, disodium salt of ethylenediaminetetraacetic acid (trilon B), water for injection.
5 ml - ampoules (5) blister packs (1) - cardboard packs.
5 ml - ampoules (5) blister packs (2) - cardboard packs.
5 ml - ampoules (10) - packs of cardboard.
pharmachologic effect
Depolarizing muscle relaxant of peripheral action. Causes blockade of neuromuscular transmission. Interacting with n-cholinergic receptors, causes depolarization of the end plate. The process extends to the adjacent membranes, a generalized disorganized contraction of myofibrils occurs (i.e., the development of the blockade is preceded by muscle twitches - the result of a short-term relief of neuromuscular transmission). The membranes, remaining depolarized, do not respond to additional impulses, since repeated impulses associated with repolarization of the end plate are required to maintain muscle tone, spastic paralysis occurs. After intravenous administration, muscle relaxation occurs in the following sequence: muscles of the fingers, eyes, legs, neck, back; then intercostal muscles and diaphragm. Increases cerebral blood flow and intracranial pressure under general anesthesia.
After the / m administration, the action develops after 2-4 minutes; after intravenous administration - after 54-60 seconds, after 2-3 minutes, muscle relaxation reaches a maximum and remains in full for 3 minutes. Duration of action - 5-10 minutes. The severity of the action depends on the size of the administered dose: 100 mcg / kg - relaxation of the skeletal muscles without a significant effect on the respiratory system; 0.2-1 mg / kg - complete relaxation of the muscles of the abdominal wall and respiratory muscles (there is a significant limitation or complete cessation of spontaneous breathing). For prolonged muscle relaxation, repeated administration is necessary. The rapid onset of the effect and the subsequent rapid recovery of muscle tone allow you to create a controlled controlled relaxation of the muscles.
Pharmacokinetics
Distribution
After intravenous administration, it is distributed in plasma and extracellular fluid. Does not penetrate the intact BBB. Does not accumulate.
Metabolism
More than 90% is hydrolyzed by blood cholinesterase to succinic acid and choline.
breeding
T 1/2 is 90 seconds at a normal level of cholinesterase. Excreted by the kidneys - 10% unchanged.
Indications
Interventions requiring short-term muscle relaxation:
- shutdown of spontaneous breathing (intratracheal intubation, bronchoscopy);
- complete muscle relaxation (endoscopy, reduction of dislocations, reduction of fractures, gynecological, thoracic and abdominal operations);
— prevention of convulsions during electropulse therapy;
- strychnine poisoning;
- tetanus (symptomatic therapy).
Contraindications
— malignant hyperthermia (including history);
- myasthenia gravis;
— congenital and dystrophic myotonia;
- Duchenne muscular dystrophy;
- angle-closure glaucoma;
- acute liver failure;
-pulmonary edema;
- penetrating eye injury;
— deficiency of cholinesterase;
-bronchial asthma;
— hyperkalemia;
-pregnancy;
- children's age up to 1 year;
- Hypersensitivity to the components of the drug.
Carefully: emergency surgery in patients with a "full stomach", decreased serum cholinesterase activity (end-stage liver failure), anemia, cachexia, prolonged fasting, chronic infections, widespread burns, trauma, postpartum period, tetanus, heart failure, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, collagen diseases, after plasma transfusion, plasmapheresis, cardiopulmonary bypass, acute or chronic intoxication with insecticides - cholinesterase inhibitors (when ingested) or anticholinesterase agents (neostigmine, physostigmine, distigmine, phospholine), simultaneous administration of drugs that compete with suxamethonium for cholinesterase (including IV procaine).
Dosage
The drug is administered intravenously (stream, drip), intramuscularly.
Adults administered in / in slowly, stream or drip. Depending on the clinical situation, with intravenous administration, a single dose varies from 100 mcg / kg to 1.5-2 mg / kg.
V / m is administered at a dose of 3-4 mg / kg, but not more than 150 mg.
children the drug is administered intramuscularly in doses up to 2.5 mg/kg, but not more than 150 mg, intravenously - at a dose of 1-2 mg/kg.
For performing tracheal intubation the dose is 200-800 mcg/kg; for muscle relaxation and shutdown of spontaneous breathing the dose is 0.2-1 mg/kg; for relaxation of skeletal muscles during reduction of dislocations and reposition of bone fragments in fractures- 100-200 mcg/kg, for endoscopy the dose is 200 mcg/kg; for prevention of complications during electroshock therapy (convulsions, avulsion of muscles and tendons)- 0.1-1 mg / kg IV, but not more than 150 mg. For long-term relaxation of the muscles during the entire operation, it can be administered fractionally, after 5-7 minutes, at a dose of 0.5-1 mg/kg. Repeated doses last longer.
Side effects
Allergic reactions: anaphylactic shock, bronchospasm.
From the side of water and electrolyte balance: hyperkalemia.
From the side of cardio-vascular system: arrhythmias, decreased blood pressure, bradycardia (more often in children, with repeated administration - in children and adults), conduction disturbances, cardiogenic shock.
From the side of the organ of vision: increase in intraocular pressure.
From the musculoskeletal system: myalgia (in the postoperative period), rhabdomyolysis with the development of myoglobinemia and myoglobinuria.
From the respiratory system: prolonged paralysis of the respiratory muscles (associated with a genetically determined violation of the production of pseudocholinesterase).
Others: hypersalivation, fever.
Overdose
Symptoms: stop breathing.
Treatment: artificial ventilation of the lungs, in case of a decrease in the content of cholinesterase in the blood serum - whole blood transfusion.
drug interaction
Suxamethonium chloride enhances the effects of cardiac glycosides, reduces the effectiveness of drugs for the treatment of myasthenia gravis.
Anticholiesterase agents, procaine, procainamide, lidocaine, antibiotics of the aminoglycoside group, procainamide, verapamil, beta-blockers, amphotericin B, clindamycin, cyclopropane, propanidide, organophosphorus insecticides, magnesium and lithium salts, quinidine, quinine, pancuronium, as well as drugs with potential the ability to reduce the activity of blood cholinesterase (aprotinin, diphenhydramine, promethazine, estrogens, oxytocin, corticosteroids in high doses, oral contraceptives) increase the intensity and duration of the muscle relaxant action.
Pharmaceutical interaction
Suxamethonium chloride is pharmaceutically incompatible with donor blood (hydrolysis occurs), blood preservatives, serum preservatives, blood products, barbiturate solutions (precipitation forms) and alkaline solutions.
Suxamethonium chloride is compatible with 0.9% sodium chloride solution, Ringer's solution, 5% fructose solution and 6% dextran solution.
Suxamethonium chloride is compatible with other muscle relaxants, opioid analgesics.
special instructions
The drug should be used only in the conditions of a specialized department, in the presence of equipment for artificial ventilation of the lungs and personnel who own this equipment, and against the background of general anesthesia.
The introduction of d-tubocurarine (3-4 mg) or diplacin (10-13 mg) 1 min before suxamethonium almost completely prevents muscle twitching and subsequent myalgia.
With the appropriate dose and repeated administration, suxamethonium can be used for longer operations, however, for prolonged muscle relaxation, non-depolarizing muscle relaxants are usually used, which are administered after preliminary tracheal intubation against the background of suxamethonium.
To prevent severe bradycardia, increased bronchial secretion and other effects associated with the m-anticholinergic action, it is recommended to administer atropine before the administration of suxamethonium.
In patients with chronic renal failure (without signs of hyperkalemia and neuropathy), suxamethonium is administered once at medium doses, but not used for repeated administration or at elevated doses due to the risk of hyperkalemia.
Prolonged muscle relaxation with possible apnea can be caused by several reasons: serum pseudocholinesterase, hereditary deficiency of serum cholinesterase or a temporary decrease in its level in severe liver disease, severe anemia, after prolonged starvation, cachexia, dehydration. In febrile conditions, after acute poisoning, or chronic exposure to insecticides - cholinesterase inhibitors (when ingested) or anticholinesterase agents (neostigmine, physostigmine, distigmine, phospholine), as well as with the simultaneous use of drugs that compete with suxamethonium for cholinesterase (including procaine IV). With prolonged administration at doses of 3-5 mg / kg, the so-called double block may develop - a prolonged curare-like effect that can be eliminated by neostigmine.
Pregnancy and lactation
For impaired liver function
With caution: a decrease in serum cholinesterase activity (end-stage liver failure.
Terms and conditions of storage
List A. The drug should be stored in a place protected from light at a temperature of 2 ° to 8 ° C. Shelf life - 3 years.
Keep out of reach of children.
Terms of dispensing from pharmacies
The drug is dispensed by prescription.
Interventions requiring short-term muscle relaxation:
Disabling spontaneous breathing (intratracheal intubation, bronchoscopy);
Complete muscle relaxation (endoscopy, reduction of dislocations, reduction of fractures, gynecological, thoracic and abdominal operations);
Prevention of seizures during electropulse therapy;
Strychnine poisoning;
Tetanus (symptomatic therapy).
Application for violations of kidney function
Application for violations of liver function
With caution: a decrease in serum cholinesterase activity (end-stage liver failure.special instructions
The drug should be used only in the conditions of a specialized department, in the presence of equipment for artificial ventilation of the lungs and personnel who own this equipment, and against the background of general anesthesia.
The introduction of d-tubocurarine (3-4 mg) or diplacin (10-13 mg) 1 min before suxamethonium almost completely prevents muscle twitching and subsequent myalgia.
With the appropriate dose and repeated administration, suxamethonium can be used for longer operations, however, for prolonged muscle relaxation, non-depolarizing muscle relaxants are usually used, which are administered after preliminary tracheal intubation against the background of suxamethonium.
To prevent severe bradycardia, increased bronchial secretion and other effects associated with the m-anticholinergic action, it is recommended to administer atropine before the administration of suxamethonium.
In patients with chronic renal failure (without signs of hyperkalemia and neuropathy), suxamethonium is administered once at medium doses, but not used for repeated administration or at elevated doses due to the risk of hyperkalemia.
Prolonged muscle relaxation with possible apnea can be caused by several reasons: serum pseudocholinesterase, hereditary deficiency of serum cholinesterase or a temporary decrease in its level in severe liver disease, severe anemia, after prolonged starvation, cachexia, dehydration. In febrile conditions, after acute poisoning, or chronic exposure to insecticides - cholinesterase inhibitors (when ingested) or anticholinesterase agents (neostigmine, physostigmine, distigmine, phospholine), as well as with the simultaneous use of drugs that compete with suxamethonium for cholinesterase (including procaine IV). With prolonged administration at doses of 3-5 mg / kg, the so-called double block may develop - a prolonged curare-like effect that can be eliminated by neostigmine.
On our website you will find detailed information about the drug SUXAMETHONIUM CHLORIDE (solution) and its instructions for use in Russian. Instructions for use contain information about the composition, indications for use, contraindications, dosage, features of admission in children, during pregnancy and lactation, interaction with other drugs, about side effects and an overdose of SUXAMETHONIUM CHLORIDE. You can also get acquainted with the conditions and shelf life of the drug SUXAMETHONIUM CHLORIDE and its analogues.