A drug: SUXAMETHONIUM CHLORIDE (SUXAMETHONIUM CHLORIDE)
Active substance: suxamethonium chloride
ATX code: M03AB01
KFG: Muscle relaxant of peripheral action of the depolarizing type
ICD-10 codes (indications): A35, T65.1, Z51.4
Reg. number: Р №003409/01
Date of registration: 12.12.08
The owner of the reg. Award: SYNTHESIS (Russia)
PHARMACEUTICAL 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 injections.
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.
The description of the drug was approved by the manufacturer in 2005.
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 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: 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 skeletal muscles without a significant effect on respiratory system; 0.2-1 mg / kg - complete relaxation of the muscles abdominal wall and respiratory muscles (there is a significant limitation or complete cessation of spontaneous breathing). For prolonged muscle relaxation, repeated administration is necessary. Rapid onset of effect and subsequent fast recovery muscle tone allows you to create controlled controlled muscle relaxation.
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:
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).
DOSING MODE
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 EFFECT
Allergic reactions: anaphylactic shock, bronchospasm.
From the side of water and electrolyte balance: hyperkalemia.
From the side of the cardiovascular 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.
CONTRAINDICATIONS
Malignant hyperthermia (including history);
myasthenia;
Congenital and dystrophic myotonia;
Duchenne muscular dystrophy;
Angle-closure glaucoma;
Acute liver failure;
Pulmonary edema;
Penetrating eye injury;
Cholinesterase deficiency;
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).
PREGNANCY AND LACTATION
The drug is contraindicated for use during pregnancy.
Data on the safety of the drug during lactation is not provided.
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.
Protracted 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 fasting, with 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.
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 INTERACTIONS
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.
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.
Suxamethonium chloride (Suxamethonium chloride)
Group:
Active ingredients:
Dosage form:
solution for intravenous and intramuscular administration
Pharmachologic 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 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: 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 disturbances, 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. Overdose. Symptoms: respiratory arrest. Treatment: IVL, in case of a decrease in serum cholinesterase - fresh blood transfusion.
Dosage and administration:
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 - a prolonged curare-like effect, 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. Halogen-containing drugs for general anesthesia increase, and sodium thiopental and atropine reduce the undesirable effect on the cardiovascular system. 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.
Before using the drug Suxamethonium chloride consult your doctor!
In medical practice, a number of drugs are used, which are necessary, for example, to bring the patient's body into the state required for performing a surgical intervention. Certain procedures require artificially induced absolute muscle relaxation. For this purpose, the drug "Suxamethonium chloride" is often used (the trade name of the drug is "Listeon"). This medication is mostly used in specialized medical institutions. What is the essence of its pharmacological action? Is it dangerous to use the agent in question? What should be prepared for when using the substance "Suxamethonium chloride"? Description of the drug and some features of its use will be discussed later in this article.
Compound
The main active ingredient of the drug in question is suxamethonium chloride. Also, the composition of the drug includes such auxiliary components as ethylenediaminetetraacetic acid disodium salt or disodium edetate, as well as water for injection.
Release form
"Suxamethonium chloride", as a rule, is produced by manufacturers in the form of a solution (for both intramuscular and intravenous administration).
pharmachologic effect
The drug in question is a depolarizing muscle relaxant. Its action is short-lived. The active components of the drug effectively block neuromuscular transmission.
Muscle relaxation always occurs in the same sequence, which must be taken into account by medical personnel. So, it begins with the muscles of the eyelids, then affects the chewing muscles and the muscles of the fingers, eyes and all limbs. Then muscle relaxation reaches the neck area, the muscles of the back, abdomen and vocal cords relax. The last to react to the action of the drug are the intercostal muscles and the diaphragm.
If the medicine was administered intramuscularly, then it will begin to act after two to four minutes, and if intravenously, already after a minute. Maximum muscle relaxation occurs three minutes after the administration of the drug. This action lasts for five to ten minutes, depending on the dose of the substance.
The drug is evenly distributed in blood plasma and extracellular fluid after a short time after the introduction of the solution (subject to intravenous administration). About ninety percent of the substance is hydrolyzed, transforming into choline or succinic acid. Provided that the concentration of cholinesterase in the blood is maintained at a sufficient level, the half-life of the drug is only ninety seconds. The substance is fully excreted by the kidneys (including ten percent - unchanged).
Indications for use
The drug in question is used in cases where an intervention is required that requires complete relaxation of the muscles. These conditions include bronchoscopy, endoscopy, abdominal surgery, fracture reduction, reduction of dislocations, and endotracheal intubation.
Mode of application
The substance "Suxamethonium chloride" can be administered intramuscularly and intravenously (both drip and jet). For this method of application, a 0.1% solution of the substance is used. The working dose in which suxamethonium chloride and iodide are used is prescribed individually by a specialist in accordance with the individual characteristics of a particular patient and, as a rule, with intravenous administration ranges from 0.1 to 2 milligrams per kilogram, and with intramuscular injection - from 3 to 4 micrograms per kilogram. In this case, in general, for the course of treatment, the total volume of the administered substance should not exceed one hundred and fifty micrograms.
Contraindications
Some patients should never receive Suxamethonium Chloride. Instructions for use of this drug informs about the following contraindications to the use of the drug: individual hypersensitivity to any of the constituent components of the drug, myasthenia gravis, bronchial asthma, angle-closure glaucoma, pulmonary edema, hyperkalemia, acute liver failure, congenital and dystrophic myotonia, cholinesterase deficiency, mechanical eye injury. It is also forbidden to use the medicine in question for children under one year old and for women during the period of bearing a child or breastfeeding.
Side effects
In rare cases, "Suxamethonium chloride" (solution for injection) can cause a number of unpleasant symptoms and manifestations from various systems organism. Among them are various kinds of allergic reactions (for example, bronchospasm and anaphylactic shock), paralysis of the respiratory muscles (occurs if there are genetic disorders in the formation of serum cholinesterase), arrhythmia, myalgia, fever, bradycardia, hyperkalemia, hypersalivation, cardiogenic shock, decline blood pressure, violation of conductivity, increase in intraocular pressure. In order to avoid the occurrence of the above problems, it is important to strictly adhere to the recommendations regarding the use of the drug "Suxamethonium chloride". Analogues of the drug (at least some of them) have a much smaller number of side effects. Therefore, sometimes it would be wise to turn to them.
Overdose
In case of unintentional or deliberate excess of the recommended dose of the drug, some undesirable consequences for the patient's body may occur. The most dangerous of these is respiratory arrest. In this case, one cannot do without the help of specialists, otherwise a fatal outcome is possible. Urgent ventilation is required. Sometimes the level of cholinesterase in the blood serum drops sharply. Some experts recommend a fresh blood transfusion or, often safer, blood substitutes to treat this condition.
Special Instructions
It is recommended to administer high-quality non-depolarizing muscle relaxants one minute before the administration of the drug "Suxamethonium chloride". The description of the substance contains information that such an interaction eliminates the risk of subsequent manifestation of myalgia and muscle twitches. It is important to use the drug only in specialized departments of medical institutions, subject to the availability of the necessary equipment (including a ventilator) and competent personnel able to properly use this technique and make decisions in stressful situations. Since the use of the agent in question can cause bradycardia in the patient, it is recommended to administer the drug "Atropine" to the patient before using "Suxamethonium chloride".
Possibility of combination with other drugs
When using other medicines simultaneously with the drug in question, attention should be paid to whether such an interaction is permissible. "Suxamethonium chloride" instructions for use do not recommend the use in parallel with antimyasthenic drugs, as it significantly reduces the effectiveness of their action. The drug in question also enhances the pharmaceutical effect of glycosides. In no case should "Suxamethonium chloride" be used simultaneously with donor blood, as it provokes a hydrolysis reaction, any blood products, alkaline solutions and barbiturate solutions (contributes to precipitation).
Influence on the ability to concentrate attention (driving vehicles and complex mechanisms)
"Suxamethonium chloride" has a significant effect on the ability to concentrate and maintain attention. This means that in order to avoid accidents, it is necessary to avoid driving vehicles and any other activities that pose a threat to human life and health and require increased concentration attention, as well as a quick reaction and instant decision-making on the first day after the termination of the drug in question.
Storage conditions and shelf life
You can store "Suxamethonium chloride" under strictly defined conditions. Namely: the temperature in the place of storage should range from two to eight degrees Celsius. The drug should be located out of reach for children. The maximum shelf life of the medicinal product is three years from the date of its manufacture. After the specified period, it is not recommended to use the drug, because in this case it loses its beneficial features and may be dangerous to the patient.
The safety of the patient, the safety of his life is the responsibility of the doctors who treat him. Therefore, it is important that the heads of medical institutions make sure that the personnel of these institutions are competent in the use of drugs, the side effects of these drugs, and methods for eliminating the adverse reactions that have arisen. Similarly, hospital staff must have the necessary knowledge and skills to properly use the equipment at their disposal that can save a patient's life. This is especially true for drugs whose possible side effects can threaten the onset lethal outcome. It is to this group of drugs that "Suxamethonium chloride" belongs. Therefore, it should be used only if competent specialists who are able to use a ventilator are present during the procedure. This may be necessary if an adverse reaction such as respiratory arrest occurs. In this case, the coherence of the actions of doctors and their professional competence will be the decisive factors that will determine whether the patient will survive.
Sometimes doctors, for certain reasons (if there are some contraindications), decide to use another muscle relaxant - an analogue of Suxamethonium chloride (for example, Ditilin, which cannot be used only in the presence of glaucoma). It is important to trust the authoritative opinion of experts in this matter. Therefore, you should be sure of the professional competence of the doctor with whom you are cooperating.
Before you opt for the drug in question, you should learn everything about the substance "Suxamethonium chloride": trade name, analogues, contraindications, possible side effects, features of use and recommended dosages. The patient must also be well versed in what kind of medicine is administered to him. "Listenone" ("Suxamethonium chloride") is the trade name for the substance in question. Therefore, when you hear this name from the lips of a doctor, you will understand well how it will act in your body. This knowledge is necessary in order not to put your life at unnecessary risk. It is important to be as careful as possible about which drugs are given to you during treatment.
Trust your health only to professionals, choose the highest quality methods of treatment and the best drugs! Take care of yourself!
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 synaptic cholinesterase, therefore causing prolonged depolarization 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-polarizing block with the development of prolonged respiratory depression and apnea. Promotes the release of histamine from the depot. The effect develops after 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.
Contraindications
Hypersensitivity, bronchial asthma, myasthenia gravis, pregnancy.
Side effects of the substance Suxamethonium chloride
glaucoma attack, muscle pain in the postoperative period, arrhythmias, bradycardia, hypersalivation, bronchospasm, hypotension, rhabdomyolysis with the development of myoglobinemia and myoglobinuria, fever, allergic reactions.
Interaction
Potentiates respiratory suppression, vagal effects, histamine release caused by narcotic analgesics, cardiotonic activity of cardiac glycosides, reduces the effectiveness of antimyasthenic drugs. Anticholinesterase agents, magnesium and lithium salts, procainamide, quinidine, antidepolarizing muscle relaxants prolong the action.
Dosage form: Solution for intravenous and intramuscular administration. Compound:Composition per 1 ml.
Active substance: suxamethonium chloride - 20 mg.
Excipients: disodium edetate (ethylenediaminetetraacetic acid disodium salt [trilon B]), sodium chloride, water for injection.
Description:Clear or slightly opalescent, colorless or slightly yellowish solution.
Pharmacotherapeutic group:Muscle relaxant depolarizing peripheral action. ATX:M.03.A.B Choline derivatives
Pharmacodynamics:Short acting depolarizing muscle relaxant. Causes blockade of neuromuscular transmission. By stimulating n-cholinergic receptors, it 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: 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 intramuscular injection, 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. The duration of action is 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 muscles, 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.
Pharmacokinetics:After intravenous administration, it is distributed in plasma and extracellular fluid. More than 90% is hydrolyzed by blood cholinesterase to succinic acid and holim. The half-life is 90 s at normal concentrations of cholinesterase. Excreted by the kidneys (10% unchanged). Does not penetrate the intact blood-brain barrier. Does not accumulate. 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, cholinesterase deficiency, bronchial asthma, hyperkalemia, childhood up to 1 year, pregnancy and lactation. 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, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, systemic connective tissue diseases, conditions after plasma transfusion, plasmapheresis, operations under cardiopulmonary bypass, acute or chronic intoxication with insecticides - cholinesterase inhibitors (when ingested) or anticholinesterase agents (, physostigmine, ecotiopata iodide), simultaneous administration of drugs that compete with suxamethonium chloride for cholinesterase (for example, i.v.). Dosage and administration:Intravenously (stream, drip), intramuscularly.
Adults: intravenously 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. Intramuscularly - 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 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 electroencephalography - 0.2 mg / kg; for the prevention of complications during electrical impulse therapy (convulsions, avulsion of muscles and tendons) - 0.1-1 mg / kg intravenously and up to 2.5 mg / kg intramuscularly, 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 0.5-1 mg / kg. Repeated doses last longer.
Side effects: Allergic reactions (anaphylactic shock, bronchospasm); hyperkalemia, lowering blood pressure, arrhythmias, bradycardia (more often in children, 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. Overdose:Symptoms: respiratory arrest.
Treatment: artificial ventilation of the lungs, in case of a decrease in serum cholinesterase - transfusion of fresh blood.
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% sodium chloride solution, Ringer's solution, 5% fructose solution and 6% dextran solution.
Anticholinesterase agents, beta-blockers, aminoglycoside antibiotics, amphotericin B, cyclopropane, organophosphorus insecticides, magnesium and lithium salts, quinine, pancuronium bromide, enhance and lengthen the muscle relaxant action. Compatible with other muscle relaxants, narcotic analgesics.
Halogen-containing agents for general anesthesia increase, and sodium thiopental and reduce the undesirable effect on cardiovascular system. Drugs with the potential ability to reduce the activity of blood cholinesterase (aprotipine, estrogens, high-dose glucocorticosteroids, oral contraceptives) enhance and prolong the muscle relaxant effect of suxamethonium.
Special instructions:The introduction of non-depolarizing muscle relaxants 1 min before suxamethonium chloride 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 chloride. 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 suxamethonium chloride before administration. 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 agents (eg, physostigmine,