Composition, form of production and packaging
Solution for intravenous and / m administration 1 ml 1 amp.
suxamethonium iodide 20 mg 100 mg
5 ml - ampoules (10) - packs of cardboard.
5 ml - ampoules (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Depolarizing short-acting muscle relaxant. It causes a blockade of the neuromuscular transmission. Interacting with H-holinoretseptorami, causes depolarization of the terminal plate. The process extends to adjacent membranes, a generalized disorganized contraction of myofibrils occurs (that is, the development of 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 administration, muscle relaxation occurs in the following sequence: the muscles of the eyelids, the chewing muscles, the muscles of the fingers, the eyes, the limbs, the neck, the back and the abdomen, the vocal cords, then the intercostal muscles and the diaphragm.
Causes an increase in cerebral blood flow and increased intracranial pressure. After iv introduction, the effect begins after 54-60 sec, after 2-3 min the muscle relaxation reaches a maximum and remains in full for 3 min. The duration of action is 5-10 minutes.
The severity of the action depends on the amount of the administered dose: 0.1 mg / ml - 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
After intravenous administration is distributed in plasma and extracellular fluid. More than 90% is hydrolyzed by cholinesterase of blood to succinic acid and choline.The half-life period is 90 sec with a normal level of pseudocholinesterase. It is excreted by the kidneys. Does not penetrate the intact blood-brain barrier. Do not cumulate.
INDICATIONS
- disabling of spontaneous breathing (intracela intubation, bronchoscopy);
- complete miorelaxation (endoscopy, correction of dislocations, reposition of fractures, gynecological, thoracic, abdominal operations);
- prevention of seizures in electropulse therapy;
- Strychnine poisoning;
- tetanus (symptomatic therapy).
DOSING MODE
Adults: iv, slow, jet or drip (for long-term drip infusion use 0.1% solution). Depending on the clinical situation, with iv administration, a single dose varies from 100 Ојg / kg to 1.5-2 mg / kg body weight.
For 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 when sprains are dislocated and reposition of bone fragments at fractures - 0.1-0.2 mg / kg; for endoscopy - 0.2 mg / kg; for prevention of complications during electropulse therapy (convulsions, muscle and tendon rupture) - 0.1-1 mg / kg IV, but not more than 150 mg.
For a long relaxation of the musculature throughout the operation can be introduced fractionally, after 5-7 minutes at 0.5-1 mg / kg. Repeated doses last longer.
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.
SIDE EFFECT
Allergic reactions (anaphylactic shock, bronchospasm); hyperkalemia.
Decrease in blood pressure, cardiac arrhythmia, arrhythmia, bradycardia (more often in children, with repeated administration in children and adults), 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. In children, young patients and women (mainly in the vagotonics), a short-term bradycardia may occur, in some cases, asystole.
After 10-12 hours after using the drug, muscle pain may occur. With repeated administration of the drug, excessively prolonged muscle relaxation and prolonged apnea can sometimes develop.
CONTRAINDICATIONS
hypersensitivity;
- malignant hyperthermia (including in the anamnesis);
- Myasthenia gravis;
- congenital and dystrophic myotonia;
- Duchenne muscular dystrophy;
- an angle-closure glaucoma;
acute liver failure;
- pulmonary edema;
penetrating eye trauma;
- bronchial asthma;
- gynecology;
- Children's age up to 1 year;
- Pregnancy;
lactation period.
Precautions: decrease in serum pseudocholinesterase activity (terminal stage of hepatic insufficiency, anemia, cachexia, prolonged fasting, chronic infections, common burns, traumas), postpartum period, tetanus, tuberculosis, malignant neoplasms, chronic renal failure, myxedema, systemic connective tissue diseases, state after plasma transfusion, plasmapheresis, artificial circulation, acute and chronic intoxication with insecticides - cholinesterase inhibitors (if ingested) or anticholinesterase drugs (neostigmine, physostigmine, distigmine bromide), simultaneous use of drugs competing with succinylcholine for cholinesterase (procaine intravenous), emergency surgical interventions in patients with a "full stomach".
PREGNANCY AND LACTATION
It is forbidden to take this drug during pregnancy and lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution: chronic renal failure. 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.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated: acute liver failure. With caution in reducing the activity of serum pseudocholinesterase (terminal stage of hepatic insufficiency).
APPLICATION FOR CHILDREN
It is forbidden to take the drug to children under the age of 1 year.
SPECIAL INSTRUCTIONS
Applied only in a specialized department with the availability of equipment for artificial ventilation and against general anesthesia. Pre-introduction for 1 minute before the infusion of suxamethonium iodide drug 3-4 mg tubocurarine chloride or 10-15 mg diplatcin chloride prevents fibrillar muscle twitching, and the subsequent appearance of muscle pain. With the appropriate dose and repeated administration, it can also be used for longer operations, however, for the long-term relaxation of the musculature, nondepolarizing muscle relaxants are usually used, which are administered after a pre-intubation of the trachea against a background of suxamethonium iodide.
Slow introduction of the drug, as well as preliminary intravenous injection of atropine at a dose of 1-1.5 mg significantly prevents bradycardia and increased bronchial secretion.
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. 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 level. If the drug is injected repeatedly and 25-30 minutes after the last injection, the patient does not restore muscle tone, there is superficial breathing, one can think of the transition of the depolarizing unit to an antidepolarizing one (the occurrence of a "double block"). To remove this effect, you should use proserine according to the usual method: pre-atropine is administered to the vein at a dose of 0.5-0.7 mg (0.5-0.7 ml of 0.1% solution), pulse arrivals are waiting and after 1-2 minutes IV injected prozerin at a dose of 1.5 mg (3 ml of a 0.05% solution).
OVERDOSE
Symptoms: increased severity of side effects, stopping breathing.
Treatment: artificial ventilation, in case of a decrease in the content of cholinesterase in the blood serum - transfusion of fresh blood.
DRUG INTERACTION
Pharmaceutically incompatible with donor blood and blood preparations (hydrolysis occurs), with solutions of barbiturates and alkaline solutions (a precipitate is formed).
Compatible with isotonic solutions of sodium chloride, Ringer's solution, 5% fructose solution and 6% dextran solution.
Anticholinesterase drugs, procaine, procainamide, lidocaine, verapamil, beta-adrenoblockers, aminoglycoside antibiotics, amphotericin B, clindamycin, cyclopropane, propanidide, organophosphate insecticides, Mg 2+ and Li + salts, quinidine, quinine, chloroquine, pancuronium strengthen and prolong the myorelaxing action .
Compatible with other muscle relaxants narcotic analgesics.
Strengthens the cardiac effects of cardiac glycosides (bradycardia).
Reduces the effectiveness of antimiasthenic drugs.
Halogen-containing agents for general anesthesia are enhanced, and thiopental sodium and atropine reduce the unwanted effects on the cardiovascular system.
Drugs that have the potential to reduce blood cholinesterase activity (aprotinin, diphenhydramine, promegazine, estrogens, oxytocin, high-dose glucocorticosteroids, oral contraceptives) increase and prolong the muscle relaxant action of suxamethonium iodide.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List A.
The drug should be stored in a place protected from light, inaccessible to children, at a temperature of +2 to +8 В° C. Freezing is not allowed.
Shelf life is 1 year and 6 months. Do not use after the expiry date printed on the package.
