Composition, form of production and packaging
The solution for intravenous administration is transparent or almost transparent, from colorless to light yellow in color.
1 ml of 1 amp.
atracurium bezylate 10 mg 50 mg
[PRING] benzenesulfonic acid to pH 3.0-3.8, water d / and up to 5 ml.
5 ml - ampoules (5) - contour plastic packaging (1) - cardboard packs.
5 ml - ampoules (5) - contour plastic packaging (2) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Nondepolarizing muscle relaxant of peripheral action. Reducing the sensitivity of N-holinoretseptorov skeletal muscles to acetylcholine, blocks neuromuscular transmission, causes a temporary relaxation of skeletal muscles (including respiratory). It has a rapid onset of action (within 2-2.5 minutes), which allows intubation of the trachea in the first 90 seconds from the moment of its administration in doses of 0.5-0.6 mg / kg.
In doses of 0.2-0.6 mg / kg causes a predicted, proportional to the amount of the administered dose, the relaxation of skeletal muscles lasting 20-35 minutes. The rate of recovery of the neuromuscular transmission after the administration of atracurium bezylate (single and repeated) is constant, which allows the administration of repeated doses at predetermined time intervals. Restoration of normal neuromuscular transmission without the use of cholinesterase inhibitors - after 35 min, does not depend on the magnitude of the total dose and the function of the excretory and metabolism organs. Promotes the release of histamine.
The clinical duration of action after intravenous administration (the period of spontaneous recovery of 25% contractility of skeletal muscles) is 35-45 min, the total duration (the period of spontaneous recovery of 90% contractility of skeletal muscles) is 60-70 min.
PHARMACOKINETICS
Binding to plasma proteins is high. The time to reach C max in blood plasma is 1.7-10 minutes (on average 3-5 minutes). The duration of neuromuscular blocking action does not depend on the intensity of hepatic metabolism and the rate of excretion by the kidneys. At physiological values, the pH of the blood and body temperature without the participation of enzymes decays (Hoffman's elimination) into laudanosine and quaternary monoacrylate; in a small degree hydrolyzed by butyrylcholinesterase, therefore the duration of action does not depend on the function of the liver and kidneys. Metabolites are pharmacologically inactive.Physiological changes in blood pH have little effect on the duration of the action. Under hypothermia (body temperature 25-26 В° C), the rate of inactivation decreases.Do not cumulate. Do not penetrate the placental barrier at clinically significant concentrations. The half-distribution period is 2-3.4 minutes. T 1/2 - 20 min. It is excreted by the kidneys and intestines (less than 10% - unchanged).
INDICATIONS
- to maintain myoplegia and intubation of the trachea and artificial ventilation (IVL) during surgical operations;
- for ventilation in intensive care units.
DOSING MODE
In / in.
Adults
Doses of Ridelat-S are set individually and depend on the necessary duration and depth of the neuromuscular blockade.
Bolus injection
Recommended doses for adults are 0.3-0.6 mg / kg (depending on the required duration of neuromuscular blockade), which provide adequate myoplegia within 15-35 minutes.
Intubation of the trachea can be performed within 90 seconds after intravenous administration of Ridelat-C in a dose of 0.5-0.6 mg / kg.
The duration of a complete neuromuscular block can be increased by the addition of additional doses of Ridelat-C at a rate of 0.1-0.2 mg / kg, which is not accompanied by a cumulation of the effect of the drug.
Neuromuscular conduction can be quickly restored under the influence of cholinesterase inhibitors (neostigmine methyl sulfate and eudrophonia chloride) in combination with atropine (without signs of recurrence).
Infusion introduction
After initial bolus administration of Ridelat-C in a dose of 0.3-0.6 mg / kg, it can be administered by continuous infusion at a rate of 03-0.6 mg / kg / h to maintain neuromuscular blockade during prolonged surgical operations. This way of administering Ridelat-C can be recommended for operations on the lungs and heart. With artificial hypothermia to maintain complete myoplegia, the infusion rate should be reduced approximately 2-fold.
Children
The dose in children 1-24 months is 0.3-0.4 mg / kg; Children older than 1 year of Ridelat-S are prescribed in the same doses as adults , in terms of body weight.Dosages for children younger than 1 month are not established.
Elderly people
Elderly patients of Ridelat-S are prescribed in standard doses, however, it is preferable to use the lower level of the recommended dose range and administer the drug slowly.
Application for violations of the liver or kidney function
If the liver and / or kidney function is impaired, incl. at the terminal stage of hepatic or renal failure, Ridelat-C is administered in standard doses.
Application for diseases of the cardiovascular system
In patients with severe cardiovascular pathology, the initial dose of Ridelat-C should be administered for at least 60 seconds.
Application in intensive care units
To maintain myoplegia after initial bolus administration at a dose of 0.3-0.6 mg / kg, Ridelat-C can be administered by continuous infusion at a rate of 11-13 Ојg / kg / min (0.65-0.78 mg / kg / h). In different patients, the dose is not the same and may change over time. Some patients may require low doses such as 4.5 Ојg / kg / min (0.27 mg / kg / h), and high doses such as 29.5 Ојg / kg / min (1.77 mg / kg / h). Spontaneous recovery of neuromuscular conduction usually occurs approximately 60 minutes after the infusion of Ridelat-C and its rate does not depend on the duration of administration of the drug.
Instruction for breeding
Ridelat-C is compatible with the following infusion solutions.
Infusion solutions Stability period
Sodium chloride solution for intravenous infusions (0.9%) 24 h
Dextrose solution for intravenous infusions (5%) 8 h
Ringer's injection for 8 hours
A solution of sodium chloride (0.18%) and dextrose (4%) for IV infusions 8 h
Hartman's solution for injections 4 h
The solution of Ridelat-C, when diluted with compatible infusion solutions until atraquarium besylate concentration is at least 0/5 mg / ml, remains stable for a specified period of time under normal illumination at temperatures up to 30 В° C.
SIDE EFFECT
From the cardiovascular system: a decrease or increase in blood pressure, moderate tachycardia, arrhythmia.
Allergic reactions: bronchospasm, laryngospasm, edema, erythema, skin rash, hives, itchy skin, anaphylactoid reactions.
Other: increased intraocular pressure, drooling, rhabdomyolysis, manifested by myoglobinemia and myoglobinuria (may, especially in children, lead to the development of acute kidney failure), malignant hyperthermia, convulsions.
Local reactions: hyperemia at the injection site.
CONTRAINDICATIONS
- newborns and children under 1 month (more sensitive to the effects of nondepolarizing muscle relaxants, doses for children under 1 month are not established);
- Hypersensitivity to the drug (or its components) and to histamine.
With caution: bronchial cancer, dysfunction of the respiratory system (including respiratory depression), dehydration, severe disturbances of acid-base balance, hypotension, hypothermia, myasthenia gravis, pregnancy, lactation.
PREGNANCY AND LACTATION
Ridelat-S should not be used during pregnancy if the potential benefit to the mother does not exceed the possible risk to the fetus.
Ridelat-C can be used for the purpose of muscle relaxation during a caesarean section, because when administered at the recommended dose range, it penetrates the placenta in small amounts.
Penetrating through the placenta in small amounts, does not cause side effects in newborns, so it can be used during caesarean section (always bear in mind the potential for respiratory depression and decreased muscle activity in newborns).
There are no data on the penetration of the drug into breast milk.
APPLICATION FOR FUNCTIONS OF THE LIVER
In case of impaired renal function, incl. at the terminal stage of renal failure, Ridelat-C is administered in standard doses.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
When the liver function is impaired, incl. at the terminal stage of hepatic insufficiency, Ridelat-C is administered in standard doses.
APPLICATION FOR CHILDREN
The dose in children 1-24 months is 0.3-0.4 mg / kg; Children older than 1 year of Ridelat-S are prescribed in the same doses as adults , in terms of body weight.Dosages for children younger than 1 month are not established.
Contraindicated in newborns and children up to 1 month (more sensitive to the effects of nondepolarizing muscle relaxants).
APPLICATION IN ELDERLY PATIENTS
Elderly patients of Ridelat-S are prescribed in standard doses, however, it is preferable to use the lower level of the recommended dose range and administer the drug slowly.
SPECIAL INSTRUCTIONS
Like other muscle relaxants, atracurium bezylate causes paralysis of skeletal muscles, including the respiratory muscles, but does not affect consciousness, atracuria besylate should be used only during general anesthesia under the supervision of a qualified anesthesiologist in departments where there is equipment for intubation of the trachea and ventilation.
With the introduction of drugs for general anesthesia through the same needle or catheter, after each injection, the catheter should be washed with 0.9% sodium chloride solution.
The advantage over other non-depolarizing muscle relaxants is the absence of cumulation in repeated injections (with repeated bolus and drip administration there is no need to change the dosage regimen). The evoked neuromuscular block is quickly and completely eliminated by neostigmine bromide, which is preceded by the administration of atropine (complete neuromuscular blockade is eliminated after 5-10 min and does not depend on the total amount of administered dose, on the age of the patient and on the presence of hepatic-renal pathology).
In patients with severe myasthenia gravis, other neuromuscular diseases and severe electrolyte imbalance, hypersensitivity phenomena can occur.
It does not affect consciousness, therefore, the drug should be used only in combination with adequate general anesthesia, under the supervision of an experienced anesthesiologist and with funds for endotracheal intubation and ventilation.
When assigned to the recommended dose range of atracurium, besylate does not block the vagus nerve and nerve ganglia, does not significantly affect the heart rate and does not prevent bradycardia caused by anesthetics or vagal nerve stimulation during surgery.
Atracurium bezylate is inactivated in an alkaline medium and should not be mixed in one syringe with sodium thiopental or alkaline solutions. A solution of atracurium bezylate is hypotonic and should not be used simultaneously through a single system with blood transfusions.
In patients with burns, resistance to non-depolarizing muscle relaxants may develop, which will require an increase in the doses of these drugs, the magnitude of which depends on the length of time since the burn and on the surface area of ​​the burn.
OVERDOSE
Symptoms: lengthening of the neuromuscular block and its consequences (excessive decrease in blood pressure, collapse, respiratory arrest, paralysis of muscles, shock).
Treatment: IVL on the background of sedation before the restoration of spontaneous breathing, the introduction of antagonists - inhibitors of cholinesterase in combination with atropine, in case of collapse and shock - recovery of the circulating blood volume, the appointment of hypertensive medications, symptomatic therapy.
DRUG INTERACTION
Ether diethyl, to a lesser extent halothane, hexobarbital, sodium thiopental strengthen and prolong the action of atracurium besylate.
Aminoglycosides and polypeptide antibiotics (polymyxins), spectinomycin, capreomycin, amphotericin B, trimethoprim, tetracyclines, lincomycin, clindamycin, antiarrhythmics (propranolol, slow calcium channel blockers, lidocaine, procainamide, quinidine), procaine ), diuretics (furosemide, ethacrynic acid, indapamide, mannitol, thiazide, acetazolamide), glucocorticosteroids (GCS), mineralocorticoids, magnesium sulfate, ketamine, lithium salts, ganglion blockers (trimetaphane camsylate, hexamethonium benzenesulfonate), depolaris guides relaxants, citrate enhance neuromuscular blockade.
Atracuria bezilat reduces the effect of cholinesterase inhibitors, incl. eudrophonia chloride (you may need to adjust their doses).
Antibiotics, beta-blockers (propranolol, oxprenolol), antiarrhythmic drugs (procainamide, quinidine), antirheumatic drugs (chloroquine, D-penicillamine), trimetaphane camsylate, chlorpromazine, steroids, phenytoin, lithium preparations can enhance or unmask the latent myasthenia gravis or cause myasthenic syndrome, which can lead to the development of hypersensitivity to the drug.
Opioid analgesics increase respiratory depression.
High doses of sufentanil reduce the need for high initial doses of nondepolarizing muscle relaxants. Nonprolarizing muscle relaxants prevent or reduce the rigidity of muscles caused by high doses of opioid analgesics (including alfentanil, fentanyl, sufentanil), while the risk of bradycardia and lowering blood pressure caused by opioid analgesics (especially in patients with impaired myocardial function and / destination or background beta-blockers), moreover - increases the risk of hypotension (use of histamine H 1 - or H 2 receptor may reduce or prevent the development of the severity of these adverse effects).
Atracuria besylate increases histamine-dependent side effects caused by opioid analgesics (with the exception of alfentanil, fentanyl and sufentanil, not causing histamine release).
Inhalational anesthetics (including enflurane, isoflurane) enhance the effect (the dose of peripheral muscle relaxants should be reduced to 1 / 3-1 / 2 of the usually recommended).
Calcium preparations reduce the effect.
Doxapram temporarily masks the residual effects of muscle relaxants.
The depolarizing muscular relaxant suxamethonium chloride should not be prescribed to increase the duration of neuromuscular conduction caused by nondepolarizing blockers, as this can cause a blockade that is complex for the inhibition of cholinesterase inhibitors and its lengthening.
Do not mix in one syringe with thiopental sodium or other alkaline solution (inactivation).
The Ridelat-S solution is hypotonic and should not be applied simultaneously through a single system with blood transfusions.
Compatible with the following solutions for infusions (at a concentration of 0.5-0.9 mg / ml in daylight and temperature up to 30 В° C): 0.9% sodium chloride solution for IV administration - for at least 24 hours, 5% dextrose solution for / in the introduction of -8 h, Ringer's injection for 8 hours, a solution of sodium chloride 0.18% and dextrose 4% for iv injection - 8 hours, solution of sodium salt of lactic acid (Hartman's solution) for IV administration - 4 h .
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
In the dark place at a temperature of 2 to 8 В° C. Do not freeze. Keep out of the reach of children.
Shelf life - 2 years. Do not use after the expiration date printed on the package.
