Atracuria besilate
Like other muscle relaxants, atracurium besilate causes paralysis of skeletal muscles, including respiratory muscles, but does not affect consciousness or pain threshold. The drug should only be used during general anesthesia under the supervision of a qualified anesthesiologist in departments where there is equipment for tracheal intubation and mechanical ventilation, and anticholinesterase drugs should also be available.
Atracurium besilate cannot be administered intramuscularly.
Atracurium besylate intravenous solution has an acidic pH and should not be mixed with alkaline solutions (eg, barbiturate solutions) in the same syringe or administered simultaneously during intravenous infusion through the same needle. Depending on the resulting pH of such mixtures, atracurium besylate may be inactivated to form free acids.
Atracurium besilate solution for intravenous administration contains benzyl alcohol. In neonates, benzyl alcohol has been associated with an increased incidence of neurological and other complications, sometimes fatal. For use in this category of patients, a dosage form of the drug that does not contain benzyl alcohol should be used.
Since there is a risk of cross-allergic reactions to drugs of this pharmacological group, it is necessary to request information from patients about the presence of anaphylactic reactions to other muscle relaxants in the past.
As with other muscle relaxants, atracurium besylate may cause histamine release reactions in predisposed patients and should therefore be used with caution if there is a history of histamine hypersensitivity.
When administered within the recommended dosage range, the drug does not block the vagus nerve and nerve ganglia, has no clinically significant effect on heart rate, and does not prevent bradycardia caused by anesthetics or vagal stimulation during surgery.
As with other non-depolarizing muscle relaxants, increased sensitivity to atracurium besylate may occur in patients with myasthenia gravis, other neuromuscular diseases and severe electrolyte imbalances. The development of neuromuscular blockade caused by non-depolarizing muscle relaxants is slowed down and its duration is reduced in patients receiving long-term anticonvulsant therapy.
Neuromuscular blockade is quickly and completely eliminated by neostigmine methyl sulfate and the preceding administration of atropine (after 5-10 minutes). In patients prone to low blood pressure, such as those with hypovolemia, atracurium besylate is recommended to be administered over at least 60 seconds.
Atracurium besylate is inactivated in an alkaline environment and should not be mixed in the same syringe with sodium thiopental or alkaline solutions.
If a small-caliber peripheral vein is used to inject the drug solution, then after the injection it should be washed with a 0.9% sodium chloride solution.
Atracurium besilate solution is hypotonic and should not be used simultaneously through the same system with blood transfusions.
Atracurium besilate does not cause malignant hyperthermia.
The safety of the drug has not been established in patients with bronchial asthma.
Patients with burns may develop resistance to non-depolarizing muscle relaxants, which requires increasing doses of these drugs, the amount of which depends on the time elapsed after the burn and on its surface area.
Patients who have received the drug should refrain from potentially hazardous activities associated with the need for concentration and increased speed of psychomotor reactions.
Cisatracurium besylate 2 mg/ml 2.5 ml No. 5 ampoules
Content
Pharmacological action Indications Dosage regimen Side effects Contraindications for use Use during pregnancy and lactation Use for impaired liver function Use for impaired renal function Use for children Use for elderly patients Special instructions Drug interactions Storage conditions Shelf life
pharmachologic effect
Medium-acting non-depolarizing muscle relaxant, benzylisoquinoline derivative. It binds to cholinergic receptors of motor terminals and acts as an acetylcholine antagonist, causing a competitive blockade of neuromuscular transmission. Causes paralysis of the respiratory muscles, as well as other skeletal muscles, without affecting consciousness and the threshold of pain sensitivity.
Cisatracurium besilate does not have significant vagolytic or ganglion-blocking activity, does not have a significant effect on heart rate and does not eliminate the bradycardia that develops under the influence of many anesthetic agents or when stimulating the vagus nerve during surgery.
Indications
To relax muscles and maintain myoplegia during general anesthesia during surgical operations (including tracheal intubation); to provide mechanical ventilation in the ICU (in combination with sedatives).
Dosage regimen
The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.
Individual, depending on age, indications, type of anesthesia, clinical situation, concomitant diseases.
Side effect
- From the cardiovascular system: possible bradycardia, arterial hypotension, hot flashes.
- Allergic reactions: possible skin rash, bronchospasm.
Contraindications for use
Hypersensitivity to cisatracurium besylate, atracurium besylate, and benzene sulfonic acid.
Use during pregnancy and breastfeeding
Use during pregnancy and lactation is possible only in cases where the expected benefit to the mother outweighs the potential risk to the fetus or child.
Experimental studies have shown that cisatracurium besylate does not have a teratogenic effect. The effect on reproductive function has not been studied.
It is unknown whether cisatracurium besylate or its metabolites are excreted in human breast milk.
Use for liver dysfunction
No dosage adjustment is required in patients with impaired liver function.
Use for renal impairment
Patients with insufficient renal function do not require dose adjustment.
Use in children
There is no clinical experience with the use of cisatracurium besilate in children under 1 month of age.
Use in elderly patients
Elderly patients do not require dose adjustment.
special instructions
The effectiveness and safety of the use of cisatracurium besilate during cardiac surgery under conditions of hypothermia (25-28°C) have not been studied.
Cisatracurium besylate can only be used by an anesthesiologist or other specialist who has experience in the use of muscle relaxants and has studied their effect. In this case, it is necessary to have conditions for emergency tracheal intubation, mechanical ventilation and adequate blood oxygenation.
Use with extreme caution in patients with a history of allergic reactions to other muscle relaxants, taking into account the possibility of cross-reactions.
In patients with severe disturbances in blood hormone and/or electrolyte metabolism, changes in sensitivity to muscle relaxants that affect neuromuscular transmission are possible.
The effectiveness and safety of cisatracurium besylate in patients with a history of malignant hyperthermia have not been studied. Experimental studies conducted in pigs susceptible to malignant hyperthermia indicate that cisatracurium besylate does not cause this syndrome.
When using cisatracurium besylate (as well as other non-depolarizing muscle relaxants) in patients with burns, the possibility of increasing the required dose and shortening the duration of action should be considered.
Patients with insufficient renal or liver function, as well as the elderly, do not require dose adjustment.
There is no clinical experience with the use of cisatracurium besilate in children under 1 month of age.
The carcinogenicity of cisatracurium besilate has not been studied. The risk of mutagenic action of cisatracurium besylate is considered negligible.
Drug interactions
The effect of cisatracurium besilate is enhanced by its simultaneous use with anesthetic agents (including enflurane, isoflurane, halothane, ketamine), other non-depolarizing muscle relaxants, antibiotics (including aminoglycosides, polymyxins, spectinomycin, tetracyclines, lincomycin and clindamycin), antiarrhythmics (including propranolol, calcium channel blockers, lidocaine, procainamide and quinidine), diuretics (including furosemide, and possibly thiazides, mannitol and acetazolamide), magnesium salts, salts lithium, ganglion blocking agents (including trimethaphan, hexamethonium).
The effect of cisatracurium besylate is reduced in cases of previous long-term use of phenytoin or carbamazepine.
Administration of suxamethonium to prolong the duration of action of nondepolarizing muscle relaxants may result in prolonged or complex blockade that may be difficult to reverse with anticholinesterase agents.
In rare cases, some drugs may cause latent myasthenia gravis to worsen or manifest, or actually cause myasthenic syndrome; as a result, increased sensitivity to cisatracurium besylate may occur. Such drugs include various antibiotics, beta-blockers (propranolol, oxprenolol), antiarrhythmics (procainamide, quinidine), antirheumatic drugs (chloroquine, D-penicillamine), trimetaphan, chlorpromazine, steroids, phenytoin and lithium.
Storage conditions
In a place protected from light at a temperature of 2 °C to 8 °C. Do not freeze.
Keep out of the reach of children.
Best before date
2 years.
Do not use after the expiration date stated on the package.
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Atracurium-Novo
Ethyl ether, and to a lesser extent halothane, hexobarbital, and sodium thiopental enhance and prolong the effect of atracurium besylate.
Aminoglycosides and polypeptide antibiotics (polymyxin), spectinomycin, capreomycin, amphotericin B, trimetaprim, tetracyclines, lincomycin, clindamycin, antiarrhythmic drugs (propranolol, BMCC, lidocaine, procainamide, quinidine), procaine (iv), diuretics (furosemide, ethacrynic acid , indapamide, mannitol, thiazide, acetazolamide), corticosteroids, mineralocorticoids, magnesium sulfate, ketamine, Li+ salts, ganglion blockers (trimetaphane camsylate, hexamethonium benzosulfonate), depolarizing muscle relaxants, citrates enhance neuromuscular blockade.
Reduces the effect of cholinesterase inhibitors, edrophonium chloride (dosage adjustment may be required).
Antibiotics, beta-blockers (propranolol, oxprenolol), antiarrhythmic drugs (procainamide, quinidine), antirheumatic drugs (chloroquine, D-penicillamine), trimetaphane camsylate, chlorpromazine, steroids, phenytoin, Li+ drugs can enhance or unmask 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. Underpolarizing muscle relaxants prevent or reduce muscle stiffness caused by high doses of opioid analgesics (including alfentanil, fentanyl, sufentanil), while the risk of developing bradycardia and lowering blood pressure caused by narcotic analgesics is not reduced (especially in patients with impaired myocardial function and/or or against the background of the prescription of beta-blockers), moreover, it increases the risk of arterial hypotension (the use of H1- or H2-histamine receptor blockers can prevent the development or reduce the severity of these adverse effects). Increases histamine-dependent side effects caused by narcotic analgesics (with the exception of alfentanil, fentanyl and sufentanil, which do not cause histamine release)
Inhaled 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).
Ca2+ drugs reduce the effect. Doxapram temporarily masks the residual effects of muscle relaxants.
Compatible with the following solutions for infusion (at a concentration of 0.5-0.9 mg/ml in daylight and temperatures up to +30 degrees C): 0.9% NaCl solution for intravenous administration - for at least 24 hours, 5% dextrose solution for intravenous administration - 8 hours, Ringer's solution for injection - 8 hours, solution of NaCl 0.18% and dextrose 4% for intravenous administration - 8 hours, sodium lactic acid solution (Hartmann solution) for intravenous administration - 4 hours .
Do not mix in the same syringe with sodium thiopental or other alkaline solution (inactivation).