Description
Release form
Injection
Packaging
5 pcs
Pharmacological action
Nimbex – non-depolarizing, muscle relaxant.
Binds to n-cholinergic receptors of motor nerve endings and acts as an acetylcholine antagonist, causing competitive blockade of neuromuscular conduction, which can be quickly eliminated by anticholinesterase drugs such as neostigmine and edrophonium.
The effect of Nimbacks on patients with malignant hyperthermia has not been studied.
Pharmacokinetics of
In the body, at physiological pH and body temperature, Hoffman is eliminated to form laudanosine and mono-quaternary acrylate. The latter undergoes hydrolysis by nonspecific plasma esterases with the formation of mono-quaternary alcohol. Metabolites are excreted by the liver and kidneys, they do not possess muscle relaxant properties.
In elderly patients, there is a slight increase in the volume of distribution (+ 17%) and T1 / 2 (+4 min) of the drug.
There are no clinically significant differences in the pharmacokinetics of cisatracuria besilate in patients with end-stage renal failure and in healthy volunteers.
In liver failure, there is a slight difference in the volume of distribution (+ 21%) and clearance (+ 16%) of cisatracuria besilate, but T1 / 2 and excretion of the drug do not change.
With infusion or bolus administration, the average clearance is 6.9 ml / kg / min, and T1 / 2 – 28 min. Withdrawal of the drug does not depend on the duration of the infusion.
In doses up to 8 times higher than ED95 (the average dose required to 95% suppress the reaction of the abductor muscle of the thumb in response to stimulation of the ulnar nerve), does not cause a dose-dependent release of histamine.
ED95 cisatracuria besilate during opioid anesthesia (thiopental / fentanyl / midazolam) is 0.05 mg / kg in children during halotan anesthesia – 0.04 mg / kg.
Cisatracuria besilate causes paralysis of the respiratory and skeletal muscles, but does not affect the consciousness and threshold of pain sensitivity.
There are separate reports of the development of seizures in patients in intensive care units, who received atracuria besilate in combination with other drugs (administration of laudanosine, an metabolite of cisatracuria besilate and high doses of atracuria besilate, to animals is associated with transient hypotension and, in some cases, with symptoms of cerebral cortex excitation).
Since they usually suffered from one or more diseases predisposing to the appearance of seizures (for example, traumatic brain injury, hypoxic encephalopathy, cerebral edema, viral encephalitis, uremia), a causal relationship between the development of seizures and laudanosine has not been established. In addition, it should be borne in mind that the concentration of laudanosine in blood plasma with the introduction of Nimbacks is 3 times less than with the infusion of atracuria besilate.
Contraindications
Hypersensitivity to cisatracuria, atracuria and benzenesulfonic acid, children (up to 2 years old). Precautions: impaired CBS or electrolyte balance, burns, carcinomatosis, neuromuscular diseases (including myasthenia, myasthenia syndrome or myasthenia other conditions that can lead to prolonged neuromuscular blockade, hemiparesis, paraparesis, pregnancy, lactation.
Special instructions
Dose adjustment is not required in elderly patients, in patients with impaired renal, hepatic, or cardiovascular diseases. The drug causes paralysis of the respiratory and other skeletal muscles, but does not affect the consciousness or pain threshold.
It should be administered only by an anesthetist or specialist with experience in using muscle relaxants, with the possibility of intubation of the trachea, mechanical ventilation and adequate blood oxygenation.
When diluted in Ringer’s lactate solution, the injection preparation is chemically unstable, stable only in acidic solutions, so it should not be mixed in the same syringe or injected simultaneously through one needle with alkaline solutions, such as sodium thiopental.
Composition
Active ingredient:
cisatracuria besilate 2 mg
Excipients:
solution of benzenesulfonic acid 32%
water for injection
Dosage and Administration
Intravenous, bolus. In adults and children from 1 month. up to 12 years for tracheal intubation – 0.15 mg / kg, quickly, for 5-10 s. 2-3 minutes after the administration, a neuromuscular block sets in enough for tracheal intubation.
With higher doses, the block comes faster. Consistent administration of maintenance doses does not lead to a progressive increase in the duration of the effect.
After spontaneous recovery of the neuromuscular block has begun, its speed does not depend on the total dose administered.
Drug interaction
effect is enhanced by drugs for inhalation general anesthesia (halotane, ether), other non-depolarizing muscle relaxants antibiotics (aminoglycosides, polymyxins, spectinomycin, tetracyclines, lincomycin and clindamycin) antiarrhythmic drugs (propranolol, BMCC, lidocaine, procainamide, quinidine) diuretics (furosemide, thiazides) MD2 + salts, Li + salts, ganglion blocking drugs (trimethafan, hexamethonium). The previous long-term use of phenytoin or carbamazepine is a weakening of the effect of the drug.
The preliminary administration of suxamethonium does not affect the duration of the neuromuscular block. The introduction of suxamethonium in order to increase the duration of the neuromuscular block caused by non-depolarizing muscle relaxants can lead to a long and complex blockade, which can be difficult to eliminate with anticholinesterase drugs. Incompatible with ketorolac, trometamol, propofol.
Overdose of
Symptoms: the expected symptoms are due to prolonged paralysis of the respiratory muscles and its consequences.
Treatment: Until adequate spontaneous breathing is restored, it is very important to maintain lung ventilation and blood oxygenation.
When signs of spontaneous recovery of neuromuscular conduction appear, it can be accelerated by the introduction of anticholinesterase drugs.
Storage conditions
Store in a dark place at a temperature of 2-8 gr. FROM.
Active ingredient
Tsisatrakuriya besylate
dosage form
solution for infusion
GlaxoSmithKline, UK
