Universal reference book for medicines
Product name: KRUARON (KRUARON)

Active substance: rocuronium bromide

Type: Muscle relaxant of peripheral action of nondepolarizing competitive type

Manufacturer: ЛЭНС-ФАРМ (Russia)
Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Nondepolarizing muscle relaxant with a short (closer to average) duration of action.
It is a competitive antagonist of acetylcholine with respect to n-cholinergic receptors of neuromuscular synapses of skeletal musculature. Virtually does not have ganglioblokiruyuschego and m-holinoblokiruyuschego action, to a small extent affects the release of histamine. Can cause tachycardia (in 30% of cases), the effect on the heart rate is less pronounced than in pancuronium bromide, and more than vecuronium bromide.
ED 90 (the dose needed to inhibit the contractile ability of the thumb muscle to stimulate the ulnar nerve by 90%) with IV general anesthesia is about 0.3 mg / kg body weight.
After intravenous administration at a dose of 0.6 mg / kg (2 x ED 90 ), complete neuromuscular blockade is achieved after 60-70 seconds; general relaxation of skeletal muscles, adequate for any surgical interventions - within 2 minutes; the clinical duration of action (time to spontaneous recovery of contractile ability of skeletal muscles to 25% of the control level) is 30-40 min; the average time of spontaneous recovery of contractility from 25 to 75% of the reference level (recovery index) is 14 minutes; total duration (time to spontaneous recovery of the contractile ability of skeletal muscles to 90% of the control level) - 50 min.
The time to achieve the maximum effect depends on the dose, age and choice of type of anesthetic: in patients aged 18-64 with anesthesia on the background of opioids / dinitrogen oxide at a dose of 0.45 mg / kg - 3 min, at a dose of 0.6 mg / kg - 1.8 min, 0.9 mg / kg - 1.4 min, 1.2 mg / kg - 1 min;
for patients older than 65 years at a dose of 0.6 mg / kg - 3.7 min, 0.9 mg / kg - 2.5 min, 1.2 mg / kg - 1.3 min.
In children aged 3 months against a background of halothane anesthesia at a dose of 0.6 mg / kg, the maximum effect develops after 0.8 minutes, at a dose of 0.8 mg / kg - after 0.7 minutes;
in children 1-12 years with a dose of 0.6 mg / kg - after 1 min, 0.8 mg / kg - 0.5 min. The duration of action depends on the dose and age: in patients 18-64 years with a dose of 0.45 mg / kg - 22 min, 0.6 mg / kg - 31 min, 0.9 mg / kg - 58 min, 1.2 mg / kg - 67 min; in patients older than 65 years with a dose of 0.6 mg / kg - 46 min, 0.9 mg / kg - 62 min, 1.2 mg / kg - 94 min. In children 3 months duration of action at a dose of 0.6 mg / kg - 41 minutes, 0.8 mg / kg - 40 minutes; in children 1-12 years with a dose of 0.6 mg / kg - 26 minutes, 0.8 mg / kg - 30 minutes. At doses exceeding 3 x ED 90, the conditions of intubation are not significantly improved; The duration of the action, however, increases. Doses in excess of 4 x ED 90 have not been studied. The duration of the effect of supporting doses of 0.15 mg / kg with the use of enflurane and isoflurane anesthesia in patients of senile age and in patients with liver and / or kidney diseases may be somewhat larger (approximately 20 min) than in patients without liver and / or kidney dysfunction approximately 13 minutes).
Binding to plasma proteins - 30%.
The distribution has a two-phase character. The half-distribution period in the fast phase is 1-2 min, in the slow phase - 14-18 min. Vd - 0.26 l / kg; with liver failure - 0.53 l / kg; in patients with a kidney transplant - 0.34 l / kg; in children 3-12 months - 0.3 l / kg, 1-3 years - 0.26 l / kg, 3-8 years - 0.21 l / kg. Penetrates through the placental barrier in small amounts. Metabolized in the liver with the formation of a weakly active metabolite - 17-deacetyl-rocuronium. It is excreted by the liver and kidneys. During the first 12 hours, kidneys receive 13-30.8% of the total administered dose as an unchanged drug. With hepatic failure, the clearance is 2 times increased. When anesthetized against the background of opioids and dinitrogen oxide T 1/2 - 1.4 h, against isoflurane with normal liver function - 2.4 h, with liver failure - 4.3 h, with a renal transplant - 2.4 h; against halothane T 1/2 in children 3-12 months - 1.3 hours, 1-3 years - 1.1 hours, 3-8 years - 0.8 hours. Cumulative effect with repeated administration of maintenance doses was not observed.
For short-term miorelaxation (for the purpose of endotracheal intubation and ventilation).

Only in / in.
When intubation, as well as to maintain muscle relaxancy for 30 minutes (anesthesia with opioids and dinitrogen oxide) or longer (in the background of halothane, isoflurane or enflurane), in the initial dose - 0.6 mg / kg. To reduce the duration of muscle relaxation (22 min - against opioids / dinitrogen oxide and 12-15 min - against halothane, isoflurane or enflurane) - 0.45 mg / kg.
To achieve the maximum miorelaxing effect and longer duration of action, doses of 0.9 mg / kg and 1.2 mg / kg on the background of opioids / dinitrogen oxide are used;
the duration of the effect is 58 and 67 minutes, respectively. Supportive doses (introduced when restoring muscle contractility to 25% of the reference level) - 0.1, 0.15 and 0.2 mg / kg provide an increase in the duration of the effect by 12, 17 and 24 minutes, respectively.
With the appearance of early signs of muscle activity after the initial dose, it is possible to use as a continuous infusion with an initial rate of 0.01-0.012 mg / kg / min;
in some cases, to achieve the necessary miorelaxation, bolus administration is permitted.
The rate of administration and dose are selected and calculated individually, so that the contractile response of skeletal muscles is at the level of 10% of the control, the average dose is 4-16 Ојg / kg / min.
In patients with excessive body weight or obesity, it is recommended to calculate, based on the dose per 1 kg of muscle mass. If the body weight by 30% or more exceeds the "ideal" body weight, the dose should be reduced, recalculating to "ideal".
Application in pediatric practice: the initial dose of 0.6 mg / kg against a background of general anesthesia with halothane provides sufficient miorelaxation for 41 minutes in children from 3 to 12 months and 27 minutes in children 1-12 years old.
Supporting doses that provide muscle relaxation for an additional 7-10 minutes, bolus 0.075-0.125 mg / kg or as a continuous infusion at a rate of 0.012 mg / kg / min while restoring 10% of muscle activity (the rate of correction is adjusted depending on the patient's reaction) . Children under 3 months of doses are not established.
In patients older than 65 years, doses of 0.6, 0.9 or 1.2 mg / kg, respectively, against a background of opioids / dinitrogen oxide are used to achieve relaxation for 46, 62 or 94 min.
The maintenance dose is 0.1-0.15 mg / kg.
As solvents, 5% dextrose solution, 0.9% sodium chloride solution, Ringer-lactate solution or sterile water for injection can be used.
The solution is suitable for 24 hours after preparation; unused solution is disposed of.
From the cardiovascular system: less often - a decrease or increase in blood pressure;
rarely - arrhythmia (including tachycardia).
From the digestive system: rarely - hiccups, nausea, vomiting.

Allergic reactions: rarely - angioedema, skin rash, bronchospasm, dyspnea.

Local reactions: swelling and pain at the injection site (with extravasation).

Infant age (up to 3 months), hypersensitivity to rocuronium chloride.

The use of the drug during pregnancy and during lactation is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or infant.

Use with caution in renal failure.

Use with caution in liver failure.

Contraindicated in infancy (up to 3 months).
In children older than 3 months, the application is possible according to the dosing regimen.
Use with caution in old age.

Use with caution in case of violation of KCHR and electrolyte balance, burns, cachexia, severe chronic heart failure, neuromuscular transmission disorders (including myasthenia gravis), hypertension in the "small" circulation, heart defects, hepatic and / or renal failure , elderly age, pregnancy, lactation.

When an overdose is observed excessive decrease in blood pressure, collapse, prolonged relaxation of the muscles, apnea, shock.
Treatment of an overdose: IVL, the administration of antagonists of muscle relaxants (neostigmine, pyridostigmine), symptomatic therapy.
Increased action is promoted by hypokalemia (eg, after severe vomiting, diarrhea, digitalisation, diuretic therapy), hypermagnesia, hypocalcemia (eg, after massive blood transfusions), hypoproteinemia, dehydration, acidosis, hypercapnia, cachexia.

Before use, it is necessary to eliminate changes in blood pH, severe electrolyte disturbances, dehydration.

When applied at a dose of more than 0.9 mg / kg body weight, an increase in heart rate is possible, which can counteract bradycardia caused by other anesthetics or arising from stimulation of n.vagus.

It should be borne in mind that during the general anesthesia, even in the absence of known provoking agents, the development of malignant hyperthermia is possible, so specialists should carefully monitor the early manifestations confirming the diagnosis of malignant hyperthermia.
In experimental studies it was shown that rocuronium bromide is a factor provoking the development of malignant hyperthermia.
Because the drug causes paralysis of the respiratory muscles, it is necessary to carry out mechanical ventilation until adequate recovery of self-breathing.

Impact on the ability to drive vehicles and manage mechanisms

Within 24 hours after complete recovery of neuromuscular conduction, it is not recommended to drive and engage in potentially hazardous activities in terms of injury.

The effect of rocuronium bromide strengthens general anesthetics (it is recommended to reduce their infusion rate by 40%), other nondepolarizing muscle relaxants, aminoglycosides, polymyxin, tetracycline, vancomycin, bacitracin, colistin, quinidine, metronidazole (in high doses), diuretics, alpha-blockers, adrenoblockers, thiamine, MAO inhibitors, protamine sulfate, magnesium salts, suxamethonium, GCS, mineralocorticoids.

Roqueronium bromide exhibits antagonist properties of anticholinesterase agents (including prozeryn, neostigmine, pyridostigmine).
Aminophylline, theophylline, norepinephrine, azathioprine, calcium chloride, aminopyridine derivatives, phenytoin, crabamazepine reduce the effect.
Atropine, hyoscyamine and other anticholinergics increase the risk of developing tachycardia.

Phenylephrine in nasal drops increases the risk of tachycardia in children, increased blood pressure and resistance to muscle relaxants.

Pharmaceutically incompatible with amphotericin, amoxicillin, azathioprine, cefazolin, dexamethasone, diazepam, erythromycin, famotidine, furosemide, hydrocortisone, insulin, methylprednisolone, prednisolone, trimethoprim, vancomycin, intralipid.

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