Cisatracurium bezylate - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

"N-holinoblokatory (muscle relaxants, curare-like remedies)"

Included in the formulation

Nimbex®

solution in / in

GlaxoSmithKline Trading, ZAO Russia

Cisatracurium bezylate

solution in / in

OBNINSKAYA CHEMICAL - PHARMACEUTICAL COMPANY, CJSC Russia

АТХ:

M.03.A.C.11 Cisatracurium bezylate

Pharmacodynamics:

Nondepolarizing moderate muscle relaxant, benzylisoquinoline derivative. It binds to the cholinoceptors of the motor endings and acts as an antagonist of acetylcholine, causing a competitive blockage of the neuromuscular transmission. It causes paralysis of the respiratory muscles, as well as other skeletal muscles, without affecting the consciousness and threshold of pain sensitivity.

Cisatracurium bezylate does not have significant vagolytic or ganglion blocking activity, it does not significantly affect the heart rate and does not eliminate bradycardia, which develops under the influence of many means for anesthesia or for the stimulation of the vagus nerve during the operation.

Pharmacokinetics:

Cisatracurium bezylate is metabolized in the body at physiological pH and temperature with the formation of laudanosine and mono-quaternary acrylate metabolite.The latter undergoes hydrolysis under the action of nonspecific plasma esterases to form a mono-quaternary alcohol metabolite. Metabolites do not have muscle relaxant activity.

It is excreted by the liver and kidneys in the form of metabolites

Indications:

To relax the muscles and maintain myoplegia during general anesthesia during surgical operations (including intubation of the trachea); to provide ventilation in general intensive care (in combination with sedatives).

ICD-10

XXI.Z40-Z54.Z51.4 Preparatory procedures for subsequent treatment, not elsewhere classified

Contraindications:

Hypersensitivity, including to other benzylquinoline derivatives (including atrakury, Mivakury).

Carefully:

Violation of acid-base balance or electrolyte balance, burns, carcinomatosis, neuromuscular diseases (including myasthenia gravis, myasthenic syndrome), or other conditions that can lead to prolonged neuromuscular blockade, hemiparesis, paraparesis, age under 2 years (absent sufficient clinical experience).

Pregnancy and lactation:

Action category for the fetus by FDA - B.

At pregnancy and thoracal feeding application is possible only in the event that the expected effect at application exceeds potential harm for a fetus and the child. Adequate and strictly controlled studies in pregnant women are not carried out, there is no information on the penetration into breast milk.

In animal studies, embryotoxic and teratogenic effects of subparalytic (4 mg / kg subcutaneously) and paralytic (0.5-1 mg / kg intravenously) doses were not detected.

Dosing and Administration:

Individual, depending on age, indications, type of anesthesia, clinical situation, concomitant diseases.

Intravenous bolus. Adults: the initial dose (for intubation of the trachea) is intravenously 0.15-0.2 mg / kg, rapidly within 5-10 seconds. Maintenance doses for prolongation of muscle relaxation: in surgery, intravenous 0.03 mg / kg with an interval of about 20 minutes, or continuous intravenous infusion of 0.003 mg / kg / min (initial dose) with a decrease to 0.001-0.002 mg / kg / min; more rare or less maintenance doses are used in patients on inhalation anesthesia (enflurane, isoflurane), the infusion rate decreases by 30-40%.Intensive care: 0.003 mg / kg / min with further dose adjustment if necessary (0.0005-0.0101 mg / kg / min).

Children older than 2 years: the initial dose is 0.1 mg / kg intravenously for 5-10 seconds; maintenance doses: for surgical interventions - intravenous infusion of 0.003 mg / kg / min, followed by dose reduction to 0.001-0.002 mg / kg / min; with intensive therapy - 0,003 mg / kg / min, dose adjustment is possible.

Dose adjustments in elderly patients, patients with impaired renal function, liver, and diseases of the cardiovascular system are not required.

Side effects:

From the side of cardio-vascular system: possible bradycardia, arterial hypotension, hot flashes.

Allergic reactions: possible skin rash, bronchospasm.

Overdose:

Symptoms: lengthening of muscle relaxation.

Treatment: maintaining adequate ventilation until the recovery of adequate neuromuscular conduction; specific therapy with anticholinesterase drugs (neostigmine 0.04-0.07 mg / kg) is performed only after the onset of spontaneous reduction simultaneously with anticholinergics (atropine). Antagonists (neostigmine and others) should not be used with a complete neuromuscular block (peripheral neurostimulation is recommended to confirm recovery).It is necessary to carry out mechanical ventilation until the breathing is fully restored.

Interaction:

The effect of cisatracurium bezilate is enhanced when it is used simultaneously with anesthetics (including enflurane, isoflurane, halothane, ketamine), other nondepolarizing muscle relaxants, antibiotics (including aminoglycosides, polymyxins, spectinomycin, tetracyclines, lincomycin and clindamycin), antiarrhythmic drugs drugs (including with propranolol, calcium channel blockers, lidocaine, procainamide and quinidine), diuretics (including furosemide and possibly thiazides, mannitol and acetazolamide), magnesium salts, lithium salts, ganglion-blocking agents (including trimetaphane, hexamethonium).

The effect of cisatracurium bezylate decreases in cases of previous long-term use of phenytoin or carbamazepine.

The introduction of suxamethonium in order to increase the duration of action of nondepolarizing muscle relaxants can lead to a prolonged or complex blockade, which can be difficult to eliminate with the help of anticholinesterase agents.

In rare cases, some drugs may cause an increase or manifestation of a latent myasthenia gravis or in fact cause a myasthenic syndrome; as a result, there may be increased sensitivity to cisatracurium bezylate. To such drugs include various antibiotics, beta-blockers (propranolol, oxprenolol), antiarrhythmic agents (procainamide, quinidine), antirheumatic drugs (chloroquine, D-penicillamine), trimetaphane, chlorpromazine, steroids, phenytoin and lithium.

Special instructions:

The efficacy and safety of the use of cisatracurium bezilate in cardiac surgery under hypothermia (25-28 ° C) have not been studied.

Cisatracurium bezylate can be used only by an anesthesiologist or other specialist who has experience with the use of muscle relaxants and has studied their effect. At the same time, it is necessary to have conditions for urgent intubation of the trachea, mechanical ventilation and adequate oxygenation of the blood.

With special care apply in patients with allergic reactions to other muscle relaxants in anamnesis, given the possibility of cross reactions.

In patients with severe disturbances of acid-base equilibrium and / or electrolyte metabolismthere may be changes in the sensitivity to muscle relaxants that affect neuromuscular transmission.

The efficacy and safety of the use of cisatracurium bezilate in patients with malignant hyperthermia in the anamnesis have not been studied. Experimental studies conducted on pigs susceptible to malignant hyperthermia indicate that cisatracurium bezylate does not cause this syndrome.

When using cisatracurium besylate (as well as other nondepolarizing muscle relaxants), patients with burns should consider the possibility of increasing the required dose and shortening the duration of the action.

Patients with insufficient kidney or liver function, as well as elderly people, do not need dose adjustment.

Clinical experience of the use of cisatracurium bezilate in children under the age of 1 month is absent.

The carcinogenicity of cisatracurium bezylate has not been studied. The risk of mutagenic action of cisatracurium bezilate is considered insignificant.

Instructions

Cisatracurium bezylate (Cisatracurii besilas)