Vecuronium bromide (Vecuronii bromidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

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

Included in the formulation
АТХ:

M.03.A.C.03   Vecuronium bromide

M.03.A.C   Other quaternary ammonium compounds

Pharmacodynamics:

Peripheral muscle relaxant of a nondepolarizing competitive type of action. It is a mono-quaternary ammonium compound of the steroid structure. It violates the neuromuscular transmission as a result of the blockade of N-cholinergic receptors in skeletal muscle and eliminate the depolarizing action of acetylcholine on them. After intravenous injection, the relaxation of the striated muscle develops after 1.5-2 minutes and lasts for 20-30 minutes. Miorelaxation is not accompanied by fasciculations and muscle pains. Vecuronium bromide ganglioblokiruyuschimi has weak activity, to a small degree m-blocking cholinergic receptors of the heart, somewhat enhances the release of histamine from mast cells.

Pharmacokinetics:

The time of reaching and the duration of the effect are dose-dependent. The average effective dose inducing muscle relaxation by 90%, is 0.057 mg / kg (0.049 to 0.062 mg / kg according to various studies). After intravenous dose 0.08-0.10 mg / kg primary effect develops after about 1 minute, after intubation possible 2.5-3 min, maximum muscle relaxant effect in most patients achieved after 3-5 min.Recovery of neuromuscular transmission by 25% occurs in 25-40 minutes and by 95% at 45-65 min after administration with balanced anesthesia. With the introduction of an initial dose 5 minutes after the onset of inhalation anesthesia (enflurane, isoflurane, halothane) or when the equilibrium state is reached, the dose is reduced by 15%. The repeated administration of maintenance doses practically does not affect the duration of the neuromuscular block. With balanced anesthesia after the initial dose of 0.08-0.10 mg / kg, the first maintenance dose of 0.010-0.015 mg / kg is administered after 25-40 minutes, the subsequent maintenance doses are administered with an interval of 12-15 minutes. Halothane anesthesia slightly increases the duration of action of maintenance doses. After the onset of spontaneous reduction, its rate exceeds that of pancuronium bromide, is accelerated by the administration of anticholinesterase agentspyridostigmine bromide, neostigmine methylsulfate) in combination with m-cholinolytic agents (atropine and others). It binds to plasma proteins by 60-80%. Metabolised in the liver with the formation of 5-hydroxyvekuronium. The half-life is 65-75 minutes.Slightly cumulates. Output is 65% with bile in the form of inactive metabolites, 35% - in the unchanged form of the kidneys.

Indications:

Relaxation of skeletal muscles (with surgical operations under general anesthesia).

ICD-10

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

Contraindications:

Hypersensitivity to vecuronium or bromides.

Carefully:

Use with caution in diseases of the liver.

Use with caution in renal failure.

In elderly people, an increase in the duration of the neuromuscular blockade is possible.

Pregnancy and lactation:

Perhaps, if the expected effect of therapy exceeds the potential risk to the fetus. Data on the use of vecuronium bromide in pregnancy in animals and humans is not enough. Can be used for caesarean section.

FDA Action Category - C.

Data on penetration into breast milk are absent.

Dosing and Administration:

Intravenously. The initial dose (for intubation of the trachea) in adults is 80-100 μg / kg, maintaining a dose of 20-30 μg / kg. Patients with obesity - the dose is calculated on the value of the ideal body weight. In newborns and infants up to 4 months, the initial dose is 10-20 μg / kg.

Side effects:

From the coagulation system: a reduction in partial thromboplastin and prothrombin time has been described.

Allergic reactions: rarely - bronchospasm and anaphylactic reactions.

Local reactions: local hypersensitivity reactions at the site of vecuronium bromide administration are possible.

Overdose:

Symptoms: weakness of skeletal musculature, hypopnea, apnea, excessive decrease HELL, collapse, paralysis, shock.

Treatment: artificial ventilation, to eliminate the myorelaxing effect - cholinesterase inhibitors (neostigmine methylsulfate, pyridostigmine bromide), symptomatic therapy.

Interaction:

Like other nondepolarizing muscle relaxants, vecuronium bromide can reduce partial thromboplastin time and prothrombin time.

The action of vecuronium bromide is enhanced by simultaneous use with the following drugs: anesthetics (halothane, diethyl ether, cyclopropane, propofol; increased doses of thiopentone, metohexiton, ketamine, sodium oxybutyrate, etomidate), other nondepolarizing muscle relaxants; antibiotics aminoglycosides, polypeptide antibiotics,acylaminopenicillin, metronidazole in high doses, diuretics, beta-adrenoblockers, thiamine, inhibitors monoamine oxidase, quinidine, protamine, alpha-adrenergic agents, magnesium salts.

The effect of vecuronium bromide decreases with simultaneous use with neostigmine, eudrophonia, pyridostigmine, aminopyridine derivatives; with prolonged prior application glucocorticosteroids, phenytoin or carbamazepine; with norepinephrine, azathioprine (passing or limited effect), theophylline, calcium chloride.

Variable effect can be observed with the use of depolarizing muscle relaxants (including succinylcholine) after the introduction of vecuronium bromide.

Special instructions:

Vecuronium bromide should be used only in a specialized hospital with artificial ventilation specialists-anaesthesiologists. Before anesthesia begins, the electrolyte balance should be normalized, acid-base balance and eliminate dehydration.

With caution apply for diseases of the liver and bile ducts, kidney failure.

Patients with cardiovascular diseases, edema, and also in the elderly can increase the duration of the neuromuscular blockade.

With extreme caution vecuronium bromide, like other neuromuscular blockers, should be used in patients with myasthenia gravis or myasthenic syndrome.

In the conditions of intraoperative hypothermia, the muscular-relaxing effect of vecuronium bromide is enhanced.

Instructions
Up