Description

Atracurium besylate, the bisbenzenesulfonate salt of atracurium, is designated as 2-(2-Carboxyethyl)-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-veratrylisoquinolinium benzenesulfonate, pentamethylene ester. It is a synthetic dibenzensulfonate derivative muscle relaxant, Atracurium Besylate acts as a non-depolarizing neuromuscular blocking agent, with short to intermediary duration of action and no significant cardiovascular effects. Not dependent on kidney function for elimination, it provides clinical advantages over other non-depolarizing, neuromuscular blocking agents.

Atracurium besylate is a complex molecule containing four sites at which different stereochemical configurations can occur. The symmetry of the molecule, however, results in only ten, instead of sixteen, possible different isomers. The manufacture of atracurium besylate results in these isomers being produced in unequal amounts but with a consistent ratio. Those molecules in which the methyl group attached to the quaternary nitrogen projects on the opposite side to the adjacent substituted-benzyl moiety predominate by approximately 3:1.

Atracurium Besylate Injection

Atracurium Besylate Injection is a clear, colourless or faint yellow, sterile solution for injection. Each mL contains 10 mg atracurium besylate. The pH is adjusted to 3.00 to 3.65 with benzenesulfonic acid. The multiple dose vial contains 0.9% benzyl alcohol added as a preservative. Atracurium besylate injection slowly loses potency with time at the rate of approximately 6% per year under refrigeration (5°C). Atracurium besylate injection should be refrigerated at 2°C to 8°C (36°F to 46°F) to preserve potency. Rate of loss in potency increases to approximately 5% per month at 25°C (77°F). Upon removal from refrigeration to room temperature storage conditions (25°C / 77°F), use atracurium besylate injection within 14 days even if rerefrigerated.

Use

Atracurium besylate is a nondepolarizing skeletal muscle relaxant. Atracurium besylate Injection is indicated as an adjunct to general anaesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.

Nondepolarizing agents antagonize the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine.

Atracurium can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. The duration of neuromuscular block produced by atracurium is approximately one-third to one-half the duration of block by d-tubocurarine, metocurine, and pancuronium at initially equipotent doses. As with other nondepolarizing neuromuscular blockers, the time to onset of paralysis decreases and the duration of maximum effect increases with increasing atracurium doses.

Special precautions for storage

DBL? Atracurium Besylate Injection should be stored at 2 to 8°C. Do not freeze. Protect from light. Any unused atracurium besilate from opened ampoules should be discarded.