Cisatracurium Besylate CAS NO 96946-42-8 Inquire about Cisatracurium Besylate
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What is Cisatracurium Besylate?
Cisatracurium (usually as Cisatracurium Besylate, trade name Nimbex) is a neuromuscular-blocking drug. It is one of the ten isomers of atracurium. Its active metabolites contains less laudanosine (which causes hypotension, central nervous system excitement, and seizures) than that of atracurium. It is considered an intermediate-acting agent in terms of duration of action.
Cisatracurium Besylate Structure
It is a bisbenzyltetrahydroisoquinolinium agent in the quaternary ammonium compound family.
Cisatracurium Besylate Metabolism
80% is metabolized to laudanosine via Hofmann degradation (which is dependent on the pH and the temperature of the plasma) and 20% is metabolized hepatically or excreted renally. Since Hofmann elimination is organ-independent, the use of cisatracurium may pose less risk in patients with liver or renal disease than other neuromuscular blockers. 10-15% of the dose is excreted unchanged in the urine.
Pharmacology and Clinical Uses
Cisatracurium Besylate (besylate) is a nondepolarising neuromuscular blocking agent with an intermediate duration of action. It is the R-cis, R’-cis isomer of atracurium Besylate and is approximately 3-fold more potent than the mixture of isomers that constitute the parent drug. The ED95 for cisatracurium Besylate (dose required to produce 95% suppression of twitch response to nerve stimulation) in adults is 0.05 mg/kg during N2O/O2 opioid anaesthesia.
As for atracurium Besylate, the primary route of elimination of cisatracurium Besylate is by spontaneous degradation. Cisatracurium Besylate is not associated with dose-related histamine release (at bolus doses of < or = 8 x ED95) and, consistent with this, has demonstrated cardiovascular stability in both healthy patients (< or = 8 x ED95) and those with coronary artery disease (< or = 6 x ED95).
In clinical trials, Cisatracurium Besylate has been used successfully to facilitate intubation (at 2 to 4 x ED95) and as a muscle relaxant during surgery and in intensive care. Compared with vecuronium, Cisatracurium Besylate was associated with a significantly faster recovery after continuous infusion in patients in intensive care. Relative to atracurium Besylate, Cisatracurium Besylate has a lower propensity to cause histamine release is more potent but has a slightly longer onset time at equipotent doses. It also offers a more predictable recovery profile than vecuronium after prolonged use in patients in intensive care. Thus, comparative data provide some indication of the potential of Cisatracurium Besylate as an intermediate-duration neuromuscular blocking agent but further comparisons with other like agents are required to define precisely its relative merits.
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