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QuickView for Cisatracurium Besylate (compound)


DrugBank
Identification
Name: cisatracurium besylate
Name (isomeric): DB00565
Drug Type: small molecule
Brand: Atracurium Besylate, Nimbex, Tracrium Preservative Free, Atracurium Besylate Preservative Free
Category: Neuromuscular Blocking Agents
CAS number: 96946-42-8
Pharmacology
Indication: For inpatients and outpatients as an adjunct to general anesthesia, to facilitate tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation in the ICU.
Pharmacology:
Cisatracurium Besylate is a nondepolarizing skeletal muscle relaxant for intravenous administration. Cisatracurium Besylate acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The neuromuscular block produced by cisatracurium besylate is readily antag...
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Mechanism of Action:
Cisatracurium Besylate binds to the nicotinic acetycholine (cholinergic) receptors in the motor endplate and blocks access to the receptors. In the process of binding, the receptor is actually activated - causing a process known as depolarization. Since it is not degraded in the neuromuscular junction, the depolarized membrane remains depolarized a...
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Protein binding: The binding of cisatracurium to plasma proteins has not been successfully studied due to its rapid degradation at physiologic pH.
Biotransformation: The degradation of cisatracurium is largely independent of liver metabolism. Results from in vitro experiments suggest that cisatracurium undergoes Hofmann elimination (a pH and temperature-dependent chemical process) to form laudanosine and the monoquaternary acrylate metabolite. The monoquaternary acrylate undergoes hydrolysis by non-specific plasma esterases to form the monoquaternary alcohol metabolite. The monoquaternary alcohol metabolite can also undergo Hofmann elimination but at a much slower rate than cisatracurium. Laudanosine is further metabolized to desmethyl metabolites which are conjugated with glucuronic acid and excreted in the urine.
Route of elimination: Biliary and urinary excretion were the major routes of excretion of radioactivity (totaling >90% of the labeled dose within 7 hours of dosing), of which atracurium represented only a minor fraction.
Half Life: Elimination half-life of 22 minutes.
Toxicity: Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia.
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
ColistimethateColistimethate may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. If possible, avoid concomitant use of these products. Monitor for deeper, prolonged neuromuscular-blocking effects (respiratory paralysis) in patients receiving concomitant neuromuscular-blocking agents and polymyxin antibiotics (e.g., colistimethate, polymyxin B).

Targets