Cisatracurium

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Cisatracurium
Systematic (IUPAC) name
5-[3-[(1R,2R)-1-[(3,4-dimethoxyphenyl)methyl]-6,7- dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-2-yl] propanoyloxy]pentyl 3-[(1R,2R)-1-[(3,4-dimethoxy phenyl)methyl]-6,7-dimethoxy-2-methyl-3,4-dihydro- 1H-isoquinolin-2-yl]propanoate
Identifiers
CAS number	96946-42-8
ATC code	M03AC11
PubChem	62887
DrugBank	APRD00874
Chemical data
Formula	C₅₃H₇₂N₂O₁₂⁺²
Mol. mass	929.145 g/mol
Pharmacokinetic data
Bioavailability	N/A - IV use only
Protein binding	Unknown due to rapid degradation
Metabolism	80% Hoffman elmination/ Hepatic
Half life	20-29 minutes
Excretion	10-15% unchanged
Therapeutic considerations
Pregnancy cat.	B
Legal status
Routes	IV only

Cisatracurium (usually as cisatracurium besilate, trade name Nimbex) is a neuromuscular-blocking drug. It is one of the ten isomers of atracurium. Its active metabolites contain less laudanosine which cause hypotension, central nervous system excitement, and seizures than that of atracurium. It is considered an intermediate-acting agent in terms of duration of action.

[edit] Structure

It is a benzyl-isoquinolinium agent in the quaternary ammonium compound family.

[edit] Metabolism

80% is metabolized to laudanosine via Hofmann elimination (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.

[edit] External links

Esmaoglu A, Akin A, Mizrak A, Turk Y, Boyaci A (2006). "Addition of cisatracurium to lidocaine for intravenous regional anesthesia.". J Clin Anesth 18 (3): 194–7. doi:10.1016/j.jclinane.2005.08.003. PMID 16731321.
Melloni C, Devivo P, Launo C, Mastronardi P, Novelli G, Romano E (2006). "Cisatracurium versus vecuronium: a comparative, double blind, randomized, multicenter study in adult patients under propofol/fentanyl/N2O anesthesia.". Minerva Anestesiol 72 (5): 299–308. PMID 16675938.
Serra C, Oliveira A (2006). "Cisatracurium: myographical and electrophysiological studies in the isolated rat muscle.". Fundam Clin Pharmacol 20 (3): 291–8. doi:10.1111/j.1472-8206.2006.00395.x. PMID 16671964.

v • d • e

Skeletal Muscle relaxants (M03)

Peripherally acting
(primarily antinicotinic,
neuromuscular-blocking drugs)

Curare Alkaloids (Non-Depolarising)	Alcuronium, Dimethyltubocurarine, Tubocurarine

quaternary ammonium compounds (Non-Depolarising)	Atracurium, Cisatracurium, Doxacurium chloride, Fazadinium bromide, Gallamine, Hexafluronium, Metocurine, Mivacurium chloride, Pancuronium, Pipecuronium bromide, Rocuronium bromide,Vecuronium

Choline Derivatives (Depolarising)	Suxamethonium, Succinylcholine

Other	Botulinum toxin