Description
Doxacurium chloride is an injectable, noncumulative, nondepolarizing neuromuscular
blocking agent which exhibits no significant cardiovascular effects. It is a mixture of
(lR, l′S, 2S, 2′R), (lR, l′R, 2S, 2′s) and (lS, l′S, 2R, 2′R) isomers of a
bis-benzylisoquinolinium diester.Doxacurium chloride provides satisfactory
intubation with duration of action similar to d-tubocurarine or pancuronium. However,
it is reported to be 2 to 3 times as potent as pancuronium.
Chemical Properties
Amorphous solid. Soluble in water.
Originator
Wellcome (United Kingdom)
Uses
Neuromuscular blocking agent.
Brand name
Nuromax (Abbott).
General Description
The molecular structure of doxacuriumchloride, 1,2,3,4-tetrahydro-2-(3-hydroxypropyl)-6,7,8-trimethoxy2-methyl-1-(3,4,5-trimethoxybenzyl) isoquinoliniumchloride succinate (Nuromax), provides thepossibility for 10 stereoisomers: 4 d,l pairs and two mesoforms. Of the 10 stereoisomers, 3 are all-trans configuration,and these are the only active ones. Doxacurium chlorideis a long-acting nondepolarizing blocking agent. The drugdiffers from drugs such as gallium and pancuronium in thatit has no vagolytic activity. It is used as a skeletal musclerelaxant in surgical procedures expected to last longer than90 minutes.
Pharmacokinetics
Doxacurium is a mixture of three trans, trans-stereoisomers, a dl pair [(1R,1′R,2S,2′S) and (1S,1′S,2R,2′R)] and a meso form (1R,1′S,2S,2′R).
Doxacurium is hydrophilic, has a small volume of distribution, and is distributed primarily to extracellular fluids. It is not metabolized by plasma
cholinesterase or hepatic enzymes and does not undergo Hofmann elimination.
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