DOXACURIUM CHLORIDE

Reaction

Ligand for the palladium catalyzed aqueous Lipshutz-Negishi cross-coupling of alkyl halides with aryl electrophiles.

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.

Originator

Wellcome (United Kingdom)

Uses

Doxacurium Chloride is a nondepolarizing neuromuscular blocking agent that is minimally hydrolyzed by human plasma cholinesterase.

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.

Raw materials

Preparation Products