Mivacurium chloride

DescriptionMivacurium chloride,a mixture of three stereoisomers, is an intravenously administered, short-acting skeletal muscle relaxant introduced as an adjunct to general anesthesia. Structurally mivacurium chloride is closely related to doxacurium chloride introduced in 1991 by Wellcome as a muscle relaxant. It is a nondepolarizing neuromuscular blocking agent reportedly with a shorter duration of action and a more rapid rate of spontaneous recovery than other nondepolarizing agents. In extensive clinical trials mivacurium chloride was well tolerated with few side effects.

DescriptionMivacurium is an antagonist of nicotinic acetylcholine receptors (nAChRs) and muscarinic M2 and M3 receptors (ED50s = 0.08, 0.3, and 0.1 mg/kg for ex vivo human skeletal muscle nAChRs, guinea pig cardiac M2 receptors, and guinea pig bronchial M3 receptors, respectively). It inhibits acetylcholine-induced activation of neuronal nAChRs (IC50s = 69.04, 3.71, 1.52, and 2.90 for human α3β2-, α3β4-, α4β2-, and α7-containing nAChRs expressed in Xenopus oocytes). Mivacurium also inhibits adult human muscular α1β1εδ-containing nAChRs (IC50 = 3.69 nM in Xenopus oocytes expressing the human recombinant receptor). In vivo, mivacurium inhibits bradycardia and bronchoconstriction induced by vagal stimulation or acetylcholine in guinea pigs. It also induces neuromuscular blockade (ED95 = 80 μg/kg) in sheep with a more rapid onset time than atracurium and vecuronium . Formulations containing mivacurium have been used for pediatric anesthesia.

UsesNon-depolarizing neuromuscular blocking agent. Muscle relaxant (skeletal)

General DescriptionMivacurium chloride, 1,2,3,4-tetrahydro-2-(3-hydroxypropyl)-6,7-dimethoxy-2-methyl-1-(3,4,5-trimethoxybenzyl)isoquinolinium chloride, (E)-4-octandioate (Mivacron), is a mixture of three stereoisomers,the trans-trans, cis-trans, and cis-cis diesters, each ofwhich has neuromuscular blocking properties. The cis-cisisomer is about one tenth as potent as the other isomers.Mivacurium chloride is a short-acting nondepolarizing drugused as an adjunct to anesthesia to relax skeletal muscle.The drug is hydrolyzed by plasma esterases, and it is likelythat anticholinesterase agents used as antidotes could prolongrather than reverse the effects of the drug.