Векуроний бромид

Описание

Vecuronium, 1-[(2β,3α,5α,16β,17β,)-3,17-bis(acetyloxy)-2-(1-piperidinyl) androstan-16-yl]-1-methylpiperidinium bromide (15.1.9), differs from panuronium only in the extent of alkylation. Only the piperidine substituent on C16 of the steroid skeleton is transformed into a quaternary salt.

Химические свойства

White Solid

Использование

An aminosteroid, competitive neuromuscular blocker agent.

Определение

ChEBI: The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium su stituents.

Биологические функции

Vecuronium bromide (Norcuron) is chemically identical to pancuronium except for a tertiary amine in place of a quaternary nitrogen. However, some of the drug will exist as the bisquaternary compound, depending on body pH. Vecuronium has a moderate onset of action (2.4 minutes) and a duration of effect of about 50 minutes. Like pancuronium, it does not block ganglia or vagal neuroeffector junctions, does not release histamine, and is eliminated by urinary excretion.

Общее описание

Vecuronium bromide, 1-(3 ,17 -dihydroxy-2 -piperidino-5 -androstan-16 -yl)-1-methylpiperidinium bromide diacetate (Norcuron), is themonoquaternary analog of pancuronium bromide. It belongsto the class of nondepolarizing neuromuscular blockingagents and produces effects similar to those of drugs in thisclass. It is unstable in the presence of acids and undergoesgradual hydrolysis of its ester functions in aqueous solution.Aqueous solutions have a pH of about 4.0.

Механизм действия

Vecuronium bromide is a bisquaternary nitrogen compound that acts by competitively binding to nicotinic cholinergic receptors. The binding of vecuronium decreases the opportunity for acetylcholine to bind to the nicotinic receptor at the postjunctional membrane of the myoneural junction. As a result, depolarization is prevented, calcium ions are not released and muscle contraction does not occur.

Фармаколо?гия

Vecuronium bromide is steroidal agent that was developed in an attempt to reduce the cardiovascular effects of pancuronium. I t is similar in structure to the older drug, differing only in the loss of a methyl group from one quaternary ammonium radical. Thus it is a monoquaternary amine. An intubating dose of 0.1mgkg^-1 produces profound neuromuscular block within 3min. This dose produces clinical block for about 30min. Vecuronium rarely produces histamine release, nor does it have any direct cardiovascular effects, although it allows the cardiac effects of other anaesthetic agents, such as bradycardia produced by the opioids, to go unchallenged. Vecuronium is excreted through the kidneys (30%), although to a lesser extent than pancuronium, and undergoes hepatic deacetylation; the deacetylated metabolites have neuromuscular blocking properties. Repeated doses should be used with care in patients with renal or hepatic disease because they accumulate.

Клиническое использование

Vecuronium Bromide is usedmainly to produce skeletal muscle relaxation during surgeryand to assist in controlled respiration after general anesthesiahas been induced.