Vecuroniumbromid Chemische Eigenschaften,Einsatz,Produktion Methoden
R-S?tze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-S?tze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Beschreibung
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.
Chemische Eigenschaften
White Solid
Verwenden
An aminosteroid, competitive neuromuscular blocker agent.
Definition
ChEBI: The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium su
stituents.
Biologische Funktion
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.
Allgemeine Beschreibung
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.
Mechanism of action
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.
Pharmakologie
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.
Clinical Use
Vecuronium Bromide is usedmainly to produce skeletal muscle relaxation during surgeryand to assist in controlled respiration after general anesthesiahas been induced.
Vecuroniumbromid Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte