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外観
白色〜ほとんど白色, 結晶〜粉末
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溶解性
、エタノール(99.5)に極めて溶けやすく、うすい塩酸に溶け、水及びアセトンに溶けにくい。
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用途
神経筋接合部のアセチルコリ ンによる神経から筋への興奮伝達を遮断し、 D-ツボクラリンと同様非脱分極性神経遮断作 用を示します。
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用途
神経筋接合部のアセチルコリ
ンによる神経から筋への興奮伝達を遮断し、
D- ツボクラリンと同様非脱分極性神経遮断作
用を示します。
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効能
骨格筋弛緩薬, 神経筋遮断薬, ムスカリン受容体拮抗薬
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説明
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.
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化学的特性
White Solid
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使用
An aminosteroid, competitive neuromuscular blocker agent.
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定義
ChEBI: The organic bromide salt of a 5alpha-androstane compound having 3alpha-acetoxy-, 17beta-acetoxy-, 2beta-piperidinino- and 16beta-N-methylpiperidinium su
stituents.
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生物学の機能
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.
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一般的な説明
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.
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薬理学
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.
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臨床応用
Vecuronium Bromide is usedmainly to produce skeletal muscle relaxation during surgeryand to assist in controlled respiration after general anesthesiahas been induced.
