パンクロニウムブロミド

化学的特性White or off-white crystalline or crystalline powder, faintly odorous, bitter taste. Hygroscopic. 1g dissolves in 30 parts chloroform, 1 part water (20°C). Soluble in water, ethanol, methanol, chloroform or dichloromethane; insoluble in diethyl ether. Acute toxicity LD₅₀ in mice (mg/kg): 0.047 intravenous injection, 0.152 intraperitoneal injection, 0.167 subcutaneous injection, 21.9 oral administration. Acute toxicity LD₅₀ in rats and rabbits (mg/kg): 0.153, 0.016 intravenous injection.

用途アセチルコリン受容体遮断作 用を示します。

用途アセチルコリン受容体遮断作 用を示します。

説明Pancuronium bromide, a bisquaternary amine and the first steroid N MBA used clinically, was developed by Savege and Hewitt and marketed in 1964. The intubating dose is 0.1mgkg–1, which takes 3-4min to reach its maximum effect. The clinical duration of action of the drug is long, especially in the presence of potent inhalational agents or renal dysfunction, as 60% of a dose of the drug is excreted unchanged through the kidneys. I t is also deacetylated in the liver; some of the metabolites have neuromuscular blocking properties.Pancuronium does not stimulate histamine release; however, it has direct vagolytic and sympathomimetic effects which may cause tachycardia and hypertension. It slightly inhibits plasma cholinesterase and therefore potentiates any drug metabolised by this enzyme, such as suxamethonium and mivacurium.

使用Pancuronium Bromide has been used as an analgesic in various experiments.

純化方法The bromide forms odourless crystals with a bitter taste which are purified through acid-washed Al2O3 and eluted with isoPrOH/EtOAc (3:1) to remove impurities (e.g. the monomethobromide) and eluted with isoPrOH to give the pure dibromide which is recrystallised from CH2Cl2/Me2CO or isoPrOH/Me2CO. It is soluble in H2O (10%) and CHCl3 (3.3%) at 20o. It is a non-depolarising muscle relaxant. [Buckett et al. J Med Chem 16 1116 1973.]