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顺式阿曲库铵

[Cisatracurium].

作者信息

Ortiz J R, Percaz J A, Carrascosa F

机构信息

Departamento de Anestesiología y Cuidados Intensivos, Clínica Universitaria de Navarra. Facultad de Medicina.

出版信息

Rev Esp Anestesiol Reanim. 1998 Jun-Jul;45(6):242-7.

PMID:9719722
Abstract

Cisatracurium is one of ten isomers that form the racemic mix of atracurium (51W89 or 1 R-cis, 1'R-cis atracurium). It is three times more potent than atracurium itself and hemodynamically stable thanks to its scarce release of histamine. Cisatracurium is hydrolyzed mainly by the pathway of Hofmann (77%) and to a lesser degree it is metabolized by organ-dependent modes (mainly by the kidney (16%)). Dose therefore hardly needs to be changed for elderly patients or those with liver, kidney or cardiovascular disease. The calculated ED95 is 0.05 mg.kg-1 (0.04 mg.kg-1 in children), although a dose two to four times greater is used under clinical conditions to shorten tracheal intubation time because of low onset of blockade, particularly in comparison with rocuronium. The period of deep blockade (lack of response to neurostimulation) is prolonged by the higher dose, but recovery is dose-independent and recovery indices are similar. Cisatracurium has proven useful in intensive care because of its hemodynamic stability, which is comparable to that of steroid derivatives but with faster recovery from blockade once administration is discontinued. Its metabolism predominantly through Hofmann's pathway, with less laudanosine formation than is produced by atracurium, is also appreciated. Cisatracurium is described as the nondepolarizing muscle relaxant of choice for medium-to-long-term surgery on hemodynamically unstable patients or those with kidney or liver disease, and for neuromuscular blockade in intensive care.

摘要

顺式阿曲库铵是构成阿曲库铵(51W89或1R-顺式,1'R-顺式阿曲库铵)消旋混合物的十种异构体之一。它的效力是阿曲库铵本身的三倍,并且由于其组胺释放较少,血流动力学稳定。顺式阿曲库铵主要通过霍夫曼途径水解(77%),在较小程度上通过器官依赖模式代谢(主要通过肾脏(16%))。因此,对于老年患者或患有肝、肾或心血管疾病的患者,剂量几乎无需改变。计算得出的ED95为0.05mg·kg-1(儿童为0.04mg·kg-1),尽管在临床情况下,由于起效较慢,尤其是与罗库溴铵相比,为缩短气管插管时间会使用两到四倍大的剂量。较高剂量会延长深度阻滞期(对神经刺激无反应),但恢复与剂量无关,恢复指标相似。顺式阿曲库铵因其血流动力学稳定性已被证明在重症监护中有用,其稳定性与类固醇衍生物相当,但一旦停药,从阻滞中恢复得更快。人们也认识到它主要通过霍夫曼途径代谢,与阿曲库铵相比,形成的劳丹诺辛较少。顺式阿曲库铵被认为是对血流动力学不稳定患者或患有肾脏或肝脏疾病的患者进行中到长期手术以及在重症监护中进行神经肌肉阻滞时的首选非去极化肌松药。

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