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新型神经肌肉阻滞药物。其临床药理学与治疗应用概述。

Newer neuromuscular blocking drugs. An overview of their clinical pharmacology and therapeutic use.

作者信息

Mirakhur R K

机构信息

Department of Anaesthetics, Queen's University, Belfast, Northern Ireland.

出版信息

Drugs. 1992 Aug;44(2):182-99. doi: 10.2165/00003495-199244020-00003.

DOI:10.2165/00003495-199244020-00003
PMID:1382013
Abstract

Four new nondepolarising muscle relaxants, pipecuronium bromide, doxacurium chloride, mivacurium chloride and Org 9426 (rocuronium) offer alternatives to the established agents atracurium besilate and vecuronium bromide. Pipecuronium and Org 9426 are steroidal compounds, the latter being a monoquaternary agent, whereas doxacurium and mivacurium are bisquaternary benzylisoquinolinium compounds. Pipecuronium and doxacurium have a relatively slow onset and a long duration of action. Pipecuronium produces maximum block in 3 to 6 min when given in a dose of 45 to 80 micrograms/kg, and a duration of clinical relaxation of between 40 and 110 min. Doxacurium is more potent, but is the least rapid and the longest acting relaxant currently available. When administered in doses of 37 to 80 micrograms/kg, it produces maximum block within 3.5 to 10 min, with a duration of clinical relaxation of 77 to 164 min. The advantage of both pipecuronium and doxacurium is their cardiovascular stability. Both agents are primarily eliminated via the kidneys and both have now been licensed for use in the US. Mivacurium is a muscle relaxant with a short duration of action. When administered in doses of 0.1 to 0.25 mg/kg it produces maximum block in 2 to 4 min, but the duration of clinical relaxation is less than 20 min. Higher doses which could induce a faster neuromuscular block are unfortunately associated with some histamine liberation. The drug is metabolised by plasma cholinesterase. Mivacurium has also been licensed for use in the US. Org 9426 is an agent with a rapid onset but an intermediate duration of action. A dose of 0.5 to 0.6 mg/kg induces maximum block in about 1.5 min and has a duration of clinical relaxation of about 30 min. The rapid onset of effect could be useful for early intubation as an alternative to suxamethonium chloride. However, much more clinical experience is needed with this agent, particularly with regard to duration of action of larger doses and occurrence of side effects. The drug is mainly eliminated via the liver.

摘要

四种新型非去极化肌肉松弛剂,哌库溴铵、多库氯铵、米库氯铵和Org 9426(罗库溴铵)为已有的阿曲库铵苯磺酸盐和维库溴铵提供了替代选择。哌库溴铵和Org 9426是甾体化合物,后者是单季铵盐类药物,而多库氯铵和米库氯铵是双季铵苄基异喹啉化合物。哌库溴铵和多库氯铵起效相对较慢,作用持续时间较长。哌库溴铵按45至80微克/千克的剂量给药时,3至6分钟内产生最大阻滞作用,临床松弛持续时间为40至110分钟。多库氯铵效力更强,但却是目前起效最慢、作用时间最长的肌肉松弛剂。按37至80微克/千克的剂量给药时,它在3.5至10分钟内产生最大阻滞作用,临床松弛持续时间为77至164分钟。哌库溴铵和多库氯铵的优点是它们对心血管系统有稳定性。这两种药物主要通过肾脏排泄,目前在美国均已获得使用许可。米库氯铵是一种作用持续时间短的肌肉松弛剂。按0.1至0.25毫克/千克的剂量给药时,2至4分钟内产生最大阻滞作用,但临床松弛持续时间不到20分钟。遗憾的是,能诱导更快神经肌肉阻滞的更高剂量会伴有一些组胺释放。该药物由血浆胆碱酯酶代谢。米库氯铵在美国也已获得使用许可。Org 9426是一种起效迅速但作用持续时间中等的药物。0.5至0.6毫克/千克的剂量在约1.5分钟内诱导最大阻滞作用,临床松弛持续时间约为30分钟。其快速起效作用可用于早期插管,作为氯琥珀胆碱的替代药物。然而,对于这种药物还需要更多的临床经验,特别是关于更大剂量的作用持续时间和副作用的发生情况。该药物主要通过肝脏排泄。

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