Onrust S V, Foster R H
Adis International Limited, Mairangi Bay, Auckland, New Zealand.
Drugs. 1999 Nov;58(5):887-918. doi: 10.2165/00003495-199958050-00011.
Rapacuronium bromide (rapacuronium) is an aminosteroid, nondepolarising neuromuscular blocking agent (NMBA). At the recommended dose for endotracheal intubation (1.5 mg/kg), an intravenous bolus of rapacuronium has a rapid onset (approximately 1.2 to 1.8 minutes) and short duration of action (10.2 to 16.5 minutes) in adults undergoing elective surgery. Rapacuronium 1.5 mg/kg produced clinically acceptable intubating conditions in 68 to 89% of these patients at about 1 minute after administration. The onset, extent and duration of action and clinical efficacy of an intubating dose of rapacuronium appeared to be similar in the general adult population, adult patients with renal or hepatic dysfunction, patients undergoing Caesarean section, and elderly, paediatric or obese adult patients. Onset time with rapacuronium 1.3 to 2.5 mg/kg (0.9 to 1.8 minutes) was similar to or slower than that with a 1 mg/kg dose of the depolarising NMBA suxamethonium chloride (0.8 to 1.2 minutes). Intubating conditions were clinically acceptable about I minute after administration in 86 to 100% of patients with rapacuronium 1.3 to 2.5 mg/kg compared with in 88 to 97% of patients with suxamethonium chloride 1 or 1.5 mg/kg. Spontaneous recovery was slower with rapacuronium than with suxamethonium chloride, but neostigmine 0.04 or 0.05 mg/kg administered 2 or 5 minutes after rapacuronium 1.3 or 1.5 mg/kg accelerated recovery. In the few available comparative clinical trials, rapacuronium 1.5 mg/kg appeared to have a more rapid onset of action than the nondepolarising NMBAs mivacurium chloride 0.25 mg/kg, rocuronium bromide 0.45 or 0.6 mg/kg or vecuronium bromide 0.07 mg/kg, and a shorter duration of action than rocuronium bromide 0.45 or 0.6 mg/kg or vecuronium bromide 0.07 mg/kg. Additional boluses (< or =3) of rapacuronium 0.5 or 0.55 mg/kg after an intubating bolus of 1.5 mg/kg provided continued skeletal muscle relaxation during short surgical procedures in adult patients. However, these patients may recover more slowly than those who receive a single bolus of the drug. Bronchospasm was the most common treatment-related adverse event with rapacuronium 0.3 to 3 mg/kg (3.4% of adult patients). Tachycardia, injection site reaction and hypotension were also reported in small proportions of patients (1.6, 1.1 and 0.9%). The overall incidence of drug-related adverse events was similar with rapacuronium 1.5 or 2.5 mg/kg or suxamethonium chloride 1 mg/kg (8 vs. 6%) but bronchospasm, tachycardia and injection site reaction tended to occur more often with rapacuronium.
At the recommended dose of 1.5 mg/kg, the nondepolarising NMBA rapacuronium has a rapid onset and short duration of action. It may provide a nondepolarising alternative to suxamethonium chloride for endotracheal intubation. Rapacuronium may be preferred over rocuronium bromide, vecuronium bromide or mivacurium chloride in this indication.
溴瑞帕库铵(瑞帕库铵)是一种氨基甾体类非去极化神经肌肉阻滞剂(NMBA)。在气管插管推荐剂量(1.5mg/kg)下,静脉推注瑞帕库铵后,择期手术成年患者起效迅速(约1.2至1.8分钟)且作用持续时间短(10.2至16.5分钟)。给予1.5mg/kg瑞帕库铵后,约1分钟时,68%至89%的这些患者达到临床可接受的插管条件。在普通成年人群、有肾或肝功能障碍的成年患者、剖宫产患者以及老年、儿科或肥胖成年患者中,插管剂量的瑞帕库铵的起效、作用程度和持续时间以及临床疗效似乎相似。1.3至2.5mg/kg瑞帕库铵的起效时间(约0.9至1.8分钟)与1mg/kg剂量的去极化NMBA氯化琥珀胆碱(0.8至1.2分钟)相似或更慢。给予1.3至2.5mg/kg瑞帕库铵后,约1分钟时,86%至100%的患者插管条件临床可接受,而给予1或1.5mg/kg氯化琥珀胆碱的患者中这一比例为88%至97%。瑞帕库铵的自主恢复比氯化琥珀胆碱慢,但在给予1.3或1.5mg/kg瑞帕库铵后2或5分钟给予0.04或0.05mg/kg新斯的明可加速恢复。在少数可用的比较临床试验中,1.5mg/kg瑞帕库铵的起效似乎比非去极化NMBA 0.25mg/kg氯米库铵、0.45或0.6mg/kg罗库溴铵或0.07mg/kg维库溴铵更快,且作用持续时间比0.45或0.6mg/kg罗库溴铵或0.07mg/kg维库溴铵更短。在给予1.5mg/kg插管剂量后,追加0.5或0.55mg/kg瑞帕库铵(≤3次)可在成年患者的短手术过程中持续提供骨骼肌松弛。然而,这些患者的恢复可能比单次给予该药物的患者更慢。支气管痉挛是0.3至3mg/kg瑞帕库铵最常见的与治疗相关的不良事件(成年患者的3.4%)。小部分患者还报告有心动过速、注射部位反应和低血压(分别为1.6%、1.1%和0.9%)。1.5或2.5mg/kg瑞帕库铵与1mg/kg氯化琥珀胆碱的药物相关不良事件总发生率相似(分别为8%和6%),但瑞帕库铵导致支气管痉挛、心动过速和注射部位反应的情况往往更常见。
在推荐剂量1.5mg/kg下,非去极化NMBA瑞帕库铵起效迅速且作用持续时间短。它可为气管插管提供一种替代氯化琥珀胆碱的非去极化药物选择。在此适应证中,瑞帕库铵可能比罗库溴铵、维库溴铵或氯米库铵更受青睐。