Suzuki Takahiro, Saeki Shigeru, Takeda Junzo, Ozaki Makoto, Iwao Yasuhide
Department of Anesthesiology, Surugadai Nihon University Hospital, Tokyo 101-8309.
Masui. 2006 Apr;55(4):419-27.
The purpose of this study was to examine pharmacodynamics, pharmacokinetics and safety of Org 9426 (rocuronium bromide) in Japanese patients.
Seventy-eight patients anesthetized with thiopental, droperidol, fentanyl and nitrous oxide, were randomized to receive either a single dose of Org 9426 0.3 mg x kg(-1), 0.6 mg x kg(-1) or 0.9 mg x kg(-1). Contraction of the adductor pollicis to the ulnar nerve stimulation (0.1 Hz) was measured by acceleromyography. Blood was sampled over 6 hr and pharmacokinetic variables were calculated by plasma concentrations of Org 9426.
Onset times for patients receiving 0.3 mg x kg(-1), 0.6 mg x kg(-1) or 0.9 mg x kg(-1) were 271.5 s, 140.0s and 125.4s, respectively. There was a dose-dependent increase in clinical durations until 25% recovery of twitch height (17.4 min in 0.3 mg x kg(-1) group, 37.2 min in 0.6 mg x kg(-1) and 60.4 min in 0.9 mg x kg(-1) group). Pharmacokinetic study revealed that elimination half life, steady state volume of distribution and plasma clearance of Org 9426 were 48-76 min, 146-181 ml x kg(-1), and 3.8-4.5 ml x min(-1) x kg(-1), respectively. No adverse effects were found except a case of local erythema on a forearm.
The efficacy of neuromuscular block, stable pharmacokinetic behavior and excellent safety of Org 9426 were also confirmed in Japanese surgical patients.
本研究旨在考察Org 9426（罗库溴铵）在日本患者中的药效学、药代动力学及安全性。
78例接受硫喷妥钠、氟哌利多、芬太尼和氧化亚氮麻醉的患者，随机接受单次剂量的Org 9426，剂量分别为0.3 mg·kg⁻¹、0.6 mg·kg⁻¹或0.9 mg·kg⁻¹。通过加速度描记法测量尺神经刺激（0.1 Hz）引起的拇内收肌收缩。在6小时内采集血样，并根据Org 9426的血浆浓度计算药代动力学变量。
接受0.3 mg·kg⁻¹、0.6 mg·kg⁻¹或0.9 mg·kg⁻¹的患者起效时间分别为271.5秒、140.0秒和125.4秒。临床作用持续时间呈剂量依赖性增加，直至颤搐高度恢复25%（0.3 mg·kg⁻¹组为17.4分钟，0.6 mg·kg⁻¹组为37.2分钟，0.9 mg·kg⁻¹组为60.4分钟）。药代动力学研究表明，Org 9426的消除半衰期、稳态分布容积和血浆清除率分别为48 - 76分钟、146 - 181 ml·kg⁻¹和3.8 - 4.5 ml·min⁻¹·kg⁻¹。除1例前臂局部红斑外，未发现不良反应。
在日本外科手术患者中也证实了Org 9426神经肌肉阻滞的有效性、稳定的药代动力学行为及出色的安全性。
