Ornstein E, Lien C A, Matteo R S, Ostapkovich N D, Diaz J, Wolf K B
Department of Anesthesiology, College of Physicians and Surgeons of Columbia University, New York 10032, USA.
Anesthesiology. 1996 Mar;84(3):520-5. doi: 10.1097/00000542-199603000-00005.
Cisatracurium, one of ten stereoisomers that comprise atracurium, is more potent than atracurium and has less propensity to release histamine. This study compares the pharmacokinetics and pharmacodynamics of cisatracurium in elderly and young patients.
Twelve elderly (aged 65-82 yr) and 12 younger patients (aged 30-49 yr) were anesthetized with nitrous oxide, fentanyl, and isoflurane (0.7%, end-tidal). The mechanomyographic response to train-of-four stimulation was assessed every 15 s after the administration of cisatracurium (0.1 mg/kg). Arterial samples were obtained over 6 h. Plasma cisatracurium concentration versus time data were fit to compartmental models. Pharmacokinetic parameters were determined assuming that elimination occurred from the central compartment only. This provides accurate clearance and half-life estimates but underestimates V(ss) (reported herein as V(ss). The pharmacodynamic response was described by the neuromuscular blocking profile.
Onset to 90% paralysis (mean +/- SD) was delayed in the elderly (3.4 +/- 1.0 vs. 2.5 +/- 0.6 min). Recovery profiles were the same for both groups. Elimination half-life was minimally prolonged in the elderly (25.5 +/- 3.7 vs. 21.5 +/- 2.4 min). The Vss was larger in the elderly (126 +/- 16 vs. 108 +/- 13 ml/kg), although the clearances were the same for the two groups (5.0 +/- 0.9 vs. 4.6 +/- 0.8 ml.kg(-1).min(-1).
There are minor differences in the pharmacokinetics of cisatracurium between elderly and young patients. These differences are not associated with changes in recovery profile after a single bolus dose, although the mean time to onset was approximately 1 min longer in elderly patients.
顺式阿曲库铵是组成阿曲库铵的十种立体异构体之一，其效力比阿曲库铵更强，且释放组胺的倾向较小。本研究比较了顺式阿曲库铵在老年和年轻患者中的药代动力学和药效学。
12名老年患者（年龄65 - 82岁）和12名年轻患者（年龄30 - 49岁）接受氧化亚氮、芬太尼和异氟烷（呼气末浓度0.7%）麻醉。给予顺式阿曲库铵（0.1mg/kg）后每15秒评估一次对四个成串刺激的肌机械反应。在6小时内采集动脉血样。血浆顺式阿曲库铵浓度与时间数据拟合房室模型。假设仅从中枢室消除来确定药代动力学参数。这可提供准确的清除率和半衰期估计，但会低估稳态分布容积（本文报告为V(ss)）。药效学反应通过神经肌肉阻滞曲线描述。
老年患者达到90%麻痹的起效时间（平均值±标准差）延迟（3.4±1.0分钟 vs. 2.5±0.6分钟）。两组的恢复曲线相同。老年患者的消除半衰期略有延长（25.5±3.7分钟 vs. 21.5±2.4分钟）。老年患者的稳态分布容积更大（126±16 vs. 108±13ml/kg），尽管两组的清除率相同（5.0±0.9 vs. 4.6±0.8ml·kg⁻¹·min⁻¹）。
老年和年轻患者之间顺式阿曲库铵的药代动力学存在微小差异。这些差异与单次推注剂量后的恢复曲线变化无关，尽管老年患者的平均起效时间约长1分钟。
