Geisslinger G, Hering W, Thomann P, Knoll R, Kamp H D, Brune K
Department of Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nuernberg, Germany.
Br J Anaesth. 1993 Jun;70(6):666-71. doi: 10.1093/bja/70.6.666.
In a randomized, double-blind study, we have examined the stereoselective disposition and pharmacodynamic characteristics of ketamine in surgical patients after i.v. administration of S(+)-ketamine 1 mg/kg body weight (25 patients) or racemic ketamine 2 mg/kg body weight (25 patients). S(+)-Ketamine was not inverted to R(-)-ketamine. After racemate administration we observed statistically significant (P < 0.01) smaller clearance and volume of distribution for R(-)-ketamine compared with S(+)-ketamine. In contrast, the pharmacokinetic variables of S(+)-ketamine were not significantly different between treatment groups. Systolic and diastolic arterial pressure and heart rate increased significantly (P < 0.005) in both groups. At 1, 3 and 15 min after S(+)-ketamine administration, significantly greater increase in systolic and diastolic pressures were observed compared with the racemate group. There was no correlation between the changes in haemodynamic variables and plasma catecholamine concentrations, which remained unaffected after administration of the medications.
在一项随机双盲研究中，我们研究了静脉注射1 mg/kg体重的S(+)-氯胺酮（25例患者）或2 mg/kg体重的消旋氯胺酮（25例患者）后，氯胺酮在手术患者中的立体选择性处置和药效学特征。S(+)-氯胺酮未转化为R(-)-氯胺酮。给予消旋体后，我们观察到与S(+)-氯胺酮相比，R(-)-氯胺酮的清除率和分布容积在统计学上显著更小（P < 0.01）。相比之下，S(+)-氯胺酮的药代动力学变量在治疗组之间无显著差异。两组的收缩压和舒张压以及心率均显著升高（P < 0.005）。在给予S(+)-氯胺酮后1、3和15分钟，与消旋体组相比，收缩压和舒张压的升高显著更大。血流动力学变量的变化与血浆儿茶酚胺浓度之间无相关性，给药后血浆儿茶酚胺浓度未受影响。
