Department of Anaesthesiology, Hospital GOOI-NOORD, Blaricum, The Netherlands.
Clin Drug Investig. 1998;15(4):309-17. doi: 10.2165/00044011-199815040-00007.
In order to investigate the influence of general anaesthesia on the pharmacokinetics of bupivacaine 0.5% after a single, epidurally injected dose of 20ml (= 100mg), 5 patients, scheduled for surgical procedures appropriate for epidural anaesthesia without the need for combination with general anaesthesia, were studied. In all patients an arterial, central venous and intrathecal catheter were inserted for sampling of, respectively, arterial and central venous blood and cerebrospinal fluid (CSF), at regular intervals up to 12 hours after administration. Bupivacaine was analysed by gas chromatography. The drug appeared after 2 minutes in the plasma and CSF samples, and was still detectable after 12 hours. There were no significant differences between the bupivacaine concentrations in the arterial and central venous plasma samples at all times. The same applied for the calculated plasma pharmacokinetic parameters at all intervals. The bupivacaine concentrations in the CSF were many dozen times higher than in the plasma samples at all times. There was no clear evidence of a pulmonary retention of bupivacaine in this study. From a pharmacokinetic point of view the epidural anaesthesia was largely spinal anaesthesia.
为了研究单次硬膜外注射 20ml（=100mg）0.5%布比卡因后全身麻醉对布比卡因药代动力学的影响，选择 5 例需行硬膜外麻醉手术的患者，且这些手术无需与全身麻醉联合进行。所有患者均置入动脉、中心静脉和鞘内导管，以便在给药后 12 小时内定时抽取动脉和中心静脉血及脑脊液（CSF）样本，用于布比卡因分析。采用气相色谱法分析布比卡因。注药后 2 分钟，在血浆和 CSF 样本中即可检测到药物，12 小时后仍可检测到药物。在所有时间点，动脉和中心静脉血浆样本中的布比卡因浓度均无显著差异。在所有时间点，计算出的血浆药代动力学参数也无显著差异。CSF 中的布比卡因浓度在所有时间点均高于血浆样本的数十倍。在本研究中，无明显证据表明布比卡因存在肺蓄积。从药代动力学角度来看，硬膜外麻醉主要为脊髓麻醉。
