Stanton-Hicks M, Murphy T M, Bonica J J, Mather L E, Tucker G T
Br J Anaesth. 1976 Jun;48(6):575-86. doi: 10.1093/bja/48.6.575.
Five healthy, unmedicated male volunteers, aged 19-25 yr, participated in a double-blind, crossover study. Each subject received, on separate occasions and via a catheter placed at L2, 1.5% etiodocaine HCl20 ml with adrenaline 5 mug/ml, or 0.75% bupivacaine HCl 20 ml with adrenaline 5 mug/ml for extradural analgesia. In addition, in order to calculate the absorption rate of the local anaesthetic agent, each subject received on two further occasions etidocaine HCl 75 mg and bupivacaine HCl 75 mg respectively by i.v. infusion, over a period of 10 min. Spread of sensory analgesia to four segments above and below the site of injection was faster with etidocaine (13 +/- 3 min) (mean +/- SD) than with bupivacaine (22 +/- 8 min). Two-segment regression occurred later for bupivacaine (260 +/- 57 min) than for etidocaine (180 +/- 96 min). Caudal spread of analgesia was more extensive with etidocaine than with bupivacaine. The onset of motor blockade tended to be faster with etidocaine (5.8 +/- 3.0 min), than with bupivacaine (10.0 +/- 3.5 min); regression of motor blockade by one unit was longer with etidocaine (306 +/- 103 min) than bupivacaine (238 +/- 75 min). Sudomotor block occurred earlier with etidocaine (4.0 +/- 2.1 min) than bupivacaine (13.7 +/- 4.8 min). Significant changes in cardiac stroke work and stroke volume occurred. For etidocaine these measurements remained below control values for 120-210 min after injection. The mean maximum arterial plasma concentration of etidocaine was 1.52 +/- 0.64 mug/ml, at 14 +/- 2 min and of bupivacaine was 1.35 +/- 0.63 mug/ml, achieved at 20 +/- 4 min. The systemic absorption of both drugs occurred in a biphasic pattern with a fast and slow half-life of 0.3 and approximately 8 h respectively.
5名年龄在19至25岁之间、身体健康且未接受药物治疗的男性志愿者参与了一项双盲交叉研究。每位受试者在不同时间通过置于L2的导管分别接受1.5%盐酸依替卡因20毫升加肾上腺素5微克/毫升或0.75%盐酸布比卡因20毫升加肾上腺素5微克/毫升用于硬膜外镇痛。此外,为了计算局部麻醉剂的吸收率,每位受试者在另外两个时间分别通过静脉输注接受75毫克盐酸依替卡因和75毫克盐酸布比卡因,持续10分钟。依替卡因使感觉镇痛向注射部位上下四个节段扩散的速度更快(13±3分钟)(平均值±标准差),快于布比卡因(22±8分钟)。布比卡因出现两节段消退的时间(260±57分钟)晚于依替卡因(180±96分钟)。依替卡因的镇痛向尾端扩散比布比卡因更广泛。依替卡因导致运动阻滞的起效往往比布比卡因更快(5.8±3.0分钟对10.0±3.5分钟);依替卡因运动阻滞消退一个单位的时间(306±103分钟)比布比卡因更长(238±75分钟)。依替卡因导致的汗腺运动阻滞比布比卡因更早出现(4.0±2.1分钟对13.7±4.8分钟)。心脏每搏功和每搏量发生了显著变化。对于依替卡因,这些测量值在注射后120至210分钟内仍低于对照值。依替卡因的平均最大动脉血浆浓度在14±2分钟时为1.52±0.64微克/毫升,布比卡因在20±4分钟时达到的平均最大动脉血浆浓度为1.35±0.63微克/毫升。两种药物的全身吸收均呈双相模式,快速半衰期为0.3小时,慢速半衰期约为8小时。