Kanai Y, Tateyama S, Nakamura T, Kasaba T, Takasaki M
Department of Anesthesiology, Miyazaki Medical College, Kiyotake, Japan.
Reg Anesth Pain Med. 1999 Sep-Oct;24(5):444-52. doi: 10.1016/s1098-7339(99)90012-3.
Commercially available bupivacaine is a racemic mixture of S (-)- and R(+)-enantiomers. Although the S(-)-enantiomers levobupivacaine and ropivacaine are less toxic to the cardiovascular and central nervous systems than bupivacaine, their relative efficacy has not been determined. This study directly compares the dose response of levobupivacaine, ropivacaine, and bupivacaine following epidural and intrathecal administration in the rat.
The time course of change in tail-flick latency and qualitative motor function was studied in rats following epidural or intrathecal administration of 0.25-0.75% levobupivacaine, ropivacaine, or bupivacaine in blinded, randomized fashion.
Levobupivacaine and bupivacaine produced comparable and significantly enduring antinociceptive effects compared with ropivacaine at all test concentrations following both epidural and intrathecal administrations. Duration of motor block at lower local anesthetic concentrations (epidurally and intrathecally) was comparable with levobupivacaine and ropivacaine but significantly shorter than with bupivacaine. Epidural 0.75% levobupivacaine and bupivacaine showed more enduring motor block than ropivacaine.
Levobupivacaine, given epidurally or intrathecally, produces longer lasting antinociceptive action than ropivacaine at equivalent concentrations and similar motor blocking effect at lower concentrations in both epidural and intrathecal administrations. Levobupivacaine-induced prolongation of the tail-flick latency is comparable to that of bupivacaine, as is motor blocking effect at higher concentrations. The possibility of significant differential block with levobupivacaine compared with bupivacaine warrants further study.
市售布比卡因是S(-)-和R(+)-对映体的外消旋混合物。尽管左旋布比卡因和罗哌卡因这两种S(-)-对映体对心血管和中枢神经系统的毒性低于布比卡因,但其相对疗效尚未确定。本研究直接比较了大鼠硬膜外和鞘内注射左旋布比卡因、罗哌卡因和布比卡因后的剂量反应。
采用双盲、随机方式,对大鼠硬膜外或鞘内注射0.25 - 0.75%左旋布比卡因、罗哌卡因或布比卡因后甩尾潜伏期和定性运动功能的变化时间过程进行了研究。
在硬膜外和鞘内给药后的所有测试浓度下,与罗哌卡因相比,左旋布比卡因和布比卡因产生了相当且显著持久的镇痛效果。在较低局部麻醉药浓度(硬膜外和鞘内)下,运动阻滞持续时间与左旋布比卡因和罗哌卡因相当,但明显短于布比卡因。硬膜外注射0.75%左旋布比卡因和布比卡因的运动阻滞比罗哌卡因更持久。
硬膜外或鞘内注射时,左旋布比卡因在等效浓度下产生的镇痛作用比罗哌卡因更持久,在硬膜外和鞘内给药的较低浓度下具有相似的运动阻滞效果。左旋布比卡因引起的甩尾潜伏期延长与布比卡因相当,在较高浓度下的运动阻滞效果也相当。与布比卡因相比,左旋布比卡因存在显著差异阻滞的可能性,值得进一步研究。