The addition of dilute epinephrine produces equieffectiveness of bupivacaine enantiomers for cutaneous analgesia in the rat
The addition of dilute epinephrine produces equieffectiveness of bupivacaine enantiomers for cutaneous analgesia in the rat
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DOI：
10.1097/00000539-200008000-00034
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发表时间：
2000-08-01
影响因子：
5.7
通讯作者：
Strichartz, GR
中科院分区：
文献类型：
--
作者：
Khodorova, AB;Strichartz, GR
本文研究了布比卡因（Bup）立体异构体对雄性大鼠皮肤的镇痛作用。作为浸润麻醉的模型，通过皮下注射0.6 mL不同浓度的R-、S-和外消旋-Bup来抑制疼痛性反射，通过针刺未能引起疼痛性运动反应的次数的分数来定量评价。R-Bup在阻滞程度上更有效;然而，S-Bup在较小剂量下具有更持久的作用。当R-Bup和S-Bup分别以0.06%和0.075%的等效剂量给药时，该显著差异明显。共注射肾上腺素（Epi）与这些等效剂量的增强和延长的阻滞作用的两个Bup立体异构体，虽然在稀释度为1：100，000至1：1，000，000 Epi本身诱导部分，短暂的镇痛。在1：2，000，000稀释度下，Epi单独没有镇痛作用;然而，当与作用较短的R-Bup（0.06%）共同注射时，Epi延长其阻滞作用，使其与等效S-Bup（0.075%）诱发的阻滞持续时间相等。我们的结论是R-Bup是更有效的皮肤镇痛和较长的时间阻滞S-Bup可能源于血管收缩活性。
We in investigated the effectiveness for cutaneous analgesia of bupivacaine (Bup) stereoisomers in male rats. As a model of infiltration anesthesia, inhibition of a nocifensive reflex by subcutaneous injection of 0.6 mL of different concentrations of R-, S-, and racemic-Bup was evaluated quantitatively by the fraction of times a pinprick failed to evoke a nocifensive motor response. R-Bup was more potent in the extent of block; however, S-Bup had a longer-lasting action at smaller doses. This significant difference was apparent when R-Bup and S-Bup were administered in equipotent doses of 0.06% and 0.075%, respectively. Co-injection of epinephrine (Epi) with these equipotent doses enhanced and prolonged the blocking effects of both Bup stereoisomers, although at dilutions of 1:100,000 to 1:1,000,000 Epi itself induced partial, transient analgesia. At 1:2,000,000 dilution, Epi alone had no analgesic effect; however, when co-injected with the shorter-acting R-Bup (0.06%), Epi prolonged its blocking effect to equal the duration of block evoked by equipotent S-Bup (0.075%). We conclude R-Bup is more potent for cutaneous analgesia and that the longer duration of block by S-Bup probably originates from vasoconstrictor activity.