Meert T F, Lu H R, van Craenndonck H, Janssen P A
Janssen Research Foundation, Department of Neuropsychopharmacology, Beerse, Belgium.
Eur J Anaesthesiol. 1988 Sep;5(5):313-21.
The effects of epidural fentanyl, sufentanil, carfentanil, lofentanil and alfentanil were compared in the rat. All five opiates produced analgesia with the relative order of potency being lofentanil greater than carfentanil greater than sufentanil greater than fentanyl greater than alfentanil, and the relative order of duration at comparative doses lofentanil greater than sufentanil greater than carfentanil greater than fentanyl greater than alfentanil. Because epidural administered opiates still exert some effects within the brain, specificity ratios (defined as the ratio between the ED50s for a prolongation of the tail-withdrawal reaction latency and a blockade of the pinna reflex) were calculated. The relative order of specificity between the five opiates was fentanyl greater than lofentanil greater than sufentanil greater than carfentanil greater than alfentanil. These results are discussed in the context of the search for a safe and sufficiently long-acting lipid soluble epidural analgesic. It is concluded that of these five opiates, sufentanil appears to be the best drug of choice for epidural analgesia.
在大鼠中比较了硬膜外给予芬太尼、舒芬太尼、卡芬太尼、洛芬太尼和阿芬太尼的效果。所有这五种阿片类药物均产生镇痛作用,效价的相对顺序为洛芬太尼>卡芬太尼>舒芬太尼>芬太尼>阿芬太尼,在比较剂量下作用持续时间的相对顺序为洛芬太尼>舒芬太尼>卡芬太尼>芬太尼>阿芬太尼。由于硬膜外给予的阿片类药物仍会在脑内发挥一些作用,因此计算了特异性比值(定义为延长甩尾反应潜伏期的ED50与阻断耳廓反射的ED50之比)。这五种阿片类药物之间特异性的相对顺序为芬太尼>洛芬太尼>舒芬太尼>卡芬太尼>阿芬太尼。在寻找一种安全且作用足够持久的脂溶性硬膜外镇痛药的背景下对这些结果进行了讨论。得出的结论是,在这五种阿片类药物中,舒芬太尼似乎是硬膜外镇痛的最佳选择药物。