The analgesic effect of nalbuphine and its long-acting prodrug, nalbuphine pivalate, in rats.

Acta anaesthesiologica Sinica Pub Date : 2002-12-01

Kuan-Ting Chen, Oliver Yoa-Pu Hu, Shung-Tai Ho, Yu-Wen Chen, Jhi-Joung Wang

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Abstract

Background: Nalbuphine is an opioid-analgesic with agonist-antagonist properties. Recently, we have synthesized a nalbuphine prodrug, nalbuphine pivalate. The aim of the present study was to evaluate the analgesic effect and the analgesic duration of this prodrug.

Methods: Forty-eight male Sprague-Dawley rats (4 groups, n = 12 in each group) were used. Rats in group 1 received nalbuphine HCl 25 mumol/kg (in saline) intramuscular injection; rats in group 2 received nalbuphine pivalate 25 mumol/kg (in sesame oil) intramuscular injection, whereas those in groups 3 and 4 received saline and sesame oil respectively. The analgesic effects of testing agents were evaluated using the cold ethanol tail-flick test (-30 degrees C).

Results: Both nalbuphine HCl and nalbuphine pivalate demonstrated significant analgesic effects. The analgesic duration of nalbuphine HCl was 2 h while that of nalbuphine pivalate was 30 h.

Conclusions: Nalbuphine pivalate has a very long duration of analgesic action. This fascinating finding is worth further evaluation.

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纳布啡及其长效前药哌酸纳布啡对大鼠的镇痛作用。

背景:纳布啡是一种具有激动-拮抗剂特性的阿片类镇痛药。最近，我们合成了一种纳布啡前药，私家纳布啡。本研究的目的是评价该前药的镇痛效果和镇痛持续时间。方法:雄性Sprague-Dawley大鼠48只，分为4组，每组12只。1组大鼠给予盐酸纳布啡25 μ mol/kg(生理盐水)肌内注射;第2组大鼠肌肉注射盐酸纳布啡25 μ mol/kg(麻油中)，第3组和第4组大鼠分别注射生理盐水和麻油。采用冷乙醇甩尾试验(-30℃)评价试验剂的镇痛效果。结果:盐酸纳布啡和哌酸纳布啡均有明显的镇痛效果。盐酸纳布啡的镇痛时间为2 h，而哌酸纳布啡的镇痛时间为30 h。结论:哌酸纳布啡具有很长的镇痛作用时间。这一有趣的发现值得进一步评价。

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Acta anaesthesiologica Sinica

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