• Kuan-Ting Chen, Oliver Yoa-Pu Hu, Shung-Tai Ho, Yu-Wen Chen, and Jhi-Joung Wang.
• Department of Anesthesiology, Chi-Mei Medical Center, Tainan, Taiwan, R.O.C.
• Acta Anaesthesiol. Sin. 2002 Dec 1; 40 (4): 191-5.

BackgroundNalbuphine 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.MethodsForty-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).ResultsBoth 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.ConclusionsNalbuphine pivalate has a very long duration of analgesic action. This fascinating finding is worth further evaluation.

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