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

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

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)

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 μmol/kg (in saline) intramuscular injection; rats in group 2 received nalbuphine pivalate 25 μmol/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°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.

Original languageEnglish
Pages (from-to)191-195
Number of pages5
JournalActa Anaesthesiologica Sinica
Volume40
Issue number4
Publication statusPublished - Dec 1 2002
Externally publishedYes

Keywords

  • Analgesia
  • Nalbuphine
  • Nalbuphine pivalate
  • Prodrug

ASJC Scopus subject areas

  • Anesthesiology and Pain Medicine

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