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 language | English |
|---|---|
| Pages (from-to) | 191-195 |
| Number of pages | 5 |
| Journal | Acta Anaesthesiologica Sinica |
| Volume | 40 |
| Issue number | 4 |
| Publication status | Published - Dec 1 2002 |
| Externally published | Yes |
Keywords
- Analgesia
- Nalbuphine
- Nalbuphine pivalate
- Prodrug
ASJC Scopus subject areas
- Anesthesiology and Pain Medicine