Journal Article

Antinociceptive effect of a novel long‐acting nalbuphine preparation

K. S. Liu, O. Y. P. Hu, S. T. Ho, J. I. Tzeng, Y. W. Chen and J. J. Wang

in BJA: British Journal of Anaesthesia

Published on behalf of the British Journal of Anaesthesia

Volume 92, issue 5, pages 712-715
Published in print May 2004 | ISSN: 0007-0912
Published online May 2004 | e-ISSN: 1471-6771 | DOI: https://dx.doi.org/10.1093/bja/aeh126
Antinociceptive effect of a novel long‐acting nalbuphine preparation†

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Background. A long‐acting analgesic may be particularly desirable in patients suffering from long‐lasting pain. The aim of the study was to evaluate the antinociceptive effect of a novel nalbuphine preparation and to determine its duration of action.

Methods. The antinociceptive effects of i.m. nalbuphine HCl in saline and nalbuphine base in sesame oil were evaluated in rats. The in vitro drug‐releasing profiles of nalbuphine HCl and base in different preparations were also evaluated.

Results. We found that i.m. nalbuphine HCl 25, 50 and 100 µmol kg–1 produced dose‐related antinociceptive effects with a duration of action of 1.5, 2 and 3 h, respectively. I.M. nalbuphine base 100, 200 and 400 µmol kg–1 also produced dose‐related antinociceptive effects but with longer durations of action: 27, 49 and 55 h, respectively. In vitro studies demonstrated that nalbuphine base in sesame oil had the slowest drug‐releasing profile of the different preparations.

Conclusions. I.M. injection of an oil formulation of nalbuphine base produced a long‐lasting antinociceptive effect.

Br J Anaesth 2004; 92: 712–15

Keywords: analgesics opioid, nalbuphine; nerve, long‐acting antinociception

Journal Article.  2266 words.  Illustrated.

Subjects: Anaesthetics

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