The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain

@article{Gear1999TheKO,
  title={The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain},
  author={Robert William Gear and Christine Miaskowski and Newton C. Gordon and Steven M Paul and Philip H. Heller and Jon D. Levine},
  journal={PAIN},
  year={1999},
  volume={83},
  pages={339-345}
}
Nalbuphine, pentazocine, and butorphanol, mixed agonist/antagonist opioids that induce analgesia by acting predominantly at kappa opioid receptors, have recently been shown in single-dose studies to have greater analgesic efficacy in women than in men. In the current experiments, the first placebo controlled dose response study of opioid analgesic efficacy that examines for gender differences, nalbuphine (5, 10, or 20 mg) and placebo were evaluated in 62 men and 69 women for the treatment of… Expand
Action of naloxone on gender-dependent analgesic and antianalgesic effects of nalbuphine in humans****
TLDR
Coadministration of naloxone, which had no analgesic action administered alone, not only reversed the expected pain-enhancing effect of n albuphine in men, but produced a similar degree of long-lasting analgesia in both sexes, suggesting this drug combination might become an important new pharmacological therapy for pain relief. Expand
A subanalgesic dose of morphine eliminates nalbuphine anti-analgesia in postoperative pain.
TLDR
It is shown that morphine, given in a subanalgesic dose, reverses nalbuphine-induced anti- analgesia in males, perhaps by a similar mechanism to that of naloxone. Expand
Dose ratio is important in maximizing naloxone enhancement of nalbuphine analgesia in humans
TLDR
The hypothesis that an important determinant of nAloxone enhancement of nalbuphine analgesia is the dose ratio of n albuphines to naloxone is tested is tested, suggesting that the anti-analgesic effect of nnalbu phine is present in both sexes at the 2.5 mg dose and that this is an importanteterminant of the analgesic efficacy of this combination. Expand
Combination of low-dose nalbuphine and morphine in patient-controlled analgesia decreases incidence of opioid-related side effects.
  • Y. Yeh, T. Lin, +4 authors W. Sun
  • Medicine
  • Journal of the Formosan Medical Association = Taiwan yi zhi
  • 2009
TLDR
Combination of low-dose nalbuphine and morphine in PCA decreases the incidence of opioid-related nausea, without affecting the analgesia and PCA requirement. Expand
Neuroleptics antagonize nalbuphine antianalgesia.
TLDR
It is demonstrated that neuroleptics can block the antianalgesic effect of agonist-antagonist kappa opioids, resulting in enhanced analgesia and elimination of the sex differences. Expand
Sexual dimorphism in very low dose nalbuphine postoperative analgesia
TLDR
The present study evaluated the effect of a lower dose of nalbuphine, with and without naloxone, on dental postoperative pain and found that the anti-analgesic effect of nAlbuphines, present in both sexes at the 5 mg dose disappears at the lower dose, and the mild analgesia in women produced by this lower dose is antagonized by nAloxone. Expand
Influences of Gender on Intravenous Nalbuphine Actions After Major Abdominal Surgery: A Multicenter Study
TLDR
The hypothesis that although nalbuphine was found to be an effective and well-tolerated analgesic after major abdominal surgery, females were statistically more responsive than males is supported. Expand
Experimental Pain Models Reveal No Sex Differences in Pentazocine Analgesia in Humans
TLDR
Findings indicate significant analgesic responses to pentazocine in both men and women across multiple experimental pain assays, and the absence of sex differences contrasts with previous data from the oral surgery model, suggesting that sex differences in opioid analgesia may be specific to certain types of pain. Expand
Absence of nalbuphine anti-analgesia in the rat
TLDR
Data do not support the hypothesis that the naloxone-sensitive anti-analgesic effect of nalbuphine observed in humans is present in the rat and could explain, at least in part, the opposite direction of the sex differences for kappa agonist-antagonist opioid analgesia observed in these two species. Expand
NOP receptor mediates anti-analgesia induced by agonist–antagonist opioids
TLDR
The results strongly support the suggestion that clinically used agonist-antagonists act at the NOP receptor to produce anti-analgesia, which is not mediated by kappa-opioid receptors. Expand
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