Dose ratio is important in maximizing naloxone enhancement of nalbuphine analgesia in humans
Section snippets
Acknowledgements
We thank Gretchen Summer, R.N., for excellent technical assistance. This work was supported by NIH grant NR03923 and the Kaiser Community Services Program.
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Cited by (22)
Sex differences in the response to opioids for pain relief: A systematic review and meta-analysis
2019, Pharmacological ResearchNOP receptor mediates anti-analgesia induced by agonist-antagonist opioids
2014, NeuroscienceCitation Excerpt :Furthermore, nalbuphine co-administered with naloxone at the same fixed dose ratio that was maximally effective in patients (12.5:1) blocked anti-analgesia without affecting analgesia, whereas a slightly higher dose of naloxone (dose ratio: 12.5:2) also reversed analgesia, again closely replicating our findings in patients with postoperative pain (Gear et al., 2000). To explain our clinical findings, we proposed that the receptor at which an agonist–antagonist acts to produce analgesia (Gutstein and Akil, 2001) is different from the receptor at which it acts to produce anti-analgesia (Gear et al., 2000; Gear et al., 2003; Kshirsagar et al., 2008). This suggestion is supported by our current observation that the selective κ-receptor agonist U69593 only induces analgesia, and confirmed by the failure of the selective kappa antagonist nor-BNI to block nalbuphine-induced anti-analgesia.
Sex differences in kappa opioid pharmacology
2011, Life SciencesCitation Excerpt :In women, morphine had no effect on nalbuphine-induced analgesia (Gear et al., 2008). Gear et al. (2003a) found a low dose of the opioid antagonist naloxone (0.2 mg), blocked the anti-analgesic effects of nalbuphine (2.5 mg) in men. In a separate study naloxone at 0.4 mg had no effect by itself in either sex but in women naloxone (0.4 mg) co-administered with 5 mg of nalbuphine enhanced the analgesic effect, while in men this co-administration paradigm blocked the anti-analgesic of nalbuphine (Gear et al., 2000).
A Subanalgesic Dose of Morphine Eliminates Nalbuphine Anti-Analgesia in Postoperative Pain
2008, Journal of PainCitation Excerpt :An alternative explanation—one that is more consistent with the current findings—is that nalbuphine analgesia is unmasked by morphine blockade of the action of nalbuphine at an anti-analgesia receptor. Previously, we showed that the opioid receptor antagonist naloxone enhances nalbuphine analgesia in both sexes (males > females),11 a finding that formed the basis of a 2-receptor hypothesis for the effect of nalbuphine on postoperative pain.5,7,8,11 According to this hypothesis, nalbuphine induces anti-analgesia as well as analgesia by acting at distinct “anti-analgesia” and “analgesia” opioid receptors.
Neuroleptics antagonize nalbuphine antianalgesia
2006, Journal of Pain
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