A novel finding of nalbuphine-6-glucuronide, an active opiate metabolite, possessing potent antinociceptive effects: Synthesis and biological evaluation

Liang, Ren-Jong; Lai, Yen-Hsun; Kao, Yu-Ting; Yang, Ting-Hsuan; Chen, Yen-Lun; Wang, Hong-Jaan

doi:10.1016/j.ejmech.2019.06.028

Cited by 6 publications

(2 citation statements)

References 25 publications

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“…24 As a combined opioid agonist-antagonist, nalbuphine acts on the κ-receptor to produce analgesic and sedative effects, and it exerts μ-receptor antagonistic effects in the presence of other μ-receptor agonists. 8,25,26 Clinical observations show the analgesic efficacy of nalbuphine is similar to morphine with only a slight respiratory depression and a capping phenomenon. 27 Our results demonstrate that nalbuphine can improve generalized pain postoperatively as evidence by lower NRS scores and postoperative analgesic requirements, possibly due to its modulatory action on central κ-receptors.…”

Section: Discussionmentioning

confidence: 99%

<p>Preemptive Nalbuphine Attenuates Remifentanil-Induced Postoperative Hyperalgesia After Laparoscopic Cholecystectomy: A Prospective Randomized Double-Blind Clinical Trial</p>

Hu¹,

Chen²,

Zhu³

et al. 2020

JPR

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Background: Remifentanil-induced hyperalgesia (RIH) is a paradoxical phenomenon that may increase sensitivity to painful stimuli. Nalbuphine, which is both a μ-receptor antagonist and κ-receptor agonist, may affect RIH. The aim of this study was to evaluate the effects of nalbuphine on RIH during laparoscopic cholecystectomy. Methods: A total of 96 patients were divided into the following four groups: 0.4 μg/kg/min of remifentanil with 0.2 mg/kg of nalbuphine (HRNA), 0.4 μg/kg/min of remifentanil with saline (HRSA), 0.1 μg/kg/min of remifentanil with 0.2 mg/kg of nalbuphine (LRNA), and 0.1 μg/kg/min of remifentanil with saline (LRSA). The pain thresholds of postoperative mechanical hyperalgesia were measured with von Frey filaments. Pain intensity and analgesic consumption were recorded up to 48 h after surgery. Results: Pain thresholds on the inner forearm decreased in the HRSA group compared with the HRNA (P = 0.0167), LRNA (P = 0.0027), and LRSA (P = 0.0318) groups at 24 h after surgery. Pain thresholds on the peri-incisional area decreased in the HRSA group compared with HRNA, LRNA, and LRSA (all P < 0.0001) groups at 24 h after surgery. Patients in the HRNA group showed lower numeric rating scale scores at 1 h (P = 0.0159), 3 h (P = 0.0118), 6 h (P = 0.0213), and 12 h (P = 0.0118) than those in the HRSA group. Postoperative requirement for sufentanil was greater in the HRSA group than the HRNA group during the first 3 h (P = 0.0321) and second 3 h (P = 0.0040). Postoperative sufentanil consumption was also greater in the LRSA group than in the LRNA group during the first 3 h (P = 0.0321) and second 3 h (P = 0.0416). Conclusion: Preemptive nalbuphine can ameliorate postoperative hyperalgesia induced by high-dose remifentanil in patients undergoing laparoscopic cholecystectomy.

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Section: Discussionmentioning

confidence: 99%

<p>Preemptive Nalbuphine Attenuates Remifentanil-Induced Postoperative Hyperalgesia After Laparoscopic Cholecystectomy: A Prospective Randomized Double-Blind Clinical Trial</p>

Hu¹,

Chen²,

Zhu³

et al. 2020

JPR

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“…20 Recently, in 2019, nalbuphine-6-glucuronide, a metabolite of nalbuphine, was found to exhibit a stronger analgesic response than that of nalbuphine in both Randall-Selitto and cold ethanol tests in rats. 153…”

Section: Iii6 Nalbuphinementioning

confidence: 99%