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Anaes VivasAnaesthetic adjuncts

Anaes Vivas · Anaesthetic adjuncts

Data viva — opioid receptors, biased agonism and opioid-induced hyperalgesia

A data viva on the opioid-receptor pharmacology. The mu (beta-endorphin; supraspinal and spinal analgesia; euphoria; marked respiratory depression; morphine, fentanyl). The kappa (dynorphin; spinal analgesia; dysphoria and psychotomimetic; less respiratory depression; pentazocine, nalbuphine). The delta (enkephalin; analgesia; convulsant at high dose; experimental). The Gi/Go signalling (inhibit adenylate cyclase, close Ca, open K). The biased agonism (G-protein versus beta-arrestin; oliceridine versus sufentanil on PONV). The tolerance (rightward shift) versus OIH (lowered pain threshold; NMDA, glia, descending facilitation, dynorphin). The OIH management (ketamine, opioid rotation, alpha-2 agonists).

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Prompt
A table comparing the mu, kappa and delta opioid receptors (endogenous ligand, analgesic site, mood effect, respiratory depression, clinical agonists) and a graph showing the dose-response shift of tolerance versus the pain-threshold lowering of opioid-induced hyperalgesia. Interpret and explain.

Stimulus

A table compares the three classical opioid receptors across endogenous ligand, analgesic site, mood effect and respiratory depression, and a second graph shows two dose-response curves: tolerance drawn as a rightward shift, and opioid-induced hyperalgesia drawn as a downward shift of the pain threshold. Interpret the table and the graph and explain the clinical implications.

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References6ShowHide
  1. [1]Wang H, et al. Molecular mechanism of allosteric modulation of opioid receptors. Signal Transduct Target Ther, 2026.PMID 42362532
  2. [2]Kurowska K, et al. Kinetic profiling of opioid receptor ligands. J Cheminform, 2026.PMID 42363184
  3. [7]Lee M, et al. A comprehensive review of opioid-induced hyperalgesia. Pain Physician, 2011.PMID 21412369
  4. [8]Zollner C, et al. Opioids. Handb Exp Pharmacol, 2007.PMID 17087119
  5. [5]Liu F, et al. Impact of oliceridine versus sufentanil on postoperative nausea and vomiting in patients undergoing thyroid surgery: a prospective, double-blind, randomized controlled trial. Ann Med, 2026.PMID 42339818
  6. [6]Voronkov M, et al. Does Kappa Agonism Improve Reversal of Opioid Overdose? Pharmaceuticals (Basel), 2026.PMID 42356464
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