PSC 433 Chapter Notes - Chapter 14: Μ-Opioid Receptor, Opioid Overdose, Pethidine
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Opioid analgesics and antagonists: strong agonists: alfentanil, fentanyl, heroin, meperidine, methadone, morphine, remifentanil, Sufentanil: moderate/low agonists: codeine, oxycodone, propoxyphene, mixed agonist-antagonists and partial agonists: buprenorphine, butorphanol, nalbuphine, Opioid receptors: opioids interact stereospecifically with protein receptors on the membranes of certain cells in the. Cns, on nerve terminal in the periphery, and on cells of the gi tract and other anatomic regions: the major effects of the opioids are mediated by three major receptor families: (mu), (kappa), Effects of opioids: stimulate opioid receptors in cns and gi tract ( constipation, analgesia, antitussive action, euphoria, respiratory depression, pupillary constriction: pin point pupils, constipation, histamine release, tolerance and cross tolerance (exceptions!! Miosis and constipation: withdrawal: acute and protracted, se: constipation, sedation, confusion, nausea/vomiting, respiratory depression. Patients treated with morphine are still aware of the presence of pain, but the sensation is not unpleasant.