Category:Opioid analgesics: Difference between revisions
Category page
More actions
Create canonical category-page article (history-first) |
Rewrite per canonical category-page spec (history-first article) |
||
| Line 11: | Line 11: | ||
The pharmacology of the contemporary opioid is, in clinical use, dominated by the relation between analgesia and respiratory depression. The two effects are produced by activation of the same receptor and have not been successfully separated in any medicine of full agonist class, although the partial agonist [[Buprenorphine|buprenorphine]] approaches that separation at the expense of a ceiling on its analgesic effect. The atypical opioid [[Tramadol|tramadol]], introduced by Grünenthal in 1977, is a weak mu agonist combined with a serotonin- and noradrenaline-reuptake inhibitor, and its descendant [[Tapentadol|tapentadol]] (2008) retains the dual mechanism without the serotonergic component; both have a lower respiratory-depression profile than the corresponding-potency mu agonists and a different but real adverse-effect profile that includes serotonin syndrome (tramadol) and seizure (both). The mixed agonist-antagonists ([[Pentazocine|pentazocine]], nalbuphine, butorphanol) are now of limited use because their kappa-receptor activity produces dysphoria. | The pharmacology of the contemporary opioid is, in clinical use, dominated by the relation between analgesia and respiratory depression. The two effects are produced by activation of the same receptor and have not been successfully separated in any medicine of full agonist class, although the partial agonist [[Buprenorphine|buprenorphine]] approaches that separation at the expense of a ceiling on its analgesic effect. The atypical opioid [[Tramadol|tramadol]], introduced by Grünenthal in 1977, is a weak mu agonist combined with a serotonin- and noradrenaline-reuptake inhibitor, and its descendant [[Tapentadol|tapentadol]] (2008) retains the dual mechanism without the serotonergic component; both have a lower respiratory-depression profile than the corresponding-potency mu agonists and a different but real adverse-effect profile that includes serotonin syndrome (tramadol) and seizure (both). The mixed agonist-antagonists ([[Pentazocine|pentazocine]], nalbuphine, butorphanol) are now of limited use because their kappa-receptor activity produces dysphoria. | ||
The opioid analgesics are, in the present clinical context, among the most consequential medicines to prescribe. The United States overdose mortality from opioid medicines, beginning with the 1996 introduction and aggressive marketing of controlled-release [[Oxycodone|oxycodone]] under the trade name OxyContin and amplified after 2013 by illicit fentanyl analogues, has been documented as one of the few sustained declines in U.S. life expectancy of the post-war period.<ref name="cdc2024">Centers for Disease Control and Prevention. Drug overdose deaths in the United States, 1999-2023. ''NCHS Data Brief''. 2024;(522):1-8.</ref> The contemporary prescriber works in a framework that has changed in the last decade: a presumption against chronic opioid use for non-cancer pain except where carefully considered, careful documentation of indication and duration, naloxone co-prescription, and an explicit clinical pathway to | The opioid analgesics are, in the present clinical context, among the most consequential medicines to prescribe. The United States overdose mortality from opioid medicines, beginning with the 1996 introduction and aggressive marketing of controlled-release [[Oxycodone|oxycodone]] under the trade name OxyContin and amplified after 2013 by illicit fentanyl analogues, has been documented as one of the few sustained declines in U.S. life expectancy of the post-war period.<ref name="cdc2024">Centers for Disease Control and Prevention. Drug overdose deaths in the United States, 1999-2023. ''NCHS Data Brief''. 2024;(522):1-8.</ref> The contemporary prescriber works in a framework that has changed in the last decade: a presumption against chronic opioid use for non-cancer pain except where carefully considered, careful documentation of indication and duration, naloxone co-prescription, and an explicit clinical pathway to medicine-assisted treatment for opioid use disorder (buprenorphine, [[Methadone|methadone]], or extended-release naltrexone) when use becomes problematic. | ||
== Classes indexed == | == Classes indexed == | ||