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Oxymorphazone
Oxymorphazone is an opioid analgesic drug related to oxymorphone. Oxymorphazone is a potent and long acting μ-opioid agonist which binds irreversibly to the receptor, forming a covalent bond which prevents it from detaching once bound.〔Galetta S, Ling GS, Wolfin L, Pasternak GW. Receptor binding and analgesic properties of oxymorphazone. ''Life Sciences''. 1982 Sep 20-27;31(12-13):1389-92. PMID 6183551〕〔Hahn EF, Carroll-Buatti M, Pasternak GW. Irreversible opiate agonists and antagonists: the 14-hydroxydihydromorphinone azines. ''Journal of Neuroscience''. 1982 May;2(5):572-6. PMID 6176696〕 This gives it an unusual pharmacological profile, and while oxymorphazone is only around half the potency of oxymorphone, with higher doses the analgesic effect becomes extremely long lasting, with a duration of up to 48 hours.〔France CP, Jacobson AE, Woods JH. Discriminative stimulus effects of reversible and irreversible opiate agonists: morphine, oxymorphazone and buprenorphine. ''Journal of Pharmacology and Experimental Therapeutics''. 1984 Sep;230(3):652-7. PMID 6206224〕 However, tolerance to analgesia develops rapidly with repeated doses,〔Ling GS, Galetta S, Pasternak GW. Oxymorphazone: a long-acting opiate analgesic. ''Cellular and Molecular Neurobiology''. 1984 Mar;4(1):1-13. PMID 6204757〕〔Williams CL, Bodnar RJ, Clark JE, Hahn EF, Burks TF, Pasternak GW. Irreversible opiate agonists and antagonists. IV. Analgesic actions of 14-hydroxydihydromorphinone hydrazones. ''Journal of Pharmacology and Experimental Therapeutics''. 1988 Apr;245(1):8-12. PMID 2452249〕〔Benyhe S, Hoffmann G, Varga E, Hosztafi S, Toth G, Borsodi A, Wollemann M. Effects of oxymorphazone in frogs: long lasting antinociception in vivo, and apparently irreversible binding in vitro. ''Life Sciences''. 1989;44(24):1847-57. PMID 2472540〕 as chronically activated opioid receptors are rapidly internalised by β-arrestins, similar to the results of non-covalent binding by repeated doses of agonists with extremely high binding affinity such as lofentanil.〔Marie N, Aguila B, Allouche S. Tracking the opioid receptors on the way of desensitization. ''Cellular Signalling''. 2006 Nov;18(11):1815-33. PMID 16750901〕〔DuPen A, Shen D, Ersek M. Mechanisms of opioid-induced tolerance and hyperalgesia. ''Pain Management Nursing''. 2007 Sep;8(3):113-21. PMID 17723928〕
==See also==
* Chlornaltrexamine, an irreversible mixed μ-opioid agonist-antagonist
* Chloroxymorphamine, another irreversible μ-opioid full agonist
* Naloxazone, an irreversible μ-opioid antagonist
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