Chemistry:Noroxycodone
From HandWiki
Short description: Chemical compound
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| Dependence liability | High (same oxycodone) |
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| Formula | C17H19NO4 |
| Molar mass | 301.342 g·mol−1 |
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Noroxycodone is the major metabolite of the opioid analgesic oxycodone.[1][2][3] It is formed from oxycodone in the liver via N-demethylation predominantly by CYP3A4.[1][2][3] Noroxycodone binds to and activates the μ-opioid receptor (MOR) similarly to oxycodone, although with one-third of the affinity of oxycodone and 5- to 10-fold lower activational potency.[1][4][5] However, although a potent MOR agonist, noroxycodone poorly crosses the blood-brain-barrier into the central nervous system, and for this reason, is only minimally analgesic in comparison.[6][5][4][7]
See also
References
- ↑ 1.0 1.1 1.2 "Opioids for Pain". Pain and Chemical Dependency. Oxford University Press, USA. 25 April 2008. pp. 195–. ISBN 978-0-19-530055-0. https://books.google.com/books?id=T88C-9VTDXMC&pg=PA195.
- ↑ 2.0 2.1 "Toxicology and Therapeutic Drug Monitoring". Henry's Clinical Diagnosis and Management by Laboratory Methods. Elsevier Health Sciences. 31 March 2016. pp. 336–. ISBN 978-0-323-41315-2. https://books.google.com/books?id=xAzhCwAAQBAJ&pg=PA336.
- ↑ 3.0 3.1 "Drugs against Acute and Chronic Pain". Metabolism of Drugs and Other Xenobiotics. John Wiley & Sons. 29 May 2012. pp. 420–. ISBN 978-3-527-32903-8. https://books.google.com/books?id=ulcB7zYIresC&pg=PA420.
- ↑ 4.0 4.1 "Pharmacological characterization of noroxymorphone as a new opioid for spinal analgesia". Anesthesia and Analgesia 106 (2): 463–70, table of contents. February 2008. doi:10.1213/ane.0b013e3181605a15. PMID 18227301.
- ↑ 5.0 5.1 "Central Nervous System Penetration of the Opioid Oxycodone". Neuropathology of Drug Addictions and Substance Misuse Volume 3: General Processes and Mechanisms, Prescription Medications, Caffeine and Areca, Polydrug Misuse, Emerging Addictions and Non-Drug Addictions. Elsevier Science. 25 April 2016. pp. 462–464. ISBN 978-0-12-800677-1. https://books.google.com/books?id=Yu9eBwAAQBAJ&pg=PA462.
- ↑ "Pharmacokinetics and pharmacodynamics of oral oxycodone in healthy human subjects: role of circulating active metabolites". Clinical Pharmacology and Therapeutics 79 (5): 461–479. May 2006. doi:10.1016/j.clpt.2006.01.009. PMID 16678548.
- ↑ "Contribution of oxycodone and its metabolites to the overall analgesic effect after oxycodone administration". Expert Opinion on Drug Metabolism & Toxicology 9 (5): 517–528. May 2013. doi:10.1517/17425255.2013.779669. PMID 23488585.
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