Noroxycodone Explained

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. 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.^{[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] [7]}

See also

• Norbuprenorphine
• Norbuprenorphine-3-glucuronide
• Norhydrocodone
• Normorphine
• Noroxymorphone

Notes and References

1. Book: Smith HS, Vanderah TW, McClean G . Opioids for Pain . Smith H, Passik S . Pain and Chemical Dependency. https://books.google.com/books?id=T88C-9VTDXMC&pg=PA195. 25 April 2008. Oxford University Press, USA. 978-0-19-530055-0. 195–.
2. Book: Pincus MR, Bluth MH, Abraham Jr NZ . Toxicology and Therapeutic Drug Monitoring . McPherson RA, Pincus MR . Henry's Clinical Diagnosis and Management by Laboratory Methods . https://books.google.com/books?id=xAzhCwAAQBAJ&pg=PA336. 31 March 2016. Elsevier Health Sciences. 978-0-323-41315-2. 336–.
3. Book: Somogyi AA, Coller JK . Drugs against Acute and Chronic Pain . Anzenbacher P, Zanger UM . Metabolism of Drugs and Other Xenobiotics. https://books.google.com/books?id=ulcB7zYIresC&pg=PA420. 29 May 2012. John Wiley & Sons. 978-3-527-32903-8. 420–.
4. Lemberg KK, Siiskonen AO, Kontinen VK, Yli-Kauhaluoma JT, Kalso EA . Pharmacological characterization of noroxymorphone as a new opioid for spinal analgesia . Anesthesia and Analgesia . 106 . 2 . 463–70, table of contents . February 2008 . 18227301 . 10.1213/ane.0b013e3181605a15 . 16524280 . free .
5. Book: Kokki H, Kokki M . Central Nervous System Penetration of the Opioid Oxycodone . Preedy VR . 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. https://books.google.com/books?id=Yu9eBwAAQBAJ&pg=PA462. 25 April 2016. Elsevier Science. 978-0-12-800677-1. 462–464.
6. Lalovic B, Kharasch E, Hoffer C, Risler L, Liu-Chen LY, Shen DD . 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 . 16678548 . 10.1016/j.clpt.2006.01.009 . 21372271 .
7. Klimas R, Witticke D, El Fallah S, Mikus G . 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 . 23488585 . 10.1517/17425255.2013.779669 . 22857902 .