|Naloxone||Opioid receptor antagonist|
|AHFS/Drugs.com||International Drug Names
UK Drug Information
The oxycodone component is an opioid and is responsible for the pain-relieving effects. Naloxone opposes the effects of opioids but is poorly absorbed into the body when given orally, meaning almost all the dose stays within the gastrointestinal tract and reduces the local side effects from the oxycodone. Constipation was significantly relieved in a 2008 study. The drug was released in 2006 in Germany and is available in some other European countries since 2009.
If the drug is used off license by crushing the tablet and dissolving it for injection, it may precipitate severe opiate withdrawal symptoms due to the much higher bioavailability of intravenous naloxone compared to oral naloxone. In simpler terms, since naloxone is an opioid antagonist, it will bind to the opioid receptors in the brain and block the analgesic effect of the oxycodone.
- Simpson K, et al. (December 2008). "Fixed-ratio combination oxycodone/naloxone compared with oxycodone alone for the relief of opioid-induced constipation in moderate-to-severe noncancer pain". Curr Med Res Opin. 24 (12): 3503–3512. doi:10.1185/03007990802584454. PMID 19032132. Retrieved 2009-04-09.
- Mundipharma (2009-01-26). "Targin (oral oxycodone/naloxone prolonged-release tablet) now launching across Europe to control severe chronic pain with significantly reduced risk of opioid-induced constipation". Retrieved 2009-04-09.
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