Oxycodone/naloxone explained

Oxycodone/naloxone, sold under the brand name Targin among others, is a combination pain medication. It is available as modified-release tablets and is taken by mouth.

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, namely constipation as the naloxone binds to the opioid receptors in the gut, preventing the opioid from attaching. This does not affect its analgesic efficacy compared to Oxycontin. Constipation was significantly relieved in a 2008 study.^[1] The drug was released in 2006 in Germany and is available in some other European countries since 2009. In the UK, the 10 mg oxycodone / 5 mg naloxone and 20 mg/10 mg strengths were approved in December 2008, and the 40 mg/20 mg and 5 mg/10 mg strengths in July 2019.^[2]

Preliminary evidence suggests that oxycodone/naloxone may be an effective treatment for severe, refractory restless legs syndrome if first-line therapies have not been effective.^{[3] [4] [5]}

Notes and References

1. Simpson K, Leyendecker P, Hopp M, Müller-Lissner S, Löwenstein O, De Andrés J, Troy Ferrarons J, Bosse B, Krain B, Nichols T, Kremers W, Reimer K . 6 . Fixed-ratio combination oxycodone/naloxone compared with oxycodone alone for the relief of opioid-induced constipation in moderate-to-severe noncancer pain . Current Medical Research and Opinion . 24 . 12 . 3503–3512 . December 2008 . 19032132 . 10.1185/03007990802584454 . 73061000 . 2009-04-09 . dead . https://archive.today/20130126165345/http://www.informapharmascience.com/doi/abs/10.1185/03007990802584454 . 2013-01-26 .
2. Web site: Mundipharma. Targin (oral oxycodone/naloxone prolonged-release tablet) now launching across Europe to control severe chronic pain with significantly reduced risk of opioid-induced constipation. 2009-01-26. 2009-04-09. 2009-03-17. https://web.archive.org/web/20090317092117/http://www.prnewswire.com/mnr/targin/36704/. live.
3. de Biase S, Valente M, Gigli GL . Intractable restless legs syndrome: role of prolonged-release oxycodone-naloxone . Neuropsychiatric Disease and Treatment . 12 . 417–425 . 2016 . 26966363 . 4770072 . 10.2147/NDT.S81186 . free .
4. Trenkwalder C, Beneš H, Grote L, García-Borreguero D, Högl B, Hopp M, Bosse B, Oksche A, Reimer K, Winkelmann J, Allen RP, Kohnen R . 6 . Prolonged release oxycodone-naloxone for treatment of severe restless legs syndrome after failure of previous treatment: a double-blind, randomised, placebo-controlled trial with an open-label extension . English . The Lancet. Neurology . 12 . 12 . 1141–1150 . December 2013 . 24140442 . 10.1016/S1474-4422(13)70239-4 . 35122538 .
5. de Oliveira CO, Carvalho LB, Carlos K, Conti C, de Oliveira MM, Prado LB, Prado GF . Opioids for restless legs syndrome . The Cochrane Database of Systematic Reviews . 2016 . 6 . CD006941 . June 2016 . 27355187 . 6885031 . 10.1002/14651858.CD006941.pub2 .