|Naloxone||Opioid receptor antagonist|
|Trade names||Targin, Targiniq, Targinact, others|
|AHFS/Drugs.com||International Drug Names|
UK Drug Information
Oxycodone/naloxone, sold under the brand names Targin and Targinact 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. 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.
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.
If the drug is used off-label 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, the normal injection dose of naloxone is far smaller than the oral dose due to more of an intravenous dose being absorbed and active in the body.
- ^ http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=355284&agid=%28PrintDetailsPublic%29&actionid=1
- ^ https://www.tga.gov.au/resources/prescription-medicines-registrations/oxonal-au-pharma-pty-ltd
- ^ "Targiniq ER- oxycodone hydrochloride/naloxone hydrochloride tablet, film coated, extended release". DailyMed. 22 December 2016. Retrieved 18 March 2023.
- ^ Simpson K, Leyendecker P, Hopp M, Müller-Lissner S, Löwenstein O, De Andrés J, 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". Current Medical Research and Opinion. 24 (12): 3503–3512. doi:10.1185/03007990802584454. PMID 19032132. S2CID 73061000. Archived from the original on 2013-01-26. 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.
- ^ de Biase S, Valente M, Gigli GL (2016). "Intractable restless legs syndrome: role of prolonged-release oxycodone-naloxone". Neuropsychiatric Disease and Treatment. 12: 417–425. doi:10.2147/NDT.S81186. PMC 4770072. PMID 26966363.
- ^ Trenkwalder C, Beneš H, Grote L, García-Borreguero D, Högl B, Hopp M, et al. (December 2013). "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". The Lancet. Neurology. 12 (12): 1141–1150. doi:10.1016/S1474-4422(13)70239-4. PMID 24140442. S2CID 35122538.
- ^ de Oliveira CO, Carvalho LB, Carlos K, Conti C, de Oliveira MM, Prado LB, Prado GF (June 2016). "Opioids for restless legs syndrome". The Cochrane Database of Systematic Reviews. 2016 (6): CD006941. doi:10.1002/14651858.CD006941.pub2. PMC 6885031. PMID 27355187.
- "Naloxone mixture with oxycodone". Drug Information Portal. U.S. National Library of Medicine.