oxycodone/naloxone
{{Short description|Combination pain relief drug}}
{{Use dmy dates|date=July 2024}}
{{cs1 config |name-list-style=vanc |display-authors=6}}
{{Drugbox
| verifiedrevid = 412310397
| image = Oxycodone.svg
| image_class = skin-invert-image
| image2 = Naloxone.svg
| image_class2 = skin-invert-image
| type = combo
| component1 = Oxycodone
| component2 = Naloxone
| class2 = Opioid receptor antagonist
| tradename = Targin, Targiniq, Targinact, others
| Drugs.com = {{drugs.com|international|targin}}
{{drugs.com|UK|targinact-5-mg-2-5-mg-10-mg-5-mg-20-mg-10-mg-and-40-mg-20-mg-prolonged-release-tablets-1301}}
| DailyMedID = Oxycodone hydrochloride/naloxone hydrochloride
| pregnancy_AU = C
| pregnancy_category =
| routes_of_administration = By mouth
| ATC_prefix = N02
| ATC_suffix = AA55
| legal_AU = S8
| legal_AU_comment = {{Cite web | url=http://www.ebs.tga.gov.au/servlet/xmlmillr6?dbid=ebs/PublicHTML/pdfStore.nsf&docid=355284&agid=%28PrintDetailsPublic%29&actionid=1 | title=Public Summary | publisher=Australian Government, Department of Health and Aged Care | access-date=2024-05-20 | website=www.ebs.tga.gov.au}}{{cite web | title=Oxonal (AU Pharma Pty Ltd) | website=Therapeutic Goods Administration (TGA) | date=28 September 2022 | url=https://www.tga.gov.au/resources/prescription-medicines-registrations/oxonal-au-pharma-pty-ltd | access-date=9 April 2023 | archive-date=18 March 2023 | archive-url=https://web.archive.org/web/20230318070824/https://www.tga.gov.au/resources/prescription-medicines-registrations/oxonal-au-pharma-pty-ltd | url-status=live }}
| legal_CA = Schedule I
| legal_UK = POM
| legal_US = Schedule II
| legal_status = Rx-only
| CAS_number = 92522-88-8
| PubChem =
| DrugBank_Ref =
| DrugBank =
}}
Oxycodone/naloxone, sold under the brand name Targin among others, is a combination pain medication available as modified-release tablets administered by mouth.
The oxycodone component is an opioid and is responsible for the pain-relieving effects. Naloxone, an opioid antagonist, opposes the effects of opioids but is poorly absorbed into the blood stream when administered orally; therefore, most of the dose remains in the gastrointestinal tract. This local presence reduces opioid-induced constipation by preventing oxycodone from binding to gut opioid receptors, without diminishing overall analgesic efficacy compared to oxycodone alone. A 2008 study demonstrated a significant reduction in constipation.{{cite journal | vauthors = 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 | display-authors = 6 | title = Fixed-ratio combination oxycodone/naloxone compared with oxycodone alone for the relief of opioid-induced constipation in moderate-to-severe noncancer pain | journal = Current Medical Research and Opinion | volume = 24 | issue = 12 | pages = 3503–3512 | date = December 2008 | pmid = 19032132 | doi = 10.1185/03007990802584454 | s2cid = 73061000 | url = http://www.informapharmascience.com/doi/abs/10.1185/03007990802584454 | access-date = 2009-04-09 | url-status = dead | archive-url = https://archive.today/20130126165345/http://www.informapharmascience.com/doi/abs/10.1185/03007990802584454 | archive-date = 2013-01-26 | url-access = subscription }} Oxycodone/naloxone was released in 2014 in the United States, in 2006 in Germany, and has been available in some other European countries since 2009. In the United Kingdom, 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 received approval in July 2019.{{cite web|author=Mundipharma|title=Targin (oral oxycodone/naloxone prolonged-release tablet) now launching across Europe to control severe chronic pain with significantly reduced risk of opioid-induced constipation|date=2009-01-26|url=http://www.prnewswire.com/mnr/targin/36704/|access-date=2009-04-09|archive-date=2009-03-17|archive-url=https://web.archive.org/web/20090317092117/http://www.prnewswire.com/mnr/targin/36704/|url-status=live}}
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.{{cite journal | vauthors = de Biase S, Valente M, Gigli GL | title = Intractable restless legs syndrome: role of prolonged-release oxycodone-naloxone | journal = Neuropsychiatric Disease and Treatment | volume = 12 | pages = 417–425 | date = 2016 | pmid = 26966363 | pmc = 4770072 | doi = 10.2147/NDT.S81186 | doi-access = free }}{{cite journal | vauthors = 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 | display-authors = 6 | title = 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 | language = English | journal = The Lancet. Neurology | volume = 12 | issue = 12 | pages = 1141–1150 | date = December 2013 | pmid = 24140442 | doi = 10.1016/S1474-4422(13)70239-4 | s2cid = 35122538 }}{{cite journal | vauthors = de Oliveira CO, Carvalho LB, Carlos K, Conti C, de Oliveira MM, Prado LB, Prado GF | title = Opioids for restless legs syndrome | journal = The Cochrane Database of Systematic Reviews | volume = 2016 | issue = 6 | pages = CD006941 | date = June 2016 | pmid = 27355187 | pmc = 6885031 | doi = 10.1002/14651858.CD006941.pub2 }}
Adverse effects
{{Further|Oxycodone#Adverse effects}}
References
{{Reflist}}
{{Laxatives}}
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{{Opioidergics}}
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