Oxycodone/naloxone

Oxycodone/naloxone, sold under the brand name Targin among others, is a combination pain medication available as modified-release tablets administered by mouth.^[5]

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.^[6] Oxycodone/naloxone was released in 2014 in the United States,^[5] 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.^[7]

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.^[8][9][10]

Adverse effects

References

1. ^ "Public Summary". www.ebs.tga.gov.au. Australian Government, Department of Health and Aged Care. Retrieved 2024-05-20.
2. ^ "Oxonal (AU Pharma Pty Ltd)". Therapeutic Goods Administration (TGA). 28 September 2022. Archived 18 March 2023 at the Wayback Machine. Retrieved 9 April 2023.
3. ^ "Targin Product information". Health Canada. 22 October 2009. Archived 29 April 2023 at the Wayback Machine. Retrieved 9 April 2023.
4. ^ "Targinact 5 mg/2.5 mg prolonged-release tablets - Summary of Product Characteristics (SmPC)". (emc). 16 March 2021. Archived 10 April 2023 at the Wayback Machine. Retrieved 9 April 2023.
5. ^ "Targiniq ER- oxycodone hydrochloride/naloxone hydrochloride tablet, film coated, extended release". DailyMed. 22 December 2016. Archived 18 March 2023 at the Wayback Machine. Retrieved 18 March 2023.
6. ^ 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 (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 2013-01-26 at the Wayback Machine. Retrieved 2009-04-09.
7. ^ 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". Archived 2009-03-17 at the Wayback Machine. Retrieved 2009-04-09.
8. ^ 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
9. ^ 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 (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
10. ^ 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). doi:10.1002/14651858.CD006941.pub2. PMC 6885031. PMID 27355187