Buprenorphine/naloxone

Not to be confused with Bupropion/naltrexone.

Buprenorphine/naloxone
Buprenorphine, an opioid
Naloxone, an opioid antagonist
Combination of
BuprenorphineOpioid modulator
NaloxoneOpioid antagonist
Clinical data
Trade namesSuboxone, Bunavail, Zubsolv, others[1]
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: C
Routes of
administration		Sublingual, buccal
ATC code
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
KEGG
CompTox Dashboard (EPA)

Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a fixed-dose combination medication that includes buprenorphine and naloxone.[3] It is used to treat opioid use disorder, and reduces the mortality of opioid use disorder by 50% (by reducing the risk of overdose on full-agonist opioids such as heroin or fentanyl).[3][5][6] It relieves cravings to use and withdrawal symptoms.[7] Buprenorphine/­naloxone is available for use in two different forms, under the tongue or in the cheek.[1]

Side effects may include respiratory depression (decreased breathing), small pupils, sleepiness, and low blood pressure.[3] The risk of overdose with buprenorphine/­naloxone (unless combined with other sedating substances) is exceedingly low, and lower than with methadone,[7] but people are more likely to stop treatment on buprenorphine/­naloxone than methadone.[7] Buprenorphine (like methadone) is a treatment option during pregnancy.

At lower doses, buprenorphine results in the usual opioid effects; high doses beyond a certain level do not result in greater effects.[8] This is believed to result in a lower risk of overdose than some other opioids.[8] Naloxone is an opioid antagonist that competes with and blocks the effect of other opioids (including buprenorphine) if given by injection.[3] Naloxone is poorly absorbed when taken by mouth and is added to decrease the risk that people will misuse the medication by injection.[1] Misuse by injection or use in the nose still occurs, and more recently the efficacy of naloxone in preventing misuse by injection has been brought into question and preparations including naloxone could even be less safe than preparations containing solely buprenorphine.[3][9] Rates of misuse in the U.S. appear to be lower than with other opioids.[10]

The combination formulation was approved for medical use in the U.S. in 2002,[3][10][11] and in the European Union in 2017.[4] A generic version was approved in the U.S. in 2018.[12] In 2019, it was the 272nd most commonly prescribed medication in the U.S., with more than 1 million prescriptions.[13]

  1. ^ a b c "Buprenorphine". www.samhsa.gov. 31 May 2016. Retrieved 3 December 2017.
  2. ^ "Health product highlights 2021: Annexes of products approved in 2021". Health Canada. 3 August 2022. Retrieved 25 March 2024.
  3. ^ a b c d e f g Cite error: The named reference Suboxone FDA label was invoked but never defined (see the help page).
  4. ^ a b "Zubsolv EPAR". European Medicines Agency (EMA). 17 September 2018. Retrieved 29 September 2020.
  5. ^ Fisher GL, Roget NA (11 November 2008). Encyclopedia of Substance Abuse Prevention, Treatment, and Recovery. SAGE Publications. pp. 570–. ISBN 978-1-4129-5084-8.
  6. ^ Sordo L, Barrio G, Bravo MJ, Indave BI, Degenhardt L, Wiessing L, et al. (April 2017). "Mortality risk during and after opioid substitution treatment: systematic review and meta-analysis of cohort studies". BMJ. 357: j1550. doi:10.1136/bmj.j1550. PMC 5421454. PMID 28446428.
  7. ^ a b c Srivastava A, Kahan M, Nader M (March 2017). "Primary care management of opioid use disorders: Abstinence, methadone, or buprenorphine-naloxone?". Canadian Family. 63 (3): 200–205. PMC 5349718. PMID 28292795.
  8. ^ a b "Buprenorphine for Chronic Pain: A Review of the Clinical Effectiveness". Canadian Agency for Drugs and Technologies in Health. 6 January 2017. PMID 28727399.
  9. ^ Blazes CK, Morrow JD (11 September 2020). "Reconsidering the Usefulness of Adding Naloxone to Buprenorphine". Frontiers in Psychiatry. 11: 549272. doi:10.3389/fpsyt.2020.549272. PMC 7517938. PMID 33061915.
  10. ^ a b Yokell MA, Zaller ND, Green TC, Rich JD (March 2011). "Buprenorphine and buprenorphine/naloxone diversion, misuse, and illicit use: an international review". Current Drug Abuse Reviews. 4 (1): 28–41. doi:10.2174/1874473711104010028. PMC 3154701. PMID 21466501.
  11. ^ "Drug Approval Package: Subutex (Buprenorphine HCI) Suboxone (Buprenorphine HCI & Naloxone HCI Dihydrate) NDA #020732 & 020733". U.S. Food and Drug Administration (FDA). Retrieved 29 September 2020.
  12. ^ "FDA approves first generic versions of Suboxone sublingual film, which may increase access to treatment for opioid dependence". U.S. Food and Drug Administration (FDA) (Press release). Retrieved 23 June 2018.
  13. ^ "Buprenorphine; Naloxone – Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.