Buprenorphine

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In pharmacology, buprenorphine is "a derivative of the opioid alkaloid thebaine that is a more potent and longer lasting analgesic than morphine. It appears to act as a partial agonist at mu and kappa opioid receptors and as an antagonist at delta receptors. The lack of delta-agonist activity has been suggested to account for the observation that buprenorphine tolerance may not develop with chronic use."[1]

History

In the United States, an injectable version was approved with a New Drug Application (NDA) by the FDA in 1981.[2] An oral/sublingual version (Subutex) was approved with a New Drug Application (NDA) by the FDA in 2002.[3] An oral/sublingual version combined with naloxone (Suboxone) was approved with a New Drug Application (NDA) by the FDA in 2002.[4]

An injectable generic version was approved with a Abbreviated New Drug Application (ANDA) in 1996.[5]

Pharmacology

Metabolism

Buprenorphine is metabolized by cytochrome P-450, specifically the .[6]

Uses

Opiate withdrawal

Buprenorphine is more effective than clonidine or lofexidine and possibly more effective than methadone for treating opiate withdrawal according to a meta-analysis by the Cochrane Collaboration.[7]

Opiate dependence

Buprenorphine is less effective than methadone for treating opiate dependence according to a meta-analysis by the Cochrane Collaboration.[8] Although buprenorphine–naloxone may be less effective than methadone[9], it has more predictable dosing[10], and can be prescribed by qualifying office-based physicians.[11]

Veterinary medicine

Burprenorphine does not cause the hyperexcitation in cats that classically has been associated with pure agonists, and provides analgesia.

External links

The most up-to-date information about Buprenorphine and other drugs can be found at the following sites.


References

  1. Anonymous (2015), Buprenorphine (English). Medical Subject Headings. U.S. National Library of Medicine.
  2. Drugs@FDA. U S Food and Drug Administration
  3. Drugs@FDA. U S Food and Drug Administration
  4. Drugs@FDA. U S Food and Drug Administration
  5. Drugs@FDA. U S Food and Drug Administration
  6. Picard N, Cresteil T, Djebli N, Marquet P (2005). "In vitro metabolism study of buprenorphine: evidence for new metabolic pathways.". Drug Metab Dispos 33 (5): 689-95. DOI:10.1124/dmd.105.003681. PMID 15743975. Research Blogging.
  7. Gowing L, Ali R, White JM (2009). "Buprenorphine for the management of opioid withdrawal.". Cochrane Database Syst Rev (3): CD002025. DOI:10.1002/14651858.CD002025.pub4. PMID 19588330. Research Blogging.
  8. Mattick RP, Kimber J, Breen C, Davoli M (2008). "Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence.". Cochrane Database Syst Rev (2): CD002207. DOI:10.1002/14651858.CD002207.pub3. PMID 18425880. Research Blogging.
  9. Schottenfeld RS, Chawarski MC, Pakes JR, Pantalon MV, Carroll KM, Kosten TR (2005). "Methadone versus buprenorphine with contingency management or performance feedback for cocaine and opioid dependence.". Am J Psychiatry 162 (2): 340-9. DOI:10.1176/appi.ajp.162.2.340. PMID 15677600. Research Blogging. Review in: Evid Based Ment Health. 2005 Nov;8(4):112
  10. Simoens S, Matheson C, Bond C, Inkster K, Ludbrook A (2005). "The effectiveness of community maintenance with methadone or buprenorphine for treating opiate dependence.". Br J Gen Pract 55 (511): 139-46. PMID 15720937. PMC PMC1463190.
  11. Sullivan LE, Fiellin DA (2008). "Narrative review: buprenorphine for opioid-dependent patients in office practice.". Ann Intern Med 148 (9): 662-70. PMID 18458279.