Buprenorphine
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.
- Buprenorphine - FDA approved drug information (drug label) from DailyMed (U.S. National Library of Medicine).
- Buprenorphine - Drug information for consumers from MedlinePlus (U.S. National Library of Medicine).
- Buprenorphine - Detailed information from DrugBank.
References
- ↑ Anonymous (2024), Buprenorphine (English). Medical Subject Headings. U.S. National Library of Medicine.
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ Drugs@FDA. U S Food and Drug Administration
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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
- ↑ 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.
- ↑ Sullivan LE, Fiellin DA (2008). "Narrative review: buprenorphine for opioid-dependent patients in office practice.". Ann Intern Med 148 (9): 662-70. PMID 18458279.