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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 receptor]]s 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."<ref>{{MeSH}}</ref> | 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 receptor]]s 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."<ref>{{MeSH}}</ref> | ||
==History== | ==History== | ||
In the [[United States]], an injectable version was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/NewDrugApplicationNDA/ New Drug Application] (NDA) by the FDA in 1981.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=019880 Drugs@FDA]. U S Food and Drug Administration</ref> An oral/sublingual version (Subutex) was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/NewDrugApplicationNDA/ New Drug Application] (NDA) by the FDA in 2002.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=020732 Drugs@FDA]. U S Food and Drug Administration</ref> An oral/sublingual version combined with [[naloxone]] (Suboxone) was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/NewDrugApplicationNDA/ New Drug Application] (NDA) by the FDA in 2002.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=020733 Drugs@FDA]. U S Food and Drug Administration</ref> | In the [[United States of America]], an injectable version was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/NewDrugApplicationNDA/ New Drug Application] (NDA) by the FDA in 1981.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=019880 Drugs@FDA]. U S Food and Drug Administration</ref> An oral/sublingual version (Subutex) was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/NewDrugApplicationNDA/ New Drug Application] (NDA) by the FDA in 2002.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=020732 Drugs@FDA]. U S Food and Drug Administration</ref> An oral/sublingual version combined with [[naloxone]] (Suboxone) was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/NewDrugApplicationNDA/ New Drug Application] (NDA) by the FDA in 2002.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=020733 Drugs@FDA]. U S Food and Drug Administration</ref> | ||
An injectable generic version was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/AbbreviatedNewDrugApplicationANDAGenerics/ Abbreviated New Drug Application] (ANDA) in 1996.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=074137 Drugs@FDA]. U S Food and Drug Administration</ref> | An injectable generic version was approved with a [http://www.fda.gov/Drugs/DevelopmentApprovalProcess/HowDrugsareDevelopedandApproved/ApprovalApplications/AbbreviatedNewDrugApplicationANDAGenerics/ Abbreviated New Drug Application] (ANDA) in 1996.<ref>[http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.SearchAction&SearchType=BasicSearch&Search_Button=Submit&searchTerm=074137 Drugs@FDA]. U S Food and Drug Administration</ref> | ||
==Pharmacology== | |||
===Metabolism=== | |||
Buprenorphine is metabolized by [[cytochrome P-450]], specifically the .<ref name="pmid15743975">{{cite journal| author=Picard N, Cresteil T, Djebli N, Marquet P| title=In vitro metabolism study of buprenorphine: evidence for new metabolic pathways. | journal=Drug Metab Dispos | year= 2005 | volume= 33 | issue= 5 | pages= 689-95 | pmid=15743975 | |||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=15743975 | doi=10.1124/dmd.105.003681 }} <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref> | |||
==Uses== | ==Uses== | ||
| Line 12: | Line 19: | ||
===Opiate dependence=== | ===Opiate dependence=== | ||
Although buprenorphine–naloxone may be less effective than methadone<ref name="pmid15677600">{{cite journal| author=Schottenfeld RS, Chawarski MC, Pakes JR, Pantalon MV, Carroll KM, Kosten TR| title=Methadone versus buprenorphine with contingency management or performance feedback for cocaine and opioid dependence. | journal=Am J Psychiatry | year= 2005 | volume= 162 | issue= 2 | pages= 340-9 | pmid=15677600 | Buprenorphine is less effective than [[methadone]] for treating [[opiate dependence]] according to a [[meta-analysis]] by the [[Cochrane Collaboration]].<ref name="pmid18425880">{{cite journal| author=Mattick RP, Kimber J, Breen C, Davoli M| title=Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence. | journal=Cochrane Database Syst Rev | year= 2008 | volume= | issue= 2 | pages= CD002207 | pmid=18425880 | ||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=18425880 | doi=10.1002/14651858.CD002207.pub3 }} <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref> Although buprenorphine–naloxone may be less effective than methadone<ref name="pmid15677600">{{cite journal| author=Schottenfeld RS, Chawarski MC, Pakes JR, Pantalon MV, Carroll KM, Kosten TR| title=Methadone versus buprenorphine with contingency management or performance feedback for cocaine and opioid dependence. | journal=Am J Psychiatry | year= 2005 | volume= 162 | issue= 2 | pages= 340-9 | pmid=15677600 | |||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=15677600 | doi=10.1176/appi.ajp.162.2.340 }} [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=16246888 Review in: Evid Based Ment Health. 2005 Nov;8(4):112] <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref>, it has more predictable dosing<ref name="pmid15720937">{{cite journal| author=Simoens S, Matheson C, Bond C, Inkster K, Ludbrook A| title=The effectiveness of community maintenance with methadone or buprenorphine for treating opiate dependence. | journal=Br J Gen Pract | year= 2005 | volume= 55 | issue= 511 | pages= 139-46 | pmid=15720937 | | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=15677600 | doi=10.1176/appi.ajp.162.2.340 }} [http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=16246888 Review in: Evid Based Ment Health. 2005 Nov;8(4):112] <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref>, it has more predictable dosing<ref name="pmid15720937">{{cite journal| author=Simoens S, Matheson C, Bond C, Inkster K, Ludbrook A| title=The effectiveness of community maintenance with methadone or buprenorphine for treating opiate dependence. | journal=Br J Gen Pract | year= 2005 | volume= 55 | issue= 511 | pages= 139-46 | pmid=15720937 | ||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=15720937 | pmc=PMC1463190 }} <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref>, and can be prescribed by qualifying office-based physicians.<ref name="pmid18458279">{{cite journal| author=Sullivan LE, Fiellin DA| title=Narrative review: buprenorphine for opioid-dependent patients in office practice. | journal=Ann Intern Med | year= 2008 | volume= 148 | issue= 9 | pages= 662-70 | pmid=18458279 | | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=15720937 | pmc=PMC1463190 }} <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref>, and can be prescribed by qualifying office-based physicians.<ref name="pmid18458279">{{cite journal| author=Sullivan LE, Fiellin DA| title=Narrative review: buprenorphine for opioid-dependent patients in office practice. | journal=Ann Intern Med | year= 2008 | volume= 148 | issue= 9 | pages= 662-70 | pmid=18458279 | ||
| url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=18458279 }} <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref> | | url=http://www.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pubmed&retmode=ref&cmd=prlinks&id=18458279 }} <!--Formatted by http://sumsearch.uthscsa.edu/cite/--></ref> | ||
===Veterinary medicine=== | |||
Burprenorphine does not cause the hyperexcitation in cats that classically has been associated with pure agonists, and provides analgesia. | |||
==External links== | ==External links== | ||
Latest revision as of 10:49, 2 February 2023
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 of America, 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.