buprenorphine (Buprenex, Subutex, Temgesic, Sublocade, Butrans 'professional man's methadone')
Introduction
Tradenames: Buprenex, Subutex, Sublocade.
DEA-controlled substance: class 5.
Certification & special DEA # required for prescription.
Drug Addiction Treatment Act (DATA 2000) waiver
(8 hours of training) - if used to treat opiate addiction
No special DEA # required if used to treat chronic pain []
Pharmacists can check if a prescriber has a DATA 2000 waiver because the DEA number will always start with an 'X'.
For prescribers to obtain a DATA 2000 waiver see[8].
For physicians in each state who have DATA 2000 waivers see[9] (list is not always complete)
* The White House recommends providing more training for clinicians to prescribe buprenorphine in states with high levels of misuse.[14]
Indications
- treatment of opioid dependence, opiate abuse* & opiate withdrawal (use Suboxone for maintenance)
- neonatal abstinence syndrome[17]
- treatment of acute pain
- as partial opioid agonist, of little use in treating acute cancer pain
- also used for treatment of chronic pain (not FDA-approved for this)
- preventing ongoing use of non-prescribed opiates (includes pregnant women)[21]
* buprenorphine reduces suicide mortality in patients with opiate abuse by 65%[23]
Contraindications
- treatment of acute cancer pain
Dosage
- pain
- 0.3 mg IV/IM every 6 hours (Buprenex)
- 0.2 mg sublingual tablets (Temgesic)
- opioid addiction
Sublingual: 0.2 mg (Temgesic), 2 mg, 8 mg (Subutex, Suboxone) Implant: 80 mg[15] Sublocade: monthly depot injection[18][20] Butrans: transdermal patch 5, 7.5, 10, 15 & 20 ug/hour weekly[24]
Pharmacokinetics
elimination via liver
Adverse effects
- as partial opioid agonist, has low risk of respiratory depression
- drug adverse effects of opiates
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- drugs that inhibit cyt P450 3A4 may increase levels of buprenorphine
- drugs that induce cyt P450 3A4 may diminish levels of buprenorphine
- drug interaction(s) of benzodiazepine with opiates
- drug interaction(s) of antidepressant with opiates
- drug interaction(s) of Z-drugs with opiates
- drug interaction(s) of alcoholic beverage with opiates
- drug interaction(s) of pregabalin with opiates
- drug interaction(s) of gabapentin with opiates
Laboratory
Mechanism of action
- partial opioid agonist
Notes
- drug of abuse[11]
- patient limit is 100 for clinicians prescribing buprenorphine for opioid use disorders; the White House recommends increasing this to 200[14]
- 20% of buprenorphine prescribers treat only a few patients[16]
More general terms
More specific terms
Additional terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Journal Watch 20(24):193, 2000
- ↑ Prescriber's Letter 9(11):65 2002
- ↑ Prescriber's Letter 12(9): 2005 Expanded Use of Buprenorphine (Subutex/ Suboxone) for Opioid Dependence Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=211009&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Action Report, Medical Board of California, 85:8 (April) 2003
- ↑ http://www.buprenorphine.samhsa.gov
- ↑ Prescriber's Letter 16(1): 2009 Drugs with Special Prescribing and Dispensing Requirements Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250101&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 8.0 8.1 Drug Addiction Treatment Act (DATA 2000) waiver http://www.suboxone.com/hcp/certification/
- ↑ 9.0 9.1 Physicians in each state who have DATA 2000 waivers http://www.buprenorphine.samhsa.gov (866) 287-2728
- ↑ Wikipedia: Buprenorphine http://en.wikipedia.org/wiki/Buprenorphine
- ↑ 11.0 11.1 Centers for Disease Control and Prevention Buprenorphine Prescribing Practices and Exposures Reported to a Poison Center - Utah, 2002-2011. MMWR. December 14, 2012 / 61(49);997-1001 http://www.cdc.gov/mmwr/preview/mmwrhtml/mm6149a1.htm
- ↑ Deprecated Reference
- ↑ 13.0 13.1 Sigmon SC et al. A randomized, double-blind evaluation of buprenorphine taper duration in primary prescription opioid abusers. JAMA Psychiatry 2013 Oct 23 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/24153411 <Internet> http://archpsyc.jamanetwork.com/article.aspx?articleid=1761270
- ↑ 14.0 14.1 14.2 Young K, Fairchild DG, Di Francesco L White House Announces New Measures Aimed at Curbing Opioid Misuse. Physician's First Watch, March 30, 2016 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org
White House Press Release. March 29, 2016 Fact Sheet: Obama Administration Announces Additional Actions to Address the Prescription Opioid Abuse and Heroin Epidemic. https://www.whitehouse.gov/the-press-office/2016/03/29/fact-sheet-obama-administration-announces-additional-actions-address - ↑ 15.0 15.1 15.2 Rosenthal RN, Lofwall MR, Kim S et al Effect of Buprenorphine Implants on Illicit Opioid Use Among Abstinent Adults With Opioid Dependence Treated With Sublingual Buprenorphine. A Randomized Clinical Trial. JAMA. 2016;316(3):282-290 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27434441 <Internet> http://jama.jamanetwork.com/article.aspx?articleid=2533504
Compton WM, Volkow ND Improving Outcomes for Persons With Opioid Use Disorders. Buprenorphine Implants to Improve Adherence and Access to Care. JAMA. 2016;316(3):277-279 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27434440 <Internet> http://jama.jamanetwork.com/article.aspx?articleid=2533484 - ↑ 16.0 16.1 Stein BD et al. Physician capacity to treat opioid use disorder with buprenorphine-assisted treatment. JAMA 2016 Sep 20; 316:1211. <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27654608 <Internet> http://jama.jamanetwork.com/article.aspx?articleid=2553439
- ↑ 17.0 17.1 Kraft WK, Adeniyi-Jones SC, Chervoneva I et al Buprenorphine for the Treatment of the Neonatal Abstinence Syndrome. N Engl J Med. May 4, 2017 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/28468518 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1614835
- ↑ 18.0 18.1 18.2 18.3 18.4 Indivior PLC. Oct 31, 2017 FDA Advisory Committees Recommend Approval of Indivior's RBP-6000 for the Treatment of Opioid Use Disorder. https://www.prnewswire.com/news-releases/fda-advisory-committees-recommend-approval-of-indiviors-rbp-6000-for-the-treatment-of-opioid-use-disorder-300546838.html
Brooks M FDA Okays Once-Monthly Buprenorphine Shot for Opioid Use Disorder Medscape - Dec 01, 2017. https://www.medscape.com/viewarticle/889462
FDA News Release. Nov 30, 2017 FDA approves first once-monthly buprenorphine injection, a medication-assisted treatment option for opioid use disorder. https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm587312.htm - ↑ Martin SA, Chiodo LM, Bosse JD, Wilson A. The next stage of buprenorphine care for opioid use disorder. Ann Intern Med 2018 Oct 23; PMID: https://www.ncbi.nlm.nih.gov/pubmed/30357262
Hawk K, D'Onofrio G. Time to change the way we approach opioid use disorder: A challenge to the status quo. Ann Intern Med 2018 Oct 23; PMID: https://www.ncbi.nlm.nih.gov/pubmed/30357257 - ↑ 20.0 20.1 Haight BR, Learned SM, Laffont CM et al. Efficacy and safety of a monthly buprenorphine depot injection for opioid use disorder: A multicentre, randomised, double-blind, placebo-controlled, phase 3 trial. Lancet. 2019 Feb 23;393(10173):778-790 PMID: https://www.ncbi.nlm.nih.gov/pubmed/30792007 https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(18)32259-1/fulltext
- ↑ 21.0 21.1 NEJM Knowledge+ Internal Medicine Board Review https://myknowledgeplus.nejm.org/flow/flowjs.html
- ↑ 22.0 22.1 Williams AR, Samples H, Crystal S, Olfson M. Acute care, prescription opioid use, and overdose following discontinuation of long-term buprenorphine treatment for opioid use disorder. Am J Psychiatry 2019 Dec 2; PMID: https://www.ncbi.nlm.nih.gov/pubmed/31786933 https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.2019.19060612
- ↑ 23.0 23.1 Watts BV et al. Association of medication treatment for opioid use disorder with suicide mortality. Am J Psychiatry 2022 Apr; 179:298. PMID: https://www.ncbi.nlm.nih.gov/pubmed/35360916 https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.2021.21070700
Mooney LJ. Medication treatment for opioid use disorder reduces suicide risk. Am J Psychiatry 2022 Apr; 179:262. PMID: https://www.ncbi.nlm.nih.gov/pubmed/35360917 https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.20220173 - ↑ 24.0 24.1 HIGHLIGHTS OF PRESCRIBING INFORMATION Butrans <TM> (buprenorphine) transdermal system, CIII https://app.purduepharma.com/xmlpublishing/pi.aspx?id=b
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=2476
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5311033
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=644073
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5281090
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=40400
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5281091
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3033050