Contents

Search

buprenorphine (Buprenex, Subutex, Temgesic, Sublocade, Butrans 'professional man's methadone')

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 - doses > 2 mg/day may be needed - several years of therapy may be needed - < 1 year of therapy associated with higher risk of relapse [22] - 4 weeks taper [13] - once monthly injection (Sublocade) FDA approved Dec 2018 [18] - 2 monthly initial doses of 300 mg SQ followed by 100 mg SQ monthly maintenance [18] - up to 300 mg SQ monthly may be considered for patients for whom the benefits outweigh the risks [18] - 4 80 mg implants every 6 months (24 weeks) [15] 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: - metabolized by cyt P450 3A4 Adverse effects: - as partial opioid agonist, has low risk of respiratory depression Drug interactions: 1) drugs that inhibit cyt P450 3A4 may increase levels of buprenorphine 2) drugs that induce cyt P450 3A4 may diminish levels of buprenorphine Laboratory: - buprenorphine in specimen - buprenorphine in blood - buprenorphine in gastric fluid - buprenorphine in meconium - buprenorphine in saliva - buprenorphine in serum/plasma - buprenorphine in serum/plasma/blood - buprenorphine in urine 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]

Interactions

drug interactions drug adverse effects (more general classes)

Related

buprenorphine/naloxone (Bunavail, Suboxone)

Specific

Buprenorphine Implant (Probuphine)

General

mixed opioid agonist-antagonist (analgesic narcotic partial-mixed agonist)

Properties

INHIBITS: opiate MISC-INFO: elimination route LIVER pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Journal Watch 20(24):193, 2000
  3. Prescriber's Letter 9(11):65 2002
  4. Prescriber's Letter 12(9): 2005 Expanded Use of Buprenorphine (Subutex/ Suboxone) for Opioid Dependence Detail-Document#: 211009 (subscription needed) http://www.prescribersletter.com
  5. Action Report, Medical Board of California, 85:8 (April) 2003
  6. http://www.buprenorphine.samhsa.gov
  7. Prescriber's Letter 16(1): 2009 Drugs with Special Prescribing and Dispensing Requirements Detail-Document#: 250101 (subscription needed) http://www.prescribersletter.com
  8. Drug Addiction Treatment Act (DATA 2000) waiver http://www.suboxone.com/hcp/certification/
  9. Physicians in each state who have DATA 2000 waivers http://www.buprenorphine.samhsa.gov (866) 287-2728
  10. Wikipedia: Buprenorphine http://en.wikipedia.org/wiki/Buprenorphine
  11. 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
  12. Deprecated Reference
  13. Sigmon SC et al. A randomized, double-blind evaluation of buprenorphine taper duration in primary prescription opioid abusers. JAMA Psychiatry 2013 Oct 23 PMID: 24153411 http://archpsyc.jamanetwork.com/article.aspx?articleid=1761270
  14. 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. 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 PMID: 27434441 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 PMID: 27434440 http://jama.jamanetwork.com/article.aspx?articleid=2533484
  16. Stein BD et al. Physician capacity to treat opioid use disorder with buprenorphine-assisted treatment. JAMA 2016 Sep 20; 316:1211. PMID: 27654608 http://jama.jamanetwork.com/article.aspx?articleid=2553439
  17. 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 PMID: 28468518 http://www.nejm.org/doi/full/10.1056/NEJMoa1614835
  18. 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
  19. 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: 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: 30357257
  20. 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: 30792007 https://www.thelancet.com/journals/lancet/article/PIIS0140-6736(18)32259-1/fulltext
  21. NEJM Knowledge+ Internal Medicine Board Review https://myknowledgeplus.nejm.org/flow/flowjs.html
  22. 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: 31786933 https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.2019.19060612
  23. Watts BV et al. Association of medication treatment for opioid use disorder with suicide mortality. Am J Psychiatry 2022 Apr; 179:298. PMID: 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: 35360917 https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.20220173
  24. HIGHLIGHTS OF PRESCRIBING INFORMATION Butrans (buprenorphine) transdermal system, CIII https://app.purduepharma.com/xmlpublishing/pi.aspx?id=b

Component-of

buprenorphine/naloxone (Bunavail, Suboxone)