Buprenorphine

Administration

  • Type: Opioid- maintenance therapy in opioid use disorder, rapid detox
  • Dosage Forms: injectable solution, sublingual tablet
  • Dosage Strengths: injectable solution: 0.3 mg/mL; sublingual tablet: 2, 8mg
  • Routes of Administration: Buccal, sublingual, intradermal, transdermal, IV, IM
  • Common Trade Names: Suboxone (buprenorphine + naloxone), Buprex

Adult Dosing

Highly variable, dependent on individual. The below dosing is for the traditional induction, although there are also options including a micro-induction (low-dose induction) for patients not in opioid withdrawal or a high-dose induction. [1]

Opioid withdrawal

  • For Clinical Opioid Withdrawal Scale (COWS) >=8: 4 to 8mg, observe 30 to 45min, redose if COWS remains >=8. Then discharge home with 16 mg a day to bridge until follow-up (an X-waiver is no longer required to prescribe buprenorphine).
  • For Clinical Opioid Withdrawal Scale (COWS) 0-7: Consider observing the patient until their COWS score is >8 for the standard buprenorphine induction. Alternatively, you can prescribe consider unobserved home induction instructions available on paper [2][3] and app[4] [5].
  • If sublingual tablets/films unavailable then intravenous/intramuscular formulation (dose 0.3-0.9 mg every 6-12 hours) has been used for opioid withdrawal in the ED[6] and hospitalized[7] patients.
NIH National Institute on Drug Abuse ED Buprenorphine algorithm[8]

Pediatric Dosing

Variable

Special Populations

  • Pregnancy Rating: C (but buprenorphine is preferred over methadone in pregnant patients due to neonatal outcomes)
  • Lactation risk: Infant risk has been demonstrated
  • Hepatic dosing: reduce dose or do not use in moderate - severe impairment
  • Renal dosing:

Contraindications

  • Allergy to class/drug
  • SBO, paralytic ileus
  • Acute/severe asthma (if unmonitored), respiratory depression

Adverse Reactions

Serious

  • Hypotension, prolonged QT, MI
  • Respiratory depression
  • SBO
  • Hepatotoxicity
  • Stroke
  • Sedation, coma
  • Drug dependence or withdrawal

Common

  • Pruritus
  • Constipation, nausea, diarrhea, xerostomia
  • Dizziness, headache, somnolence
  • URI symptoms

Pharmacology

  • Half-life: 24-48 hours
  • Metabolism: Extensive hepatic, CYP3A4 substrate
  • Excretion: Mostly fecal, some renal

Mechanism of Action

  • Mixed opiate agonist-antagonist, partial mu-opioid agonist, kappa-opioid antagonist

Comments

  • Combined with naloxone to deter abuse. The naloxone has no effect when used as intended under the tongue. The naloxone is only active when abused by crushing/injection. Buprenorphine and buprenorphine/naloxone are interchangeable. Buprenorphine/naloxone is now generic in the USA.
  • The DATA 2000 Waiver (aka X Waiver) is no longer required [9]

See Also

References

  1. Weimer MB, Herring AA, Kawasaki SS, Meyer M, Kleykamp BA, Ramsey KS. ASAM Clinical Considerations: Buprenorphine Treatment of Opioid Use Disorder for Individuals Using High-potency Synthetic Opioids. J Addict Med. 2023 Jul 28. doi: 10.1097/ADM.0000000000001202. Epub ahead of print. PMID: 37505909.
  2. A Guide for Patients Beginning Buprenorphine Treatment at Home https://medicine.yale.edu/edbup/quickstart/Home_Buprenorphine_Initiation_338574_42801_v1.pdf
  3. A Patient’s Guide to Starting Buprenorphine at Home from ASAM https://www.asam.org/docs/default-source/education-docs/unobserved-home-induction-patient-guide.pdf
  4. Buprenorphine Home Induction Apple App Store https://apps.apple.com/us/app/buprenorphine-home-induction/id1449302173
  5. Starting Buprenorphine from Google Play Store https://play.google.com/store/apps/details?id=com.amstonstudio.bup&hl=en_US&gl=US
  6. Berg ML, et. al. Evaluation of the use of buprenorphine for opioid withdrawal in an emergency department. Drug Alcohol Depend. 2007 Jan 12;86(2-3):239-44. https://doi.org/10.1016/j.drugalcdep.2006.06.014. Epub 2006 Aug 22. PMID: 16930865.
  7. Welsh CJ, Suman M, Cohen A, et al. The use of intravenous buprenorphine for the treatment of opioid withdrawal in medically ill hospitalized patients. Am J Addict. 2002;11(2):135-40 https://doi.org/10.1080/105500490290087901
  8. https://d14rmgtrwzf5a.cloudfront.net/sites/default/files/algorithm.pdf
  9. https://www.drugabuse.gov/nidamed-medical-health-professionals/discipline-specific-resources/initiating-buprenorphine-treatment-in-emergency-department/frequently-asked-questions-about-ed-initiated-buprenorphine