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.

Opioid withdrawal

• For Clinical Opioid Withdrawal Scale (COWS) ≥8: give 4 to 8mg of Buprenorphine, 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 and app .

• 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 and hospitalized patients.

NIH National Institute on Drug Abuse ED Buprenorphine algorithm

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

See Also

• Opioids
• Opioid overdose
• Opioid withdrawal