TaperCommunitybuprenorphine / naloxone
Boxed Warning
Risk of life-threatening respiratory depression and death with concurrent benzodiazepines or other CNS depressants. Risk of dependence and abuse.
Buprenorphine/naloxone is a partial opioid agonist combination used for opioid use disorder treatment. Buprenorphine partial agonism produces a "ceiling effect" reducing overdose risk; naloxone is added to deter injection (it precipitates withdrawal if injected, but is not absorbed sublingually).
2/0.5mg, 4/1mg, 8/2mg, 12/3mg sublingual films/tablets
Sublingual film: 2/0.5, 4/1, 8/2, 12/3mg; Sublingual tablet: 2/0.5, 8/2mg; Subcutaneous depot (Sublocade): monthly buprenorphine alone
Category C
Buprenorphine: partial agonist at mu opioid receptors with high binding affinity, kappa antagonist. Naloxone: opioid antagonist (active only if injected).
Very slow taper. Compounded liquid or microdosing strategies are often required at the low end. Plan with an addiction-medicine specialist.
Buprenorphine taper is one of the longer ones in psychiatry. Hyperbolic reductions, especially below 2mg, are usually necessary. Many patients choose long-term maintenance over taper given relapse risk.
24-72 hours after last dose (slower than short-acting opioids)
3-7 days
Acute symptoms 2-4 weeks
Post-acute withdrawal (anhedonia, sleep, anxiety) can last 3-12 months
Toxicity
Respiratory depression (less than full agonists due to ceiling), sedation, constipation, dizziness, sweating, dental problems with sublingual use. Precipitated withdrawal if started while another full agonist is on board.
Pharmacokinetics
Hepatic via CYP3A4 (buprenorphine).
~96% (buprenorphine)
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