Buprenorphine/Naloxone

Opioid agonist therapy (OAT); Partial μ-agonist + abuse-deterrent

Buprenorphine / Naloxone

Suboxone, Zubsolv, Bunavail, Cassipa

Buprenorphine/naloxone (most widely known as Suboxone) is one of the two pillars of med-assisted treatment for opioid use disorder. The partial-agonist nature of buprenorphine gives it a ceiling effect on respiratory depression, far safer than full agonists like methadone. The naloxone is essentially inert SL; it exists as an injection deterrent. See Buprenorphine for the pharmacology of the active component.

Experience

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Problems

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Titration strategies

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Effects

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Pharmacokinetics

Absorption

Buprenorphine ~30% SL; naloxone negligible.

Distribution

Buprenorphine ~96% protein binding.

Metabolism

Buprenorphine: CYP3A4 → norbuprenorphine (active). Naloxone: hepatic glucuronidation.

Elimination

Fecal (buprenorphine and metabolites); renal (naloxone glucuronide).

Interactions

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Pregnancy and lactation

Prefer buprenorphine monoproduct (Subutex) in pregnancy when possible, more pregnancy data.

Monitoring

Withdrawal scale (COWS) during induction; LFTs at baseline + periodically; toxicology screens per program.

Patient counseling

Precipitated withdrawal: do not induct until in moderate withdrawal (COWS ≥ 8–12). Hold under tongue until fully dissolved, do not chew or swallow. Combine with counseling and recovery support.

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See also

Buprenorphine, Methadone, Naltrexone, Naloxone

References

Summary

Classes

Opioid agonist therapy (OAT); Partial μ-agonist + abuse-deterrent

Common uses

Opioid use disorder (OUD) maintenance▲0▼, Opioid withdrawal▲0▼

Pharmacy

Starting dose

Induction: 2/0.5 to 4/1 mg SL once in moderate withdrawal; titrate to 12–16/3–4 mg/d by day 2–3

Preparations

SL film or tablet, 2/0.5 to 12/3 mg per dose

US FDA Max

24/6 mg/d (most labels)

Pharmacology

Routes

Sublingual film or tablet (buccal for some)

Onset

30–60 min (SL)

Duration

24–36 h (driven by buprenorphine)

Half-life

24–42 h (buprenorphine); 1–2 h (naloxone)

Bioavailability

Buprenorphine ~30% SL; naloxone <10% SL (intentional, inactive sublingually, matters only if injected)

Pregnancy

Category C (buprenorphine-only formulations preferred in pregnancy)

Legal status

Schedule III in US; X-waiver no longer required (as of 2023)

Purported mechanism

Buprenorphine: high-affinity partial agonist at the μ-opioid receptor with ceiling effect on respiratory depression. Naloxone: abuse-deterrent, inactive SL but precipitates withdrawal if injected.