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Opioid partial agonist (μ-receptor partial agonist, κ-antagonist) Pregnancy: Caution — neonatal abstinence syndrome at delivery; buprenorphine has milder NAS than methadone (MOTHER trial). Continue maintenance therapy in pregnancy under specialist supervision.

Buprenorphine

Brand names: BuTrans (transdermal), Transtec (transdermal), Subutex (sublingual), Suboxone (with naloxone), Sublocade (depot SC monthly), Temgesic (sublingual)

Adult dose

Dose: Chronic pain (BuTrans patch): 5/10/15/20 mcg/hr — apply weekly. Transtec: 35/52.5/70 mcg/hr — change every 4 days (twice weekly). Acute pain (Temgesic SL): 200–400 mcg every 6–8 hours; max 1.6 mg/day. Opioid use disorder (Subutex/Suboxone): induction 4 mg SL on day 1 (after onset of withdrawal), titrate to 12–24 mg/day; maintenance 8–24 mg/day.
Route: Sublingual / Transdermal / Subcutaneous (depot) / IV (rare)
Frequency: Once daily (SL maintenance), weekly or 4-day patches
Max: Pain: 20 mcg/hr patch (BuTrans) or 70 mcg/hr (Transtec); OUD: 32 mg SL/day
Patches in opioid-naïve patients: start at lowest strength. SL tablets: hold under tongue 5–10 min, do not swallow. AVOID with full agonist opioids — partial agonism precipitates withdrawal.

Dose adjustments

Renal

No adjustment required in mild–moderate renal impairment (no active metabolites). Caution in severe.

Hepatic

Reduce dose 50% in moderate impairment. Avoid in severe.

Clinical pearls

  • Ceiling effect on respiratory depression — the safest opioid in overdose, BUT not protective when combined with benzodiazepines/alcohol.
  • OUD: induce only after onset of objective opioid withdrawal (COWS ≥8) to avoid precipitated withdrawal — 4 mg start, escalate by 4–8 mg.
  • Suboxone (with naloxone) deters IV diversion — naloxone is bioavailable IV/IM but not SL.
  • Sublocade (monthly depot SC injection) eliminates daily adherence problem — specialist clinics only.
  • Transdermal patches: do NOT cut. External heat (hot bath, heating pad, fever) ↑ release rate → respiratory depression risk.
  • Convert from morphine: BuTrans 10 mcg/hr ≈ morphine 30 mg PO/24 hr. Always titrate, never substitute mg-for-mg.

Contraindications

  • Severe respiratory depression
  • Acute alcohol intoxication, delirium tremens
  • Recent (within 24 hr) full opioid agonist (morphine, oxycodone, methadone) — precipitates withdrawal
  • Severe hepatic impairment (Child-Pugh C)
  • Concurrent MAOI within 14 days
  • Untreated raised intracranial pressure or head injury
  • Hypersensitivity

Side effects

  • Nausea, vomiting, constipation (less than morphine)
  • Headache, dizziness, somnolence
  • Sweating, dry mouth
  • Application site reactions (transdermal — rotate sites)
  • Respiratory depression (ceiling effect at high doses — safer than full agonists)
  • QT prolongation (dose-related, especially methadone-treated patients)
  • Precipitated withdrawal if given before opioid washout
  • Hepatotoxicity (especially Suboxone IV misuse)

Interactions

  • Full opioid agonists: precipitated withdrawal (partial agonism)
  • CNS depressants (benzodiazepines, alcohol, gabapentinoids): potentiated respiratory depression — major mortality risk in OUD population
  • CYP3A4 inhibitors (ritonavir, ketoconazole, clarithromycin): ↑ levels — caution
  • CYP3A4 inducers (rifampicin, carbamazepine, phenytoin): ↓ levels — withdrawal
  • Naloxone (in Suboxone): inactive when SL but blocks IV misuse

Monitoring

  • LFTs at baseline and during OUD treatment
  • ECG if other QT drugs
  • Respiratory rate, sedation score (acute pain)
  • Urine drug screen (OUD)

Reference: BNF 90; SmPC BuTrans / Suboxone / Sublocade; NICE TA114 / TA354; UK Drug Misuse and Dependence Guidelines 2017 ('Orange Book'); MOTHER trial NEJM 2010. Verify against your local formulary and the latest BNF before prescribing.

Related

Curated clinical cross-links plus same-class fallbacks.

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