Generic Name

Buprenorphine

Mechanism

• Buprenorphine – a *partial μ‑opioid receptor agonist* with high affinity, slowly dissociates, producing a ceiling effect on respiratory depression while providing analgesia and euphoric suppression.
• Naloxone – an *opioid antagonist* that is poorly absorbed orally but rapidly competes for the receptor in the gastrointestinal tract when administered sublingually. It prevents diversion by injecting the medication.
• The combination lowers withdrawal severity, reduces cravings, and averts misuse, while the naloxone component discourages intravenous abuse.

Pharmacokinetics

Indications

• Opioid Use Disorder (OUD) – for acute induction and maintenance of opioid dependence, including pain‑managed OUD when combined with opioid analgesia.
• Substitution Therapy – for treatment‑employed reduction of withdrawal symptoms and cravings while patients taper off higher‑potency opioids.

Contraindications

• Contraindications
• Known hypersensitivity to buprenorphine, naloxone, or excipients.
• Severe respiratory depression or acute opioid intoxication without detoxification.
• Severe hepatic impairment (Child‑Pugh B/C).
• Warnings
• Risk of respiratory depression in opioid naïve patients or when combined with CNS depressants.
• Potential for precipitated withdrawal if initiated before opioids are cleared (> 12 h).
• Use cautiously in the elderly, those with cardiac disease, or ongoing benzodiazepine use.

Dosing

• Initial Induction
• Start with 2 mg (one half‑tablet).
• After 12–24 h, if withdrawal symptoms are mild or moderate, titrate to 4 mg, then 8 mg, not exceeding 24 mg/day.
• Maintenance
• Typical daily range: 8–24 mg, divided into 1–2 doses.
• Goal: achieve minimal craving without opioid use; adjust by 2–4 mg increments.
• Formulations
• Sublingual tablet (offset displacement of buprenorphine).
• Extended‑release transdermal patch (for chronic pain) – separate dosing continuum.
• Special Situations
• In pregnancy, use only if benefits outweigh uncertainties; no FDA contraindication.
• Peri‑operative: may be paused 48 h before surgery; resume post‑pain management.

Adverse Effects

• Common (≤ 10 %)
• Nausea, vomiting, constipation, abdominal pain.
• Somnolence, dizziness, headache.
• Dysphoria, insomnia.
• Serious (≤ 1 %)
• Respiratory depression (especially with co‑prescribed CNS depressants).

‑ Severe hypotension and bradycardia (rare).
• Hepatotoxicity—monitor LFTs if liver impairment suspected.
• Severe skin reactions with patches (contact dermatitis).
• Withdrawal Symptoms (if discontinuation)
• Tachycardia, chills, sweating, nausea, myalgias, insomnia.
• Can require rescue therapy with full agonists or transition to methadone.

Monitoring

Clinical Pearls

• "Double‑Trouble" Diversion Prevention – The naloxone component is only fractionally absorbed orally (< 0.01 %) but expels 20–30 mg when injected, making the drug less attractive to abusers while preserving efficacy.
• Start Low, Go Slow – Induction should begin ≤ 2 mg to check for withdrawal precipitation; jump 2 mg increments every 12–24 h.
• Caution with CYP3A4 Interaction Partners – St. John’s wort, rifampicin, or carbamazepine may dramatically lower buprenorphine exposure; dose adjustments or alternative therapies should be considered.
• Pregnancy Apology – Though limited data, buprenorphine (but not naloxone) has a better safety record than methadone; apply the same V‑rating: “caution but not contraindicated.”
• Patch‑to‑Tablet Bridge – For chronic pain patients discontinuing patch therapy for OUD, begin low‑dose sublingual Suboxone while patch dose is tapered to zero (avoid simultaneous high buprenorphine exposure).
• Non‑Opioid Pain – Use Suboxone only if the patient has a history of OUD; otherwise start with non‑opioid analgesics to avoid supereffectiveness of buprenorphine in naïve pain patients.

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• *This drug card is intended for educational purposes; clinical decisions should incorporate up‑to‑date guidelines and individual patient factors.*