Buprenorphine/ naloxone
SUBOXONE
What it isBuprenorphine partial mu agonist plus poorly absorbed sublingual naloxone; maintenance treatment for opioid use disorder.
Why this oneThe naloxone is a misuse deterrent: negligible sublingually, but it precipitates withdrawal if the product is dissolved and injected.
What limits itStarting it too soon after a full agonist precipitates withdrawal. Benzodiazepines and other sedatives still increase respiratory risk.
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Opioid dependence (induction) | Adults (short-acting opioid dependence) | Day 1: up to 8 mg/2 mg (divided doses); Day 2: up to 16 mg/4 mg QD | — | 16 mg/4 mg on Day 2 |
| Opioid dependence (maintenance) | Adults | Titrate from induction dose | 4 mg/1 mg to 24 mg/6 mg QD | 24 mg/6 mg QD |
Renal Undefined
Hepatic Not recommended in severe hepatic impairment; may not be appropriate in moderate hepatic impairment
Instructions
- Administer sublingually or buccally as a single daily dose
- Administer whole — do not cut, chew, or swallow the film
- Induct when objective signs of opioid withdrawal appear (>=6 h after last opioid)
- When discontinuing, gradually taper to avoid withdrawal
- Strongly consider prescribing an opioid overdose reversal agent
Cautions
- Addiction, abuse, and misuse
- Life-threatening respiratory/CNS depression (esp. with benzodiazepines/CNS depressants)
- Unintentional pediatric exposure (may be fatal)
- Neonatal opioid withdrawal syndrome
- Adrenal insufficiency
- Hepatitis/hepatic events
- Precipitation of opioid withdrawal
- Overdose risk in opioid-naive patients (not an analgesic)
Adverse reactions
- Oral hypoesthesia
- Glossodynia
- Oral mucosal erythema
- Headache
- Nausea/vomiting
- Constipation
- Withdrawal signs/symptoms
- Insomnia
Pregnancy Limited data do not indicate increased malformation risk from buprenorphine; prolonged use can cause neonatal opioid withdrawal syndrome; dose adjustments may be needed.
Lactation Buprenorphine present in low levels in human milk; oral naloxone absorption limited; monitor infant.
NO BOXED WARNINGS
Classes and tags
Clinical profile
Mechanism of action: Buprenorphine/ naloxone ballicule
Open Buprenorphine/ naloxone in the interactive console ↗
Memory aids: mascots and interaction avatars
pinpoint pupils → opioid
dilated pupils → opioid blocker
SUBmarine periscope on bumper car