Buprenorphine-Naloxone
Buprenorphine-naloxone is a partial opioid agonist combination used for opioid use disorder treatment. Reduces cravings and withdrawal without significant euphoria.
About Buprenorphine-Naloxone
Buprenorphine-Naloxone is a partial opioid agonist / opioid antagonist combination also sold under brand names including Suboxone, Zubsolv, and Bunavail. It is primarily used to opioid Use Disorder Medication Assisted Treatment Opioid Dependence Opioid Withdrawal Management. Buprenorphine-Naloxone is available in sublingual tablet (2 mg/0.5 mg, 8 mg/2 mg), sublingual film (2 mg/0.5 mg, 4 mg/1 mg, 8 mg/2 mg, 12 mg/3 mg), and buccal film (2.1 mg/0.3 mg, 4.2 mg/0.7 mg, 6.3 mg/1 mg) form. Healthcare providers commonly prescribe Buprenorphine-Naloxone for conditions including Attention Deficit Hyperactivity Disorder (ADHD), Coronary Artery Disease (CAD), and Heart Failure Due to Coronary Artery Disease.
Buprenorphine-Naloxone at a Glance
- Brand names
- Suboxone, Zubsolv, Bunavail
- Drug class
- Partial Opioid Agonist / Opioid Antagonist Combination
- DEA schedule
- Schedule Schedule III (controlled substance)
- Pregnancy category
- FDA Category Category C — Buprenorphine-naloxone has shown adverse effects in animal reproduction studies. Buprenorphine monotherapy is generally preferred over the combination product during pregnancy because naloxone may precipitate withdrawal in an opioid-dependent fetus. Use during pregnancy only if the potential benefit justifies the potential risk.
- Available forms
- Sublingual tablet (2 mg/0.5 mg, 8 mg/2 mg), Sublingual film (2 mg/0.5 mg, 4 mg/1 mg, 8 mg/2 mg, 12 mg/3 mg), Buccal film (2.1 mg/0.3 mg, 4.2 mg/0.7 mg, 6.3 mg/1 mg)
- Therapeutic categories
- Addiction Medicine, Substance Use, Opioids, Controlled Substances
- Conditions treated
- 3 related conditions on this site
What Buprenorphine-Naloxone Is Used For
Dosage Quick Reference
These are general dosage guidelines for Buprenorphine-Naloxone. Your doctor will determine the appropriate dose for your specific situation.
| Phase | Starting Dose | Maintenance Dose |
|---|---|---|
| Induction (opioid-dependent, short-acting opioids) | 2 mg/0.5 mg to 4 mg/1 mg on Day 1 | Titrate in 2–4 mg increments to control withdrawal symptoms |
| Stabilization (Days 2–7) | Adjust to suppress withdrawal and cravings | Target 8 mg/2 mg to 16 mg/4 mg per day |
| Long-term maintenance | 16 mg/4 mg per day (typical) | 4 mg/1 mg to 24 mg/6 mg per day; max 24 mg/6 mg |
Side Effects
Common Side Effects:
- Headache
- Nausea
- Vomiting
- Constipation
- Sweating
- Insomnia
- Pain
- Peripheral edema
- Drug withdrawal syndrome
Serious Side Effects:
- Respiratory depression
- Precipitated opioid withdrawal
- Neonatal opioid withdrawal syndrome
- Hepatotoxicity
- Allergic reactions
- Adrenal insufficiency
- Hypotension
- Serotonin syndrome
See also: Drug Interactions ↓
Drug Interactions
Buprenorphine-naloxone has important pharmacological interactions that require careful management.
- Benzodiazepines (e.g., diazepam, alprazolam, clonazepam): Concurrent use with buprenorphine carries a serious risk of profound sedation, respiratory depression, coma, and death. If combined use is necessary, limit dose and duration, and monitor patients closely. An FDA boxed warning applies.
- Other CNS depressants (e.g., alcohol, sedating antihistamines, gabapentin, pregabalin): Additive CNS depression increases the risk of fatal respiratory depression. Patients should be counseled to avoid alcohol and non-prescribed sedating substances.
- CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, clarithromycin): May increase buprenorphine plasma levels, potentially intensifying both therapeutic and adverse effects. Monitor for excess sedation.
- CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine): May reduce buprenorphine efficacy by accelerating its metabolism, potentially precipitating withdrawal symptoms or loss of therapeutic effect.
- Full opioid agonists (e.g., morphine, oxycodone, heroin): Buprenorphine has a higher receptor binding affinity than most full agonists and may precipitate acute withdrawal if administered while a full agonist is still occupying receptors. Conversely, full agonists taken during buprenorphine maintenance may have blunted effects.
Key Considerations
Controlled substance
Buprenorphine-Naloxone is a Schedule Schedule III controlled substance under federal law. Prescriptions are regulated, refills may be restricted, and the medication has recognized potential for misuse or dependence. Use exactly as prescribed.
Known drug interactions
Buprenorphine-Naloxone has documented interactions with other medications, supplements, and certain foods. Review the Drug Interactions section below and tell your healthcare provider about every medication you take, including over-the-counter products. Jump to section →
Multiple forms available
Buprenorphine-Naloxone comes in more than one form (Sublingual tablet (2 mg/0.5 mg, 8 mg/2 mg), Sublingual film (2 mg/0.5 mg, 4 mg/1 mg, 8 mg/2 mg, 12 mg/3 mg), Buccal film (2.1 mg/0.3 mg, 4.2 mg/0.7 mg, 6.3 mg/1 mg)). The right form for you depends on your condition, ease of use, and your provider's recommendation.
Additional Information
Buprenorphine/naloxone is a combination medication used for the treatment of opioid use disorder. This formulation combines buprenorphine (a partial opioid agonist) with naloxone (an opioid antagonist) to reduce the potential for misuse while providing effective treatment for opioid dependence.
Mechanism of Action
The combination works through complementary mechanisms. Buprenorphine is a partial mu-opioid receptor agonist that relieves cravings and withdrawal symptoms while producing a ceiling effect on respiratory depression. Naloxone is an opioid antagonist with poor sublingual/oral bioavailability (approximately 3%) but high parenteral bioavailability. When taken sublingually as directed, naloxone contributes minimally to the clinical effect because it is poorly absorbed. However, if the medication is dissolved and injected, naloxone becomes active and precipitates withdrawal, deterring intravenous misuse. This design helps ensure the medication is taken as prescribed.
Available Formulations
Buprenorphine/naloxone is available in several sublingual and buccal formulations. Sublingual tablets come in 2/0.5 mg and 8/2 mg strengths. Sublingual films are available in 2/0.5 mg, 4/1 mg, 8/2 mg, and 12/3 mg strengths. Generic formulations are available. The sublingual administration requires placing the medication under the tongue and allowing it to dissolve completely without chewing or swallowing.
Medical Uses
Buprenorphine/naloxone is FDA-approved for the treatment of opioid use disorder as part of a complete treatment plan that includes counseling and psychosocial support. It is used for both induction and maintenance therapy. The combination is preferred over buprenorphine alone in most cases due to its lower abuse potential. Clinical studies demonstrate that buprenorphine/naloxone significantly reduces illicit opioid use, improves treatment retention, and decreases opioid-related morbidity and mortality.
Dosing Guidelines
Treatment typically begins with induction when the patient is in mild to moderate opioid withdrawal (usually 12-24 hours after last short-acting opioid use or 24-72 hours after last long-acting opioid use). On day 1, a starting dose of 2/0.5 mg or 4/1 mg is given, with additional doses as needed up to 8/2 mg. On day 2, doses may increase to 16/4 mg. Maintenance doses typically range from 16/4 mg to 24/6 mg daily. Single daily dosing is standard, though some patients may benefit from divided doses. Precipitated withdrawal can occur if started too soon.
Important Safety Information
The medication carries a boxed warning regarding serious, life-threatening respiratory depression (especially with benzodiazepines or other CNS depressants), addiction/abuse/misuse potential, and neonatal opioid withdrawal syndrome. Patients should be instructed to keep the medication secure and away from children or others who may misuse it. Precipitated withdrawal occurs if administered before adequate withdrawal from full opioid agonists. Hepatotoxicity has been reported. Do not switch between buccal and sublingual products on a mg-per-mg basis due to different bioavailabilities.
Drug Interactions
CNS depressants (benzodiazepines, alcohol, other opioids, sedatives) significantly increase risk of respiratory depression and death. CYP3A4 inhibitors may increase buprenorphine levels; CYP3A4 inducers may decrease levels. Full opioid agonists will have diminished effect due to buprenorphine's high receptor affinity. Naltrexone blocks buprenorphine effects; a washout period is needed when switching. Serotonergic medications may increase serotonin syndrome risk.
Special Populations
For pregnant women with opioid use disorder, buprenorphine monotherapy (without naloxone) is generally preferred due to limited safety data on naloxone in pregnancy. However, some women may continue buprenorphine/naloxone if they were stable on it before pregnancy. Neonatal opioid withdrawal syndrome should be anticipated. The medication is excreted in breast milk; women on stable doses may breastfeed with monitoring. Safety in pediatric patients has not been established. Elderly patients may need lower doses. Use with caution in hepatic impairment.
Frequently Asked Questions
Medical Disclaimer: This information is for educational purposes only and should not be considered medical advice. Always consult with your healthcare provider before starting, stopping, or changing any medication. Your doctor can provide personalized recommendations based on your specific health condition and medical history.