What is Suboxone (buprenorphine and naloxone)?

Suboxone (Buprenorphine and Naloxone)

Suboxone is a prescription medication containing buprenorphine (a partial opioid agonist) and naloxone (an opioid antagonist) in a 4:1 ratio, used primarily for medication-assisted treatment of opioid use disorder. 1, 2

Mechanism of Action

• Buprenorphine component: Acts as a partial agonist at mu-opioid receptors with high binding affinity but low efficacy, producing a ceiling effect that limits respiratory depression while providing sufficient activity to prevent withdrawal symptoms 3
• Naloxone component: Included to deter intravenous misuse - when taken sublingually as prescribed, naloxone has minimal effect, but if injected, it can precipitate withdrawal in opioid-dependent individuals 4

Formulation and Administration

• Available as sublingual tablets or films
• Must be administered whole and placed under the tongue until completely dissolved
• Patients should not eat or drink until the tablet/film is fully dissolved
• For doses requiring multiple tablets, patients can either place all tablets at once or two at a time under the tongue 2

Clinical Use

Indications

• Treatment of opioid dependence as part of a complete program that includes counseling and behavioral therapy 2
• Used for both induction/detoxification and maintenance treatment

Dosing

1. Induction Phase:

   • Should only be started when patient is in moderate opioid withdrawal (COWS score >8)
   • For short-acting opioid dependence: Begin at least 4 hours after last opioid use
   • For long-acting opioids (e.g., methadone): Begin at least 24 hours after last use
   • Initial dose: 4-8mg sublingually on day 1, with target of 16mg total first-day dose 1, 2

2. Maintenance Phase:

   • Target dosage is typically 16mg daily
   • Maintenance range: 4-24mg daily (doses higher than 24mg show no clinical advantage)
   • Duration of treatment is individualized with no maximum recommended length 2

Effectiveness

• Reduces illicit opioid use by approximately 80% in patients who remain in treatment 1
• Similar effectiveness to methadone in retaining patients in treatment and reducing illicit opioid use 1, 4
• More effective than clonidine or lofexidine for opioid detoxification 5

Safety Considerations

Risks and Warnings

• Can cause serious and life-threatening respiratory depression
• Risk of overdose increases when combined with benzodiazepines, sedatives, or alcohol
• Physical dependence can develop with chronic use
• Can cause neonatal opioid withdrawal syndrome if used during pregnancy 2

Contraindications

• Hypersensitivity to buprenorphine or naloxone
• Severe respiratory or hepatic impairment

Monitoring and Follow-up

• Regular visits with urine drug testing and prescription monitoring program checks
• Assess for continued illicit drug use, medication compliance, and side effects
• Consider prescribing naloxone for overdose prevention, especially for patients also using benzodiazepines 1

Special Populations

• Pregnant women: Should be treated with buprenorphine alone (without naloxone)
• Hepatic impairment: May require dose adjustments and periodic monitoring of liver function 1

Practical Considerations

• Controlled substance (Schedule III) with potential for abuse and diversion
• Requires special DEA waiver for prescribers (though requirements have been modified in recent years)
• Should be stored securely away from children as accidental ingestion can be fatal 2

Suboxone represents an important advancement in the treatment of opioid use disorder, offering a safer alternative to full opioid agonists while effectively managing withdrawal symptoms and cravings.