Summary
Buprenorphine is a partial μ-opioid agonist and κ-opioid antagonist used for opioid use disorder treatment and pain management. It has a ceiling effect for respiratory depression and euphoria at therapeutic doses, making it safer than full opioid agonists. However, this ceiling effect is removed when combined with benzodiazepines or alcohol. When used for opioid dependence treatment, buprenorphine must be started when moderate withdrawal symptoms appear to avoid precipitated withdrawal. Often combined with naloxone (Suboxone) to deter IV misuse, though naloxone's deterrent effect has been questioned.
Dose Information
| ROA | Light | Common | Strong | Heavy |
|---|---|---|---|---|
| Sublingual | 1-2mg | 2-4mg | 4-8mg | 8mg+ |
| Oral | 0.2-0.4mg | 0.4-0.8mg | 0.8-1.5mg | 1.5mg+ |
| Insufflated | 0.2-0.4mg | 0.4-0.8mg | 0.8-1.5mg | 1.5mg+ |
Light
Common
Strong
Heavy
Onset, Duration & After-effects
| ROA | Onset | Comeup | Peak | Offset | After Effects |
|---|---|---|---|---|---|
| Sublingual | 30-80 min | 1-2 hrs | 1.5-4 hrs | 6-12 hrs | 24-72 hrs |
| Transdermal | 12-24 hrs | - | 24-48 hrs | 12-24 hrs | 24-72 hrs |
| Intravenous | 2-5 min | 5-15 min | 30-60 min | 4-8 hrs | 12-24 hrs |
| Intramuscular | 15-30 min | 30-60 min | 1-2 hrs | 4-8 hrs | 12-24 hrs |
| Oral | 60-90 min | - | - | - | 1.0-16.0 hrs |
| Insufflated | 30-60 min | - | 4-8 hrs | - | 1-3 hrs |
Tolerance
Build-up
develops slowly due to partial agonist ceiling; still produces opioid cross-tolerance
Reset
7–14 days for partial reset; full reset may take weeks — tolerance loss greatly increases overdose risk
Cross-tolerance
Effects
Positive
- Analgesia
- Physical euphoria
- Pain relief
- Cough suppression
Negative
- Respiratory depression
- Nausea
- Dry Mouth
- Sedation
- Itchiness
- Difficulty urinating
- Relaxant
- Pupil constriction
Positive
- Cognitive euphoria
- Anxiety suppression
- Euphoria
- Mood lift
- Cognitive Euphoria
- Anxiety Suppression
- Dream potentiation
Negative
- Constipation
- Dizziness
- Compulsive redosing
Positive
- Visual geometry
- Increased music appreciation
Negative
- Appetite suppression
- Decreased Libido
- Appetite Suppression
- Spatial disorientation
- Dulled perception
- Internal hallucinations
- Internal hallucination
- Visual and auditory hallucinations