Buprenorphine (Suboxone, Subutex)
Partial mu-opioid agonist with high receptor affinity and slow dissociation kinetics, producing a ceiling effect on respiratory depression at high doses. Sublingual administration provides oral bioavailability of ~30%, with considerable interindividual variability. Primary use is opioid use disorder maintenance and acute analgesia. Norbuprenorphine metabolite is weaker and not clinically significant. Strong CYP3A4 substrate; interactions with inducers/inhibitors can significantly alter exposure.
Projected serum levels — 8 mg, once daily
Maintenance schedule: 8 mg once daily (sublingual).
Loading schedule: 21.8 mg on day 1, then 8 mg once daily — reaching therapeutic levels sooner.
Modeled steady state after ~4 days: peak ≈ 6.3 mg, trough ≈ 4.1 mg body load. Population-based estimate over 15 days for a 8 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Opioid
- Route modeled
- Sublingual
- Model confidence
- inferred
- Half-life
- 37 h
- Common dose
- 8 mg
- Suggested maximum
- 24 mg/day
- Reference dose range
- 0.20–24 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 8 mg sublingual — Cmax 0.004 mg/L at 1.7 h
Documented interactions
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contraindicated
Efavirenz (Sustiva) + Buprenorphine (Suboxone, Subutex)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Buprenorphine (Suboxone, Subutex) AUC by ~0.16x
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contraindicated
Rifampin + Buprenorphine (Suboxone, Subutex)
Rifampin inducer of CYP3A4 predicted to change Buprenorphine (Suboxone, Subutex) AUC by ~0.16x
-
danger
7-Hydroxymitragynine (7-OH) + Buprenorphine (Suboxone, Subutex)
Buprenorphine (Suboxone, Subutex) reversible_inhibitor of CYP3A4 predicted to change 7-Hydroxymitragynine (7-OH) AUC by ~2.20x
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danger
Alfuzosin (Uroxatral) + Buprenorphine (Suboxone, Subutex)
Buprenorphine (Suboxone, Subutex) reversible_inhibitor of CYP3A4 predicted to change Alfuzosin (Uroxatral) AUC by ~3.33x
-
danger
Alprazolam (Xanax) + Buprenorphine (Suboxone, Subutex)
Buprenorphine (Suboxone, Subutex) reversible_inhibitor of CYP3A4 predicted to change Alprazolam (Xanax) AUC by ~3.33x
-
danger
Amlodipine (Norvasc) + Buprenorphine (Suboxone, Subutex)
Amlodipine (Norvasc) reversible_inhibitor of CYP3A4 predicted to change Buprenorphine (Suboxone, Subutex) AUC by ~2.07x
Serum checks 442 modeled interaction pairings for buprenorphine (suboxone, subutex) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Bioavailability of sublingual buprenorphine
Bioavailability study in healthy volunteers demonstrating sublingual buprenorphine achieves oral bioavailability of approximately 30% with high interindividual variability compared to IV reference.
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Human Pharmacokinetics of Intravenous, Sublingual, and Buccal Buprenorphine
Comparative pharmacokinetic study showing sublingual buprenorphine bioavailability of 51.4% with considerable interindividual variability, higher than buccal route (27.8%).
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Pharmacokinetics and Subjective Effects of Sublingual Buprenorphine, Alone or in Combination with Naloxone
Clinical pharmacokinetic study in opioid-dependent patients showing nonlinear dose-dependent kinetics of sublingual buprenorphine and naloxone combination formulation.
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Buprenorphine maintenance versus placebo or methadone maintenance for opioid dependence
Landmark Cochrane review (31 trials, 5,430 participants) showing buprenorphine retains patients in opioid-dependence treatment better than placebo and suppresses illicit opioid use at flexible doses; comparable efficacy…
5 published studies referenced in the app, each with a plain-language summary.