Table 1.
Buprenorphine formulations
| Buprenorphine Formulation (brand name, generic name, year of FDA approval) |
Dose Range |
Formulations | Time to Peak Concentrati on (hours) |
Mean Half Life (hours) |
Comments |
|---|---|---|---|---|---|
| Indicated for Pain | |||||
| Intravenous/Intramuscular (Buprenex, buprenorphine hyrdocholoride, 1985) | 0.3-0.6mg q6h/PRN | 0.3 mg | <1 | 1.2–7.2 | for acute or post-operative pain |
| Transdermal System (Butrans, buprenorphine transdermal system, 2010) | 5 mcg/hr (if < 30mg oral morphine equivalents per day) or 10-20 mcg/hr (if 30-80mg oral morphine equivalents per day) | 5, 7.5, 10, 15, 20 mcg/hr | 72 | 26 (after patch removal) | 7-day Transdermal patch |
| Buccal Film (Belbuca, buprenorphine buccal film, 2015) | 75mcg daily or q12h (for first 4 days) - 900mcg q12h | 75, 150, 300, 450, 600, 750, 900 mcg | 2.5–3 | 16.4–38.8 | dosed daily or q12h, has an adhesive and blocking layer to help fully absorb, peppermint flavored |
| Indicated for Opioid Use Disorder | |||||
| Sublingual Tablet (Subutex [now only generic], buprenorphine, 2002) | 2-8mg daily (first day) - 24mg daily | 2mg, 8 mg | 1.6-4.0 | 31-35 | may be safer for use in pregnancy because does not contain naloxone |
| Sublingual Film (Suboxone [also generic], buprenorphine and naloxone, 2002) | 2-8/.05-2 mg daily (first day) - 24/6mg daily | 2 mg/0.5 mg 4 mg/1 mg 8 mg/2 mg 12 mg/3 mg (buprenorphine/naloxone) | 0.5–2.5 | 24–42 (buprenorphine) 2–12 (naloxone) | sublingual film absorbs faster than the tablet |
| Sublingual Tablet (Zubsolv, buprenorphine and naloxone, 2013) | 1.4-2.8/0.36-0.72mg (1st dose, up to 5.7/1.4mg 1st day) - 17.1/4.2mg daily | 0.7 mg/0.18 mg 1.4 mg/0.36 mg 2.9 mg/0.71 mg 5.7 mg/1.4 mg 8.6 mg/2.1 mg 11.4 mg/2.9 mg (buprenorphine/naloxone) | 0.5–2.5 | 24–42 (buprenorphine 2–12 (naloxone) | higher bioavailability vs. Subutex or Suboxone - 2.9mg of buprenorphine in Zubsolv equivalent to 4mg in Suboxone |
| Buccal Film (Bunavail, buprenorphine and naloxone,2014) | 2.1/0.3mg - 12.6mg/2.1mg daily | 2.1 mg/0.3, mg 4.2 mg/0.7 mg, 6.3 mg/1 mg (buprenorphine/naloxone) | 0.5–2.5 | 16.4–27.5 (buprenorphine) 1.9–2.4 (naloxone) | has an adhesive and blocking layer to help fully absorb, citrus flavored |
| Implant (Probuphine, buprenorphine implant, 2016) | 74.2mg (1 dose only), 4 implants at a time | 74.2 mg of buprenorphine per implant released over 6 months | 12 | 24-48 | cannot be dosed more than 8mg sublingual equivalents daily; implants must be removed after completion of 6 month dosing interval |
| Long acting injectable (Sublocade, buprenorphine extended-release, 2017) | 300mg first 2 months, 100mg monthly after | 100mg/0.5mL, 300mg/1.3mL prefilled syringe | 24 | terminal plasma half life: 43-60 days | subcutaneous injection in abdomen; forms a hard nodule in subcutaneous space, requires refrigeration before administration |
| Long acting injectable (Buvidal [EU], Brixadi [us] CAM-2038 q1w, approval in EU and tentative FDA approval 2018) | 8-32mg weekly | 8mg, 16mg, 24mg, 32mg prefilled syringe | 20 | 5 days | subcutaneous injection in upper arm, abdomen, or buttocks; forms soft gel in subcutaneo us space |
| Long acting injectable (Buvidal [EU], Brixadi [US] CAM-2038 q4w, approval in EU and tentative FDA approval 2018) | 64-128mg monthly | 64mg, 96mg, 128mg, 160mg prefilled syringe | 4-10 | 19-25 days | |
FDA = Food and Drug Administration