Buprenorphine (US brand name Subutex® which has been discontinued and generic) is an opioid medication. It is a partial agonist at the mu opioid receptor (MOR) and mainly an antagonist at the kappa opioid receptor (KOR). Here is key information about this medication.
FDA-approved indications
Indicated for the treatment of opioid dependence, preferably during the induction phase of the treatment
Dosage
For induction, consideration should be given to type of opioid dependence (i.e., long- or short-acting opioid), the time since last opioid use, and the degree or level of opioid dependence.
1. Induction: Dose needs to be titrated till it is effective
a. Patients taking heroin or other short-acting opioids:
Administer at least 4 hours after the patient last used opioids or preferably when moderate objective signs of opioid withdrawal appear
b. Patients on methadone or other long-acting opioids:
Withdrawal symptoms are more likely to appear in patients maintained on higher doses of methadone (>30 mg) and when the first buprenorphine dose is administered shortly after the last methadone dose. Therefore buprenorphine monotherapy should be initiated preferably when moderate objective signs of opioid withdrawal appear.
2. Maintenance: Suboxone® (buprenorphine plus naloxone) is preferred since it can be administered without daily supervision (see below). Buprenorphine monotherapy is given only in cases where the patient is hypersensitive to presence of naloxone in Suboxone®.
Maintenance dose (monotherapy): 4–24 mg/day (to be adjusted in increments or decrements of 2–4 mg/day )
Dosage forms and strengths
Buprenorphine for sublingual use. Available in 2 mg and 8 mg strengths.
Please refer to Prescribing Information (see link below) for complete discussion of dosage, administration, warnings and precautions, contraindications, etc.
Buprenorphine plus Naloxone (Suboxone® and generic)
Buprenorphine is an agonist on mu-opioid receptor and antagonist on kappa-opioid receptor. Naloxone is an antagonist at mu-opioid receptor.
FDA-approved indications
Treatment of opioid dependence
Dosage
1. If the patient is dependent on short-acting opioid products, at least 6 hours have passed since last use, and patient is in opioid withdrawal
Day 1: up to buprenorphine 8 mg and naloxone 2 mg in divided doses
Start with 2 mg and 0.5 mg or 4 mg and 1 mg buprenorphine and naloxone and titrate upwards in 2 or 4 mg of buprenorphine every 2 hours, up to daily maximum of 8 mg and 2 mg depending on control of withdrawal symptoms.
Day 2: up to buprenorphine 16 mg plus naloxone 4 mg in a single dose
Note: If patient is dependent on methadone or long-acting opioid products, buprenorphine monotherapy is preferred on first 2 days of the treatment.
2. For maintenance treatment
Buprenorphine 16 mg plus naloxone 4 mg as a single daily dose
Administration: Can be administered by placing under the tongue (sublingual) or inside of the cheek (buccal). Do not cut, chew, or swallow sublingual film.
Dosage forms and strengths
Buprenorphine plus naloxone as a film for sublingual use. Available in the following strengths:
- 2 mg buprenorphine with 0.5 mg naloxone
- 4 mg buprenorphine with 1 mg naloxone
- 8 mg buprenorphine with 2 mg naloxone
- 12 mg buprenorphine with 3 mg naloxone
Please refer to Prescribing Information (see link below) for complete discussion of dosage, administration, warnings and precautions, contraindications, etc.
Related Pages
Clinical pearls on prescribing buprenorphine: Part one
Clinical pearls on prescribing buprenorphine: Part two
News: July 7, 2016. Buprenorphine prescribing limit raised significantly (Free)
Naloxone autoinjector (Evzio®) and intranasal spray (Narcan® nasal spray)
Tips on using naltrexone extended-release injectable (Vivitrol®)
How to order, store, and administer naltrexone extended-release injection (Vivitrol®)
Opioids in the urine drug screen
Tips for opioid dependent patients
Substance use: Index and Links (Free)
References
Suboxone® Prescribing Information
Buprenorphine Prescribing Information
Copyright 2016, Rajnish Mago, MD. All rights reserved. May not be reproduced in any form without express written permission.
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