What is the role of buprenorphine in maintenance therapy for opioid abuse?

Updated: Jun 21, 2018
  • Author: David W Dixon, DO; Chief Editor: Glen L Xiong, MD  more...
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Answer

Buprenorphine is a mu-opioid partial agonist that, like methadone, suppresses withdrawal and cravings. However, the property of partial agonism confers a "ceiling effect," at which higher doses of buprenorphine cause no additional effects. This ceiling effect affords a wider margin of safety than methadone, which can be lethal in overdose. The increased safety of buprenorphine has allowed it to become available by prescription as a Schedule III medication.

Buprenorphine has been combined with naloxone [36] in a 4:1 ratio (Suboxone, Zubsolv) or a 6-7:1 ratio (Bunavail) in order to alleviate concerns that the sublingual tablet would be dissolved and injected by addicts. Naloxone is an opioid antagonist that is poorly absorbed sublingually and orally but is well-absorbed intravenously. As a result, an opioid-dependent patient injecting buprenorphine/naloxone will suffer a withdrawal syndrome secondary to naloxone's occupation of mu-opioid receptors.


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