Also Known As: Buprenorphine, Buprenex, Subutex, Temgesic, Suboxone
Buprenorphine (sold under the trade-names of Subutex, Suboxone (buprenorphine with naloxone) - high-dose tablets used for the treatment of addiction - Temgesic, Buprenex - solutions for injection used for acute pain in primary-care settings - Norspan and Butrans - transdermal preparations used for chronic pain) is a semi-synthetic opioid that is used to treat opioid addiction in higher dosages (>2 mg), to control moderate acute pain in non-opioid-tolerant individuals in lower dosages (~200 Âµg), and to control moderate chronic pain in dosages ranging from 20â€“70 Âµg/hour.
Buprenorphine has an extremely high binding affinity at the Âµ- and Îº-opioid receptor. It has partial agonist activity at the Âµ-opioid receptor, partial or full agonist activity at the ORL1/nociceptin and Î´-opioid receptor, and competitive antagonist activity at the Îº-opioid receptor.
Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, generally available as Temgesic 0.2 mg sublingual tablets, and as Buprenex in a 0.3 mg/ml injectable formulation. In October 2002, the Food and Drug Administration (FDA) of the United States also approved Suboxone and Subutex, buprenorphine's high-dose sublingual tablet preparations indicated for detoxification and long-term replacement therapy in opioid dependency, and the drug is now used predominantly for this purpose.