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 µg), and to control moderate chronic pain in dosages ranging from 20-70 µg/hour.
Buprenorphine is one of the Bentley compounds derived from an alkaloid of the plant Papaver somniferum (the opium poppy), known as thebaine.
Buprenorphine has an extremely high binding affinity at the µ- and κ-opioid receptor. It has partial agonist activity at the µ-opioid receptor, partial or full agonist activity at the ORL1/nociceptin and δ-opioid receptor, and competitive antagonist activity at the κ-opioid receptor.
Buprenorphine hydrochloride was first marketed in the 1980s by Reckitt & Colman (now Reckitt Benckiser) as an analgesic, available generally 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 additionally approved Suboxone and Subutex, buprenorphine's high-dose sublingual pill preparations indicated for detoxification and long-term replacement therapy in opioid dependency, and the drug is now used predominantly for this purpose.
In the European Union, Suboxone and Subutex, buprenorphine's high-dose sublingual tablet preparations, were approved for opioid addiction treatment in September 2006. In the Netherlands, Buprenorphine is a List II drug of the Opium Law, though special rules and guidelines apply to its prescription and dispensation. In the USA, it has been a Schedule III drug under the United Nations' Convention on Psychotropic Substances since it was rescheduled from Schedule V just before FDA approval of Suboxone and Subutex. In recent years, buprenorphine has been introduced in most European countries as a transdermal formulation for the treatment of chronic pain.
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