Buprenorphine
Subutex, Temgesic, Buprenex, or Suboxone [buprenorphine:naloxone 4:1 preparation]; Norspan) is a semi-synthetic opioid that is used to treat opioid addiction in higher dosages (>2 mg) and to control moderate pain in non-opioid tolerant individuals in lower dosages (~200 µg).
Buprenorphine is a Bentley-derivative opioid of the phenanthrene class with 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 of America 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 pill 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.