Buprenorphine, is an
opioid drug with
partial agonist and
antagonist actions. Buprenorphine
hydrochloride was first marketed in the 1980s by Reckitt & Colman (now
Reckitt Benckiser) as an
analgesic, available generally as Buprenex in a 0.3 mg/ml injectable formulation in the United States. In October 2002, the
FDA additionally approved Suboxone and Subutex, buprenorphine's high-dose
sublingual pill preparations for
opioid addiction, and as such the drug is now also used for this purpose. It has been a
Schedule III drug under the
Convention on Psychotropic Substances[1] since it was rescheduled from
Schedule V (the schedule with the lowest restrictions and penalties) just before FDA approval of Suboxone and Subutex. In the recent years, buprenorphine has been introduced in most European countries as transdermal formulation ("patch") for the treatment of chronic pain.
Commercial preparations
British firm Reckitt & Colman (now Reckitt Benckiser) first marketed buprenorphine under the trade names Temgesic (sublingual/parenteral preparations, no active additives) and Buprenex (parenteral, no active additives). Two more recent formulations from Reckitt Benckiser have been approved for opioid addiction treatment in the U.S.: Subutex (flavorless sublingual, no active additives; in 2 mg and 8 mg dosages) and Suboxone (orange-tang flavored sublingual, one part naloxone for every four parts buprenorphine; hexagon shaped tablet in 2 mg and 8 mg dosages). Suboxone contains small doses of opiates aswell as the opioid antagonist naloxone to deter illicit intravenous preparation of the tablet. This is intended to attenuate the effects of buprenorphine on opioid-naive users should this formulation be injected - however no human studies have been done demonstrating the efficacy of this approach with buprenorphine and a growing number of street reports indicate that the naloxone is ineffective.
A solution for injection (usually by the intramuscular route) is marketed for the UK veterinary market by Alstoe Animal Health as Vetergesic, licenced for analgesia and sedation in dogs.
Since 2001 buprenorphine is also available transdermally in 35, 52.5 and 70 mcg/hour transdermal patch, that delivers the dose over 96 hours. This application form is marketed as Transtec in most European countries by Gruenenthal [2] (Napp Pharmaceuticals.in the UK [3] Norpharma in Denmark) for the treatment of moderate to severe cancer pain and severe non-cancer pain not responding to non-opioids. Moreover, a new 5, 10 and 20 mcg/hour patch is marketed as Butrans or Norspan, a once weekly patch for severe chronic pain not responding to non-opioids, marketed by Napp Pharmaceuticals Ltd., and Mundipharma and Gruenenthal respectively.