BUPRENORPHINE

Buprenorphine was first marketed in the United States in 1985 as a Schedule V narcotic analgesic. Until recently, the only available buprenorphine product in the United States has been a low-dose (0.3 mg/ml) injectable formulation under the brand name, Buprenex®. Very little abuse or diversion of this product has been reported in the United States, but diversion, trafficking and abuse of other buprenorphine products has occurred in Europe and other areas of the world.

In October 2002, the Food and Drug Administration (FDA) approved two buprenorphine products (Suboxone® and Subutex®) for the treatment of narcotic addiction. Both products are high dose (2 mg and 8 mg) sublingual (under the tongue) tablets: Subutex® is a single entity buprenorphine product and Suboxone® is a combination product with buprenorphine and naloxone in a 4:1 ratio, respectively. After reviewing all the available data and receiving a Schedule III recommendation from the Department of Health and Human Services (DHHS), the DEA placed buprenorphine and all products containing buprenorphine into Schedule III in 2002.

Buprenorphine is intended for the treatment of pain (Buprenex®) and opioid addiction (Suboxone® and Subutex®). In 2001 and 2005, the Narcotic Addict Treatment Act was amended to allow qualified physicians, under certification of the DHHS, to prescribe Schedule III-V narcotic drugs (FDA approved for the indication of narcotic treatment) for narcotic addiction (up to 30 patients/physician at any time) outside the context of clinic-based narcotic treatment programs (Pub. L. 106-310). Suboxone® and Subutex® are the only treatment drugs that meet the requirement of this exemption. Currently, there are nearly six thousand physicians who have been approved by the Substance Abuse and Mental Health Services Administration (SAMHSA) and the DEA for office-based narcotic treatment.

Buprenorphine has a unique pharmacological profile. It produces the effects typical of both pure mu agonists (like morphine) and partial agonists (like pentazocine) depending on dose, pattern of use and population taking the drug. It is about 20-30 times more potent than morphine as an analgesic and, like morphine it produces dose-related euphoria, drug liking, pupillary constriction, respiratory depression and sedation. However, acute, high doses of buprenorphine have been shown to have a blunting effect on both physiological and psychological effects due to its partial opioid activity.

Buprenorphine is a long-acting (24-72 hours) opioid that produces less respiratory depression at high doses than other narcotic treatment drugs. However, severe respiratory depression can occur when buprenorphine is combined with other central nervous system depressants, especially benzodiazepines. Deaths have resulted from this combination.

The addition of naloxone in the Suboxone® product is intended to block the euphoric high resulting from the injection of this drug by non-buprenorphine maintained narcotic abusers.

Like other opioids commonly abused, buprenorphine is capable of producing significant euphoria. Data from other countries indicate that buprenorphine has been abused by various routes of administration (sublingual, intranasal and injection) and has gained popularity as a heroin substitute as well as a primary drug of abuse. Large percentages of the drug abusing populations in some areas of France, Ireland, Scotland, India and New Zealand have reported abusing buprenorphine often by injection and often in combination with a benzodiazepine. However, there is almost no data regarding the abuse of buprenorphine in the United States.

In countries where buprenorphine has gained popularity as a drug of abuse, it is sought by a wide variety of narcotic abusers: young drug naïve individuals, non-addicted opioid abusers, heroin addicts and buprenorphine treatment clients.

Buprenorphine and all products containing buprenorphine are controlled in Schedule III of the Controlled Substances Act.