|
Drugs and Chemicals of
Concern > Buprenorphine
BUPRENORPHINE
(Trade Names: Buprenex®, Suboxone®, Subutex®)
June 2006
DEA/OD/ODE
Introduction:
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.
Licit Uses:
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.
Chemistry/Pharmacology:
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.
Illicit Uses:
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.
User Population:
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.
Control Status:
Buprenorphine and all products containing
buprenorphine are controlled in Schedule III of the Controlled Substances Act.
Comments and additional information are welcomed by the Drug and Chemical
Evaluation Section, FAX 202-353-1263 or telephone 202-307-7183.
|