Buprenorphine chemical structure
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Suboxone

Buprenorphine, also colloquially referred to as bupe, 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, yet is now primarily used for the treatment of opioid addiction. It is a Schedule III drug under the Convention on Psychotropic Substances. more...

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Commercial preparations

Britsh 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 (lemon-lime flavored sublingual, no active additives; in 2mg and 8mg dosages) and Suboxone (orange-tang flavored sublingual, one part naloxone for every four parts buprenorphine; hexagon shaped tablet in 2mg and 8mg dosages). Suboxone contains 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. It must also be noted that buprenorphine in and of itself will induce a precipitated withdrawal syndrome if ingested by an acutely opioid dependant/intoxicated individual.

Buprenorphine is also delivered transdermally in 25, 50 and 75 mcg/hour. The trade name in the UK is Transtec, and manufactured by Napp. A new 5, 10 and 20 mcg/hour patch marketed as Bu'7rans (Bu-trans), where the 7 indicates its once weekly dosage for pain in osteoarthritis.

Pharmacology and pharmacokinetics

Buprenorphine is a thebaine derivative, and its analgesic effect is due to partial agonist activity at μ-opioid receptors. Buprenorphine is also a κ-opioid receptor antagonist. The partial agonist activity means that opioid receptor antagonists (e.g., an antidote such as naloxone) only partially reverse the effects of buprenorphine.

Buprenorphine hydrochloride is administered by intramuscular injection, intravenous infusion, via a transdermal patch, or as a sublingual tablet. It is not administered orally, due to very high first-pass metabolism. Buprenorphine is metabolised by the liver, via the CYP3A4 isozyme of the cytochrome p450 enzyme system, into norbuprenorphine (by N-dealkylation) and other metabolites. The metabolites are further conjugated with glucuronic acid and eliminated mainly through excretion into the bile. The elimination half-life of buprenorphine is 20.4–72.9 hours (mean 34.6).

Clinical use

Buprenorphine is indicated for the treatment of moderate to severe pain, peri-operative analgesia, and opioid dependence. It has a longer duration of action than morphine, and sublingual tablets offer an analgesic effect for 6 to 8 hours. (Joint Formulary Committee, 2004) Australian guidelines recommend against the use of buprenorphine as an analgesic because: its effect is not reversed by naloxone, it may precipitate withdrawal symptoms in people dependent on other opioids, and it may cause dependence itself and has potential for misuse. (Rossi, 2005) When used for opioid dependence, buprenorphine remains effective in the body for up to 48 hours, curbing withdrawal symptoms and counteracting other opioids that may be administered to the patient (licitly or illicitly).

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Treating Addiction with Drugs - methadone and naltrexone
From Townsend Letter for Doctors and Patients, 7/1/01 by Jule Klotter

Drug and alcohol addictions target the pleasure areas of the brain. With long-term use, brain chemistry changes. The number of dopamine receptors in the these pleasure areas decreases, and more stimulation is needed in order to feel normal. In an attempt to address this altered biochemistry, other drugs, considered less harmful, are available to help treat heroin and alcohol addictions. No drugs have yet been developed that can block the activity of cocaine and methamphetamine.

For heroin addicts, methadone, a synthetic addictive drug, is available through specially-licensed treatment facilities. Like heroin, methadone attaches to mu receptors, resulting in a decrease in the transmission of pain signals and an increase in dopamine. It has a milder and longer lasting effect than heroin, however, and can be taken orally. According to Newsweek reporter Geoffrey Cowley, "...addicts in methadone programs are more likely to have jobs, less likely to commit crimes and less prone to HIV infection."

In contrast to methadone, which has a similar effect to heroin, the prescription drug naltrexone (Revia) prevents heroin from attaching to mu receptors, sending active drug users who take it, abruptly into withdrawal. Naltrexone is primarily used by former users to prevent a relapse. The FDA is expected to approve a new drug, buprenorphine, that has the same effect as a very low dose of methadone. Buprenorphine does not cause an intoxicating high, even at high doses. Reckitt Benckiser Pharmaceuticals (Richmond, Virginia) wants to sell it as Suboxone, an under-the-tongue-lozenge available by prescription.

The FDA is also reviewing a pill currently used in Europe to treat alcoholism, called acamprosate. The National Institute on Alcohol Abuse and Alcoholism (NIAAA) is studying the effect of acamprosate when it used in combination with the anti-craving pill naltrexone and with counseling. The drugs are being viewed merely as an aid for alcoholics who are already motivated to quit drinking; no one views them as a cure.

Ibogaine, a botanical hallucinogen that is illegal in the US, is being used elsewhere to treat many addictions. Unlike the pharmaceuticals mentioned, ibogaine is taken once to ease withdrawal and to help addicts shift their view of themselves and their lives. Deborah Mash, a neuropharmacologist at the University of Miami, has studied ibogaine's use at the Healing Visions Institute for Addiction Recovery on St. Kitts in the West Indies for five years. Writer Geoffrey Cowley quotes Mash as saying: "It doesn't work for everyone...but for detox from opiates it's a slam dunk." People with cocaine and alcohol addictions have also reported benefits.

"New Ways to Stay Clean" by Geoffrey Cowley. Newsweek, February 12, 2001

"Can This Pill Stop You from Hitting the Bottle?" by Claudia Kalb. Newsweek, February 12, 2001

COPYRIGHT 2001 The Townsend Letter Group
COPYRIGHT 2001 Gale Group

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