Buprenorphine chemical structure
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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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Enslaved to painkillers: addiction to prescription drugs such as OxyContin and Percocet is a growing crisis nationwide, including among lesbians and gay
From Advocate, The, 8/30/05 by Alan Sverdlik

It is a typical morning in the kitchen of Ramona's railroad flat in suburban Atlanta: a pot of decaf coffee, oat bran muffins, and Percocet. Ramona (not her real name) washes down three of the oval, chalky, off-white pain pills with coffee and closes her eyes. This 42-year-old lesbian mother of two becomes suddenly animated and friendly. She shakes the prescription bottle. "this is my love. This is my life. I'll take this drug till the day I die," she says, hastening that day one tablet at a time.

There are at least two potentially lethal effects of long-term painkiller use. The drugs can significantly weaken or destroy the liver. And abrupt disruption of opiate use can send the body into shock, which is potentially lethal.

Painkiller addiction has arrived, big-time, among gays and lesbians. Lisa Kiebzak, who runs a substance abuse program serving people with HIV in St. Petersburg, Fla., says many of her GLBT clients use opiates such as Percocet, Vicodin, and OxyContin to heal psychological wounds. "What I see in the gay community today is what we've seen for a long time: a lot of people medicating themselves from their pasts, their presents, and their futures," says Kiebzak, who works for the nonprofit Metropolitan Charities.

While the battle against the destructive allure of crystal meth addiction has energized gay activists nationwide, the abuse of legal painkillers poses a growing threat, experts say, largely because they're relatively cheap and available, and the addiction is much harder to overcome. "If you step taking opiates [cold], you go into withdrawal," Kiebzak says. "It can be fatal."

The Substance Abuse and Mental Health Services Administration estimates that almost a quarter of Americans age 18 to 25 take painkillers recreationally, with a 40% jump in abuse of oxycodone (the generic name for OxyContin) from 2002 to 2003. The jump was 60% among adults 26 and older.

Jeff, a 38-year old out bartender, thought he was on the road to recovery when he gave up the late-night party scene and its troika of pleasures: crystal meth, special K, and anonymous sex. But a bad traffic accident sent him to the hospital for a month, and there he was given OxyContin and Demerol. He was hooked. Even after he healed, "I couldn't get out of bed without downing a couple [of pills]," says Jeff (also a pseudonym). "No matter how many drugs I had done in the past, none of them put me in the gutter the way these did. I kept taking them all day, no matter what the [prescription] called for. At last count I was up to 14."

Heroin is the purest form of this class of drugs, which are derived from the Asian poppy. Collectively called opiates, the drugs--including Lortab and Dilaudid--touch receptors in the brain that both block pain and produce euphoria. There are many legitimate uses for the painkillers, particularly among people with painful AIDS complications such as neuropathy.

But addiction, she adds, grows less from physical pain than from psychological challenges. Even with better HIV treatments, "there are still inner conflicts," including the conflicts over mortality that plagued people with AIDS in the 1980s. "They're afraid to plan for and create a future, afraid not to give up. So they got careless and start having unsafe sex and using dangerous drugs."

Ramona, who divorced and came out after an abusive eight-year marriage, discovered painkillers while being treated by an orthopedic surgeon for herniated discs. She had never dabbled with recreational drugs before, she says. On a vacation with her girlfriend, she popped one of her remaining Percocets on a whim.

"We were sitting on the beach in Acapulco, and I felt this wave of good feeling come over me," she says. "I truly didn't connect the feeling with the drug. By the end of the trip, I was up to two, three at breakfast. I came home to Georgia with a couple left, and the only thing I could think of was how to get some more." She convinced another physician to prescribe Percocet for back pain, and then another. "I was up to six a day that first month," she says. "That's what it was taking to keep the high going."

When her supply ran out and the doctors refused to refill it, withdrawal set in. It's like "the flu times 50," says James Berman, MD, an addiction medicine specialist near Philadelphia. "Runny eyes, runny nose, goose bumps, simultaneous sweats and chills, cramp-like symptoms."

"I couldn't get out of bed," remembers Ramona, whose prominent cheek bones and black locks reflect her partially Cherokee ancestry. "I was sweating so profusely that the sheets and the pillowcases were soaked. I made up an excuse that I had some bad new strain of the flu, and my lover took the kids over to her house for the weekend. I had no energy, no concentration, no will. I just wanted to stay in bed in a fetal position and never come out."

After three days of hell, Ramona finally scored Vicodin from an online pharmacy, paying a $130 consultation fee plus $160 for a month's supply. Then she did the same on a second site. Having gone through withdrawal, Ramona says, "I could be on this stuff my whole life."

"Opiates are the most addictive substances in the world. Tobacco is number 2," says Jennie Leyva-Jones, administrator of Lanier Treatment Center, an opiate rehabilitation clinic north of Atlanta. "We had a woman withdrawing from Lortab go into seizures. She was sprawled on the bathroom floor, unable to get up."

Having hit bottom, Jeff sought help at a chemical dependency treatment facility that uses group therapy along with sedatives, blood pressure medicine, and antidepressants to ease withdrawal. But the cravings continued after he completed the program.

Then some patrons at his bar told Jeff about buprenorphine, sold as Subexone and Subutex. A physician prescribed him two a day, and the withdrawal quickly eased off. "I had tried everything to stay off the pills, but nothing worked except this," Jeff says. "I act and feel normal. It's been a godsend."

Buprenorphine pries opiates from receptors in the brain and provides users with a mild high, says Aaron Hurowitz, DO, an addiction medicine specialist in Atlanta. It's a narcotic and controlled substance--doctors must complete a training course and apply for a waiver to prescribe it--and it may cost $12 or more a day. But it's "much less addictive" than opiates, Hurowitz says.

Ramona runs a cleaning service out of her apartment and is free to take drugs at will. Her lover, who shares her stash, can't tolerate large doses of Percocet, so there's plenty for both, she says.

As far as her girls, 10 and 12, are concerned, they spend most of their time with their father, who has primary custody. She's been able to keep her habit from them. Her run with Percocet is now approaching a year, she says. "I know I'll get off of them one day," she says. "I don't know how far off that day is."

Sverdlik is a freelance writer based in Georgia.

COPYRIGHT 2005 Liberation Publications, Inc.
COPYRIGHT 2005 Gale Group

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