Bupropion chemical structure
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Bupropion (amfebutamone) is an antidepressant of the amino ketone class, chemically unrelated to tricyclics or selective serotonin reuptake inhibitors (SSRIs). It is similar in structure to the stimulant cathinone, and to phenethylamines in general. It is a chemical derivative of diethylpropion, an amphetamine-like substance used as an anorectic. Bupropion is both a dopamine reuptake inhibitor and a norepinephrine reuptake inhibitor. more...

Zoledronic acid


Bupropion was first synthesized by Burroughs Research in 1966, and patented by Burroughs-Wellcome (later Glaxo-Wellcome, and, as of 2000, GlaxoSmithKline) in 1974. It was approved by the FDA in 1985 and marketed under the name Wellbutrin as an antidepressant, but clinical trials indicated that incidence of seizure was two to four times greater than other antidepressants and the drug was quickly pulled from the market. It was subsequently discovered that reducing the dose by about half greatly reduced the risk of seizures. Glaxo then developed a sustained-release (SR) version of Wellbutrin which releases bupropion hydrochloride at a slower rate. The SR formulation is taken twice a day, in order to further decrease the possibility of adverse side effects and seizures. It is also available in generic form (Bupropion SR). Extended Release bupropion, Wellbutrin XL, is the most recent formulation of bupropion and is taken orally once a day. Because of this altered mechanism of delivery and reduced dosing, incidence of seizures with bupropion is comparable to, and in some cases, lower than that of other antidepressants.

In 1997, bupropion HCl was approved by the FDA for use as a smoking cessation aid. Glaxo subsequently marketed the drug under the name Zyban to help people stop smoking tobacco by reducing the severity of craving and addiction/withdrawal symptoms. It can be used in combination with nicotine replacement therapies. Bupropion treatment course lasts for seven to twelve weeks, with the patient halting the use of tobacco around ten days into the course.

Bupropion is also being investigated as a weight loss drug.

Mode of action

Bupropion is a selective catecholamine (norepinephrine and dopamine) reuptake inhibitor. It has only a small effect on serotonin reuptake. It does not inhibit MAO. The actual mechanism behind bupropion's action is not known, but it is thought to be due to the effects on dopaminergic and noradrenergic mechanisms.


Bupropion is metabolised in the liver. It has at least three active metabolites: hydroxybupropion, threohydrobupropion and erythrohydrobupropion. These active metabolites are further metabolised to inactive metabolites and eliminated through excretion into the urine. The half-life of bupropion is 20 hours as is hydroxybupropion's. Threohydrobupropion's half-life is 37 hours and erythrohydrobupropion's 33 hours.

Chronic hepatotoxicity in animals

In rats receiving large doses of bupropion chronically, there was an increase in incidence of hepatic hyperplastic nodules and hepatocellular hypertrophy. In dogs receiving large doses of bupropion chronically, various histologic changes were seen in the liver, and laboratory tests suggesting mild hepatocellular injury were noted.

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The surprising truth about addiction: more people quit addictions than maintain them, and they do so on their own. That's not to say it happens overnight.
From Psychology Today, 5/1/04 by Stanton Peele

Change is natural. You no doubt act very differently in many areas of your life now compared with how you did when you were a teenager. Likewise, over time you will probably overcome or ameliorate certain behaviors: a short temper, crippling insecurity:

For some reason, we exempt addiction from out beliefs about change. In both popular and scientific models, addiction is seen as locking you into an inescapable pattern of behavior. Both folk wisdom, as represented by Alcoholics Anonymous, and modern neuroscience regard addiction as a virtually permanent brain disease. No matter how many years ago your uncle Joe had his last drink, he is still considered an alcoholic. The very word addict confers an identity that admits no other possibilities. It incorporates the assumption that you can't, or won't, change.

But this fatalistic thinking about addiction doesn't jibe with the facts. More people overcome addictions than do not. And the vast majority do so without therapy. Quitting may take several tries, and people may hOt stop smoking, drinking or using drugs altogether. But eventually they succeed in shaking dependence.

Kicking these habits constitutes a dramatic change, but the change need not occur in a dramatic way. So when it comes to addiction treatment, the most effective approaches rely on the counterintuitive principle that less is often more. Successful treatment places the responsibility for change squarely on the individual and acknowledges that positive events in other realms may jump-start change.

Consider the experience of American soldiers returning from the war in Vietnam, where heroin use and addiction was widespread. In 90 percent of cases, when GIs left the pressure cooker of the battle zone, they also shed their addictions--in vivo proof that drug addiction can be just a matter of where in life you are.

Of course, it took more than a plane trip back from Asia for these men to overcome drug addiction. Most soldiers experienced dramatically altered lives when they returned. They left the anxiety, fear and boredom of the war arena and settled back into their home environments. They returned to their families, formed new relationships, developed work skills.

Smoking is at the top of the charts in terms of difficulty of quitting. But the majority of ex-smokers quit without any aid--neither nicotine patches nor gum, Smokenders groups nor hypnotism. (Don't take my word for it; at your next social gathering, ask how many people have quit smoking on their own.) In fact, as many cigarette smokers quit on their own, an even higher percentage of heroin and cocaine addicts and alcoholics quit without treatment. It is simply more difficult to keep these habits going through adulthood. It's hard to go to Disney World with your family while you are shooting heroin. Addicts who quit on their own typically report that they did so in order to achieve normalcy.

Every year, the National Survey on Drug Use and Health interviews Americans about their drug and alcohol habits. Ages 18 to 25 constitute the peak period of drug and alcohol use. In 2002, the latest year for which data are available, 22 percent of Americans between ages 18 and 25 were abusing or were dependent on a substance, versus only 3 percent of those aged 55 to 59. These data show that most people overcome their substance abuse, even though most of them do not enter treatment.

How do we know that the majority aren't seeking treatment? In 1992, the National Institute on Alcohol Abuse and Alcoholism conducted one of the largest surveys of substance use ever, sending Census Bureau workers to interview more than 42,000 Americans about their lifetime drug and alcohol use. Of the 4,500-plus respondents who had ever been dependent on alcohol, only 27 percent had gone to treatment of any kind, including Alcoholics Anonymous. In this group, one-third were still abusing alcohol.

Of those who never had any treatment, only about one-quarter were currently diagnosable as alcohol abusers. This study, known as the National Longitudinal Alcohol Epidemiologic Survey, indicates first that treatment is not a cure-all, and second that it is not necessary. The vast majority of Americans who were alcohol dependent, about three-quarters, never underwent treatment. And fewer of them were abusing alcohol than were those who were treated.

This is not to say that treatment can't be useful. But the most successful treatments are nonconfrontational approaches that allow self-propelled change. Psychologists at the University of New Mexico led by William Miller tabulated every controlled study of alcoholism treatment they could find. They concluded that the leading therapy was barely a therapy at all but a quick encounter between patient and health-care worker in an ordinary medical setting. The intervention is sometimes as brief as a doctor looking at the results of liver-function tests and telling a patient to cut down on his drinking. Many patients then decide to cut back--and do!

As brief interventions have evolved, they have become more structured. A physician may simply review the amount the patient drinks, or use a checklist to evaluate the extent of a drinking problem. The doctor then typically recommends and seeks agreement from the patient on a goal (usually reduced drinking rather than complete abstinence). More severe alcoholics would typically be referred out for specialized treatment. A range of options is discussed (such as attending AA, engaging in activities incompatible with drinking or using a self-help manual). A spouse or family member might be involved in the planning. The patient is then scheduled for a future visit, where progress can be checked. A case monitor might call every few weeks to see whether the person has any questions or problems.

The second most effective approach is motivational enhancement, also called motivational interviewing. This technique throws the decision to quit or reduce drinking--and to find the best methods for doing so--back on the individual. In this case, the therapist asks targeted questions that prompt the individual to reflect on his drinking in terms of his own values and goals. When patients resist, the therapist does not argue with the individual but explores the person's ambivalence about change so as to allow him or her to draw his own conclusions: "You say that you like to be in control of your behavior, yet you feel when you drink you are often not in charge. Could you just clarify that for me?"

Miller's team round that the list of most effective treatments for alcoholism included a few more surprises. Self-help manuals were highly successful. So was the community-reinforcement approach, which addresses the person's capacity to deal with life, notably marital relationships, work issues (such as simply getting a job), leisure planning and social-group formation (a buddy might be provided, as in AA, as a resource to encourage sobriety). The focus is on developing life skills, such as resisting pressures to drink, coping with stress (at work and in relationships) and building communication skills.

These findings square with what we know about change in other areas of life: People change when they want it badly enough and when they feel strong enough to face the challenge, not when they're humiliated or coerced. An approach that empowers and offers positive reinforcement is preferable to one that strips the individual of agency. These techniques are most likely to elicit real changes, however short of perfect and hard-won they may be.

Calling It Quits

Jason Peteda, 26, musician

I did $300-$400 of crystal meth a day. from 1994 to 1999. I raved with friends. After two years, I went to rehab. But the day I left, I got high. In the summer of 1997 I overdosed and my heart stopped. In December 1999 I woke up in a hospital. I figured I wasn't going to wake up a third time. I met a girl who wasn't into partying or drugs. I separated myself from my former friends, quit my job, changed my phone number and locked myself in my house. I fooled a lot of people those years. I mode those choices. I have to live with it,

Gene Light, 73, retired art director

After four packs a day for 46 years, I stopped because I couldn't stand the plane ride from New York to California to visit my grandkids. I still miss smoking, I know if I tried a cigarette, I would be right back to four pocks a day.

Robin Aigner, 35, copy editor/musician

I wanted to quit smoking before I was 30. But as I approached 31 and couldn't stop, I knew I'd need a huge incentive. I got on my bike to train for the Boston-New York AIDS Ride. I was nervous about quitting and thought I needed chemical support to quit, so I took Zyban. But I stopped because it gave me insomnia, I thought about cigarettes every second of every day for a month. I knew I never wanted to go through the process of qutting again. But doing it changed my life and opened a lot of doors. I felt accomplished and powerful. And I became a musician.

Thor Spangler 45, occupational therapist

I worked in a bar where coke was readily available, and I snorted it every night. I also downed five or six tequilas and smoked a pack a day. My wife was an alcoholic with her own chemical dependencies. It was hard to break free of my habits around her. After we, broke up, in the spring of 2001, I got away from the bar scene, I went back to school. And I remarried. Although I quit before I met my second wife, I would risk losing her if I relapsed. Falling in love saved my life.

Six Principles of Change

One The belief that you can change is the key to change. This is not the powerlessness message of the 12 steps but rather the message of self-efficacy. Addictions are really no different from other behaviors--believing you can change encourages commitment to the process and enhances the likelihood of success.

Two The type of treatment is less critical than the individual's commitment to change. People tan select how they want to pursue change in line with their own values and preferences. They don't need co be told now to change.

Three Brief treatments can change longstanding habits, It is not the duration of the treatment that allows people to change but rather its ability to inspire continued efforts in that direction,

Four Life skills can be the key to licking addiction. All addictions may not be equal; the community-reinforcement approach, with its emphasis on developing life skills, might be needed for chose more severely debilitated by drugs and alcohol.

Five Repeated efforts are critical to changing. People do not often get better instantly--it usually takes multiple efforts. Providing follow-up care allows people to maintain focus on their change goals, Eventually, they stand a good chance of achieving them.

Six Improvement, without abstinence, counts. People do not usually succeed all at once. But they can show significant improvements; and all improvement should be accepted and rewarded. It is counter-productive to kick people out of therapy for failing to abstain The therapeutic approach of recognizing improvement in the absence of abstinence is called harm reduction.

Psychologist Stanton Peele first wrote about addiction in the classic book Love and Addiction (with Archie Brodsky) in 1975. This summer, his latest book, 7 Tools to Beat Addiction, will be published by Random House/Three Rivers Press.

"Calling It Quits" by Neil Parmar, Jammie Salagubong and Susan A. Smith

COPYRIGHT 2004 Sussex Publishers, Inc.
COPYRIGHT 2004 Gale Group

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