In vivo activity of bupropion at the human dopamine transporter as measured by positron emission tomography

Learned-Coughlin, Susan; Bergström, Mats; Savitcheva, Irina; Ascher, John; Schmith, Virginia D.; Långström, Bengt

doi:10.1016/s0006-3223(02)01834-6

Cited by 157 publications

(98 citation statements)

References 22 publications

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“…For example, bupropion does not inhibit prolactin, which would be expected if it significantly increases central DA (Whiteman et al, 1983). Moreover, therapeutic doses of bupropion have been reported to produce just 25% occupancy of the DA transporter (Learned-Coughlin et al, 2003), which may be inadequate to account for alterations to methamphetamine-induced DA release (Dworkin et al, 1998). Finally, other data suggest that stimulants (including methamphetamine) release norepinepherine (NE) more potently than DA (Rothman et al, 2001), and this neurotransmitter system may be responsible for some of the subjective effects reported in the current study.…”

Section: Discussionmentioning

confidence: 68%

Bupropion Reduces Methamphetamine-Induced Subjective Effects and Cue-Induced Craving

Newton

Roache

Garza

et al. 2005

Neuropsychopharmacol

141

126

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Bupropion is an antidepressant with stimulant properties, which inhibits the reuptake of dopamine (DA) and norepinepherine, and is purported to enhance DA neurotransmission. Bupropion is considered an appealing candidate medication for the treatment of methamphetamine dependence. The current laboratory study was set forth to assess the impact of bupropion treatment on the subjective effects produced by methamphetamine in the laboratory. We also assessed the effects of bupropion treatment on craving elicited by exposure to videotaped methamphetamine cues. A total of 26 participants were enrolled and 20 completed the entire study (n ¼ 10 placebo and n ¼ 10 bupropion, parallel groups design). Bupropion treatment was associated with reduced ratings of 'any drug effect' (po0.02), and 'high' (po0.02) following methamphetamine administration. There was also a significant bupropion-by-cue exposure interaction on General Craving Scale total score (po0.002), and on the Behavioral Intention subscale (po0.001). Overall, the data reveal that bupropion reduced acute methamphetamine-induced subjective effects and reduced cue-induced craving. Importantly, these data provide a rationale for the evaluation of bupropion in the treatment of methamphetamine dependence.

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Section: Discussionmentioning

confidence: 68%

Bupropion Reduces Methamphetamine-Induced Subjective Effects and Cue-Induced Craving

Newton

Roache

Garza

et al. 2005

Neuropsychopharmacol

141

126

View full text Add to dashboard Cite

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“…For some targets, it is possible that a minimal occupancy may still be important. For example, the average occupancy reported for bupropion at the DAT is 14%, a level frequently not detectable, [10][11][12]41 yet DA reuptake inhibition is still considered an important therapeutic aspect of bupropion. However, the data available to interpret the minimal MAO-A occupancy differ: not only is the MAO-A occupancy of St. John's wort nonsignificant and minimal, but it is also tremendously lower than that of moclobemide.…”

Section: Discussionmentioning

confidence: 99%

“…For example, the 5-HTT occupancy of SSRIs is 80% during steady-state treatment of MDD, 6,7,9 and the dopaminergic transporter (DAT) occupancy of bupropion is 14% during steady-state treatment of MDD. [10][11][12] Despite the use of MAO inhibitors to treat MDD for over 40 years, the percentage of MAO-A sites occupied by MAO-A inhibitors during the treatment of major depressive episodes is still unclear.…”

Section: Introductionmentioning

confidence: 99%

Monoamine oxidase A inhibitor occupancy during treatment of major depressive episodes with moclobemide or St. John’s wort: an [¹¹C]-harmine PET study

Sacher

Houle

Parkes

et al. 2011

jpn

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“…Indeed, the effects of bupropion sustained-release (SR), the only approved non-nicotinic medication, are thought to be mediated by dopaminergic mechanisms such as by blocking the reuptake of dopamine. [20][21][22][23] While several placebocontrolled trials of bupropion SR for smoking cessation have demonstrated its efficacy to promote smoking cessation 21,24,25 and a recent field trial has also shown the effectiveness of bupropion in actual practice, 26,27 only a minority of smokers treated with bupropion SR quit smoking for clinically meaningful periods (approximately 25-30% at 1 year follow-up).…”

Section: Introductionmentioning

confidence: 99%

Dopamine receptor DRD2 genotype and smoking cessation outcome following treatment with bupropion SR

et al. 2004

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The A1 allele of the dopamine D2 receptor gene (DRD2) is associated with a reduced number of dopamine binding sites in the brain and with the increased likelihood of substance abuse and addictive behavior. In a study of smokers enrolled in an open-label, randomized effectiveness trial, we investigated whether variants in the DRD2 receptor gene are associated with smoking cessation outcomes following treatment with a combination of bupropion SR and behavioral counseling. Adherence to treatment and pointprevalent smoking status were assessed at 3 and 12 months, respectively, following a target quit date. Compared to women who carry both A2 alleles, women with at least one A1 allele were more likely to report having stopped taking bupropion due to medication side effects (odds ratio (OR) ¼ 1.91, 95% confidence interval (CI) ¼ 1.01-3.60; Po0.04) and at 12 months were somewhat more likely to report smoking (OR ¼ 0.76, 95% CI ¼ 0.56-1.03; Po0.076). Significant associations or trends were not observed in men. In women, individual variability in responsiveness to bupropion-based treatment may be partially due to differences in genetic variants influencing dopamine receptor function. INTRODUCTIONTobacco use remains the major preventable cause of premature disability and death in developed countries. Despite best efforts to date, 46 million people still smoke in the United States, and over 440 000 people die each year from tobaccorelated illness; the estimated smoking-related cost to the economy is $157 billion annually.1 Effective pharmacologic interventions for smoking cessation include several forms of nicotine replacement and the use of the antidepressant medication, bupropion.2 Despite treatment advances, smoking relapse after successful intervention for smoking cessation occurs in 70 to 80% of patients within 12 months. [3][4][5] Still to be determined is why some people remain nonsmokers after pharmacologic intervention and others do not.The dopaminergic mesocorticolimbic pathway in the brain is thought to play an important role in tobacco and nicotine addiction. [6][7][8] The TaqIA polymorphism of the dopamine D2 receptor gene (DRD2) results from a C/T

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In vivo activity of bupropion at the human dopamine transporter as measured by positron emission tomography

Cited by 157 publications

References 22 publications

Bupropion Reduces Methamphetamine-Induced Subjective Effects and Cue-Induced Craving

Bupropion Reduces Methamphetamine-Induced Subjective Effects and Cue-Induced Craving

Monoamine oxidase A inhibitor occupancy during treatment of major depressive episodes with moclobemide or St. John’s wort: an [¹¹C]-harmine PET study

Dopamine receptor DRD2 genotype and smoking cessation outcome following treatment with bupropion SR

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In vivo activity of bupropion at the human dopamine transporter as measured by positron emission tomography

Cited by 157 publications

References 22 publications

Bupropion Reduces Methamphetamine-Induced Subjective Effects and Cue-Induced Craving

Bupropion Reduces Methamphetamine-Induced Subjective Effects and Cue-Induced Craving

Monoamine oxidase A inhibitor occupancy during treatment of major depressive episodes with moclobemide or St. John’s wort: an [11C]-harmine PET study

Dopamine receptor DRD2 genotype and smoking cessation outcome following treatment with bupropion SR

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Monoamine oxidase A inhibitor occupancy during treatment of major depressive episodes with moclobemide or St. John’s wort: an [¹¹C]-harmine PET study