• The Korean Journal of Pain
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• v.27 no.2
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• pp.118-124
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• 2014

Background: The chronic pain can disturb physical, psychological, and social performances. Analgesic agents are widely used but some antidepressants (ADs) showed analgesia also. Bupropion is using for smoke cessation but it can change morphine withdrawal signs such as pain. This study tested the acute systemic effect of bupropion on formalin induced pain behavior in rats. Methods: Wistar male healthy rats were divided into 7 groups (control, sham, and 5 treated groups with 10, 30, 90, 120, and 200 mg/kg of bupropion, i.p.). The bupropion injected 3 hours prior to formalin induced pain behavior. Formalin (50 ${\mu}l$, 2.5%) was injected subcutaneously in dorsal region of right hindpaw in all animals. Nociceptive signs were observed continuously on-line and off-line each minute. Common pain scoring was used for pain assessment. Results: The analysis of data by one-way ANOVA showed that bupropion can reduce pain scores in the second phase but not in first phase. Bupropion decreased the licking/biting duration significantly in first and second phase of formalin test. Conclusions: The results showed that bupropion has analgesic effects at systemic application. The change of second phase of the pain behavior was significant and it revealed that central mechanisms involve in bupropion analgesia.

• Anxiety and mood
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• v.13 no.2
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• pp.66-73
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• 2017

Objective : The purpose of this study was to examine the effects of adjunctive aripiprazole versus bupropion on specific symptoms of depression. Methods : Data were from 6-week, randomized, prospective, open-label multi-center study in 103 patients with major depressive disorders. Participants were randomized to receive aripiprazole (2.5-10 mg/day) or bupropion (150-300 mg/day) for 6 weeks. Change in four subscales of the 17-item Hamilton Depression Rating Scale (HAM-D17) that capture core depression symptoms was determined, and change in individual HAM-D17 items was also assessed. Changes in three composite subscales-anxiety, insomnia, and drive were also examined. Results : Within-group change in the four core subscales was large [effect size (ES)=1.30-1.47] and it was similar to that in the HAM-D17 total score. Differences between aripiprazole and bupropion were significant for each of the four core subscales and the HAM-D17 total score favored aripiprazole (p<0.001). On three composite scales, both treatments caused substantial changes in anxiety (within-group ES=1.10 (aripiprazole) vs. 1.00 (bupropion)], insomnia (ES=0.75 vs 0.50), and drive (ES=1.17 vs 1.15). Conclusion : This results suggested that both aripiprazole and bupropion adjunctive therapies with selective serotonin reuptake inhibitors resulted in significant and clinically meaningful changes in core symptom subscales for depression.

• Archives of Obesity and Metabolism
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• v.1 no.2
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• pp.83-88
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• 2022

Obesity increases the risk of developing metabolic diseases such as hypertension, type 2 diabetes, hyperlipidemia, and cardiovascular diseases, as well as some cancers. To prevent the occurrence of these diseases and death, it is essential to manage obesity. Though there are several treatments for obesity, lifestyle interventions, such as diet and exercise, and drug therapy are most widely used in clinical practice. Among the anti-obesity drugs available, the weight loss effect of naltrexone/bupropion has been well-proven. We present a case study in which naltrexone/bupropion, a glucagon-like peptide-1 agonist, and a sodium-glucose transporter 2 inhibitor showed significant weight loss and improved metabolic parameters. Additionally, the management of type 2 diabetes and hypertension, which are common diseases in patients with obesity, was also included.

• Mood & Emotion
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• v.16 no.3
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• pp.140-151
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• 2018

Objectives : The purpose of this study was to examine effects of adjunctive aripiprazole versus bupropion, on depressive symptoms of female depression. Methods : Sixty six female patients with major depressive disorders were enrolled from a six-week, randomized prospective open-label multi-center study. Participants were randomized to receive aripiprazole (2.5-10 mg/day) or bupropion (150-300 mg/day). Montgomery Asberg Depression Rating Scale, 17-item Hamilton Depression Rating scale (HAM-D17), Iowa Fatigue Scale, Drug-Induced Extrapyramidal Symptoms Scale, Psychotropic-Related Sexual Dysfunction Questionnaire scores, and Clinical Global Impression-Severity (CGI-S) were obtained at baseline and after one, two, four, and six weeks. Changes on individual items of HAM-D17 were assessed as well as on composite scales (anxiety, insomnia and drive), and on four core subscales that capture core depression symptoms. Results : Overall, both treatments improved depressive symptoms, without causing serious adverse events. There were significant differences in the HAM-D17 total score (p=0.046) and CGI-S (p=0.004), between aripiprazole and bupropion augmentation, favoring aripiprazole over bupropion. Aripiprazole revealed significantly greater effect size in depressed mood (p=0.006), retardation (p=0.005), anxiety psychic (p=0.032), and general somatic symptom (p=0.01). Conclusion : While both treatments were effective, results of this study suggested that aripiprazole may be preferable, in treating general and core symptoms of female depression.

• Journal of Pharmaceutical Investigation
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• v.40 no.5
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• pp.313-319
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• 2010

The objectives of this study were to evaluate the effect of formulation ingredients on the drug release and to optimize the novel sustained release matrix tablet formulations of bupropion hydrochloride. A three factor, three-level Box-Behnken design was used for the optimization procedure, with the amounts of PEO ($X_1$), citric acid ($X_2$) and Compritol 888 ATO ($X_3$) as the independent variables. The selected dependent variables were the cumulative percentage values of bupropion hydrochloride that had dissolved after 1, 4 and 8 hr. Various dissolution profiles of the drug from sustained release matrix tablets were obtained. Optimization was performed for $X_1$, $X_2$ and $X_3$ using the following target ranges; $30%{\leq}Y_1{\leq}45%$; $70{\leq}Y_2{\leq}85%$; $85%{\leq}Y_3{\leq}100%$. The optimized formulation for bupropion hydrochloride was achieved with 12.5% PEO ($X_1$), 2.5% citric acid ($X_2$) and 10% Compritol 888 ATO ($X_3$). The sustained release matrix tablets with the optimized formulation provided a release profile that was close to predicted values. In addition, the dissolution profiles of the sustained release matrix tablet with the optimized formulation were similar to those of the commercial product Wellbutrin$^{(R)}$ SR tablets ($f_2$=79.83).

• Journal of the Korean Academy of Child and Adolescent Psychiatry
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• v.19 no.2
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• pp.72-82
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• 2008

The aim of this paper is to evaluate the use of non-stimulants, including atomoxetine, bupropion and modafinil, as alternative approaches to the treatment of children with attention-deficit hyperactivity disorder. A comprehensive review of the empirically based literature regarding the efficacy and the safety of the non-stimulants was performed. There is a large and increasing body of data supporting the efficacy and the safety of non-stimulants. Although the treatment effect sizes for non-stimulants may be smaller than those for stimulants, non-stimulants alone have been shown to be effective in the treatment of attention-deficit hyperactivity disorder as well as several comorbidities. These results suggest that non-stimulants are effective in the treatment of attention-deficit hyperactivity disorder. Further studies are needed to improve our understanding of alternative pharmacological medications in the treatment of attention-deficit hyperactivity disorder.

• Toxicological Research
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• v.33 no.1
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• pp.25-30
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• 2017

Saccharin, the first artificial sweetener, was discovered in 1879 that do not have any calories and is approximately 200~700 times sweeter than sugar. Saccharin was the most common domestically produced sweetener in Korea in 2010, and it has been used as an alternative to sugar in many products. The interaction between artificial sweeteners and drugs may affect the drug metabolism in patients with diabetes, cancer, and liver damage, this interaction has not been clarified thus far. Here, we examined the effects of the potential saccharin-drug interaction on the activities of 5 cytochrome P450 (CYPs) in male ICR mice; further, we examined the effects of saccharin (4,000 mg/kg) on the pharmacokinetics of bupropion after pretreatment of mice with saccharin for 7 days and after concomitant administration of bupropion and saccharin. Our results showed saccharin did not have a significant effect on the 5 CYPs in the S9 fractions obtained from the liver of mice. In addition, we observed no differences in the pharmacokinetic parameters of bupropion between the control group and the groups pretreated with saccharin and that receiving concomitant administration of saccharin. Thus, our results showed that saccharin is safe and the risk of saccharin-drug interaction is very low.

• Journal of Preventive Medicine and Public Health
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• v.51 no.5
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• pp.257-262
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• 2018

Objectives: Smoking cessation decreases morbidity and mortality due to chronic obstructive pulmonary disease (COPD). Pharmacotherapy for smoking cessation is highly effective. However, the optimal prescription rate of smoking cessation medications among smokers with COPD has not been systemically studied. The purpose of this study was to estimate the national prescription rates of smoking cessation medications among smokers with COPD and to examine any disparities therein. Methods: We conducted a retrospective study using National Ambulatory Medical Care Survey data from 2007 to 2012. We estimated the national prescription rate for any smoking cessation medication (varenicline, bupropion, and nicotine replacement therapy) each year. Multiple survey logistic regression was performed to characterize the effects of demographic variables and comorbidities on prescriptions. Results: The average prescription rate of any smoking cessation medication over 5 years was 3.64%. The prescription rate declined each year, except for a slight increase in 2012: 9.91% in 2007, 4.47% in 2008, 2.42% in 2009, 1.88% in 2010, 1.46% in 2011, and 3.67% in 2012. Hispanic race and depression were associated with higher prescription rates (odds ratio [OR], 5.15; 95% confidence interval [CI], 1.59 to 16.67 and OR, 2.64; 95% CI, 1.26 to 5.51, respectively). There were no significant differences according to insurance, location of the physician, or other comorbidities. The high OR among Hispanic population and those with depression was driven by the high prescription rate of bupropion. Conclusions: The prescription rate of smoking cessation medications among smokers with COPD remained low throughout the study period. Further studies are necessary to identify barriers and to develop strategies to overcome them.

• Korean Journal of Psychosomatic Medicine
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• v.22 no.2
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• pp.63-70
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• 2014

The prevalence of obesity and overweight is increasing in mood disorder, and it is connected to an increased cardiovascular mortality. Because of them, treatment for obesity may be an essential part of mood disorder treatment. Similar to the general population, non-pharmacological treatment such as correction of life habits should be considered first of all. If this approaches are fail, pharmacological treatment for obesity would be required as next step. Any drug for obesity is not approved officially in mood disorder. So approved drugs in general population, and drugs supported by several studies are prescribed in clinical settings. Several treatment guidelines for mood disorder and studies support that orlistat, metformin, topiramate and bupropion is effective and safe.

• Korean Journal of Biological Psychiatry
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• v.13 no.4
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• pp.252-259
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• 2006

Sexual dysfunction is a relatively common adverse effect in the use of antidepressants. The sexual side effects may result in a lack of compliance with the prescribed antidepressants. The author reviewed the prevalence and updated treatment for the antidepressant-induced adverse effects focusing on sexual dysfunction. The incidence of sexual dysfunction is reported to exceed more than 50% especially with SSRIs. In order to obtain a quantified baseline and as an ongoing evaluation tool, clinicians may use some of the established questionnaires and validated instruments such as the Arizona Sexual Experience scale and Changes in Sexual Functioning Questionnaire. Clinicians should be aware that delayed ejaculation and orgasm, symptoms most frequently associated with antidepressants, are not usually associated with depression itself. Although many antidotes have been proposed, few have been subjected to double-blind trials. Some evidences have suggested that bupropion and buspiron may be the effective antidotes for SSRI induced sexual dysfunction. Additional trials will be requied to define what role, if any, bupropion and buspiron might have in the treatment of SSRI-induced sexual side effects. The available evidence is rather limited, with only small number of trials assessing each strategy. While further randomized data is awaited, for men with antidepressant induced erectile dysfunction, the addition of sidenafil or tadalafil may appear to be an effective strategy.