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The American Journal of Drug and... Mar 2016Tobacco is the leading cause of preventable death in the world. Current cessation medications include nicotine replacement therapy (NRT), varenicline, and bupropion,... (Review)
Review
BACKGROUND
Tobacco is the leading cause of preventable death in the world. Current cessation medications include nicotine replacement therapy (NRT), varenicline, and bupropion, while combination therapy primarily entails NRT with either varenicline or bupropion. However, recent studies have examined varenicline and bupropion in combination.
OBJECTIVES
A systematic review assessing the efficacy and safety of combination varenicline and bupropion was conducted.
METHODS
PubMed and Clinicaltrials.gov were searched using terms: "varenicline combination", "bupropion combination", "bupropion AND varenicline", and "bupropion AND varenicline combination smoking cessation", yielding four studies including 1193 total patients.
RESULTS
Combination therapy yielded greater efficacy than varenicline monotherapy in two randomized controlled trials and one retrospective outcomes study. One single-arm Phase II trial provided additional efficacy and safety data. Of the prospective trials, one displayed a greater 4-week smoking abstinence for weeks 8-11 with combination (39.8%) versus monotherapy (25.9%) (OR = 1.89; 95% CI = 1.07-3.35). The other demonstrated greater prolonged abstinence (continuous abstinence from week 2) at 12 weeks (OR = 1.49; 95% CI = 1.05-2.12) and 26 weeks (OR = 1.52; 95% CI = 1.04-2.22), though results were not significant at 52 weeks in this study. The retrospective study displayed higher success rates (continuous abstinence rates at 52 weeks) with combination varenicline and bupropion (55.0%; compared to varenicline monotherapy (32.1%), p < 0.001). Subgroup analyses suggest that this combination may be more beneficial in males and patients with higher baseline nicotine dependence.
CONCLUSION
To the authors' knowledge, this is the first review conducted to compile current literature on this novel pharmacotherapy combination for smoking cessation. Combination bupropion SR and varenicline displayed greater efficacy in smoking cessation than varenicline monotherapy, though further safety analysis is warranted to rule out additive psychiatric adverse effects.
Topics: Bupropion; Delayed-Action Preparations; Drug Therapy, Combination; Humans; Smoking Cessation; Varenicline
PubMed: 26809272
DOI: 10.3109/00952990.2015.1117480 -
The Journal of Clinical Psychiatry Sep 1995The mechanism of action of the novel antidepressant bupropion remains unclear after many years of study. A review of the relevant biochemical, in vivo brain... (Review)
Review
BACKGROUND
The mechanism of action of the novel antidepressant bupropion remains unclear after many years of study. A review of the relevant biochemical, in vivo brain microdialysis, electrophysiologic, behavioral, and clinical data clarifies what is known about this unique compound and suggests possible modes of action.
METHOD
A panel of 11 experts was convened for a conference to discuss bupropion's mechanism of antidepressant activity. Four of the panelists presented current research findings, followed by a discussion.
RESULTS
(1) Biochemical studies suggest down-regulation of postsynaptic beta-adrenoceptors and desensitization of the norepinephrine-stimulated adenylate cyclase in the rat cortex occur only after chronic administration of very high doses of bupropion. (2) In vivo brain microdialysis studies demonstrate that, after chronic administration, there is an enhancement of bupropion-induced increases in extracellular dopamine in the nucleus accumbens. (3) Electrophysiologic data show that with acute dosing, bupropion reduces the firing rates of noradrenergic neurons in the locus ceruleus. The firing rates of dopaminergic neurons are reduced by bupropion in the A9 and A10 areas of the brain, but only at very high doses, and bupropion does not alter the firing rates of serotonergic neurons in the dorsal raphe. (4) Behavioral studies show that the most active metabolite of bupropion, hydroxybupropion (306U73), appears to be responsible for a large part of the compound's effects in animal models of antidepressant activity. (5) Clinical studies indicate that bupropion enhances noradrenergic functional activity as reflected by an increased excretion of the hydroxy metabolite of melatonin, while at the same time producing a presumably compensatory decrease in norepinephrine turnover. In one study, bupropion elevated plasma levels of the dopamine metabolite homovanillic acid in nonresponders, but not in responders.
CONCLUSION
The mechanism of action of bupropion appears to have an unusual, not fully understood, noradrenergic link. The bupropion metabolite hydroxybupropion probably plays a critical role in bupropion's antidepressant activity, which appears to be predominantly associated with long-term noradrenergic effects. The mild central nervous system activating effects of bupropion appear to be due to weak dopaminergic mechanisms. There is some evidence that dopamine may contribute to bupropion's antidepressant properties. Antidepressant effects of bupropion are not serotonergically mediated.
Topics: Animals; Antidepressive Agents; Brain; Bupropion; Depressive Disorder; Dopamine; Down-Regulation; Humans; Locus Coeruleus; Mice; Microdialysis; Neurons; Norepinephrine; Raphe Nuclei; Rats; Receptors, Adrenergic, beta; Serotonin; Synaptic Transmission; Treatment Outcome
PubMed: 7665537
DOI: No ID Found -
Expert Review of Neurotherapeutics Jul 2006Over the past decade, bupropion has become a major pharmacotherapy for smoking cessation in the Western world. Unlike other smoking cessation pharmacotherapies,... (Review)
Review
Over the past decade, bupropion has become a major pharmacotherapy for smoking cessation in the Western world. Unlike other smoking cessation pharmacotherapies, bupropion is a non-nicotine treatment. Compared with a placebo control, bupropion approximately doubles smoking quit rates. Most smoking cessation pharmacotherapies are thought to work, in part, by reducing nicotine withdrawal and craving. This article reviews preclinical, human laboratory and clinical trial studies of the effect of bupropion on nicotine withdrawal and craving. Preclinical studies demonstrate that in rats undergoing nicotine withdrawal, bupropion can dose-dependently lower changes in brain-reward threshold and somatic signs of nicotine withdrawal. Human laboratory studies have demonstrated that bupropion can alleviate some nicotine withdrawal symptoms, including depressed mood, irritability, difficulty concentrating and increased appetite. Moreover, bupropion has shown some efficacy in alleviating craving to smoke. Clinical trials of bupropion have offered mixed support of its ability to reduce nicotine withdrawal, weight gain during treatment and craving. Strong mediational evidence of bupropion's action through relief of withdrawal and craving in smoking cessation is growing. Greater understanding of the psychological mechanisms of bupropion action will likely be obtained through advances in the conceptualization and measurement of withdrawal and craving. Improvements in the efficacy of bupropion may be achieved through pharmacogenetic studies, with particular emphasis on its metabolites. Ultimately, the efficacy of bupropion may be augmented by combination with other agents that target withdrawal and craving through complementary neurobiological processes.
Topics: Antidepressive Agents, Second-Generation; Bupropion; Clinical Trials as Topic; Dose-Response Relationship, Drug; Drug Administration Schedule; Humans; Nicotine; Practice Patterns, Physicians'; Smoking Cessation; Substance Withdrawal Syndrome; Tobacco Use Disorder; Treatment Outcome
PubMed: 16831112
DOI: 10.1586/14737175.6.7.965 -
Expert Review of Neurotherapeutics Sep 2006A total of 17 years after its introduction, bupropion remains a safe and effective antidepressant, suitable for first-line use. Bupropion undergoes metabolic... (Review)
Review
A total of 17 years after its introduction, bupropion remains a safe and effective antidepressant, suitable for first-line use. Bupropion undergoes metabolic transformation to an active metabolite, 4-hydroxybupropion, through hepatic cytochrome P450-2B6 (CYP2B6) and has inhibitory effects on cytochrome P450-2D6 (CYP2D6), thus raising concern for clinically-relevant drug interactions. Common side effects are nervousness and insomnia. Nausea appears slightly less common than with the SSRI drugs and sexual dysfunction is probably the least of any antidepressant. Bupropion is relatively safe in overdose with seizures being the predominant concern. The mechanism of action of bupropion is still uncertain but may be related to inhibition of presynaptic dopamine and norepinephrine reuptake transporters. The activity of vesicular monoamine transporter-2, the transporter pumping dopamine, norepinephrine and serotonin from the cytosol into presynaptic vesicles, is increased by bupropion and may be a component of its mechanism of action. Bupropion is approved for use in major depression and seasonal affective disorder and has demonstrated comparable efficacy to other antidepressants in clinical trials. Bupropion is also useful in augmenting a partial response to selective serotonin reuptake inhibitor antidepressants, although bupropion should not be combined with monoamine oxidase inhibitors. It may be less likely to provoke mania than antidepressants with prominent serotonergic effects. Bupropion is effective in helping people quit tobacco smoking. Anecdotal reports indicate bupropion may lower inflammatory mediators such as tumor necrosis factor-alpha, may lower fatigue in cancer and may help reduce concentration problems.
Topics: Antidepressive Agents, Second-Generation; Bupropion; Clinical Trials as Topic; Depressive Disorder; Dose-Response Relationship, Drug; Humans; Seizures
PubMed: 17009913
DOI: 10.1586/14737175.6.9.1249 -
Journal of Clinical PsychopharmacologyThere has long been a clinical belief that bupropion exacerbates anxiety. The purpose of the current retrospective study is to compare anxiety severity over time in...
PURPOSE/BACKGROUND
There has long been a clinical belief that bupropion exacerbates anxiety. The purpose of the current retrospective study is to compare anxiety severity over time in those prescribed selective serotonin reuptake inhibitors (SSRIs) versus bupropion.
METHODS/PROCEDURES
Archival data (N = 8457) from patients receiving psychiatric care from a national tele-mental health company were used. Propensity matching was used to create SSRI and bupropion groups using 17 covariates. These samples were then compared using repeated measures analysis of variance on Generalized Anxiety Disorder Scale 7 scores at start of treatment, 6 weeks, and 12 weeks.
FINDINGS/RESULTS
The SSRI and bupropion groups were significantly different across a number of variables. In the entire sample, the bupropion group had significantly greater anxiety levels. However, for propensity-matched comparisons, there were no significant interactions between group and time (ie, groups did not differ and improved comparably over time).
IMPLICATIONS/CONCLUSIONS
Using propensity matching, there were no differences in anxiety outcome between those prescribed selective serotonin reuptake inhibitor versus bupropion across 12 weeks of treatment.
Topics: Humans; Bupropion; Retrospective Studies; Depressive Disorder, Major; Selective Serotonin Reuptake Inhibitors; Anxiety
PubMed: 36706284
DOI: 10.1097/JCP.0000000000001658 -
The Journal of Clinical Psychiatry 1998Bupropion IR (immediate release) has been on the market since 1988 and is an effective and usually well-tolerated antidepressant. In late 1996, a new sustained-release... (Comparative Study)
Comparative Study Review
Bupropion IR (immediate release) has been on the market since 1988 and is an effective and usually well-tolerated antidepressant. In late 1996, a new sustained-release formulation, bupropion SR, was approved and is now available. Compared with the IR formulation, the SR formulation demonstrates similar efficacy and has been found to have similar, but to some degree fewer, side effects. Its efficacy is similar to that of other newer antidepressants. Side effects of bupropion SR are limited and are not dissimilar to those of the serotonergic antidepressants; however, bupropion SR produces neither substantial sexual side effects nor drug interactions. Study data demonstrate that seizure incidence, which is a concern with high-dose IR, is substantially lower with the new SR formulation.
Topics: Antidepressive Agents, Second-Generation; Antidepressive Agents, Tricyclic; Bupropion; Delayed-Action Preparations; Depressive Disorder; Dizziness; Dose-Response Relationship, Drug; Drug Administration Schedule; Headache; Humans; Nausea; Seizures; Sleep Initiation and Maintenance Disorders; Weight Gain
PubMed: 9554319
DOI: No ID Found -
The Journal of Clinical Psychiatry 1998The identification of nicotine dependence as a psychiatric disorder and increased knowledge of nicotine's neuropharmacologic effects have stimulated researchers to... (Review)
Review
The identification of nicotine dependence as a psychiatric disorder and increased knowledge of nicotine's neuropharmacologic effects have stimulated researchers to search for new pharmacologic interventions for smoking cessation. After reviewing the efficacy and safety of bupropion sustained release (SR) as an agent for treating smoking cessation, the Food and Drug Administration recently approved the use of bupropion SR for this indication. This paper reviews nicotine's pharmacologic effects and the factors contributing to the development of nicotine dependence, the general principles and strategies for treating nicotine dependence, and the evidence for the efficacy of bupropion SR as a treatment for smoking cessation. The release of bupropion SR as a treatment for smoking cessation may provide clinicians with additional opportunities to address smoking cessation with their patients.
Topics: Administration, Cutaneous; Adult; Ambulatory Care; Bupropion; Clinical Trials as Topic; Delayed-Action Preparations; Drug Administration Schedule; Female; Humans; Male; Mood Disorders; Nicotine; Practice Guidelines as Topic; Self Medication; Smoking Cessation; Tobacco Use Disorder; Treatment Outcome
PubMed: 9554323
DOI: No ID Found -
The Journal of Clinical Psychiatry 1998Sustained-release bupropion (bupropion SR) represents a new form of an already known effective antidepressant drug. Its pharmacokinetics, mechanism of action,... (Review)
Review
Sustained-release bupropion (bupropion SR) represents a new form of an already known effective antidepressant drug. Its pharmacokinetics, mechanism of action, metabolism, and efficacy are reviewed. Benefit relative to placebo has been demonstrated in two large multicenter trials, with low doses (100 or 150 mg) having been shown to have therapeutic efficacy. An overview of all placebo-controlled trials of bupropion SR is given, and the differential properties of bupropion and serotonergic drugs are described. The concept of a catecholamine-indolamine spectrum is presented, along with its implications for possible differential therapeutics of selective antidepressants.
Topics: 1-Naphthylamine; Antidepressive Agents, Second-Generation; Bupropion; Clinical Trials as Topic; Delayed-Action Preparations; Depressive Disorder; Drug Administration Schedule; Humans; Placebos; Serotonin Agents; Sertraline; Treatment Outcome
PubMed: 9554318
DOI: No ID Found -
Journal of Pain and Symptom Management Jan 2023Fatigue is a predominant and distressing symptom in cancer and non-cancer conditions for which there is a paucity of recommendations for pharmacological interventions.... (Review)
Review
CONTEXT
Fatigue is a predominant and distressing symptom in cancer and non-cancer conditions for which there is a paucity of recommendations for pharmacological interventions. Bupropion is a novel treatment whose efficacy and safety in the treatment of fatigue are unknown.
OBJECTIVES
This study aimed to systematically assess the evidence on the efficacy and safety of bupropion in the treatment of fatigue in people with cancer and non-cancer conditions.
METHODS
PubMed, EMBASE, and Ovid Medline databases were searched up to July 26, 2022. Studies were included if they reported bupropion as an intervention for cancer and non-cancer-related fatigue and used an objective scale to assess symptom outcomes. Experimental and quasi-experimental studies in adult patients published in English were included.
RESULTS
This review reports on seven studies (three randomized studies, three non-randomized studies, and one case series) that enrolled a total of 584 patients. Bupropion was tested in five studies for treating cancer-related fatigue and in two studies for treating fatigue in non-cancer conditions. The reviewed studies were heterogeneous in relation to the scales used to assess fatigue. Six out of seven studies reported that bupropion significantly reduced the fatigue burden without causing major adverse effects. These positive results must be taken with caution caused by the small sample sizes and low quality of the studies reviewed.
CONCLUSION
Bupropion may prove to be an effective and safe intervention for fatigue in cancer and non-cancer conditions. A high-quality randomized trial is warranted to test current preliminary results.
Topics: Adult; Humans; Bupropion; Neoplasms; Fatigue
PubMed: 36198335
DOI: 10.1016/j.jpainsymman.2022.09.011 -
Biomedical Chromatography : BMC May 2016Bupropion, a tricyclic aminoketone, is used primarily in the treatment of depression, the management of patients with bipolar and schizo-affective disorder, and the... (Review)
Review
Bupropion, a tricyclic aminoketone, is used primarily in the treatment of depression, the management of patients with bipolar and schizo-affective disorder, and the treatment of Parkinson's disease. Bupropion is marketed as a racemate, but the racemic mixture is known to have several disadvantages while the two isomers of bupropion and its metabolite differ significantly in their pharmacological activities. Therefore, the stereoselective determination of the drug enantiomers in pharamaceutical dosages, plasma or urine is of potential clinical and analytical importance. Different chromatographic methods have been employed for the separation of the two enantiomers. This is the first attempt to review the methods of enantiosepartion of bupropion using both direct and indirect approaches in both HPLC and TLC. The review presents a detailed discussion on the use of chiral stationary phase (based on polysaccharide, α1 acid glycoprotein and ovomucoid column) and chiral derivatizing reagents (based on isothiocyanate and cyanuric chloride) along with TLC separation of bupropion enantiomers using ligand exchange and impregnation methods. The focus is also on the separation mechanism for enantioresolution using the various methods described herein.
Topics: Bupropion; Chromatography, High Pressure Liquid; Chromatography, Thin Layer; Stereoisomerism
PubMed: 26230937
DOI: 10.1002/bmc.3572