A sensitive and selective liquid chromatograpy-mass spectrometry method for the determination of bupropion and its main metabolite, hydroxubupropion, in rat plasma was developed and validated. After addition of carbamazepine as internal standard (IS) and precipitation of protein with acetonitrile, the plasma samples were analyzed on an Agilent Zorbax SB-C18 (2.1 mm x 50 mm, 3.5 microm) column a...

A “cocktail”of several probe drugs is often used to evaluate metabolic activity of multiple cytochrome P450 enzymes in one session. Some interactions among probe drugs can appear and may impact the rate of biotransformation of other ones. Our presented work was to aim on the influence of bupropion on rat cytochrome P450-mediated metabolism of tolbutamide. The biotransformation rates of tolbutam...

Interferon (IFN)-α therapy for chronic hepatitis C virus (HCV) infection is frequently associated with major depressive episodes. Bupropion, a commonly used antidepressant agent, has recently found to have strong anti-inflammatory effects in animal models. Despite of the theoretical relevancy, the antidepressant effect of bupropion in IFN-alpha-induced depression has never been studied. Ten HCV...

Clinical trials rigorously demonstrate the efficacy of new products and justify their marketing. However, it is only after use in real-life settings that the clinical value (effectiveness) of a new treatment is fully known. The purpose of this review was to summarise the effectiveness data for bupropion SR as an aid to smoking cessation. Available reports of effectiveness data for bupropion SR ...

The objective of this study was to assess whether treatment with sustained-release bupropion (Wellbutrin-SR) produces alterations in electroencephalographic (EEG) sleep that are associated with clinical response to the drug. EEG sleep was measured in 20 patients with unipolar major depressive disorder before and after treatment with sustained-release bupropion. Each EEG sleep session consisted ...

There is considerable variability in the rate of response and remission following treatment with antidepressant drugs or placebo in depression patients. No pharmacogenetic studies of bupropion response have been done. We investigated 532 tagging single nucleotide polymorphisms (SNPs) in 34 candidate genes for association with remission and response to either bupropion (n=319) or placebo (n=257)...

Administration of bupropion [(±)-2-(tert-butylamino)-1-(3-chlorophenyl)propan-1-one] and its preformed active metabolite, hydroxybupropion [(±)-1-(3-chlorophenyl)-2-[(1-hydroxy-2-methyl-2-propanyl)amino]-1-propanone], to rats with measurement of unbound concentrations by quantitative microdialysis sampling of plasma and brain extracellular fluid was used to develop a compartmental pharmacokinet...

CONTEXT African Americans disproportionately experience greater smoking attributable morbidity and mortality. Few clinical trials for smoking cessation in African Americans have been conducted, despite a different profile of both smoking and quitting patterns. OBJECTIVE To compare a sustained-release form of bupropion hydrochloride (bupropion SR) with placebo for smoking cessation among Afric...

Major depressive disorder (MDD) and Parkinson's disease (PD) share symptoms such as tremor. Bupropion, a norepinephrine-dopamine reuptake inhibitor, shows weak dopamine transporter (DAT) occupancy. We report here on a patient with MDD whose hand tremors might have been misdiagnosed as PD by single-photon emission computed tomography (SPECT) under bupropion use. A 66-year-old male patient with M...

BACKGROUND The antihypertensive reserpine is an indole alkaloid from Rauwolfia serpentina and exerts also profound activity against cancer cells in vitro and in vivo. The present investigation was undertaken to investigate possible modes of action to explain its activity toward drug-resistant tumor cells. MATERIAL AND METHODS Sensitive and drug-resistant tumor cell lines overexpressing P-glyc...