The in vitro biotransformation of bupropion to hydroxybupropion was studied in human liver microsomes and microsomes containing heterologously expressed human cytochromes P450 (CYP). The mean (+/-S.E.) K(m) in four human liver microsomes was 89 (+/-14) microM. In microsomes containing cDNA-expressed CYPs, hydroxybupropion formation was mediated only by CYP2B6 at 50 microM bupropion (K(m) 85 mic...

Intraperitoneal (IP) injection of bupropion (3,6, amine (4,16 mg kg•') induced dose-dependent climbing in mice. The climbing response induced by both drugs were decreased in animals pretreated either with the 0-1 antagonist SCH 233<)0 or the 0-2 antagonist sulpiride. The α-adrenoceptor blocker phenoxybenzamine decreased the climbing induced by both bupropion and amphetamine, but the β-ad...

This study was conducted to evaluate the effect of bupropion sustained-release (SR) on smoking cessation in patients with chronic posttraumatic stress disorder (PTSD). Fifteen veterans with chronic PTSD who desired to stop smoking enrolled in a 12-week double-blind evaluation of bupropion SR and placebo. Patients were randomly assigned in a 2:1 ratio to receive either bupropion SR or placebo. B...

BACKGROUND Bupropion, which is widely used in patients with depressive disorder, may cause allergic reactions. However, the real prevalence of these side effects may be overlooked and underreported due to the delayed onset phenomenon. OBJECTIVE This study aimed to estimate the real incidence of bupropion-induced urticaria and clarify the delayed onset phenomenon. METHODS We conducted a nati...

There are documented clinical drug-drug interactions between bupropion and the CYP2D6-metabolized drug desipramine resulting in marked (5-fold) increases in desipramine exposure. This finding was unexpected as CYP2D6 does not play a significant role in bupropion clearance, and bupropion and its major active metabolite, hydroxybupropion, are not strong CYP2D6 inhibitors in vitro. The aims of thi...

Bupropion is an atypical antidepressant that also has usefulness as a smoking-cessation aid. Because hydroxybupropion, a major metabolite of bupropion, is believed to contribute to its antidepressant activity, this metabolite may also contribute to the smoking-cessation properties of bupropion. This study investigated the effects of hydrobupropion enantiomers on monoamine transporters and nicot...

we present a case report of bupropion-induced diplopia in a 26-year-old woman who suffered from atypical depression. âfter four weeks of taking bupropion (225 mg per day) she complained of headaches, blurred vision, and diplopia. no neurological and ophthalmologic abnormal signs were found. her brain magnetic resonance imaging (mrï) and magnetic resonance venography (mrv) were normal as well. â...

Bupropion is used clinically to treat depression and to promote smoking cessation. It is metabolized by CYP2B6 to its activemetabolite hydroxybupropion, yet alterations in CYP2B6 activity have little impact on bupropion plasma levels. Furthermore, less than 10%of a bupropion dose is excreted as urinary bupropion and its characterized metabolites hydroxybupropion, threohydrobupropion, and erythr...

Nicotine addiction is a chronic relapsing condition that can be difficult to treat. Until recently, pharmacological options for the treatment of tobacco dependence were primarily limited to nicotine replacement therapy (NRT). Sustained-release bupropion (bupropion SR) is the first non-nicotine pharmacological treatment approved for smoking cessation. Bupropion SR is recommended for first-line p...

N-methylbupropion was selected as a potential prodrug from our in vitro screening of analogues of bupropion described in the preceding paper. This study describes in vivo pharmacokinetics of N-methylbupropion in the guinea-pig animal model, which is reported to best predict human metabolism of bupropion. The suitability of the guinea pig was established by studying N-demethylation of N-methylbu...