Disease relevance of bupropion

• Weight gain at seven weeks was significantly less in the combined-treatment group than in the bupropion group and the placebo group (P<0.05 for both comparisons) [1].
• Safety profile of bupropion for chronic obstructive pulmonary disease [2].
• Remission of Crohn's disease on bupropion [3].
• RESULTS: Although bupropion caused a rise in supine blood pressure, it did not cause significant conduction complications, did not exacerbate ventricular arrhythmias, had a low rate of orthostatic hypotension, and had no effect on pulse rate [4].
• However, bupropion treatment was discontinued for 14% of the patients because of adverse effects, including exacerbation of baseline hypertension in two patients [4].

Psychiatry related information on bupropion

• Sustained-release bupropion for smoking cessation [5].
• Treatment of smokeless tobacco addiction with bupropion and behavior modification [6].
• The two United States Food and Drug Administration-approved medications used to treat tobacco dependence, bupropion and nicotine replacement therapy, are effective for only a fraction of smokers [7].
• Effects of sustained-release bupropion and supportive group therapy on cigarette consumption in patients with schizophrenia [8].
• Prevalence of psychosis, delusions, and hallucinations in clinical trials with bupropion [9].
• These data suggest that smokers with the CYP2B6*6 genotype have a higher liability to relapse on placebo and that they may be good candidates for bupropion treatment for smoking cessation [10].

High impact information on bupropion

• We conducted a double-blind, placebo-controlled comparison of sustained-release bupropion (244 subjects), a nicotine patch (244 subjects), bupropion and a nicotine patch (245 subjects), and placebo (160 subjects) for smoking cessation [1].
• Crohn's disease remission on bupropion [11].
• Our aim was to investigate the effect of sustained-release bupropion (amfebutamone) (SR) in promoting abstinence from smoking in patients with COPD [12].
• Of the three antidepressants included in the study, venlafaxine was associated with the highest relative risk of such switching and bupropion with the lowest risk [13].
• METHODS: In a placebo-controlled double-dummy randomized trial, 255 adults at risk for COPD or with COPD were prescribed sustained-release bupropion (bupropion SR) (150 mg twice daily) or nortriptyline (75 mg once daily) for 12 weeks [14].

Chemical compound and disease context of bupropion

• OBJECTIVE: To compare a sustained-release form of bupropion hydrochloride (bupropion SR) with placebo for smoking cessation among African Americans [15].
• The patients with MAOI- and bupropion-associated mania had a slightly lower overall rating of severity of psychopathology at admission than the subgroups with fluoxetine- and tricyclic-associated mania [16].
• BACKGROUND: Pretreatment functional brain imaging was examined for never-hospitalized outpatients with unipolar depression compared with control subjects in a crossover treatment trial involving bupropion or venlafaxine monotherapy [17].
• There was no significant difference in the pharmacokinetics of bupropion or hydroxybupropion between white subjects and Chinese subjects before and after treatment with rifampin, once corrected for body weight [18].
• RESULTS: Bupropion SR and sertraline were comparably effective, both were superior to placebo in reducing depressive symptoms. and they did not differ in their effect on anxiety symptoms [19].

Biological context of bupropion

• The "bupropion for smoking cessation" trial from a family practice perspective [20].
• Bone density loss in Crohn's disease: role of TNF and potential for prevention by bupropion [21].
• Pharmacokinetics of bupropion and its major basic metabolites in normal subjects after a single dose [22].
• Cytochrome P450 2B6 activity as measured by bupropion hydroxylation: effect of induction by rifampin and ethnicity [18].
• Pharmacokinetics profiles were determined on days 1 and 30 for bupropion and hydroxybupropion and days 29 and 30 for LPV/r. LPV/r administration significantly decreased bupropion maximum plasma concentration (C(max)) by 57% (90% confidence interval (CI), 38-76%; P<0.01) and area under the curve (AUC) infinity by 57% (90% CI, 32-83%; P<0.01) [23].

Anatomical context of bupropion

• Bupropion produced similar neurochemical responses in the striatum and the nucleus accumbens [24].
• The mild central nervous system activating effects of bupropion appear to be due to weak dopaminergic mechanisms [25].
• Pharmacogenetic determinants of interindividual variability in bupropion hydroxylation by cytochrome P450 2B6 in human liver microsomes [26].
• (3) Electrophysiologic data show that with acute dosing, bupropion reduces the firing rates of noradrenergic neurons in the locus ceruleus [25].
• Only one psychiatrist each chose thyroid augmentation or bupropion [27].

Associations of bupropion with other chemical compounds

• Behavioral counseling, sustained-release bupropion hydrochloride therapy, and nicotine replacement therapy may be safe therapeutic modalities for treatment of smokeless tobacco use [28].
• METHOD: All-night sleep EEG studies were performed before treatment and after partial or full remission on 18 men with depression diagnosed according to Research Diagnostic Criteria and randomly assigned to treatment with either bupropion (N = 7) or fluoxetine (N = 11) [29].
• Blood samples were taken for up to 72 hours after each bupropion dose, and plasma concentrations of bupropion and its active metabolites, hydroxybupropion, threohydrobupropion, and erythrohydrobupropion, were measured by HPLC [18].
• In spontaneously hypertensive rats, 16 days of bupropion, 25 mg/kg subcutaneously, had no effect on baseline BP and HR and did not antagonize the hypotensive and bradycardic effects of clonidine, 5 mg/kg iv [30].
• Incomplete symptom remission and sexual side effects are common problems for which bupropion often is added to treatment with selective serotonin and serotonin-norepinephrine reuptake inhibitors (SSRIs and SNRIs) for patients with major depressive disorder (MDD) [31].

Gene context of bupropion

• BACKGROUND: CYP2B6 is a highly variable and polymorphic cytochrome P450 (CYP) enzyme involved in the biotransformation of an increasing number of drugs, including cyclophosphamide, bupropion, and the nonnucleosidic reverse transcriptase inhibitor efavirenz [32].
• These results suggest that bupropion may be the preferred pharmacologic treatment for smokers homozygous for the DRD2 - 141 Ins C allele, while NRT may be more beneficial for those who carry the Del C allele [33].
• In addition, bupropion inhibits CYP2D6 and may reduce clearance of agents metabolized by this enzyme [34].
• Evaluation of the contribution of cytochrome P450 3A4 to human liver microsomal bupropion hydroxylation [35].
• Results showed a decrease in catalase activity of the PFC and ST after SE and death induced by cocaine and bupropion overdoses [36].

Analytical, diagnostic and therapeutic context of bupropion

• In controlled clinical trials, nicotine replacement therapy (NRT) and the antidepressant bupropion have been shown to significantly increase cessation rates only for moderate to heavy smokers (> or = 15 cigarettes/d) [37].
• However, this benefit did not continue after treatment was stopped; subsequent continuous abstinence rates were 7% (20/295) in the bupropion group and 5% (16/299) in the placebo group (P = 0.50) [38].
• A double-blind study of bupropion and placebo in depression [39].
• Therapeutic drug monitoring of bupropion [40].
• METHODS: Six hundred twenty-nine subjects with CVD who smoked >/=10 cigarettes/day were randomised in a double-blind, multicentre study to receive bupropion SR (150 mg twice daily) or placebo for 7 weeks, with a follow-up of 52 weeks [41].

References