PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 27300331-1 2016 BACKGROUND/AIMS: The study aimed at investigating the effects of multiple-dose bupropion (potent inhibitor of CYP2D6) on the pharmacokinetics (PKs) of single-dose nebivolol (CYP2D6 substrate) and to evaluate the clinical relevance of this potential drug interaction. Bupropion 79-88 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 110-116 24396053-8 2014 CYP2D6 inhibition with paroxetine, fluoxetine, bupropion and methadone significantly decreased the fraction of morphine excreted. Bupropion 47-56 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 0-6 25565674-3 2015 The aim of this study was to clarify the effect of CYP2B6*6 and secondarily CYP2D6 genotype on steady-state serum concentrations of bupropion and hydroxybupropion in a large population of psychiatric patients. Bupropion 132-141 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 76-82 24237812-9 2013 The woman was also taking fluoxetine and bupropion which are strong inhibitors of CYP 2D6. Bupropion 41-50 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 82-89 33905640-0 2021 Dose-Dependent Inhibition of CYP2D6 by Bupropion in Patients With Depression. Bupropion 39-48 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 29-35 21946596-6 2011 The same degree of increase is expected for the two other potent CYP2D6 inhibitors in the class, fluoxetine and bupropion. Bupropion 112-121 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 65-71 20880642-10 2010 Paroxetine, fluoxetine and bupropion are strong CYP2D6 inhibitors which should be avoided in tamoxifen users. Bupropion 27-36 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 48-54 18691982-13 2008 Duloxetine and bupropion are moderate inhibitors of CYP2D6, and sertraline may cause significant inhibition of this isoform, but only at high doses. Bupropion 15-24 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 52-58 18420781-1 2008 There are documented clinical drug-drug interactions between bupropion and the CYP2D6-metabolized drug desipramine resulting in marked (5-fold) increases in desipramine exposure. Bupropion 61-70 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 79-85 18420781-4 2008 In human liver microsomes using the CYP2D6 probe substrate bufuralol, erythrohydrobupropion and threohydrobupropion were more potent inhibitors of CYP2D6 activity (K(i) = 1.7 and 5.4 microM, respectively) than hydroxybupropion (K(i) = 13 microM) or bupropion (K(i) = 21 microM). Bupropion 82-91 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 36-42 18420781-4 2008 In human liver microsomes using the CYP2D6 probe substrate bufuralol, erythrohydrobupropion and threohydrobupropion were more potent inhibitors of CYP2D6 activity (K(i) = 1.7 and 5.4 microM, respectively) than hydroxybupropion (K(i) = 13 microM) or bupropion (K(i) = 21 microM). Bupropion 82-91 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 147-153 18420781-7 2008 This work indicates that the reductive metabolites of bupropion are potent competitive CYP2D6 inhibitors in vivo and provides a mechanistic explanation for the clinical drug-drug interaction between bupropion and desipramine. Bupropion 54-63 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 18420781-7 2008 This work indicates that the reductive metabolites of bupropion are potent competitive CYP2D6 inhibitors in vivo and provides a mechanistic explanation for the clinical drug-drug interaction between bupropion and desipramine. Bupropion 199-208 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 87-93 17009913-2 2006 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. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 165-184 17009913-2 2006 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. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 186-192 16368442-19 2005 In addition, bupropion inhibits CYP2D6 and may reduce clearance of agents metabolized by this enzyme. Bupropion 13-22 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 32-38 34015277-5 2021 When assessing the impact of 2D6 phenotypes on bupropion mediated CYP 2D6 DDI in Chinese cancer population, we found that AUC increased by at least 60% in extensive metabolizers (EM) and 30% in IM. Bupropion 47-56 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 66-73 22171584-10 2012 With regard to this, duloxetine and bupropion are moderate inhibitors of CYP2D6. Bupropion 36-45 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 73-79 20208386-4 2010 Studies with HLM under-predict the ability of gemfibrozil and bupropion to cause clinically significant inhibition of CYP2C8 and CYP2D6, respectively, and over-predict the ability of ezetimibe to cause clinically significant inhibition of CYP3A4. Bupropion 62-71 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 129-135 20208386-5 2010 Gemfibrozil and bupropion represent examples of glucuronidation-dependent and reduction-dependent activation to metabolites that inhibit CYP2C8 and CYP2D6, respectively, whereas ezetimibe represents an example of glucuronidation-dependent protection against metabolism-dependent inhibition of CYP3A4. Bupropion 16-25 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 148-154 15876900-0 2005 Inhibition of CYP2D6 activity by bupropion. Bupropion 33-42 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 14-20 15876900-1 2005 The purpose of this study was to assess the effect of bupropion on cytochrome P450 2D6 (CYP2D6) activity. Bupropion 54-63 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 67-86 15876900-1 2005 The purpose of this study was to assess the effect of bupropion on cytochrome P450 2D6 (CYP2D6) activity. Bupropion 54-63 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 88-94 15876900-8 2005 At baseline, all subjects were phenotypically extensive CYP2D6 metabolizers (metabolic ratio <0.3); after treatment, 6 of 13 subjects receiving bupropion, but none of those receiving placebo, had metabolic ratios consistent with poor CYP2D6 metabolizers. Bupropion 147-156 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 237-243 15876900-9 2005 Bupropion is therefore a potent inhibitor of CYP2D6 activity, and care should be exercised when initiating or discontinuing bupropion use in patients taking drugs metabolized by CYP2D6. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 45-51 15876900-9 2005 Bupropion is therefore a potent inhibitor of CYP2D6 activity, and care should be exercised when initiating or discontinuing bupropion use in patients taking drugs metabolized by CYP2D6. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 178-184 15876900-9 2005 Bupropion is therefore a potent inhibitor of CYP2D6 activity, and care should be exercised when initiating or discontinuing bupropion use in patients taking drugs metabolized by CYP2D6. Bupropion 124-133 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 178-184 12021638-0 2002 Change from the CYP2D6 extensive metabolizer to the poor metabolizer phenotype during treatment With bupropion. Bupropion 101-110 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 16-22 12021638-1 2002 Some data indicate that bupropion inhibits the cytochrome P-450 enzyme CYP2D6, but very little published data is available on the extent of this inhibition. Bupropion 24-33 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 71-77 12021638-4 2002 His CYP2D6 phenotype was assessed using the test drug dextromethorphan before, during, and after treatment with bupropion. Bupropion 112-121 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 4-10 12021638-6 2002 Although the results from a single patient should be interpreted with great caution, the extent of the interaction indicates that bupropion might be a CYP2D6 inhibitor as potent as the most powerful CYP2D6 inhibitors known, such as quinidine and paroxetine. Bupropion 130-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 151-157 12021638-6 2002 Although the results from a single patient should be interpreted with great caution, the extent of the interaction indicates that bupropion might be a CYP2D6 inhibitor as potent as the most powerful CYP2D6 inhibitors known, such as quinidine and paroxetine. Bupropion 130-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 199-205 10997936-9 2000 IC(50) values for inhibition of a CYP2D6 index reaction (dextromethorphan O-demethylation) by bupropion and hydroxybupropion were 58 and 74 microM, respectively. Bupropion 94-103 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 34-40 8885123-7 1996 The potential accumulation of hydroxybupropion after CYP2D6 inhibition may, however, contribute to toxicity and impair bupropion"s therapeutic effectiveness. Bupropion 37-46 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 53-59 35512805-1 2022 Striking stereoselective disposition of the antidepressant and smoking cessation aid bupropion and its active metabolites observed clinically influence patients" response to BUP therapy and its clinically important drug-drug interactions (DDI) with CYP2D6 substrates. Bupropion 85-94 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 249-255 33905640-1 2021 PURPOSE: The aim of this study was to investigate the potential dose-dependent CYP2D6 inhibition by bupropion (BUP) in patients with depression. Bupropion 100-109 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 79-85 33905640-1 2021 PURPOSE: The aim of this study was to investigate the potential dose-dependent CYP2D6 inhibition by bupropion (BUP) in patients with depression. Bupropion 111-114 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 79-85 33905640-9 2021 CONCLUSIONS: Bupropion exhibits a clear dose-dependent CYP2D6 inhibitory effect during treatment of patients with depression. Bupropion 13-22 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 55-61 33905640-11 2021 Half of the patients treated with high-dose BUP are converted to CYP2D6 PM phenotype. Bupropion 44-47 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 65-71 28876959-8 2018 Other significant learnings were: (1) understanding the in vivo CYP2D6 inhibitory potential of bupropion with respect to the chirality of parent drug and the metabolites; (2) the potential involvement of bupropion and metabolites towards significant down regulation of CYP2D6 mRNA; (3) significant in vivo CYP2D6 inhibitory activity (86%) exhibited by R,R-hydroxybupropion and threohydrobupropion. Bupropion 95-104 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 64-70 33161206-0 2021 Corrigendum to "In vitro to in vivo extrapolation of the complex drug-drug interaction of bupropion and its metabolites with CYP2D6; simultaneous reversible inhibition and CYP2D6 downregulation" [Biochem. Bupropion 90-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 125-131 33161206-0 2021 Corrigendum to "In vitro to in vivo extrapolation of the complex drug-drug interaction of bupropion and its metabolites with CYP2D6; simultaneous reversible inhibition and CYP2D6 downregulation" [Biochem. Bupropion 90-99 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 172-178 30842914-12 2019 The commonly used dose of 30 mg daily may have been too low to have an effect; additionally, the most frequently utilized select antidepressant, bupropion, has moderately less CYP2D6 inhibition than fluoxetine and paroxetine. Bupropion 145-154 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 176-182 28876959-8 2018 Other significant learnings were: (1) understanding the in vivo CYP2D6 inhibitory potential of bupropion with respect to the chirality of parent drug and the metabolites; (2) the potential involvement of bupropion and metabolites towards significant down regulation of CYP2D6 mRNA; (3) significant in vivo CYP2D6 inhibitory activity (86%) exhibited by R,R-hydroxybupropion and threohydrobupropion. Bupropion 95-104 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 269-275 28876959-8 2018 Other significant learnings were: (1) understanding the in vivo CYP2D6 inhibitory potential of bupropion with respect to the chirality of parent drug and the metabolites; (2) the potential involvement of bupropion and metabolites towards significant down regulation of CYP2D6 mRNA; (3) significant in vivo CYP2D6 inhibitory activity (86%) exhibited by R,R-hydroxybupropion and threohydrobupropion. Bupropion 95-104 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 269-275 27518170-7 2016 CONCLUSIONS: These results demonstrated that the effect of bupropion on CYP2D6 activity was responsible for an increased systemic exposure to atomoxetine (5.1-fold) and also for a decreased exposure to its main metabolite (1.5-fold). Bupropion 59-68 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 72-78 29267251-0 2017 Prediction of Drug-Drug Interactions with Bupropion and Its Metabolites as CYP2D6 Inhibitors Using a Physiologically-Based Pharmacokinetic Model. Bupropion 42-51 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 75-81 29267251-9 2017 The simulation suggests that bupropion and its metabolites contribute to the DDI between bupropion and CYP2D6 substrates. Bupropion 29-38 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 103-109 29054049-6 2017 Concomitant use of CYP inhibitors (e.g. paroxetine, fluoxetine and bupropion) or inducers (e.g. carbamazepine, phenobarbital and phenytoin) could counteract the clinical effect or trigger side effects of analgesics in the same manner as genetically determined differences in CYP2D6-mediated metabolism of many opioids. Bupropion 67-76 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 275-281 27836670-0 2017 In vitro to in vivo extrapolation of the complex drug-drug interaction of bupropion and its metabolites with CYP2D6; simultaneous reversible inhibition and CYP2D6 downregulation. Bupropion 74-83 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 109-115 27836670-0 2017 In vitro to in vivo extrapolation of the complex drug-drug interaction of bupropion and its metabolites with CYP2D6; simultaneous reversible inhibition and CYP2D6 downregulation. Bupropion 74-83 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 156-162 27836670-1 2017 Bupropion is a widely used antidepressant and smoking cessation aid and a strong inhibitor of CYP2D6 in vivo. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 94-100 27836670-3 2017 Four primary metabolites of bupropion, threo- and erythro-hydrobupropion and R,R- and S,S-OH-bupropion, circulate at higher concentrations than the parent drug and are believed to contribute to the efficacy and side effects of bupropion as well as to the CYP2D6 inhibition. Bupropion 28-37 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 255-261 27836670-4 2017 However, bupropion and its metabolites are only weak inhibitors of CYP2D6 in vitro, and the magnitude of the in vivo drug-drug interactions (DDI) caused by bupropion cannot be explained by the in vitro data even when CYP2D6 inhibition by the metabolites is accounted for. Bupropion 9-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 67-73 27836670-4 2017 However, bupropion and its metabolites are only weak inhibitors of CYP2D6 in vitro, and the magnitude of the in vivo drug-drug interactions (DDI) caused by bupropion cannot be explained by the in vitro data even when CYP2D6 inhibition by the metabolites is accounted for. Bupropion 9-18 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 217-223 27836670-6 2017 Bupropion and its metabolites were found to inhibit CYP2D6 stereoselectively with up to 10-fold difference in inhibition potency between enantiomers. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 52-58 27836670-8 2017 In HepG2 cells and in plated human hepatocytes bupropion and its metabolites were found to significantly downregulate CYP2D6 mRNA in a concentration dependent manner. Bupropion 47-56 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 118-124 27836670-9 2017 The in vivo DDI was quantitatively predicted by significant down-regulation of CYP2D6 mRNA and reversible inhibition of CYP2D6 by bupropion and its metabolites. Bupropion 130-139 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 120-126 27255113-10 2016 In summary, to our knowledge, this is the first comprehensive report to provide novel insight into mechanisms underlying bupropion disposition by detailing the stereoselective pharmacokinetics of individual bupropion metabolites, which will enhance clinical understanding of bupropion"s effects and DDIs with CYP2D6. Bupropion 121-130 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 309-315 27255113-10 2016 In summary, to our knowledge, this is the first comprehensive report to provide novel insight into mechanisms underlying bupropion disposition by detailing the stereoselective pharmacokinetics of individual bupropion metabolites, which will enhance clinical understanding of bupropion"s effects and DDIs with CYP2D6. Bupropion 207-216 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 309-315 27255113-10 2016 In summary, to our knowledge, this is the first comprehensive report to provide novel insight into mechanisms underlying bupropion disposition by detailing the stereoselective pharmacokinetics of individual bupropion metabolites, which will enhance clinical understanding of bupropion"s effects and DDIs with CYP2D6. Bupropion 207-216 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 309-315 26967321-7 2016 Bupropion reduced the Cmax and AUC24 of the CYP2D6-dependently formed metabolite stereoisomers of DHMA 3-sulfate, DHMA 4-sulfate, and 4-hydroxy-3-methoxymethamphetamine (HMMA sulfate and HMMA glucuronide) by approximately 40%. Bupropion 0-9 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 44-50