Source:http://linkedlifedata.com/resource/pubmed/id/20876786
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2010-12-16
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pubmed:abstractText |
We investigated genetic polymorphisms in the pregnane X receptor (NR1I2) in Korean individuals (n = 83) and the effects of NR1I2 genotypes on rifampin-mediated induction of bupropion hydroxylation. The pharmacokinetics of bupropion and hydroxybupropion were evaluated after an oral dose of bupropion (150 mg) administered before and after rifampin treatment for 7 days in 35 healthy subjects. The area under the time-concentration curve (AUC) ratio of hydroxybupropion to bupropion in CYP2B6*6 carriers was significantly lower than that in CYP2B6*6 noncarriers in both the basal and rifampin-induced states (p = 0.012). Among the CYP2B6*6 carriers (n = 13), the NR1I2 TGT (-25385T + g.7635G + g.8055T) carriers exhibited a significantly lower AUC ratio, representing the CYP2B6 hydroxylation activity, compared with the TGT noncarriers, in the induced state (11.9 versus 20.3, p = 0.045). The percent difference in the AUC ratio between the basal and induced states was also significantly different (212% versus 58.8%, p = 0.006). However, no significant difference was observed among the NR1I2 TGT genotypes for the CYP2B6*6 noncarriers (n = 22). In conclusion, it is suggested the NR1I2 TGT genotype decreases the bupropion hydroxylation induced by treatment with rifampin, particularly in CYP2B6*6 carriers.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Aryl Hydrocarbon Hydroxylases,
http://linkedlifedata.com/resource/pubmed/chemical/Bupropion,
http://linkedlifedata.com/resource/pubmed/chemical/Oxidoreductases, N-Demethylating,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Steroid,
http://linkedlifedata.com/resource/pubmed/chemical/Rifampin,
http://linkedlifedata.com/resource/pubmed/chemical/S-mephenytoin N-demethylase,
http://linkedlifedata.com/resource/pubmed/chemical/hydroxybupropion,
http://linkedlifedata.com/resource/pubmed/chemical/pregnane X receptor
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1521-009X
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
39
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
92-7
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pubmed:meshHeading |
pubmed-meshheading:20876786-Aryl Hydrocarbon Hydroxylases,
pubmed-meshheading:20876786-Asian Continental Ancestry Group,
pubmed-meshheading:20876786-Bupropion,
pubmed-meshheading:20876786-Drug Interactions,
pubmed-meshheading:20876786-Female,
pubmed-meshheading:20876786-Genotype,
pubmed-meshheading:20876786-Humans,
pubmed-meshheading:20876786-Hydroxylation,
pubmed-meshheading:20876786-Male,
pubmed-meshheading:20876786-Oxidoreductases, N-Demethylating,
pubmed-meshheading:20876786-Polymorphism, Single Nucleotide,
pubmed-meshheading:20876786-Receptors, Steroid,
pubmed-meshheading:20876786-Rifampin
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pubmed:year |
2011
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pubmed:articleTitle |
Effects of pregnane X receptor (NR1I2) and CYP2B6 genetic polymorphisms on the induction of bupropion hydroxylation by rifampin.
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pubmed:affiliation |
Department of Pharmacology and Clinical Pharmacology, Yonsei University College of Medicine and Severance Hospital, Seoul, Korea.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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