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https://hdl.handle.net/2440/44124
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dc.contributor.author | Saussele, T. | - |
dc.contributor.author | Burk, O. | - |
dc.contributor.author | Blievernicht, J. | - |
dc.contributor.author | Nussler, A. | - |
dc.contributor.author | Nussler, N. | - |
dc.contributor.author | Hengstler, J. | - |
dc.contributor.author | Eichelbaum, M. | - |
dc.contributor.author | Schwab, M. | - |
dc.contributor.author | Zanger, U. | - |
dc.date.issued | 2007 | - |
dc.identifier.citation | Clinical Pharmacology and Therapeutics, 2007; 82(3):265-274 | - |
dc.identifier.issn | 0009-9236 | - |
dc.identifier.issn | 1532-6535 | - |
dc.identifier.uri | http://hdl.handle.net/2440/44124 | - |
dc.description.abstract | The pyrazolone drug metamizole is a widely used analgesic. Analysis of liver microsomes from patients treated with metamizole revealed selectively higher expression of cytochromes P450, CYP2B6 and CYP3A4 (3.8- and 2.8-fold, respectively), and 2.9-fold higher bupropion hydroxylase activity compared with untreated subjects. Further investigation of metamizole and various derivatives on different potential target genes in human primary hepatocytes demonstrated time- and concentration-dependent induction by metamizole of CYP2B6 (7.8- and 3.1-fold for mRNA and protein, respectively, at 100 M) and CYP3A4 (2.4- and 2.9-fold, respectively), whereas other genes (CYP2C9, CYP2C19, CYP2D6, NADPH:cytochrome P450 reductase, ABCB1, constitutive androstane receptor (CAR), pregnane X receptor (PXR)) were not substantially altered. Using reporter gene assays, we show that metamizole is not acting as a direct ligand to either PXR or CAR, suggesting a phenobarbital-like mechanism of induction. These data warrant further studies to elucidate the drug-interaction potential of metamizole, especially in patients with long-term treatment. | - |
dc.description.statementofresponsibility | T Saussele, O Burk, J K Blievernicht, K Klein, A Nussler, N Nussler, J G Hengstler, M Eichelbaum, M Schwab, and U M Zanger | - |
dc.language.iso | en | - |
dc.publisher | Mosby Inc | - |
dc.rights | © 2008 American Society for Clinical Pharmacology and Therapeutics | - |
dc.source.uri | http://dx.doi.org/10.1038/sj.clpt.6100138 | - |
dc.subject | Liver | - |
dc.subject | Cells, Cultured | - |
dc.subject | Microsomes, Liver | - |
dc.subject | Hepatocytes | - |
dc.subject | Humans | - |
dc.subject | Dipyrone | - |
dc.subject | Cytochrome P-450 Enzyme System | - |
dc.subject | Aryl Hydrocarbon Hydroxylases | - |
dc.subject | Isoenzymes | - |
dc.subject | Oxidoreductases, N-Demethylating | - |
dc.subject | Receptors, Cytoplasmic and Nuclear | - |
dc.subject | Receptors, Steroid | - |
dc.subject | Transcription Factors | - |
dc.subject | DNA | - |
dc.subject | RNA | - |
dc.subject | Anti-Inflammatory Agents, Non-Steroidal | - |
dc.subject | Blotting, Western | - |
dc.subject | Reverse Transcriptase Polymerase Chain Reaction | - |
dc.subject | Enzyme Induction | - |
dc.subject | Dose-Response Relationship, Drug | - |
dc.subject | Genotype | - |
dc.subject | Plasmids | - |
dc.subject | Catalysis | - |
dc.subject | Aged | - |
dc.subject | Middle Aged | - |
dc.subject | Female | - |
dc.subject | Male | - |
dc.subject | Cytochrome P-450 CYP3A | - |
dc.subject | In Vitro Techniques | - |
dc.subject | Cytochrome P-450 CYP2B6 | - |
dc.subject | Pregnane X Receptor | - |
dc.subject | Constitutive Androstane Receptor | - |
dc.title | Selective induction of human hepatic cytochromes P450 2B6 and 3A4 by metamizole | - |
dc.type | Journal article | - |
dc.identifier.doi | 10.1038/sj.clpt.6100138 | - |
pubs.publication-status | Published | - |
Appears in Collections: | Aurora harvest 6 Pharmacology publications |
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