Effect of zolpidem on human Cytochrome P450 activity, and on transport mediated by P-glycoprotein
| Autor: | Leah M. Hesse, Lisa L. von Moltke, Barbara F. Roth-Schechter, David J. Greenblatt, Michael D. Perloff, James L. Weemhoff, Jerold S. Harmatz |
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| Rok vydání: | 2002 |
| Předmět: |
Zolpidem
Pyridines Biological Transport Active Pharmaceutical Science Pharmacology Rhodamine 123 chemistry.chemical_compound Cytochrome P-450 Enzyme System medicine Cytochrome P-450 Enzyme Inhibitors Humans Pharmacology (medical) ATP Binding Cassette Transporter Subfamily B Member 1 Cells Cultured P-glycoprotein biology CYP1A2 Cytochrome P450 General Medicine Transport protein Isoenzymes chemistry Mediated transport Microsomes Liver biology.protein Microsome medicine.drug |
| Zdroj: | Biopharmaceutics & Drug Disposition. 23:361-367 |
| ISSN: | 1099-081X 0142-2782 |
| Popis: | The influence of high concentrations of zolpidem (100 microM, corresponding to approximately 200 times maximum therapeutic concentrations) on the activity of six human Cytochrome P450 (CYP) enzymes was evaluated in a model system using human liver microsomes. Zolpidem produced negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19, 2D6, and 3A. Transport of rhodamine 123, presumed to be mediated mainly by the energy-dependent efflux transport protein P-glycoprotein, was studied in a cell culture system using a human intestinal cell line. High concentrations of zolpidem (100 microM), exceeding the usual therapeutic range by more than 100-fold, produced only modest impairment of rhodamine 123 transport. The findings indicate that zolpidem is very unlikely to cause clinical drug interactions attributable to impairment of CYP activity or P-gp mediated transport. |
| Databáze: | OpenAIRE |
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