Pub. Date : 2005 Jun
PMID : 15788540
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
1 | In vitro-in vivo extrapolation of CYP2D6 inactivation by paroxetine: prediction of nonstationary pharmacokinetics and drug interaction magnitude. | Paroxetine | cytochrome P450, family 2, subfamily d, polypeptide 3 | Rattus norvegicus |
2 | Recent data have provided evidence for mechanism-based inactivation of CYP2D6 by paroxetine. | Paroxetine | cytochrome P450, family 2, subfamily d, polypeptide 3 | Rattus norvegicus |
3 | We have predicted the pharmacokinetic consequences of CYP2D6 inactivation by paroxetine from in vitro inactivation kinetics (kinact 0.17 min(-1), unbound KI 0.315 microM), in vivo inhibitor concentrations, and an estimated CYP2D6 degradation half-life of 51 h, using a mathematical model of mechanism-based inhibition. | Paroxetine | cytochrome P450, family 2, subfamily d, polypeptide 3 | Rattus norvegicus |
4 | We have predicted the pharmacokinetic consequences of CYP2D6 inactivation by paroxetine from in vitro inactivation kinetics (kinact 0.17 min(-1), unbound KI 0.315 microM), in vivo inhibitor concentrations, and an estimated CYP2D6 degradation half-life of 51 h, using a mathematical model of mechanism-based inhibition. | Paroxetine | cytochrome P450, family 2, subfamily d, polypeptide 3 | Rattus norvegicus |
5 | In summary, the scaling model for mechanism-based inactivation successfully predicted the pharmacokinetic consequences of CYP2D6 inactivation by paroxetine from in vitro data. | Paroxetine | cytochrome P450, family 2, subfamily d, polypeptide 3 | Rattus norvegicus |