Dose‐dependent Induction of Cytochrome P450 (CYP) 3A4 and Activation of Pregnane X Receptor by Topiramate

@article{Nallani2003DosedependentIO,
  title={Dose‐dependent Induction of Cytochrome P450 (CYP) 3A4 and Activation of Pregnane X Receptor by Topiramate},
  author={Srikanth C. Nallani and Tracy A. Glauser and Niresh Hariparsad and Kenneth D R Setchell and Donna J. Buckley and Arthur R. Buckley and Pankaj B Desai},
  journal={Epilepsia},
  year={2003},
  volume={44}
}
Summary:  Purpose: In clinical studies, topiramate (TPM) was shown to cause a dose‐dependent increase in the clearance of ethinyl estradiol. We hypothesized that this interaction results from induction of hepatic cytochrome P450 (CYP) 3A4 by TPM. Accordingly, we investigated whether TPM induces CYP3A4 in primary human hepatocytes and activates the human pregnane X receptor (hPXR), a nuclear receptor that serves as a regulator of CYP3A4 transcription. 
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