Benzodiazepines medazepam and midazolam are activators of pregnane X receptor and weak inducers of CYP3A4: Investigation in primary cultures of human hepatocytes and hepatocarcinoma cell lines

Abstract

We demonstrate that benzodiazepines medazepam and midazolam are activators of PXR nuclear receptor in transcriptional regulation of CYP3A4 as suggested in experiments on primary human hepatocytes and in HepG2 cells.

Keywords

• human hepatocytes
• cytochrome P450
• benzodiazepines
• enzyme induction