Table 2

Effect of eletriptan on the rate of decay of CYP3A4

TimeTreatment after Washout of Rifampicin2-a
UTELERIF
h
  02-b 155215521552
2411115111290
481033602724
7297und2180
  • und, below limit of detection.

  • 2-a Hepatocytes (culture FT142) were preinduced for 96 h with 10 μM rifampicin. The cells were then extensively washed with fresh culture medium to remove the inducer (washing-out) and the culture was allowed to continue for 72 h in the absence of treatment (UT), in the presence of 10 μM rifampicin (RIF), or in the presence of 25 μM eletriptan (ELE). After 24, 48, and 72 h, the levels of CYP3A4 protein were measured in microsomes prepared from the cells by immunoblot. Data reported represent the level of CYP3A4 in arbitrary units.

  • 2-b In control experiments, hepatocytes were cultured for 96 h in the absence of treatment or in the presence of 10 μM rifampicin or 25 μM eletriptan. The levels of CYP3A4 mRNA were UT, 2978; RIF, 20931; and ELE, 18200 (arbitrary units). The levels of CYP3A4 protein were UT, und; RIF, 1552; and ELE, 25.