| Synonym |
| Thai / English name |
Part Used : น้ำจากผลActivity : DRUG INTERACTIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : CeliprololDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: The peak plasma concentration (Cmax) and the area under the plasma concentration-time curve from 0 to 8 h (AUC0-8) of celiprolol significantly decreased on day 1, and the mean ratios of these values and the corresponding control-day values were 0.18 and 0.25, respectively. The Cmax and AUC0-8 returned to the control levels on days 3 and 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : OATP (ORGANIC ANION TRANSPORTER PROTEIN) INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : CeliprololDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: The peak plasma concentration (Cmax) and the area under the plasma concentration-time curve from 0 to 8 h (AUC0-8) of celiprolol significantly decreased on day 1, and the mean ratios of these values and the corresponding control-day values were 0.18 and 0.25, respectively. The Cmax and AUC0-8 returned to the control levels on days 3 and 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
Part Used : น้ำจากผลActivity : CYP3A4 INHIBITIONSolvent/Active Compound : grapefruit juice (GFJ)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 7N(Treatment) : 7Sex : MaleAge : 21-24 yrs.Route : Oral administrationDose/Conc.(herb) : *Duration : 7 daysType of interaction : PharmacokineticsInteraction with drug : CeliprololDose/Conc.(drug) : -Result : PositiveRemark : *Dose: They were orally administered celiprolol (100 mg) with water on the control day. Three days later, they ingested GFJ (200 mL) 3 times a day for 3 d. On day 1, the same drugs were administered with GFJ. On days 3 and 7, the same drugs were administered with water. Pharmacokinetics of drug was evaluated on each trial day. Result: The peak plasma concentration (Cmax) and the area under the plasma concentration-time curve from 0 to 8 h (AUC0-8) of celiprolol significantly decreased on day 1, and the mean ratios of these values and the corresponding control-day values were 0.18 and 0.25, respectively. The Cmax and AUC0-8 returned to the control levels on days 3 and 7.Note : Conclusion: The OATP inhibition caused by GFJ dissipated faster than GFJ- mediated alterations in CYP3A4 activity, which were sustained for at least 48 h. Celiprolol and midazolam are substrated of OATP and CYP3A4.
