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Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : ginsenoside Rh1Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 10-100 micromolars of Rh1Duration : 10 min incubationType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Rh1 exhibited competitive inhibition of the activity of CYP3A4 with Ki values of 57.7+/-9.6 micromolarNote : Type of experiment: Human livers were obtained from three Chinese autopsy sample (males, ages 27, 29 and 42 years). Conclusion: The degradation of ginsenosides in the gastrointestinal tract may play an important role in the ginseng-associated drug-drug interactions, but the effects might be not due to Rh1 and F1.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : ginsenoside F1Type of experiment : -Type of animal : -Type of study : -N(Total) : NSN(Treatment) : NSSex : MaleAge : 27, 29, and 42 yrs.Route : -Dose/Conc.(herb) : 10-100 micromolars of F1Duration : 10 min incubationType of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: Rb1 exhibited competitive inhibition of the activity of CYP3A4 with Ki values of 67.8+/-16.2 micromolarNote : Type of experiment: Human livers were obtained from three Chinese autopsy sample (males, ages 27, 29 and 42 years). Conclusion: The degradation of ginsenosides in the gastrointestinal tract may play an important role in the ginseng-associated drug-drug interactions, but the effects might be not due to Rh1 and F1.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 12 (M/F=6/6)N(Treatment) : 12 (M/F=6/6)Sex : Both sexAge : 67+/-5.2 yrs.Route : Oral administrationDose/Conc.(herb) : 500 mg three times daily (standardized to 50% ginsenosides)Duration : 28 daysType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : 8 mgResult : NegativeRemark :Note : Twelve healthy volunteers were randomly assigned to receive each botanical supplement for 28 days followed by a 30-day washout period. Probe drug cocktails of midazolam, caffeine, chlorzoxazone and debrisoquine were administered before (days -1, 0) and at the end of supplementation (days 27, 28). Pre- and post-supplementation phenotypic ratios were determined for CYP3A4, CYP1A2, CYP2E1 and CYP2D6 using 1-hydroxymidazolam/midazolam serum ratios (1-hour), paraxanthine/caffeine serum ratios (6-hour), 6-hydroxychlorzoxazone/chlorzoxazone serum ratios (2-hour) and debrisoquine urinary recovery ratios (8-hour), respectively.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : GinsenosidesType of experiment : in vivoType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : PhenelzineDose/Conc.(drug) : -Result : PositiveRemark : Suspected potentiation of phenelzine and nifedipine (a CYP3A4 substrate) in animal study. Enzyme-selective effects on other CYP's depend on nature of extract. Ginsenosides inhibit P-gp at high concentrations. Avoid with MAOI's nifedipine, and in cancer chemotherapy.Note : Data incomplete, data from review article.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound : GinsenosidesType of experiment : in vivoType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : NifedipineDose/Conc.(drug) : -Result : PositiveRemark : Suspected potentiation of phenelzine and nifedipine (a CYP3A4 substrate) in animal study. Enzyme-selective effects on other CYP's depend on nature of extract. Ginsenosides inhibit P-gp at high concentrations. Avoid with MAOI's nifedipine, and in cancer chemotherapy.Note : Data incomplete, data from review article.
Part Used : เหง้าActivity : CYP3A4 INHIBITIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 25 microgram/mlDuration : 5 minutesType of interaction : PharmacokineticsInteraction with drug : Midazolam*/Versed/DormicumDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Ginseng extracts: 0.44% Eleutheroside E, 0.25% Eleutheroside B. - Results: The degree of CYP3A4 inhibition of Ginseng was 14.8%Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
Part Used : เหง้าActivity : CYP3A4 INHIBITIONSolvent/Active Compound :Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 100 microgram/mlDuration : 30 minutesType of interaction : PharmacokineticsInteraction with drug : Docetaxel*/TaxotereDose/Conc.(drug) : -Result : PositiveRemark : - Details of the standardized Ginseng extracts: 0.44% Eleutheroside E, 0.25% Eleutheroside B. - Results: The degree of CYP3A4 inhibition of Ginseng was 16.8%.Note : The effects of complementary and alternative medicine (CAM) on CYP3A4-mediated metabolism of midazolam and docetaxel were determined in human liver microsomes (HLM), using liquid-chromatography coupled to tandem mass spectrometry (LC-MS/MS).
Part Used : รากActivity : CYP3A4 INHIBITIONSolvent/Active Compound : 20(S)-ginsenoside F1 (20(S)-GF1), ginsenoside Rh1(Rh1)Type of experiment : in silicoType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : PositiveRemark : Result: 20 (S)-GF1 interacted with Arg212 and Arg106 via two hydrogen bonds, while there was no potential interaction except Van der Waals between Rh1 and CYP3A4.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound :Type of experiment : in vivoType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : Non-specifiedDose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : PhenelzineDose/Conc.(drug) : -Result : PositiveRemark : Suspected potentiation of phenelzine and nifedipine (a CYP3A4 substrate) in animal study. Enzyme-selective effects on other CYP's depend on nature of extract. Ginsenosides inhibit P-gp at high concentrations. Avoid with MAOl's, nifedipine, and in cancer chemotherapy. P. quinquefolius reduced effects of warfarin in healthy volunteers, but P. ginseng had no effect.Note : Data from review, data incomplete.
Part Used : ไม่ระบุActivity : CYP3A4 INHIBITIONSolvent/Active Compound :Type of experiment : in vivoType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : Non-specifiedDose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : NifedipineDose/Conc.(drug) : -Result : PositiveRemark : Suspected potentiation of phenelzine and nifedipine (a CYP3A4 substrate) in animal study. Enzyme-selective effects on other CYP's depend on nature of extract. Ginsenosides inhibit P-gp at high concentrations. Avoid with MAOl's, nifedipine, and in cancer chemotherapy. P. quinquefolius reduced effects of warfarin in healthy volunteers, but P. ginseng had no effect.Note : Data from review, data incomplete.
