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Part Used : ไม่ระบุActivity : DRUG INTERACTIONSolvent/Active Compound :Type of experiment : humanType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : OmeprazoleDose/Conc.(drug) : -Result : PositiveRemark : Interaction reported with omeprazole in Chinese patients and fatal seizures in a patient on antieplilepsy medication. Caution if taken with warfarin, antiplatelet drugs, alprazolam, donezepil, trazodone, anticancer drugs.Note : Data incomplete, data from review article.
Part Used : ใบActivity : DRUG INTERACTIONSolvent/Active Compound : Ginkgo biloba extract (GBE)Type of experiment : humanType of animal : -Type of study : Open trialN(Total) : 40N(Treatment) : 40Sex : MaleAge : *Route : Oral administrationDose/Conc.(herb) : Two 60-mg capsules taken twice dailyDuration : 14 daysType of interaction : PharmacokineticsInteraction with drug : BupropionDose/Conc.(drug) : -Result : NegativeRemark : *Age: mean 21.3+/-1.4 yrs, range 19-25 yrs GB administration resulted in no significant effects on the AUC0-infinity value of bupropion and hydroxybupropion. Bupropion mean AUC0-infinity value was 1.4 microgram.h/ml-1 (95% Cl 1.2, 1.6) prior to GBE treatment and 1.2 microgram.h/ml-1 (95% Cl 1.1, 1.4) after 14 days of treatment. Hydroxybupropion mean AUC0-infinity value was 8.2 microgram.h/ml-1 (95% Cl 6.5, 10.4) before GBE administration and 8.7 microgram.h/ml-1 (95% Cl 7.1, 10.6) after treatment. The Cmax of hydroxybupropion increased from 221.8 nanogram/ml-1 (95% Cl 176.6, 278.6) to 272.7 nanogram/ml (95% Cl 215.0, 345.8) (p=0.038) and the t1/2 of hydroxybupropion fell from 25.0 h (95% Cl 22.7, 27.5) to 21.9 h (95% Cl 19.9, 24.1) (p=0.000).Note : - Healthy volunteers. - After an overnight fast, volunteers ingested a single oral dose of 150 mg sustained-release bupropion with water (150 ml). Blood samples for pharmacokinetic analysis were taken for 3 days post dose. Following a wash-out period of at least 7 days, volunteers took two 60-mg capsules (120 mg) of G. biloba twice daily for 14 days. On day 15, a single 15-mg oral dose of bupropion was then administered after overnight fasting. - The GBE, containing a minimum of 24% ginkgo flavones glycosides and 6% terpene lactone.
Part Used : ใบActivity : DRUG INTERACTIONSolvent/Active Compound : EGb761 (a standard form of the extract of Ginkgo biloba leaf)Type of experiment : in vivoType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : OtherDose/Conc.(herb) : The gerbils fed a standard diet were intragastrically given EGb761 (100 mg/kg/day) for one week and the gerbils were injected with MgSO4 (90 mg/kg), 30 min before MCAO*.Duration : -Type of interaction : PharmacodynamicsInteraction with drug : Magnesium sulfateDose/Conc.(drug) : Magnesium sulfate 90 mg/kg (MgSO4)Result : PositiveRemark : Result: The total infarct volumes of the four treated groups either EGb761 alone or in combination with drugs were lower than the control group by 36.1% (EGb761 alone), 40.3% (EGb761 + MgSO4), 35.3% (EGb761 + FK506), and 56.4% (EGb761 + MK-801), respectively (p < 0.01). The main affected areas of the brain in the four treated groups were significantly focused between 4 and 6 mm from the frontal pole, when compared to the control goups (p < 0.01). All animals in the five groups had infarctions in both cortex and subcortex. These results indicate that long-term pre-treatment of EGb761 administered either alone or in combination with drugs significantly effective neuroprotection on infarct volume in gerbil ischemic brains.Note : Type of animal: Gerbil. Rout: intragastric. *The infarct volume of male gerbils' brain induced by unilateral middle cerebral artery occlusion (MCAO).
Part Used : ใบActivity : DRUG INTERACTIONSolvent/Active Compound : EGb761 (a standard form of the extract of Ginkgo biloba leaf)Type of experiment : in vivoType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : OtherDose/Conc.(herb) : The gerbils fed a standard diet were intragastrically given EGb761 (100 mg/kg/day) for one week and the gerbils were injected with FK506 (0.5 mg/kg), 30 min before MCAO*.Duration : -Type of interaction : PharmacodynamicsInteraction with drug : TacrolimusDose/Conc.(drug) : Tacrolimus 0.5 mg/kg (FK506)Result : PositiveRemark : Result: The total infarct volumes of the four treated groups either EGb761 alone or in combination with drugs were lower than the control group by 36.1% (EGb761 alone), 40.3% (EGb761 + MgSO4), 35.3% (EGb761 + FK506), and 56.4% (EGb761 + MK-801), respectively (p < 0.01). The main affected areas of the brain in the four treated groups were significantly focused between 4 and 6 mm from the frontal pole, when compared to the control goups (p < 0.01). All animals in the five groups had infarctions in both cortex and subcortex. These results indicate that long-term pre-treatment of EGb761 administered either alone or in combination with drugs significantly effective neuroprotection on infarct volume in gerbil ischemic brains.Note : Type of animal: Gerbil. Rout: intragastric. *The infarct volume of male gerbils' brain induced by unilateral middle cerebral artery occlusion (MCAO).
Part Used : ใบActivity : DRUG INTERACTIONSolvent/Active Compound : EGb761 (a standard form of the extract of Ginkgo biloba leaf)Type of experiment : in vivoType of animal : otherType of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : OtherDose/Conc.(herb) : The gerbils fed a standard diet were intragastrically given EGb761 (100 mg/kg/day) for one week and the gerbils were injected with MK-801 (1 mg/kg), 30 min before MCAO*.Duration : -Type of interaction : PharmacodynamicsInteraction with drug : DizocilpineDose/Conc.(drug) : Dizocilpine 1 mg/kg (MK-801)Result : PositiveRemark : Result: The total infarct volumes of the four treated groups either EGb761 alone or in combination with drugs were lower than the control group by 36.1% (EGb761 alone), 40.3% (EGb761 + MgSO4), 35.3% (EGb761 + FK506), and 56.4% (EGb761 + MK-801), respectively (p < 0.01). The main affected areas of the brain in the four treated groups were significantly focused between 4 and 6 mm from the frontal pole, when compared to the control goups (p < 0.01). All animals in the five groups had infarctions in both cortex and subcortex. These results indicate that long-term pre-treatment of EGb761 administered either alone or in combination with drugs significantly effective neuroprotection on infarct volume in gerbil ischemic brains.Note : Type of animal: Gerbil. Rout: intragastric. *The infarct volume of male gerbils' brain induced by unilateral middle cerebral artery occlusion (MCAO).
Part Used : ใบActivity : DRUG INTERACTIONSolvent/Active Compound : Ethanol / ginkgolide A, Ginkolide C, bilobalide, quercetin, kaempferolType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : -Duration : -Type of interaction : PharmacokineticsInteraction with drug : Rifampicin*/RifampinDose/Conc.(drug) : -Result : PositiveRemark : 22 ethanol extracts and 8 compounds could activate human PXR and induce CYP3A4 reporter construct in HepG2 cells. Among them, Ginkgo biloba, Ligusticum chuanxiong, Chinese angelica, prepared Rehmannia root, Epimedium brevicornum, Atractylodes macrocephala, Schisandra chinensis, Paeonia lactifora, Ophiopogon japonicus, Polygonum multiflorum, Coptis chinensis, Artemisia scoparia, Trichosanthes kirilowii, Silybum marianum, Gardenia fruit and Lycium chinense could strongly trans-activate PXR. Moreover, ligustilide, schisantherin A, berberine hydrochloride and trans-resveratrol were identified for the first time as efficacious PXR agonists.Note : PXR = pregnane X receptor
Part Used : ไม่ระบุActivity : DRUG INTERACTIONSolvent/Active Compound : Ginkgo biloba extract*Type of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 100 microgram/ml (Lot A)Duration : -Type of interaction : PharmacokineticsInteraction with drug : Mifepristone*/RU486Dose/Conc.(drug) : 0.1 millimolarResult : NegativeRemark : Gingko biloba extract did not alter hCAR or hPXR mRNA expression. Whereas the extract (100 mg/ml) increased CYP2B6 mRNA and CYP2B6-mediated bupropion hydroxylation, the increase was not attenuated by the co-treatment with a hGR antagonist (0.1 mM miferpristone: RU486).. The same pattern of response was also obtained for CYP3A4 mRNA and CYP3A-mediated testosterone 6b-hydroxylation. Therefore, Ginkgo biloba extract induces CYP2B6 (a hCAR target gene) and CYP3A4 (a hPXR target gene) by a hGR-independent mechanism.Note : *Solvent/active compound: Ginkgo extract (Lot A) 200 micrgram/mL consist ginkogolide A, B, C, J and bilobalide as 2.2, 0.6, 2.8, 1.2 and 5.6 microgram/mL, respectively.
Part Used : ใบActivity : DRUG INTERACTIONSolvent/Active Compound : -Type of experiment : in vitroType of animal : otherType 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 Ginkgo extracts: 4.78% Quercetin, 3.73% Kaempferol, 2.13% Isorhamnetin, 12.0% Quercetin glycoside, 9.65% Kaempferol glycoside, 5.19% Isorhamnetin glycoside, 1.61% Bilobalide, 1.41% Ginkgolide A, 0.31% Ginkgolide J, 5.57% Ginkgolide B, 0.38% Ginkgolide C. - Results: The degree of CYP3A4 inhibition of Ginkgo biloba was 45.9% and IC50 values of that inhibit CYP3A4-mediated metabolism of midazolam = 75.1 microgram/ml, 95% Cl: 53.0-106.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 : ใบActivity : DRUG INTERACTIONSolvent/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 Ginkgo extracts: 4.78% Quercetin, 3.73% Kaempferol, 2.13% Isorhamnetin, 12.0% Quercetin glycoside, 9.65% Kaempferol glycoside, 5.19% Isorhamnetin glycoside, 1.61% Bilobalide, 1.41 Ginkgolide A, 0.31% Ginkgolide J, 5.57% Ginkgolide B, 0.38% Ginkgolide C. - Results: The degree of CYP3A4 inhibition of Ginkgo biloba was 45.1% and IC50 values of that inhibit CYP3A4-mediated metabolism of docetaxel = 155 microgram/ml, 95% Cl: 81.3-297.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 : ไม่ระบุActivity : DRUG INTERACTIONSolvent/Active Compound : ginkgolidesType of experiment : in vitroType of animal : -Type of study : -N(Total) : -N(Treatment) : -Sex : -Age : -Route : -Dose/Conc.(herb) : 0.1 - 10 micrograms/mLDuration : -Type of interaction : PharmacokineticsInteraction with drug : -Dose/Conc.(drug) : -Result : NegativeRemark : Within 0.1 to 10 micrograms/mL, the hydrolyzed ginkgolides showed direct inhibition against CYP1A2, 2B6,2C8,2C9,2C19,2D6,2E1,3A4m (midazolam as substrate) and 3A4t (testosterone as sustrate), with IC50 values determined to be 410 micrograms/mL (concentrations expressed as the sum of equivalent concentrations of ginkgolideA, B and K). For the metabolism-dependent inhibition studies, the preincubation of 30 min did not substantially alter the IC50 values when compared with the corresponding values in the direct inhibition studies. The activities and mRNA expression levels for CYP1A2 and 2B6 with in each drug-treated group (0.1, 1 and 10 micrograms/mL) were not affected after the 48-h incubation. For CYP3A4, the activity and mRNA expression level were not altered when incubated with 0.1 and 1 micrograms/mL of hydrolyzed ginkgolides. When incubated with hydrolyzed ginkgolides at 10 micrograms/mL, the relative activity and relative mRNA expression level of CYP3A4 remarkably increased to 4.59+/-3.67 and 17.2+/-9.16-fold of corresponding vehicle control values, respectively. The hydrolyzed ginkbolides is not likely to cause DDI via inhibition of the major human CYPs.Note : DDI = drug-drug interaction
