Search results for "Peak concentration"

showing 2 items of 2 documents

Pharmacokinetic interaction between efavirenz and ketoconazole in rats

2009

It is well known that efavirenz and ketoconazole act as an inducer and inhibitor of CYP3A4, respectively. As a result of these actions, co-administration of these drugs may result in changes in the pharmacoki- netic parameters of one or both of them. 2. Duodenum-cannulated rats have been used to compare the effect of intraduodenal (KC i.d. ) and intrave- nous administration of ketoconazole (KC i.v. ) on the pharmacokinetics of efavirenz after intraduodenal administration, as well as the potential effect of efavirenz as a CYP450 inducer on ketoconazole phar - macokinetic profile. 3. While KC i.v. did not show any significant effect on efavirenz pharmacokinetic profile, KC i.d. increased sig-…

CyclopropanesMalemedicine.medical_specialtyAntifungal AgentsEfavirenzAnti-HIV AgentsHealth Toxicology and MutagenesisPharmacologyToxicologyBiochemistryEnteral administrationDrug Administration SchedulePeak concentrationchemistry.chemical_compoundCytochrome P-450 Enzyme SystemPharmacokineticsimmune system diseasesInternal medicinemedicineAnimalsCytochrome P-450 CYP3ACytochrome P-450 Enzyme InhibitorsDrug InteractionsInducerRats WistarPharmacologyCYP3A4Chemistryvirus diseasesGeneral MedicineBenzoxazinesRatsKetoconazoleEndocrinologyAlkynesKetoconazolePharmacokinetic interactionmedicine.drugXenobiotica
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Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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