Effects of nifedipine on the pharmacokinetics of repaglinide in rats: Possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine

Choi, Jin‐Seok; Choi, In Young; Choi, Dong‐Hyun

doi:10.1016/s1734-1140(13)71502-0

Cited by 45 publications

(40 citation statements)

References 30 publications

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“…ABCB1, also known as P-glycoprotein, has been shown to play an important role in drug efflux 32) . Previous studies showed that resveratrol inhibited P-glycoprotein activity both in vitro 33) and in vivo 34) models. However, it is reported that the absorption of warfarin was independent of P-glycoprotein activity 35) .…”

Section: Discussionmentioning

confidence: 95%

<i>Trans</i>-Resveratrol Enhances the Anticoagulant Activity of Warfarin in a Mouse Model

Chiba

Kimura

Suzuki

et al. 2016

J Atheroscler Thromb

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Aim: Resveratrol is a popular ingredient in dietary supplements. Some patients concomitantly use dietary supplements and medicines in Japan. In the present study, we determined whether trans-resveratrol and melinjo (Gnetum gnemon L.) seed extract (MSE), which contains resveratrol dimers, interacted with drugs using a mouse model.Methods: Male C57BL/6J mice were fed experimental diets containing 0.005%, 0.05%, or 0.5% (w/w) trans-resveratrol or MSE for 1 or 12 weeks. The expression of liver cytochrome P-450 (CYP) mRNA and activity of liver microsomal CYP were measured. To determine the influence of resveratrol or MSE on drug efficacy, the anticoagulant activity of warfarin was examined in mice that were fed diets containing trans-resveratrol or MSE for 12 weeks.Results: When the mice were fed experimental diets for 1 week, none of the doses of trans-resveratrol and MSE affected body weight, liver weight, or plasma AST and ALT levels. Trans-resveratrol also did not affect CYP1A1, CYP1A2, CYP2C, or CYP3A activities. In contrast, 0.5% MSE slightly increased CYP1A1 activity. When the mice were fed experimental diets for 12 weeks, 0.05% trans-resveratrol increased CYP1A1, CYP2C, and CYP3A activities, whereas 0.5% MSE suppressed CYP3A activity. Under these conditions, 0.5% trans-resveratrol enhanced the anticoagulant activity of warfarin, although CYP2C activity increased. However, MSE did not affect the anticoagulant activity of warfarin.Conclusion: The 0.05% trans-resveratrol did not interact with warfarin in a mouse model, whereas 0.5% trans-resveratrol may have enhanced the anticoagulant activity of warfarin.

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Section: Discussionmentioning

confidence: 95%

<i>Trans</i>-Resveratrol Enhances the Anticoagulant Activity of Warfarin in a Mouse Model

Chiba

Kimura

Suzuki

et al. 2016

J Atheroscler Thromb

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“…For example, Choi et al found that RESV significantly reduced rhodamine123 efflux via P-gp in MCF-7/ADR cells that overexpress P-gp, and significantly increased the drug exposure of orally administered nicardipine in rats 28. In contrast, Yang et al reported that RESV exerted a stimulatory effect on P-gp, resulting in a reduction of cyclosporine oral bioavailability in rats 15.…”

Section: Discussionmentioning

confidence: 99%

Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats

Li¹,

Liu²,

Zhang³

et al. 2016

DDDT

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BackgroundThe intestinal cytochrome P450 3A (CYP 3A) and P-glycoprotein (P-gp) present a barrier to the oral absorption of saquinavir (SQV). Resveratrol (RESV) has been indicated to have modulatory effects on P-gp and CYP 3A. Therefore, this study was to investigate the effects of RESV on P-gp and CYP 3A activities in vitro and in vivo on oral SQV pharmacokinetics in rats.MethodsIn vitro, intestinal microsomes were used to evaluate RESV effect on CYP 3A-mediated metabolism of SQV; MDR1-expressing Madin–Darby canine kidney (MDCKII-MDR1) cells were employed to assess the impact of RESV on P-gp-mediated efflux of SQV. In vivo effects were studied using 10 rats randomly assigned to receive oral SQV (30 mg/kg) with or without RESV (20 mg/kg). Serial blood samples were obtained over the following 24 h. Concentrations of SQV in samples were ascertained using high-performance liquid chromatography-tandem mass spectrometry analysis.ResultsRESV (1–100 μM) enhanced residual SQV (% of control) in a dose-dependent manner after incubation with intestinal microsomes. RESV (1–100 μM) reduced the accumulation of SQV in MDCKII-MDR1 cells in a concentration-dependent manner. A double peaking phenomenon was observed in the plasma SQV profiles in rats. The first peak of plasma SQV concentration was increased, but the second peak was reduced by coadministration with RESV. The mean AUC0–∞ of SQV was slightly decreased, with no statistical significance probably due to the high individual variation.ConclusionRESV can alter the plasma SQV concentration profiles, shorten the Tmax of SQV. RESV might also cause a slight decrease tendency in the SQV bioavailability in rats.

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“…The small intestine is an important organ in the pharmacokinetics of orally administered drugs owing to the presence of drug transporters and drug-metabolizing enzymes (Choi et al, 2013;Li et al, 2013;Yoshida et al, 2013;Kostewicz et al, 2014). Thus, Caco-2 cells, a human colon carcinoma cell line, are widely used to evaluate the intestinal transport of orally administered drugs.…”

Section: Introductionmentioning

confidence: 99%

Characteristic Analysis of Intestinal Transport in Enterocyte-Like Cells Differentiated from Human Induced Pluripotent Stem Cells

Kodama

Iwao

Katano

et al. 2016

Drug Metabolism and Disposition

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We previously demonstrated that differentiated enterocytes from human induced pluripotent stem (iPS) cells exhibited drugmetabolizing activities and cytochrome P450 CYP3A4 inducibility. The aim of this study was to apply human iPS cell-derived enterocytes in pharmacokinetic studies by investigating the characteristics of drug transport into enterocyte-like cells. Human iPS cells cultured on feeder cells were differentiated into endodermal cells using activin A. These endodermal-like cells were then differentiated into intestinal stem cells by fibroblast growth factor 2. Finally, epidermal growth factor and small-molecule compounds induced the maturation of the intestinal stem cell-like cells. After differentiation, we performed transepithelial electrical resistance (TEER) measurements, immunofluorescence staining, and transport studies. TEER values increased in a time-dependent manner and reached approximately 100 V 3 cm 2 .Efflux transport of Hoechst 33342, a substrate of breast cancer resistance protein (BCRP), was observed and inhibited by the BCRP inhibitor Ko143. The uptake of peptide transporter 1 substrate glycylsarcosine was also confirmed and suppressed when the temperature was lowered to 4°C. Using immunofluorescence staining, villin and Na + -K + ATPase were expressed. These results suggest that human iPS cell-derived enterocytes had loose tight junctions, polarity, as well as uptake and efflux transport functions. In addition, the rank order of apparent membrane permeability coefficient (P app ) values of these test compounds across the enterocyte-like cell membrane corresponded to the fraction absorbance (F a ) values. Therefore, differentiated enterocytes from human iPS cells may provide a useful comprehensive evaluation model of drug transport and metabolism in the small intestine.

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Effects of nifedipine on the pharmacokinetics of repaglinide in rats: Possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine

Cited by 45 publications

References 30 publications

<i>Trans</i>-Resveratrol Enhances the Anticoagulant Activity of Warfarin in a Mouse Model

<i>Trans</i>-Resveratrol Enhances the Anticoagulant Activity of Warfarin in a Mouse Model

Effects of resveratrol on P-glycoprotein and cytochrome P450 3A in vitro and on pharmacokinetics of oral saquinavir in rats

Characteristic Analysis of Intestinal Transport in Enterocyte-Like Cells Differentiated from Human Induced Pluripotent Stem Cells

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