Effect of grapefruit juice on pharmacokinetics and pharmacodynamics of verapamil enantiomers in healthy volunteers

Ho, Ping-Chuen; Ghose, Karabi; Saville, Dorothy J.; Wanwimolruk, Sompon

doi:10.1007/s002280000189

Cited by 63 publications

(28 citation statements)

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“…Although inhibitors of P-glycoprotein have been developed as a way to overcome multidrug resistance, rapid drug metabolism may be one of the factors influencing the effect of treatment. 24 It should be noticed that there were no significant differences in IC 50 the daunorubicin + wogonin and daunorubicin-wogonin magnetic nanoparticle groups at 24 hours, but this situation changed at 48 hours and 72 hours, when the IC 50 of daunorubicin in the daunorubicin-wogonin magnetic nanoparticle group was obviously lower than that in the daunorubicin + wogonin group. Possible reasons for this phenomenon might be that a large proportion of wogonin in the daunorubicin + wogonin group may have been metabolized to a residue which could inhibit P-glycoprotein further, and there is some evidence in the literature to support this, 25 and the sustained-release properties of daunorubicin-wogonin magnetic nanoparticles might enable continuous release of the chemosensitizing agent, instead of rapid metabolism, and much more daunorubicin was released continuously from the copolymer after 24 hours.…”

Section: Discussionmentioning

confidence: 86%

Effect of magnetic nanoparticles of Fe3O4 and wogonin on the reversal of multidrug resistance in K562/A02 cell line

Chen¹

2012

IJN

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Background: Multidrug resistance is the main obstacle to the efficiency of systemic chemotherapy against hematologic malignancy. This study investigated the reversible effect of the copolymer wogonin and daunorubicin coloaded into Fe 3 O 4 magnetic nanoparticles, and the mechanism potentially involved. Methods: The growth inhibition rate of K562/A02 cells was investigated by MTT assay, and apoptosis of cells and the intracellular daunorubicin concentration were detected by flow cytometry. Distribution of nanoparticles taken up by K562/A02 cells was observed under a transmission electron microscope and demonstrated by Prussian blue staining. The transcription level of MDR1 mRNA and expression of P-glycoprotein were determined by reverse transcriptase polymerase chain reaction and Western blotting assay, respectively. Results: The reversible effect of daunorubicin-wogonin magnetic nanoparticles was 8.87-fold that of daunorubicin + wogonin and of daunorubicin magnetic nanoparticles. Transmission electron microscopy and Prussian blue staining revealed that the nanoparticles were located in the endosome vesicles of cytoplasm. Also, the apoptosis rate and accumulation of intracellular daunorubicin in the daunorubicin-wogonin magnetic nanoparticle group were significantly higher than that in the daunorubicin, daunorubicin + wogonin, and daunorubicin magnetic nanoparticle groups. Furthermore, transcription of MDR1 mRNA and expression of P-glycoprotein in K562/ A02 cells were significantly downregulated in the daunorubicin-wogonin magnetic nanoparticle group compared with the other groups. Conclusion: These findings suggest that the remarkable effects of the novel daunorubicinwogonin magnetic nanoparticle formulation on multidrug resistant K562/A02 leukemia cells would be a promising strategy for overcoming multidrug resistance.

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Section: Discussionmentioning

confidence: 86%

Effect of magnetic nanoparticles of Fe3O4 and wogonin on the reversal of multidrug resistance in K562/A02 cell line

Chen¹

2012

IJN

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“…A significant increase in the bioavailability of verapamil has been detected in recent studies (Ho et al, 2000;Fuhr et al, 2002), in contrast to an earlier investigation which observed no effect (Zaidenstein et al, 1998). Diltiazem has been found to produce no interaction with grapefruit juice in a single study (Sigusch et al, 1994), and further investigations are needed.…”

Section: Amounts and Timingmentioning

confidence: 81%

Food–drug interaction: grapefruit juice augments drug bioavailability—mechanism, extent and relevance

2003

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More than a decade has passed since it was unintentionally discovered that grapefruit juice interacts with certain drugs. The coadministration of these drugs with grapefruit juice can markedly elevate drug bioavailability, and can alter pharmacokinetic and pharmacodynamic parameters of the drug. The predominant mechanism for this interaction is the inhibition of cytochrome P-450 3A4 in the small intestine, resulting in a significant reduction of drug presystemic metabolism. An additional mechanism is, presumably, the inhibition of P-glycoprotein, a transporter that carries drug from the enterocyte back to the gut lumen, resulting in a further increase in the fraction of drug absorbed. Some calcium channel antagonists, benzodiazepines, HMG-CoA reductase inhibitors and cyclosporine are the most affected drugs. A single exposure to one glass of the juice can usually produce the maximal magnitude of the interaction. The data available so far, concerning this interaction and its clinical implications, are reviewed in this article. It is likely that more information regarding this interaction will accumulate in the future, and awareness of such is necessary for achieving optimal drug therapy.

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“…Studies that have explored the effect of grapefruit juice on diltiazem and verapamil have not reported changes in blood pressure or heart rate, despite increases in systemic drug concentrations. [42][43][44] Alcohol ingestion appears to have variable effects on the antihypertensive effects of CCBs, and intake should be limited. In addition, diltiazem and verapamil are weak inhibitors of CYP3A4, and drug interactions with HMG-CoA inhibitors, which will be discussed later, have been documented.…”

Section: Calcium Channel Blockers Mostmentioning

confidence: 99%

Drug Interactions of Medications Commonly Used in Diabetes

Triplitt¹

2006

Diabetes Spectrum

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Effect of grapefruit juice on pharmacokinetics and pharmacodynamics of verapamil enantiomers in healthy volunteers

Abstract: The present study has demonstrated an interaction between verapamil and grapefruit juice, which is likely due to an inhibition of intestinal metabolism resulting in increased oral bioavailability.

Cited by 63 publications

References 0 publications

Effect of magnetic nanoparticles of Fe3O4 and wogonin on the reversal of multidrug resistance in K562/A02 cell line

Effect of magnetic nanoparticles of Fe3O4 and wogonin on the reversal of multidrug resistance in K562/A02 cell line

Food–drug interaction: grapefruit juice augments drug bioavailability—mechanism, extent and relevance

Drug Interactions of Medications Commonly Used in Diabetes

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