The interaction effect of grapefruit juice is maximal after the first glass

Lundahl, Jonas; Regårdh, C G; Edgar, Boo; Johnsson, G.

doi:10.1007/s002280050424

Cited by 55 publications

(40 citation statements)

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“…Despite results that demonstrated higher intensity after repeated ingestions (Lilja et al, 2000a), it appears that in most cases, ingestion of a single glass (250 ml) of regular strength grapefruit juice is enough to produce the maximum effect (Rau et al, 1997;Kane & Lipsky, 2000). In this fashion, no further changes in the pharmacokinetics of felodipine have been detected following 14 days of daily intake of grapefruit juice, compared to the effects after the first glass (Lundahl et al, 1998).…”

Section: Amounts and Timingmentioning

confidence: 89%

“…Numerous studies were performed in order to investigate the interaction between grapefruit juice and these agents since the interaction was first discovered with the dihydropyridine felodipine. These studies showed increases of up to 300% in AUC and up to 430% in C max of felodipine (Bailey et al, 1991;Edgar et al, 1992;Dresser et al, 2000), as well as increase in the serum concentrations of the metaboliteFdehydrofelodipine (Bailey et al, 1995;Lundahl et al, 1998). It should be noted that an especially pronounced pharmacokinetic effect has been detected among elderly subjects .…”

Section: Amounts and Timingmentioning

confidence: 98%

“…It should be noted that an especially pronounced pharmacokinetic effect has been detected among elderly subjects . Most of these studies reported further decreases in diastolic blood pressure when felodipine was taken with grapefruit juice, as well as increase in haemodynamic-related adverse effects such as increased heart rate and orthostatic hypotension (Bailey et al, 1991;Lundahl et al, 1997Lundahl et al, , 1998. Other dihydropyridines exhibiting the interaction to a similar extent are nisoldipine (Bailey et al, 1993b;Takanaga et al, 2000) and nicardipine .…”

Section: Amounts and Timingmentioning

confidence: 99%

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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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Section: Amounts and Timingmentioning

confidence: 89%

Section: Amounts and Timingmentioning

confidence: 98%

Section: Amounts and Timingmentioning

confidence: 99%

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

2003

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“…Grapefruit juice increases the plasma concentrations of drugs that are substrates for CYP3A4 (e.g., felodipine, triazolam, midazolam, terfenadine, cyclosporine, nifedipine, and diazepam) (Bailey et al, 1998b;Lundahl et al, 1998;Edwards et al, 1999;Mohri et al, 2000), CYP1A2 (e.g., caffeine) (Fuhr et al, 1993), and CYP2A6 (e.g., coumarin) (Merkel et al, 1994). In humans, grapefruit juice exposure decreases concentrations of intestinal CYP3A4 Schmiedlin-Ren et al, 1997), does not effect CYP3A5, CYP1A1, CYP2D6 protein, or CYP3A4 mRNA , and inhibits P-glycoprotein activity (Sawada et al, 1998;Eagling et al, 1999;Edwards et al, 1999).…”

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confidence: 99%

The Effect of Bergamottin on Diazepam Plasma Levels and P450 Enzymes in Beagle Dogs

Sahi¹,

Reyner²,

Bauman³

et al. 2002

Drug Metab Dispos

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This paper is available online at http://dmd.aspetjournals.org ABSTRACT:Bergamottin, a furanocoumarin isolated from grapefruit juice, was investigated for the ability to increase diazepam bioavailability and for its effect on cytochrome P450 (P450) enzymes in the beagle dog liver and intestine. To study the effect of bergamottin on diazepam pharmacokinetics, male beagle dogs were dosed with bergamottin In hepatic microsomes, bergamottin treatment for 10 days reduced the activity of CYP3A12 by 50% and CYP1A1/2 by 75%. Tolbutamide hydroxylase activity did not change, and CYP2B11 activity was moderately induced. In jejunal microsomes, CYP3A12 activity doubled with bergamottin treatment. CYP2B11, CYP1A1/2 activity and tolbutamide hydroxylation was not detected. In conclusion, bergamottin is both an inhibitor and an inducer of P450 enzymes.

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“…Given that grapefruit juice decreases serum itraconazole concentrations in humans by a mechanism that remains to be determined (12), that voriconazole is structurally related to itraconazole, and that there is an important pharmacokinetic interaction between voriconazole and grapefruit juice in the mouse, studies of this potential interaction in humans are warranted. Patients taking voriconazole should be instructed to avoid drinking grapefruit juice (8) until further information concerning the potential interaction is available.…”

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confidence: 99%

Efficacy of Voriconazole in Treatment of Murine Pulmonary Blastomycosis

Sugar

Liu

2001

Antimicrob Agents Chemother

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We evaluated the efficacy of voriconazole, a new broad-spectrum triazole antifungal compound, in the treatment of murine pulmonary blastomycosis. Since mice metabolize voriconazole rapidly, we took advantage of our previous observation that administration of grapefruit juice to mice resulted in suitable serum voriconazole concentrations so that treatment studies with mice could be done (A. M. Sugar and X.-P. Liu, Med. Mycol. 38:209-121, 2000). Our results show that voriconazole prolonged survival in a dose-dependent fashion and that the fungal burden in the lungs was decreased by voriconazole administered at 40 mg/kg of body weight/day. Voriconazole should be studied in humans with blastomycosis.Blastomycosis is a fungal infection that occurs primarily in specific areas of the United States. While several antifungals have been useful in the treatment of patients with the disease, including itraconazole, amphotericin B, and fluconazole, additional options would be welcome. In the study described here, we used a well-described murine model of pulmonary blastomycosis to evaluate the antifungal efficacy of voriconazole, a new broad-spectrum triazole antifungal drug (5-7, 10).Early work with voriconazole documented that serum voriconazole concentrations were very low to undetectable in mice. This necessitated a switch to other animals, such as guinea pigs, in order to continue the preclinical development of voriconazole. Unfortunately, guinea pigs are resistant to the development of pulmonary blastomycosis. We then found that grapefruit juice could increase the concentrations of voriconazole in serum in the mouse to suitable levels to conduct treatment studies (14). In the present study, we made use of this pharmacokinetic interaction to study the efficacy of voriconazole in the treatment of murine pulmonary blastomycosis.Male specific-pathogen-free BALB/cByJ mice were obtained from Jackson Laboratories. Mice were housed at 10 mice per cage. They were fed mouse chow and water ad libitum. Five days before infection, the water was replaced with grapefruit juice in the water bottle and was provided to the mice ad libitum. On average, mice ingested 2 to 3 ml of grapefruit juice/day, as determined in our previous study (14).Blastomyces dermatitidis ATCC 26199 was obtained as a new culture from the American Type Culture Collection (Manassas, Va.) and was maintained in the yeast form in 1% sterile milk in yeast nitrogen broth at Ϫ70°C. Prior to an experiment, a loopful was plated on blood agar and the plate was incubated at 37°C for 4 to 6 days. A 4-to 6-day growth from a subculture of this was used to prepare inocula for infection of mice.The susceptibility of the yeast form of B. dermatitidis to voriconazole was tested according to NCCLS guidelines (11), using the microtiter plate format. The (MIC) was read at 48 h and was defined as the first clear well. The minimal fungicidal concentration (MFC) was obtained by culturing the entire contents of the clear wells, with the well showing no growth representing the MFC. The pu...

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The interaction effect of grapefruit juice is maximal after the first glass

Cited by 55 publications

References 13 publications

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

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

The Effect of Bergamottin on Diazepam Plasma Levels and P450 Enzymes in Beagle Dogs

Efficacy of Voriconazole in Treatment of Murine Pulmonary Blastomycosis

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