Grapefruit-Drug Interactions

Seden, Kay; Dickinson, Laura; Khoo, Saye; Back, David

doi:10.2165/11585250-000000000-00000

Cited by 143 publications

(123 citation statements)

References 178 publications

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“…From previous studies, we know that GFJ can cause inhibition, which lasts for days, of various enzymes by both reversible and irreversible binding (42). Some of the biological effects may plateau even at doses of 300 ml/day.…”

Section: Discussionmentioning

confidence: 99%

Grapefruit juice and licorice increase cortisol availability in patients with Addison's disease

Methlie

Husebye

Hustad

et al. 2011

European Journal of Endocrinology

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Objective: Failure to mirror the diurnal cortisol profile could contribute to the impaired subjective health status in Addison's disease (AD). Some patients report benefit from the use of various nutritional compounds. The objective of this study was to investigate the impact of licorice and grapefruit juice (GFJ) on the absorption and metabolism of cortisone acetate (CA). Design: Patients (nZ17) with AD on stable CA replacement therapy were recruited from the outpatient clinic at Haukeland University Hospital, Norway. They were assessed on their ordinary CA medication and following two 3-day periods of co-administration of licorice or GFJ. Methods: Time series of glucocorticoids (GCs) in serum and saliva were obtained, and GCs in 24 h urine samples were determined. The main outcome measure was the area under the curve (AUC) for serum cortisol in the first 2.6 h after orally administered CA. Results: Compared with the ordinary treatment, the median AUC for serum cortisol increased with licorice (53 783 vs 50 882, P!0.05) and GFJ (60 661 vs 50 882, P!0.05). Median cortisol levels in serum were also elevated 2.6 h after tablet ingestion (licorice 223 vs 186 nmol/l, P!0.05; GFJ 337 vs 186 nmol/l, P!0.01). Licorice increased the median urinary cortisol/cortisone ratio (0.43 vs 0.21, P!0.00001), whereas GFJ increased the (allo-tetrahydrocortisolCtetrahydrocortisol)/tetrahydrocortisone ratio (0.55 vs 0.43, P!0.05).

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Section: Discussionmentioning

confidence: 99%

Grapefruit juice and licorice increase cortisol availability in patients with Addison's disease

Methlie

Husebye

Hustad

et al. 2011

European Journal of Endocrinology

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“…However, recent studies have now proven examples of foods that can alter the pharmacokinetics of drugs. For example grapefruit juice inhibits cytochrome P450 (CYP) 3A4 (CYP3A4), which results in increased bioavailability of drugs such as saquinavir, cyclosporine, and felodipine (Seden et al, 2010). Phytochemicals in grapefruit juice (such as bergamottin and quercetin) and green tea catechins inhibit the cellular efflux of P-gp substrates in vitro (Zhou et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

Calorie Restriction Increases P-Glycoprotein and Decreases Intestinal Absorption of Digoxin in Mice

Renaud

Klaassen

Csanaky

2016

Drug Metabolism and Disposition

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There is wide variation in how patients respond to therapeutics. Factors that contribute to pharmacokinetic variations include disease, genetics, drugs, age, and diet. The purpose of this study was to determine the effect of calorie restriction on the expression of Abcb1a in the intestine and whether calorie restriction can alter the absorption of an Abcb1a substrate (i.e., digoxin) in mice. Ten-week-old C57BL/6 mice were given either an ad libitum diet or a 25% calorie-restricted diet for 3 weeks. To determine digoxin absorption, mice were administered [ 3 H]-labeled digoxin by oral gavage. Blood and intestine with contents were collected at 1, 2, 4, and 12 hours after digoxin administration. Concentrations of [ 3 H]-digoxin in plasma and tissues were determined by liquid scintillation. Calorie restriction decreased plasma digoxin concentrations (about 60%) at 1, 2, and 4 hours after administration. Additionally, digoxin concentrations in the small intestine of calorie-restricted mice were elevated at 4 and 12 hours after administration. Furthermore, calorie restriction increased Abcb1a transcripts in the duodenum (4.5-fold) and jejunum (12.5-fold). To confirm a role of Abcb1a in the altered digoxin pharmacokinetics induced by calorie restriction, the experiment was repeated in Abcb1a/ b-null mice 4 hours after drug administration. No difference in intestine or plasma digoxin concentrations were observed between ad libitumfed and calorie-restricted Abcb1a/b-null mice. Thus, these findings support the hypothesis that calorie restriction increases intestinal Abcb1a expression, leading to decreased absorption of digoxin in mice. Because Abcb1a transports a wide variety of therapeutics, these results may be of important clinical significance.

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“…Relevant mechanisms include modulation of the activity of cytochrome P450 (CYP) 3A, organic anion transporting polypeptide (OATP) and P-glycoprotein [3][4][5][6][7].…”

Section: Pharmacologymentioning

confidence: 99%