Drug-proof grapefruit

Drug-proof grapefruit
Nature Biotechnology 31, 186 (2013)
http://www.nature.com/nbt/journal/v31/n3/full/nbt0313-186b.html

Citrus breeders at the University of Florida’s Citrus Research and Education Center display new varieties of grapefruit and pomelo hybrids that could resolve the problem of grapefruit/drug interactions.
The team developed the hybrid fruit as a cross between grapefruit and pummelo, a citrus species…

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Effect of grapefruit juice on cabergoline pharmacokinetics in patients with Parkinson’s disease
Clinical Pharmacology & Therapeutics 77, P84 (February 2005)
M. Nagai, et. al.
http://www.nature.com/clpt/journal/v77/n2/full/clpt2005325a.html

Background: Cabergoline is one of the synthetic ergoline dopamine agonists, which is widely used for the treatment of Parkinson’s disease (PD). Cytochrome P-450 (CYP) 3A4 contributes to metabolize Cabergoline. It has been well known that grapefruit juice inhibits CYP3A4 enzyme located in the gut wall. To investigate whether grapefruit juice influences the pharmacokinetics of cabergoline, plasma level of cabergoline in patients of PD was evaluated.

Methods: Five patients with PD treated with cabergoline were enrolled. Plasma concentrations of cabergoline before and after coadministration of grapefruit juice were evaluated. The plasma concentration of cabergoline was determined using a LC/MS/MS.

Results: The plasma concentration of cabergoline increased approximately 1.7 times, when grapefruit juice was taken together with cabergoline. Adverse events were not observed during this trial.

Conclusions: Coadministration of grapefruit juice with cabergoline increases bioavailability of cabergoline. A relatively large therapeutic window of cabergoline may allow the concomitant treatment with grapefruit juice, and this combination treatment may augment the antiparkisonian effect of cabergoline.

related:

http://www.npr.org/sections/thesalt/2016/11/14/491376510/grapefruit-and-salt-the-science-behind-this-unlikely-power-couple

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