Esterase inhibition by grapefruit juice flavonoids leading to a new drug interaction.

Dmd #13268 1 Esterase Inhibition Attribute of Grapefruit Juice Leading to a New Drug Interaction

Fruit juice inhibition of uptake transport: a new type of food-drug interaction.

A new type of interaction in which fruit juices diminish oral drug bioavailability through inhibition of uptake transport is the focus of this review. The discovery was based on an opposite to anticipated finding when assessing the possibility of grapefruit juice increasing oral fexofenadine bioavailability in humans through inhibition of intestinal MDR1-mediated efflux transport. In follow-up ...

Esterase inhibition attribute of grapefruit juice leading to a new drug interaction.

This report describes a newly identified potential of grapefruit juice (GFJ) in mediating pharmacokinetic drug interactions due to its capability to inhibit esterase. The study demonstrates that GFJ inhibits purified porcine esterase activity toward p-nitrophenyl acetate and the prodrugs lovastatin and enalapril. In rat and human hepatic or gut S9 fractions and rat gut lumen, GFJ inhibited the ...

Rapid Quantitation of Furanocoumarins and Flavonoids in Grapefruit Juice using Ultra-Performance Liquid Chromatography.

INTRODUCTION Grapefruit juice can increase or decrease the systemic exposure of myriad oral medications, leading to untoward effects or reduced efficacy. Furanocoumarins in grapefruit juice have been established as inhibitors of cytochrome P450 3A (CYP3A)-mediated metabolism and P-glycoprotein (P-gp)-mediated efflux, while flavonoids have been implicated as inhibitors of organic anion transport...

An overview of interactions between grapefruit juice and drugs

Because grapefruit contains fibre, vitamin C, antioxidants and phytochemicals, the fruit and its juice are consumed widely to help meet daily nutritional requirements. However, in the past 15 years, studies have shown that grapefruit juice can induce a several-fold increase in the plasma levels of particular drugs that can result in increased therapeutic or even toxic effects. The effect seems ...