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

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

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

Our previous studies described a newly identified potential of grapefruit juice (GFJ) in mediating pharmacokinetic drug interactions due to its capability of esterase inhibition. The current study identifies the active components in GFJ responsible for its esterase-inhibitory effect. The esterase-inhibitory potential of 10 constitutive flavonoids and furanocoumarins toward p-nitrophenylacetate ...

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 ...

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 ...

Grapefruit juice and drug interactions. Exploring mechanisms of this interaction and potential toxicity for certain drugs.

Concomitant administration of grapefruit juice can increase the plasma concentration of numerous drugs in humans and decrease the concentration of a few others. Such elevations of drug plasma concentrations have, on occasion, resulted in adverse clinical effects. Increased concentrations are primarily mediated by chemicals in grapefruit juice, which inhibit the CYP 3A4 drug-metabolizing enzyme ...