Corpus ID: 89485100

Grapefruit juice and saquinavir.

  title={Grapefruit juice and saquinavir.},
  author={James Js},
  journal={AIDS treatment news},
  • James Js
  • Published 1995
  • Chemistry
  • AIDS treatment news
: One problem with saquinavir is that it is poorly absorbed by the body because it is rapidly destroyed by cytochrome P456 3A4, a liver enzyme found in the intestinal wall. Studies show that properties in grapefruit juice inhibit this enzyme and increase saquinavir's efficiency. Published studies show similar results with other drugs. However, grapefruit juice's effects on drug bioavailability could vary greatly from person to person, and there is no commercially available test to measure… Expand
Grapefruit juice-drug interactions.
In vitro findings support the flavonoid, naringin, or the furanocoumarin, 6',7'-dihydroxybergamottin, as being active ingredients, but a recent investigation indicated that neither of these substances made a major contribution to grapefruit juice-drug interactions in humans. Expand
Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics.
There is relatively little data regarding the effects of CYP3A and P-gp on peptide drugs; however, studies with the cyclic peptide immunosuppresant cyclosporine as well as peptidomimetics provide some insight into the impact of these systems on the oral absorption of peptides. Expand
Utilizing in vitro and PBPK tools to link ADME characteristics to plasma profiles: case example nifedipine immediate release formulation.
Physiologically based pharmacokinetic (PBPK) modeling was used to simulate pharmacokinetics of a nifedipine immediate release formulation following concomitant grapefruit juice ingestion, and a link between the dissolution characteristics of the formulation and its in vivo performance could be established. Expand
Strategies to overcome simultaneous P-glycoprotein mediated efflux and CYP3A4 mediated metabolism of drugs.
The current review describes the background and summarises several proposed hypotheses in modifying oral bioavailability by various drug-inhibitor interactions and suggests that the function of these proteins may be complementary and may form a co-ordinated intestinal barrier. Expand
Enzyme‐ and transporter‐mediated beverage–drug interactions: An update on fruit juices and green tea
The multiple mechanisms through which beverages can alter drug disposition are highlighted and an update on the new findings of beverage–drug interactions is provided, with a focus on fruit juices and green tea. Expand