The grapefruit: an old wine in a new glass? Metabolic and cardiovascular perspectives

Cardiovasc J Afr. Sep-Oct 2010;21(5):280-5. doi: 10.5830/cvja-2010-012.

Abstract

Grapefruit is a popular, tasty and nutritive fruit enjoyed globally. Biomedical evidence in the last 10 years has, however, shown that consumption of grapefruit or its juice is associated with drug interactions, which, in some cases, have been fatal. Grapefruit-induced drug interactions are unique in that the cytochrome P450 enzyme CYP3A4, which metabolises over 60% of commonly prescribed drugs as well as other drug transporter proteins such as P-glycoprotein and organic cation transporter proteins, which are all expressed in the intestines, are involved. However, the extent to which grapefruit-drug interactions impact on clinical settings has not been fully determined, probably because many cases are not reported. It has recently emerged that grapefruit, by virtue of its rich flavonoid content, is beneficial in the management of degenerative diseases such as diabetes and cardiovascular disorders. This potentially explosive subject is reviewed here.

Publication types

  • Review

MeSH terms

  • Beverages
  • Cardiovascular Diseases / drug therapy*
  • Citrus paradisi*
  • Cytochrome P-450 CYP3A / metabolism
  • Cytochrome P-450 Enzyme System / metabolism
  • Diabetes Mellitus / drug therapy*
  • Flavanones / pharmacology
  • Food-Drug Interactions* / physiology
  • Humans
  • Intestinal Mucosa / metabolism
  • Metabolic Syndrome / drug therapy*
  • Metabolic Syndrome / metabolism
  • Phytotherapy*

Substances

  • Flavanones
  • Cytochrome P-450 Enzyme System
  • Cytochrome P-450 CYP3A
  • CYP3A4 protein, human