Traditionally grapefruit juice has been found to contain antioxidant, antinitrosaminic, antiseptic, aperitif, cardiotonic, detoxicant, hypocholesterolemic, sedative and stomachic activities. In fact, much of the enthusiasm in its use stems from medical research that has suggested that grapefruit juice reduces atherosclerotic plaque formation and inhibits breast cancer cell proliferation and mammary cell tumorigenesis. However, the wide consumption of grapefruit juice cannot entirely be attributed to its taste, and nutritive value. Grapefruit juice combines the sweet and tangy flavour of the orange and shaddock and also provides up to 69% of the RDA for vitamin C along with as many as 250 mg of Potassium. The three major types of grapefruit that exist today are white, pink/red and ruby/rio red varieties. Since the early part of the 20th century, mutant strains of white grapefruit have appeared with pink to slightly reddish colour, and have been propagated by citriculturists into several strains of grapefruit. The grapefruit, thought to be a cross between an orange and a shaddock, was developed in the West Indies in the early 1700s and first introduced to Florida in the 1820s. In this review, we have discussed the phytochemistry of grapefruit juice, the various drugs involved in the drug – grapefruit juice eraction with their mechanisms of action and have presented the clinical implications of these interactions. In the case of many drugs, the increased serum concentration has been found to be associated with increased frequency of dose dependent adverse effects. Most notable are its effects on the calcium channel antagonist and the statin group of drugs. By inhibiting these enzyme systems, grapefruit juice alters the pharmacokinetics of a variety of medications, leading to elevation of their serum concentrations. The P – glycoprotein pump, found in the brush border of the intestinal wall which transports many of these cytochrome P – 450 3A4 substrates, has also been implicated to be inhibited by grapefruit juice. It has however, been found to be an inhibitor of the intestinal cytochrome P – 450 3A4 system, which is responsible for the first pass metabolism of many drugs. Grapefruit juice is consumed widely in today's health conscious world as a protector against cardiovascular diseases and cancers.
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