Medicinal importance of grapefruit juice and its interaction with various drugs

Jawad Kiani, Sardar Z Imam

Grapefruit juice is consumed widely in today's health conscious world as a protector against cardiovascular diseases and cancers. 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. 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. By inhibiting these enzyme systems, grapefruit juice alters the pharmacokinetics of a variety of medications, leading to elevation of their serum concentrations. Most notable are its effects on the calcium channel antagonist and the statin group of drugs. In the case of many drugs, the increased serum concentration has been found to be associated with increased frequency of dose dependent adverse effects. In this review, we have discussed the phytochemistry of grapefruit juice, the various drugs involved in the drug - grapefruit juice reaction with their mechanisms of action and have presented the clinical implications of these interactions.