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Journal of Pharmaceutical and BioSciences

 
Year : 2021  |  Volume : 9  |  Issue : 4  |  Page : 49-71

Grapefruit and medications may be a deadly mix- An overview

M. Deepalakshmi, K.P. Arun, S. Ahuja
Grapefruit juice, which is widely consumed for its positive health benefits, can have severe, sometimes fatal, interactions with drugs. The co-administration of drugs with grapefruit juice can markedly elevate drug bioavailability, and can alter pharmacokinetic and pharmacodynamic parameters of the drug. In some instances, the interaction may have a beneficial effect by increasing drug efficacy or diminishing potential side effects. The mechanism for this interaction is the inhibition of cytochrome P-450 3A4 in the small intestine, resulting in a significant reduction of drug pre-systemic metabolism. An additional mechanism is, presumably, the inhibition of P-glycoprotein, a transporter that carries drug from the enterocyte back to the gut lumen, resulting in a further increase in the fraction of drug absorbed. Usual grapefruit intake inhibits only gut CYP3A; not liver CYP3A. Therefore, grapefruit does not normally affect medications given intravenously. Recent review found that more than 85 drugs can be affected by grapefruit juice. One whole grapefruit or 200 mL (about seven ounces) of juice can be enough to cause a clinically important interaction. The data available so far, concerning this interaction and its clinical implications, are reviewed in this article. By reviewing this in the future it will create awareness. There by optimal drug therapy can be achieved.
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