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. These studies show that it is not advisable to drink grapefruit juice if you are taking any opioid drugs, including codeine, due to a risk of toxic levels.Grapefruit juice is consumed widely in today's health conscious world as a protector against cardiovascular diseases and cancers. It found that grapefruit increases the bioavailability of methadone in a patient and could result in a toxic level. A 2004 study published in “Clinical Pharmacology and Therapeutics” looked at the effects of grapefruit juice on CYP3A4 in patients taking methadone 3 4. The study showed that drinking grapefruit juice or eating a grapefruit can increase the concentrations of the drug in the body. A 2010 study published in “Basic and Clinical Pharmacology and Toxicology” looked at the effects of grapefruit juice and another opiate, oxycodone 3 4.
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The information contained on this site is for informational purposes only, and should not be used as a substitute for the advice of a professional health care provider. “Clinical Pharmacology and Therapeutics” Effects of Grapefruit Juice on the Pharmacokinetics of the Enantiomers of Methadone M.“Basic and Clinical Pharmacology and Toxicology” Grapefruit Juice Enhances the Exposure to Oral Oxycodone TH Nieminen et al.The Harvard Medical School Family Health Guide Grapefruit and Medication: A Cautionary Note February 2006.The sources cited below consist of evidence from peer-reviewed journals, prominent medical organizations, academic associations, and government data.
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