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[19] [31] For drugs recently sold on the market, drugs have information pages (monographs) that provide information on any potential interaction between a medication and grapefruit juice. [19] Because there is a growing number of medications that are known to interact with citrus, [ 1 ] patients should consult a pharmacist or physician before ...
For example, when the blood pressure drug felodipine is taken with grapefruit juice rather than water, levels of the medication in the blood can more than double and result in headache, irregular ...
The effects of grapefruit last from 3–7 days, with the greatest effects when juice is taken an hour previous to administration of the drug. [25] In addition to grapefruit, other fruits have similar effects. Noni (Morinda citrifolia), for example, is a dietary supplement typically consumed as a juice and also inhibits CYP3A4. [26]
A single report has been made of grapefruit juice possibly increasing the effects of cilostazol; [9] some drug information sources list this as a possible interaction. [10] [11] [12] The FDA-approved labeling of cilostazol notes that grapefruit juice (which is a CYP3A4 inhibitor) increases the drug's maximum concentration by around 50%. [7]
Grapefruit and grapefruit juice have been found to interact with numerous drugs, in many cases resulting in adverse effects. [4] This happens in two ways: one is that grapefruit can block an enzyme which metabolizes medication, [5] and if the drug is not metabolized, then the level of the drug in the blood can become too high, leading to an adverse effect. [5]
This prevents oxidative metabolism of certain drugs by the enzyme, resulting in an elevated concentration of drug in the bloodstream. Under normal circumstances, the grapefruit juice effect is considered to be a negative interaction, and patients are often warned not to consume grapefruit or its juice when taking medication.
"Indiana University Department of Medicine Clinical Pharmacology Drug Interactions Flockhart Table ™". "INHIBITORS, INDUCERS AND SUBSTRATES OF CYTOCHROME P450 ISOZYMES". "The Life Raft Group: Long List of Inhibitors and Inducers of CYP3A4 and CYP2D6". "DRUGBANK Online: Cytochrome P-450 Enzyme Inhibitors".
For example, in humans, bergamottin and 6',7'-dihydroxybergamottin are responsible for the "grapefruit juice effect", in which these furanocoumarins affect certain P450 liver and gut enzymes, such as the inhibition of CYP3A4 which either activates or deactivates many drugs, thus leading to higher or lower levels in the bloodstream. [12]