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Grapefruit–drug interactions that affect the pre-systemic metabolism (i.e., the metabolism that occurs before the drug enters the blood) of drugs have a different duration of action than interactions that work by other mechanisms, such as on absorption, discussed below.
That's why it's important to find out from your health care provider or a pharmacist if any of your medications interact with grapefruit. In addition, grapefruit can have the opposite effect on ...
"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".
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]
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The effect of grapefruit juice with regard to drug absorption was originally discovered in 1989. The first published report on grapefruit drug interactions was in 1991 in the Lancet entitled "Interactions of Citrus Juices with Felodipine and Nifedipine", and was the first reported food-drug interaction clinically. The effects of grapefruit last ...
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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]