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grapefruit juice-mediated inhibition of enzymes that metabolize the drug to an inactive metabolite leads to too high doses of the drug in the body [27] grapefruit juice-mediated inhibition of membrane transport proteins from the intestine to the blood, or inhibition of enzymes that activates a prodrug to an active metabolite leads to ...
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 ...
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. However, some current research is focused on the potential benefits of cytochrome P450 inhibition. [ 3 ]
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]
Furanocoumarins in grapefruit juice (i.e. bergamottin and dihydroxybergamottin) inhibit the cytochrome P450 enzyme CYP3A4, which is involved in the metabolism of most statins (however, it is a major inhibitor of only lovastatin, simvastatin, and to a lesser degree, atorvastatin) and some other medications [129] (flavonoids (i.e. naringin) were ...
Grapefruit can inhibit CYP3A4. Therefore, grapefruit can block the metabolism of Cialis, and more of the drug enters the body’s circulation. Grapefruit has been known to cause similar effects ...
Grapefruit juice raises the bioavailability of carbamazepine by inhibiting the enzyme CYP3A4 in the gut wall and in the liver. [5] Lower levels of carbamazepine are seen when administered with phenobarbital , phenytoin , or primidone , which can result in breakthrough seizure activity.
6',7'-Dihydroxybergamottin is a natural furanocoumarin found in pomelos, grapefruits, and sour oranges, [1] in both the peel and the pulp. Along with the chemically related compound bergamottin, it is believed to be responsible for a number of grapefruit–drug interactions, in which the consumption of citrus containing one or both of these compounds (especially grapefruit) affects the ...