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The effects last because grapefruit-mediated inhibition of drug metabolizing enzymes, like CYP3A4, is irreversible; [30] that is, once the grapefruit has "broken" the enzyme, the intestinal cells must produce more of the enzyme to restore their capacity to metabolize drugs that the enzyme is used to metabolize. [19]
Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1.14.13.97) is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by CYP3A4 gene. It oxidizes small foreign organic molecules ( xenobiotics ), such as toxins or drugs, so that they can be removed from the body.
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 ...
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]
Grapefruit juice can act as an enzyme inhibitor, affecting the metabolism of drugs. In pharmaceutical sciences, drug interactions occur when a drug's mechanism of action is affected by the concomitant administration of substances such as foods, beverages, or other drugs.
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.
One interaction occurs from grapefruit furanocoumarins, such as bergamottin and 6',7'-Dihydroxybergamottin, which occur in both flesh and peel. Furanocoumarins inhibit the CYP3A4 enzyme (among others from the cytochrome P450 enzyme family responsible for metabolizing 90% of drugs). [22]
A small amount of 100% fruit juice, such as 100% orange or grapefruit juice, can also fit within healthy dietary patterns and help you meet your nutrient needs.