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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 ...
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.
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 ...
Although knowing the true extent of systemic absorption (referred to as absolute bioavailability) is clearly useful, in practice it is not determined as frequently as one may think. The reason for this is that its assessment requires an intravenous reference ; that is, a route of administration that guarantees all of the administered drug ...
Because of this risk, avoiding grapefruit juice and fresh grapefruits entirely while on drugs is usually advised. [13] Other examples: Saint-John's wort, a common herbal remedy induces CYP3A4, but also inhibits CYP1A1, CYP1B1. [14] [15] Tobacco smoking induces CYP1A2 (example CYP1A2 substrates are clozapine, olanzapine, and fluvoxamine) [16]
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.