8/16/2023 0 Comments Grapefruit juice interactionsPotential adverse events result from the enhanced bioavailability, i.e. However, routine intestinal biopsy for this purpose is impractical. Patients with higher levels of CYP3A4 determined in intestinal biopsies may require higher doses of corresponding drugs, the size of the Gr effect being generally higher in such patients. The interacting drugs are generally characterized by the oral intake, low to intermediate bioavailability, and inactivation by the CYP3A4 enzyme. The interaction between medications and Gr is drug specific and is not a class effect. Medications currently documented or predicted to augment the oral bioavailability if ingested with Gr are listed and include certain calcium channel blockers, beta blockers, analgesics, corticosteroids, estrogens, benzodiazepines, statins, anticancer, and antiallergic medications. Genetic variability of the enzymes can influence patients’ susceptibility to the effects of Gr, prediction being a potential field of future research. Apart from CYP3A4, constituents of Gr, for example, furanocoumarins or bergamottin, can inhibit other cytochrome P450 isoenzymes (CYP3A4, CYP2C9, and CYP2D6) and transporters in the intestine such as P-glycoproteins. Some sorts of sweet oranges do not cause the interaction. Bitter oranges, limes, and pomelos also produce such interactions although weaker than Gr. Although some studies have tested unusually high quantities, a usual amount (200-250 ml juice or a whole Gr) has sufficient potency to cause a pertinent pharmacokinetic interaction. This mechanism explains for the increase in the plasma concentration of certain orally taken drugs under the impact of Gr. CYP3A4 enzyme participates in the inactivation of various drugs it is located in the intestinal epithelium and the liver. The main Gr-drug interaction mechanism is inactivation of the enzyme CYP3A4 by furanocoumarins. Metabolites, having no desirable therapeutic action, may cause side effects. The enhanced bioavailability means that the same therapeutic effect is achieved by a lower dose and correspondingly lower levels of metabolites of the drug. Doses of analgesic, hormonal, psychoactive, immunosuppressive, and other medications should generally be kept as low as reasonably possible. According to the concept discussed in this letter, the Gr-drug interactions can be used to decrease drug dosages. This has been discussed as a reason for contraindications to the consumption of Gr during pharmacotherapy with the interacting drugs. It is known that Gr has the potential for interactions with certain drugs enhancing their bioavailability. Gr is a source of ascorbic and folic acid, magnesium, vitamin B6, and thiamin, which are supplied in greater proportion than the calories. Citrus fruits, along with tomatoes and potatoes, are major contributors of vitamin C to the American diet. Soviet citizens, who lived in conditions of relatively high prices and shortage of citrus fruits, grapefruit (Gr) in particular, know their value. Among others, the aim of this letter has been discussion of some publications that might create a biased vision and damage the trade and production of citrus fruit.
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