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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.
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]
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. A popular example of drug–food interaction is the effect of grapefruit on the metabolism of drugs .
Grapefruit–drug interactions are common, as the juice contains furanocoumarins that interfere with the metabolism of many drugs. This can prolong and intensify the effects of those drugs, leading to multiple side-effects such as abnormal heart rhythms, bleeding inside the stomach, low blood pressure, difficulty breathing, and dizziness.
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 ...
Ingestion of naringin and related flavonoids can also affect the intestinal absorption of certain drugs, leading to either an increase or decrease in circulating drug levels. To avoid interference with drug absorption and metabolism, the consumption of citrus (especially grapefruit) and other juices with medications is advised against. [7]
Furanocoumarins have other biological effects as well. 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 ...
Naringenin is a flavanone from the flavonoid group of polyphenols. [2] It is commonly found in citrus fruits, especially as the predominant flavonone in grapefruit. [2]The fate and biological functions of naringenin in vivo are unknown, remaining under preliminary research, as of 2024. [2]