Some citrus fruits appear to have an effect on how the body metabolizes medications such as antibiotics, antidepressants, and antivirals, according to a recent study.
Grapefruit interacts with a variety of medications, altering absorption, distribution, metabolism, and excretion – Who is the most vulnerable?
Citrus fruits, particularly grapefruit, interact with a wide range of medications, from statins to antidepressants, affecting their pharmacokinetics, or the body’s absorption, distribution, metabolism, and excretion, and so decreasing their action.
In a study published in the Canadian Medical Association Journal (CMAJ), scientists revealed more than 85 drugs known to interact with grapefruit, the majority of which are licensed in Canada.
Many of the medications that interact with the popular citrus fruit are frequently prescribed and required for the treatment of common medical conditions. However, between 2008 and 2012, the number of medications that can cause major adverse effects (rhabdomyolysis, myelotoxicity, respiratory depression, gastrointestinal hemorrhage, nephrotoxicity, and the risk of sudden death) grew from 17 to 43. Researchers say that this can be traced back to the use of new drugs in medicine.
A review by Canadian researchers looked at how drug interactions with grapefruit affect people’s health. They focused on grapefruit since it is the most popular citrus fruit, but other citrus fruits can have comparable negative effects, as they explain.
Grapefruit and other citrus fruits influence drug absorption and action primarily through a class of chemicals called funarocoumarins, which suppress the activity of an enzyme that breaks down medicines in the body.
Under normal circumstances, this enzyme reduces the amount of the drug that enters the bloodstream explains Simon Maxwell, professor of clinical pharmacology at the University of Edinburgh and continues: “But if at the same time you drink grapefruit juice— or eat the fruit — the furanocoumarins stop this enzyme doing its job. This can be important for a number of widely prescribed drugs. This interaction partly occurs in the gut, enabling increased absorption, but also — significantly — in the liver, preventing it from progressively removing the drug in the hours after absorption. Together, this means that overall exposure to the drug can be significantly increased, resulting in toxic effects.”
It is a combination of actions that ultimately increases the overall exposure to the drug with a high risk of toxicity.
How dangerous is the grapefruit-drug interaction?
According to the study, doctors are reluctant to evaluate the possibility that the patient’s negative effects are caused by regular and systematic grapefruit consumption.
Who is most at risk from these interactions?
Despite the fact that the vulnerability of patients is unknown, grapefruit consumers over the age of 45 are the most common, and they also take a lot of medications, as the researchers point out. Furthermore, they claim that a substantial pharmacokinetic interaction has been observed in patients over the age of 70, implying that elderly adults are particularly prone to grapefruit and medication interactions.
All of the medicines that interact with grapefruit are taken orally, have a very low to moderate absolute bioavailability, and are processed by cytochrome P450 3A4 (CYP3A4), a key enzyme found mostly in the liver and intestine.
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