Does the grapefruit-drug interaction increase?

Dr.David Bailey of the Lawson Institute for Health Research in London and Ontario, and co-authors of the study, reported that many of the drugs found in interaction with grapefruitare prescribed frequently and are essential in the treatment of serious or well-known ailments. However, a worrying trend has recently been observed: between 2008 and 2012, the number of drugs potentially interacting with grapefruit and thus having negative effects increased from 17 to 43resulting in an average growth rate of more than 6 drugs per year. This increase is due to the introduction new chemical compounds and composition. Side effects include sudden death, acute renal failure, respiratory failure, gastrointestinal bleeding, immunosuppressed bone marrow function, kidney damage and other serious side effects. According to the authors, healthcare professionals who are unaware that the adverse event they are dealing with could have originated in the recent appearance of grapefruit in the patient’s diet are unlikely to investigate it. Moreover, he may not provide this information. Based on this, there is a general lack of knowledge of the healthcare professional regarding this interaction. There is 85 drugsthat can interact with grapefruit, 43 of which can have serious side effects. Other citrus fruits, such as Seville oranges, often used to make marmalade, lime or pomelo, also contain active ingredients (furanokumaryny). These substances are inherent in fruit and cause interaction by irreversibly inhibiting the drug metabolising enzyme CYP3A4, inactivating an estimated 50% of them. Drugs that interact with these substances have three characteristics: they are administered orally, they have a very low mediation of bioavailability (a constant percentage of an oral dose of the drug is absorbed into the bloodstream), and they are metabolized in the gastrointestinal tract by CYP3A4. For drugs with very low bioavailability, the consumption of a single normal grapefruit may be analogous to the consumption multiple doses of this drug at once. This interaction can occur even if the grapefruit has been consumed many hours before taking the medicine. Thus, even a small amount of it can affect the interaction with medications that are taken once a day at any time during the dosing interval. Frequent daily consumption of its normal amount may further increase the effect. For example simvastatin, commonly called statue name, in combination with drinking 200 ml of grapefruit juice once a day for 3 days, they are 330% more concentrated than in combination with water. People over 45 are the main buyers of grapefruit. They are also prescribed the most drugs. Due to the size of this population, their exposure to interaction is more frequent. Patients of this age also have reduced ability to tolerate excessive systemic concentrations of drugstherefore, they are particularly vulnerable to their negative effects in contact with citrus.

The authors of the study conclude that the current trend of more and more drugs that interact with grapefruit and thus cause negative effects is required to understand this interaction and apply this knowledge for safe and effective drug use in general practice. source: ScienceNews.pl

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