Statins are the most effective lipid-regulating drugs and have become one of the main drugs for the prevention and treatment of cardiovascular diseases. I believe that patients with chronic diseases are no stranger to it. So, some careful patients have raised the point that the instruction manual of Atorvastatin calcium is labeled that there is an interaction between grapefruit and statins, which will enhance the in vivo effect of statins. So, can we eat grapefruit while taking this type of medication?
It is meaningless to talk about the effect without the “amount”
First of all, let’s take a look at the instructions of the statin drugs that have been marketed in China: Atorvastatin calcium and simvastatin instructions mention that the regular consumption of grapefruit juice (250ml per cup per day) has little effect on these two drugs and is not clinically significant.
However, consumption of large amounts can inhibit the metabolism of these two drugs in the body and increase the concentration of the drugs in the body, eventually leading to enhanced drug effects, so the combined use should be avoided.
In addition, lovastatin tablets, pravastatin sodium, pitavastatin calcium, and rosuvastatin calcium are not mentioned in the instructions. No interaction has been found between fluvastatin sodium and grapefruit juice.
The point is that it is grapefruit juice that is mentioned in the instructions as affecting drug action; grapefruit juice does not affect all statins; small doses (250 ml/day) of grapefruit juice do not have a clinically significant effect on statins, and only doses of 1 L/day or more can trigger relevant clinical manifestations.
Grapefruit has an effect on some statins only
According to the drug description, grapefruit is only partially effective against statins. Grapefruit contains various chemical components, such as flavonoids, furanocoumarins (coumarin, dihydroxycoumarin, bergamot lactone), which have been shown to inhibit the activity of cytochrome P450 3A4, especially coumarin.
By reviewing the instructions we found that atorvastatin, lovastatin and simvastatin are three drugs that need to be metabolized by cytochrome P450 3A4 in the body, while other statins do not need to be metabolized by this enzyme. Therefore, theoretically, taking large amounts of grapefruit juice will affect the metabolism of these three drugs in the body and increase their concentration in the body, which will increase the effect of the drugs and also increase the risk of adverse reactions.
Therefore, patients taking atorvastatin calcium, lovastatin and simvastatin are advised to avoid taking large amounts of grapefruit. In small doses, it is recommended to take grapefruit at intervals, such as during the day if the drug is taken at night, to minimize food-drug interactions.
Grapefruit is not a “one-size-fits-all” drug
The question is, is the grapefruit that we usually eat here?
Of course not, grapefruit is not the same as grapefruit. Most of the grapefruit we usually say refers to the Mandarin grapefruit, which is larger in size. Grapefruit is a hybrid of grapefruit and orange, because of its dense growth state on the tree, from a distance, it looks like grapes, so called grapefruit (also known as grapefruit), its size is about the size of a fist.
In addition oranges, oranges and lemons are in the same citrus genus as grapefruit and contain partly the same chemical composition. Available studies show that oranges, mandarins, and southern oranges also contain some amount of naringin and furanocoumarins in the fruit.
However, the content of these components is much lower compared to grapefruit, so it is only when taken in large quantities that drug-food interactions are triggered. Therefore, grapefruit users can take small amounts, but it is best to take them in intervals with statin drugs, or to choose drugs that do not interact with each other.
