This article is from "Nankai Sun Pharmacist", which is used for medical science popularization for reference. Rosuvastatin is a statin commonly used in clinical practice, which mainly inhibits the rate-limiting enzyme (hydroxymethagyl-CoA reductase) in the process of cholesterol synthesis by selectively and competitively, thereby reducing cholesterol synthesis in the liver, reducing the levels of total cholesterol, LDL cholesterol and triglycerides in the blood, and increasing the level of HDL cholesterol. In addition to lipid-regulating effects, rosuvastatin can also prevent the formation of atherosclerotic plaques, stabilize, shrink and even reverse the formed plaques, prevent plaque rupture, and inhibit inflammatory response and protect vascular endothelial function, and long-term use can significantly reduce the incidence and mortality of cardiovascular and cerebrovascular events such as myocardial infarction and stroke.
Grapefruit, also known as grapefruit, belongs to the citrus fruit, is the product of the hybrid of grapefruit and sweet orange, rich in nutrients such as vitamin C and potassium, is a healthy fruit, its fruit, peel part contains hesperetin, naringin, Furanocoumarin and other ingredients, these can significantly inhibit the activity of the liver drug enzyme CYP3A4 (a drug-metabolizing enzyme), reduce the metabolism of statins, lead to the accumulation of drugs in the body, and the increase in blood concentration, which not only enhances the pharmacological activity, but also increases the risk of adverse reactions such as liver toxicity and muscle toxicity.
But this problem cannot be generalized, this is because lovastatin, simvastatin, atorvastatin are mainly metabolized by the liver enzyme CYP3A4, while pravastatin, fluvastatin, rosuvastatin, and pitavastatin are not metabolized by the liver enzyme CYP3A4, therefore, lovastatin, Patients with simvastatin or atorvastatin, if they eat grapefruit or drink grapefruit juice, there is a risk of drug accumulation poisoning, but it is not absolutely impossible to get grapefruit, simvastatin drug interaction under the drug label indicates that the regular drinking amount (a glass of 250 ml per day) has little effect and is not clinically significant, and atorvastatin drug intervention drug package indicates that the intake is more than 12L of grapefruit juice will significantly increase the blood concentration of atorvastatin, therefore, it is still the same sentence, and it is a hooligan to talk about toxicity without a dose.
The difference is that rosuvastatin almost does not need to be metabolized by the metabolic enzyme CYP3A4 in the body, only about 10% of rosuvastatin needs to be metabolized by another metabolic enzyme CYP2C9, and the remaining about 90% of rosuvastatin is excreted in the feces in its original form, therefore, there will be no interaction between rosuvastatin and grapefruit, inducing adverse reactions, and there is no problem with eating a few pieces of grapefruit and drinking a glass of grapefruit juice every day while taking rosuvastatin.
Grapefruit, grapefruit, lime, citrus grapefruit, lime and other rutaceae plants contain hesperetin, naringenin and furanocoumarin and other components, which can affect the metabolism and excretion of statins such as lovastatin, simvastatin, atorvastatin, etc., it is best not to consume large amounts of the above-mentioned citrus fruits or juices when taking the above-mentioned statins, and hesperetin in the peel and fruit of citrus fruits such as lemons, oranges, and sweet oranges, Ingredients such as naringenin and furanocoumarin are low in content and generally have no effect, so they can be eaten with confidenceRosuvastatin is not metabolized by CYP3A4 liver enzymes, and has no interaction with citrus fruits, so it can be consumed with confidence while taking the drug.