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Statins and Grapefruit

Shashank Nakate
Statins are used to lower cholesterol, but they don't go well with grapefruit. The interaction between statins and grapefruit leads to harmful effects on the body. In the following story, we provide more information on the same.
Statins are useful drugs which help in lowering the cholesterol levels in our body. Different enzymes present in the body carry out the breakdown of these drugs, which, in turn, help in reducing the levels of cholesterol.

What are Statins?

Statins are medicines used to bring down the level of plasma cholesterol. They inhibit the HMG-CoA reductase enzyme, which leads to reduction in the level of cholesterol, and are also known to affect the cholesterol levels in the body, viz. HDL, LDL, etc. These medicines are widely used for the treatment of cholesterol-related problems. The following paragraphs present information about the effects of the interaction between grapefruit juice and statins.

Statins and Grapefruit Juice Interaction

Grapefruit contains a chemical known as bergamottin. This chemical interacts with cytochrome P-450 and P-glycoprotein, the enzyme systems which are known for breaking down certain chemicals and transporting them from one part of the body to the other. Functioning of these enzyme systems is altered by interaction with grapefruit.
The breakdown of statins do not take place due to the interference of chemicals present in grapefruit. As a result of this process, buildup of statins in the blood take place. Rise in the level of statins is very dangerous for the health of the kidneys and liver. The CYP3A4 (enzyme) activity is affected by around half due to the effect of grapefruit.

Recommendations about Grapefruit Consumption

Grapefruit provides the body with nutrients such as vitamin C, lycopene, potassium, etc. However, the interaction of grapefruit with enzymes involved in metabolism creates problems by raising the level of drugs in the body. Let us understand when to consume grapefruit and when to avoid it.
The interaction of grapefruit juice causes levels of statin drugs to rise in the blood stream. One might wonder if it is safe to eat grapefruit in the morning and consume statin drugs in the evening. Unfortunately, grapefruit juice can interact with statin drugs 3 days after consumption, and therefore, it is risky to consume this fruit. Even a single serving of grapefruit juice is enough to build up the level of drugs in the blood stream.

List of Statin Drugs

Here is a list of statin drugs which have been known to interact with grapefruit.
  • Altoprev
  • Advicor
  • Lipitor
  • Caduet
  • Simcor
  • Mevacor
Grapefruit juice does not interact with the following statin drugs.
  • Lescol
  • Crestor
  • Pravachol
  • Lescol XL
The reason these drugs are not affected by grapefruit is that the enzymes that act in their (statin) break down are different from those which act normally. One can think of using statin drugs which get absorbed in the body in a different way. Crestor and Pravachol are used in lowering the level of cholesterol without getting affected by grapefruit juice.
One should take every possible precaution to prevent the interaction of statins with grapefruit. Advice from a medical practitioner would help greatly.
Disclaimer: The information provided in this story is solely for educating the reader. It is not intended to be a substitute for the advice of a medical expert.