What is ezetimibe? Why is it always used with statins? What should you pay attention to when using it?

Many friends who take statins, when blood lipid control is not up to standard, doctors will recommend taking it in combination with ezetimibe to increase cholesterol control. But many people don't know about ezetimibe, and asked Huazi what this medicine is, does it have to be used with statins, and can it be used alone?

Huazi said that ezetimibe is a cholesterol absorption inhibitor and its lipid-lowering effect is not high. It is not recommended to be used alone. It can only exert its anti-atherosclerotic effect when used in combination with statins.

1. Cholesterol absorption inhibitors

Cholesterol in the human body is mainly absorbed through the epithelial cells of the small intestine. 30% of cholesterol comes from diet, and 70% comes from self-synthesis. However, the cholesterol synthesized by the body will also be secreted into the intestine through bile, and then absorbed back into the blood through the epithelial cells of the small intestine. Therefore, as long as the absorption of cholesterol by the epithelial cells of the small intestine is inhibited, the cholesterol level in the blood can be reduced.

After taking, ezetimibe works directly in the intestine, inhibiting the activity of sterol carrier transporter (NPC1L1) on the small intestinal epithelial cells, thereby inhibiting the absorption of cholesterol in the intestine. When used as a single drug, it can reduce cholesterol levels by approximately 20%.

2. Enterohepatic circulation of drugs

After binding to the small intestinal epithelial cells, ezetimibe can be absorbed and enter the liver through the portal vein. It is then secreted into the bile and discharged into the small intestine, where it takes effect and is absorbed again... This process repeats itself, causing ezetimibe to circulate between the liver and small intestine, which is called the enterohepatic circulation of the drug.

Drugs with enterohepatic circulation characteristics have long-lasting effects and long elimination times, so the half-life of ezetimibe can reach 22 hours. Generally speaking, 10 mg per day can exert long-term effects. Some people are highly sensitive to drugs and can take 5 mg. The absorption of ezetimibe is not affected by diet and can be taken at any time of the day.

3. It is recommended to use it in combination with statins

Ezetimibe has a single effect, which is to inhibit the absorption of cholesterol and slightly reduce the cholesterol level. Statins can reduce cholesterol by 30% to 50%. They can also improve the metabolism of the arterial endothelium, increase the stability of plaques, and make them less likely to rupture. When used for a long time, they may even reverse the plaques.

Therefore, statins are the cornerstone drugs for the treatment of atherosclerosis. Only when statins cannot bring LDL-C levels to the target, should ezetimibe be used in combination to continue to reduce LDL-C levels by 20%.

So far, only statins can inhibit the progression of plaques and reverse plaques, which is an effect that other lipid-lowering drugs cannot replace. Therefore, ezetimibe is usually only used as a partner of statins and is generally not used alone.

4. Adverse reactions are very mild

Ezetimibe is well tolerated. Adverse reactions such as dizziness, paresthesia, and constipation may occur, but they are usually mild and transient.

When used in combination with statins, attention should be paid to whether there is an increase in liver transaminases (AST, ALT), muscle pain, and fatigue. If the transaminases increase by more than 3 times the upper limit of normal, or if creatine kinase (CK) exceeds 5 times the upper limit of normal, the dosage should be reduced or the drug should be discontinued.

Ezetimibe is not metabolized by liver enzymes and has few interactions with other drugs. It is secreted by bile and excreted by kidneys, has no effect on the kidneys, and does not require dose adjustment for patients with renal insufficiency. However, it is not recommended for patients with moderate or severe liver insufficiency.

In summary, ezetimibe is a cholesterol absorption inhibitor with few adverse reactions and weak lipid-lowering effect. It is usually not used alone. It is only considered in combination with ezetimibe when statins cannot control LDL-C to the target. The drug should be used under the guidance of a doctor. If you have any questions about the use of the drug, please consult a doctor or pharmacist. I am pharmacist Huazi, welcome to follow me and share more health knowledge.