Does ezetimibe have to be used in combination with statins? What kind of medicine is it?

A friend told Huazi that in the popular science articles about statins written by Huazi, there is always a sentence "When statins alone cannot make LDL cholesterol reach the standard, it needs to be used in combination with ezetimibe." What is ezetimibe, and does it have to be used in combination with statins?

Hua Zi said that ezetimibe is a cholesterol absorption inhibitor, which has the same main effect as statins and can reduce the level of LDL-C (low-density lipoprotein cholesterol). It can be used alone or in combination with other drugs.

1. The lower the LDL-C level, the stronger the protective effect Many tissues in the human body can synthesize cholesterol, but the liver synthesizes the most. In the process of synthesizing cholesterol, many biological enzymes are required to work together. Statins act on the most important cholesterol synthase, inhibiting the production of cholesterol, thereby reducing LDL-C levels.

Many studies have shown that the lower the LDL-C level, the stronger the protective effect on the cardiovascular system. The LDL-C control target for critically ill patients has been reduced from 1.8mmol/L to 1.4mmol/L. The dose of statins has begun to increase.

However, statins have a "6%" characteristic, which means that when using statins, doubling the dose can only increase the LDL-C lowering effect by 6%. For people with high initial LDL-C values, if they want to reach the standard, they need to use a large dose of statins.

However, as the dose increases, the incidence of various adverse reactions of statins to liver function, central nervous system, and muscle tissue will also increase significantly. Moreover, Chinese people have a poorer tolerance to large doses of statins than Europeans and Americans, and can usually only use moderate doses. Therefore, we cannot rely solely on statins to control LDL-C, and we need to find another way to lower LDL-C.

2. Ezetimibe is a cholesterol absorption inhibitor. In addition to being used by the human body, most of the cholesterol synthesized in the liver will enter the intestine with bile and then be reabsorbed back into the blood by the small intestine. Cholesterol in food is also absorbed into the blood through the small intestine. If the small intestine's absorption function of cholesterol can be inhibited, LDL-C can be lowered.

Ezetimibe is such a cholesterol absorption inhibitor. After oral administration, it acts on the villi of the small intestine, inhibiting the cholesterol transporter protein on the villi of the small intestine and preventing the cholesterol in the intestine from returning to the blood through the transporter protein. It can reduce the LDL-C level by about 20%.

3. Ezetimibe is usually used in combination therapy. Ezetimibe can be used alone, but it can only reduce LDL-C levels by 20%, which cannot meet the needs of preventing cardiovascular and cerebrovascular diseases. Intermediate-acting statins can reduce LDL-C levels by 40%, and potent statins can reduce LDL-C levels by more than 50%, so clinical control of LDL-C is still mainly based on statins.

When statins alone cannot achieve the target LDL-C level, they can be used in combination with ezetimibe, which can reduce LDL-C levels by 20% on top of the original therapeutic effect. Moreover, the adverse reactions of ezetimibe are very mild, basically similar to those of placebo, and are much safer than increasing the dose of statins.

Therefore, in actual use, ezetimibe is usually used in combination therapy, and is rarely used alone. When using ezetimibe, the dosage of statins can be reduced according to actual conditions, which can reduce the incidence of adverse reactions such as muscle pain and dizziness.

For some people who have severe adverse reactions after taking statins, they can consider using half-dose statin + ezetimibe to control LDL-C under the guidance of a doctor.

In summary, ezetimibe acts on the villi of the small intestine and is a cholesterol absorption inhibitor that can lower LDL-C and protect the cardiovascular and cerebrovascular system. It can be used alone, but the intensity of action is low when used alone, so it is often used in combination with statins to increase the effect of lowering LDL-C, and can also reduce the dosage of statins and reduce the occurrence of adverse reactions. As a reminder, the use of drugs must be carried out under the guidance of a doctor. I am pharmacist Huazi, welcome to follow me and share more health knowledge.