Hypolipidemic Agents

This article is dedicated to the therapy of high cholesterol. What are the main commonly used medications, how do they work and why are they so important?


First, let us mention that there are more types of cholesterol and other fats. There is total cholesterol, HDL-cholesterol (the "good" cholesterol), LDL-cholesterol (the "bad" cholesterol) and there are also non-cholesterol fats known as triglycerides.


Hypolipidemic drugs are very effective and they have excellent results, when used regularly. They not only decrease the level of fats in blood, but they also decrease risk of atherosclerosis and its complications. Therefore, these drugs may be used in prevention of heart attack, peripheral vascular disease and ischemic stroke.

Used medications


Statins belong among essential medicaments in the internal medicine. They help to decrease the level of both LDL-cholesterol and triglycerides and increase the HDL-cholesterol. The effect is ensured by blockage of enzyme HMG-CoA reductase, which plays an important role in synthesis of cholesterol molecules. However, there is a certain disadvantage. Our body may react by increased absorption of cholesterol from the digestive tract. Luckily, this problem can be solved by hypolipidemics containing a substance known as ezetimibe (see below).


Note: Statins are amazing drugs that significantly reduce the complications of atherosclerosis and related heart disease, but they may have dangerous side effects. The statins can sometimes cause a muscle damage, which may manifest as muscle pain and rarely, the statins may even cause dangerous rhabdomyolysis. Rhabdomyolysis means disintegration of muscle fibers. This situation may be very dangerous, because the muscles release a large amount of substances including the myoglobin, which can clog the kidney glomeruli and cause acute renal failure.


Ezetimibe is an interesting compound, which is a great complement to statins. Ezetimibe can block the absorption of cholesterol in the intestine. However, when used alone, it may induce increased production of cholesterol by our body metabolism.

Combined preparations of a statin and ezetimibe

Some preparations are combination of a statin and ezetimibe compounds. They have a much better effect, because they decrease serum cholesterol level by blocking both its metabolic production and intestinal absorption.


Drugs known as fibrates have a complex effect. Their mechanism of action is very complicated and shall not be described in such a simple text. Let us be content with the fact that by influencing a number of chemical processes in the body, fibrates can reduce levels of triglycerides (fats out other cholesterol) and increase the "good" HDL-cholesterol. The concentration of LDL-cholesterol changes only minimally. A person with high LDL-cholesterol and triglycerides may be treated by a combination of a statin and a fibrate.


They are also known as ion exchangers. They are cheap and quite effective in lowering cholesterol. Compared with statins, they are not so effective, but they also do not have so many side-effects. In some people they may cause digestive problems such as constipation.

Nicotinic acid

It was found out that nicotinic acid has also the effect of lowering serum cholesterol. However, due to a number of side effects, preparations with nicotinic acid are not so frequently used.


Jiri Stefanek, MD  Author of texts: Jiri Stefanek, MD
 Contact: jiri.stefanek@seznam.cz
 Sources: basic text sources