Cholesterol Medications: Uses and Side Effects

Cholesterol medications are helpful when all other measures to lower LDL and blood triglycerides have failed. Do you want to know about its uses and side effects? Keep reading!
Cholesterol Medications: Uses and Side Effects

Last update: 24 April, 2021

Most cardiovascular diseases are associated with the presence of high cholesterol levels. Lifestyle changes help decrease the amount of this compound in the blood. However sometimes these changes aren’t effective, and so the use of cholesterol medications is necessary.

Cholesterol is a substance that can be synthesized by the body and is also obtained from the diet. It’s a very useful compound in the body as it forms part of all our cells’ membranes, and is the precursor of steroid hormones, bile acids, and vitamin D.

The substance in question can be transported in the form of lipoproteins in the blood, these lipoproteins can be low-density (LDL) or high-density (HDL). Multiple studies have shown the relationship between high total and LDL cholesterol levels with cardiac morbidity and mortality.

Uses of cholesterol medications

Cholesterol medications prevent heart attacks.
Many of these drugs prevent the development of fatal cardiovascular events.

The main use of this group of drugs is to reduce blood levels of LDL and triglycerides. In addition, some of them are capable of increasing the levels of HDL in the blood, which is known as “good cholesterol” as it helps the liver to eliminate harmful cholesterol.

In this sense, these compounds are used in the treatment of a condition called hypercholesterolemia. This disease is characterized by the presence of high levels of total cholesterol and triglycerides in the blood associated with lifestyle.

Cholesterol medications are also helpful in treating an inherited condition known as familial hypercholesterolemia. This condition appears due to a defect in chromosome 19 in children, which generates very high levels of LDL and increases the probability of heart attacks at an early age.

Finally, these drugs are also used in patients with coronary heart disease to improve their prognosis. It’s important to know that LDL is known as “bad cholesterol”, and this is because it tends to accumulate in the blood vessels and thus produce atherosclerosis.

What are cholesterol medications?

Today there are many compounds that are used to lower serum cholesterol levels. All of them have different mechanisms of action. However, the effect obtained will be similar. In this way, among the main drugs used, the following stand out:


Statins are probably the most widely used drugs to lower blood cholesterol levels. This group of drugs are very useful as they lower the levels of LDL and triglycerides in the blood; in turn, they are also capable of increasing HDL concentrations.

Statins’ mechanism of action is very simple, they inhibit the liver enzyme hydroxy-methi-glutaryl coenzyme A (CoA) reductase. This enzyme is part of the initial step in the synthesis of cholesterol. And so, being inhibited, the liver is unable to synthesize this substance and is forced to eliminate the cholesterol found in the blood.

Generally speaking, statins are very safe compounds. However, they can cause side effects such as muscle pain, digestive problems and mental confusion. Among the most used statins, the following stand out:

  • Atorvastatin
  • Simvastatin
  • Lovastatin
  • Fluvastatin

Bile acid fixatives

Other medications used for cholesterol are bile acid-binding resins. The main function of these compounds is to lower the levels of LDL in the blood. However, they don’t affect the levels of triglycerides or HDL.

Under normal conditions, the body reabsorbs cholesterol and bile acids present in the intestine for the synthesis of bile. Bile acid fixatives bind to compounds present in the intestinal lumen, thus preventing their reabsorption and promoting their excretion through the feces.

All this process forces the liver to use cholesterol in the form of LDL present in the blood for the synthesis of new bile acids. These compounds are very useful, one of the main representatives is cholestyramine, which has shown a cholesterol reduction capacity of up to 36%.

The side effects of bile acid binders can range from abdominal pain to nausea and vomiting. In some cases, they are capable of generating metabolic disorders such as hyperchloremic acidosis. However, these are rare.


Fibrates are drugs derived from fibric acid and are prescribed in order to lower serum triglyceride levels. However, they can also increase HDL levels, thus reducing the accumulation of cholesterol in the blood vessels.

The mechanism of action of these drugs focuses on the alteration of the nuclei of certain cells, which causes lipolysis of cells rich in triglycerides. This reduces the number of cells capable of generating atherosclerosis and subsequent obstruction of the vascular lumen.

The pharmacological effect of fibrates is observed from the second week of treatment. Studies have shown its effectiveness in reducing triglycerides by up to 55% and cholesterol by up to 25%. These cholesterol medications are well tolerated and the most common side effects are gastrointestinal.

Cholesterol absorption inhibitors

Medications for cholesterol are varied.
All these drugs must be prescribed by a specialist.

Part of the cholesterol that’s circulating in the blood comes from the diet, the bile, and the desquamation of the intestinal epithelium. It enters the bloodstream through intestinal absorption. In this sense, cholesterol absorption inhibitor drugs are beneficial in reducing serum levels.

The main representative of these drugs is ezetimibe, which is believed to inhibit a transporter protein in the intestinal epithelium. The inhibition in question prevents the cholesterol present in the intestinal lumen from being incorporated into the body, thus favoring its fecal excretion.

Ezetimibe has a half-life of around 22 hours, which makes it possible to obtain beneficial results with just one daily administration. However, this drug is contraindicated in cases of liver failure. In addition, it can cause stomach pain, muscle pain, and fatigue in some patients.

A balanced diet is essential

The use of drugs to lower serum cholesterol show great results in a short space of time. However, the initial treatment of hypercholesterolemia means making changes to a person’s diet and lifestyle.

In most cases, a balanced diet and a decrease in a sedentary lifestyle are usually enough to lower LDL and triglyceride levels. The use of the aforementioned drugs is intended for patients in whom dietary changes don’t produce the desired decrease in total cholesterol levels.

Therefore, it’s vitally important to maintain a constant medical check-up. This will be the only way to detect the increase in cholesterol levels and carry out the appropriate treatment. Remember that high levels of LDL are closely related to the development of cardiovascular diseases.

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