Lipid-lowering drugs: What are they? How do they work? Types and Main Drugs of Common Use

They are a diverse group of pharmaceutical products used to treat high levels of fats (lipids), such as blood cholesterol ( hyperlipidemia ).

The importance of these substances is given by the excess of some types of lipids (cholesterol or triglycerides) or lipoproteins. It is one of the main risk factors for cardiovascular disease, the leading cause of death in developed countries.


There are several kinds of hypolipidemic drugs. They may differ in their impact on the cholesterol profile as in the adverse effects.

For example, some may reduce low-density lipoprotein (LDL) “bad cholesterol” more than others, while others may preferentially increase high-density lipoprotein (HDL), “good cholesterol.”

Clinically, the choice of an agent will depend on the patient’s cholesterol profile, the cardiovascular risk, and the patient’s liver and kidney functions, evaluated against the balance of risks and benefits of the medications.

In the United States, this is governed by the evidence-based guidelines of the National Cholesterol Education Program (NCEP) Adult Treatment Panel III (ATP III).

What are the most commonly used drugs, how do they work, and why are they important?

Lipid-lowering drugs are very effective and have excellent results when used regularly. They lower the level of fats in the blood and decrease the risk of atherosclerosis and its complications.


Therefore, these drugs can be used to prevent heart attack, peripheral vascular disease, and ischemic stroke.

Statins: are particularly suitable for reducing LDL cholesterol, the cholesterol with the most vital links to vascular diseases.

In studies using standard doses, it has been found that statins reduce LDL-C by 18% to 55%, depending on the specific statin used.

With statins, there is a risk of severe muscle damage (myopathy and rhabdomyolysis ). Cholesterol is not a risk factor for mortality in people over 70 years, and threats of statins increase more after 85 years.

Fibrates: are indicated for hypertriglyceridemia. Fibrates typically reduce triglycerides by 20% to 50%.

The level of good HDL cholesterol also increases. Fibrates can lower LDL, although generally to a lesser degree than statins. Like statins, there is a risk of severe muscle damage (myopathy and rhabdomyolysis).

Niacin: like fibrates, it is also adequate to reduce triglycerides by 20-50%. It can also lower LDL by 5-25% and increase HDL by 15-35%.

Niacin can cause hyperglycemia and can also cause liver damage. The niacin derivative acipimox is also associated with a modest decrease in LDL.

Bile acid sequestrants (resins, for example, cholestyramine): are particularly effective in reducing LDL-C by sequestering cholesterol-containing bile acids released in the intestine and preventing their reabsorption from the intestine.

It decreases LDL by 15-30% and increases HDL by 3-5%, with little effect on triglycerides but may cause a slight increase. Bile acid sequestrants can cause gastrointestinal problems and reduce the absorption of other drugs and vitamins from the intestine.

Ezetimibe: it is a selective inhibitor of cholesterol absorption in the diet.

Lomitapide: is a microsomal inhibitor of the triglyceride transfer protein (MTP).

Phytosterols: can be found naturally in plants. Similar to ezetimibe, phytosterols reduce the absorption of cholesterol in the intestine. Therefore, they are more effective when consumed with meals. However, the precise mechanism of action of phytosterols differs from ezetimibe.