How Do Statins Work?

Statin drugs work by blocking a key enzyme in the production of cholesterol. Cholesterol is a nature product of the liver and in the right amounts does not pose a problem to the body. The body, however, sometimes produces too much cholesterol. Statin drugs block the enzyme linked to the liver’s cholesterol production, HMG-CoA (3-hydroxy-3-methyglutaryl COA) reductase, thus inhibiting the liver’s ability to produce LDL. This causes an increase in the number of the LDL receptors on the surface of liver cells, resulting in more cholesterol being removed from the bloodstream and a reduction in risk for high-cholesterol related diseases.

Statin drugs have been seen to lower LDL levels from 18% - 55% and to raise HDL levels 5% - 15%. Studies have also shown that statin drugs can help the body reabsorb cholesterol that has accumulated on the artery walls. Doctors are now finding that large dosages of statin drugs may help patients avoid their first heart attack, and can help many prevent a second heart attack as well.

According to the Mayo Clinic, raising your HDL cholesterol level 1 milligram per deciliter (mg/dL) of blood can reduce your heart attack risk by 3 percent. That's another reason statins that raise HDL are considered beneficial.

Diagram from FDA website

Statins also have "pleiotropic" effects - for which they were not originally intended - related to the cardiovascular system. They reduce oxidative stress of body tissue, they reduce inflammation (like aspirin), and they stabilize plaque on the blood vessel walls. These effects operate independently of LDL-cholesterol reduction and unlike cholesterol reduction, they disappear quickly when the statins are no longer taken. People who take statins are less likely to die of pneumonia and the flu. The antioxidative and antiinflammatory properties of statins may contribute to the improvement of prognosis in patients with coronary artery disease. Indeed, other common drugs such as aspirin have anti-inflammatory effects and much as aspirin can help with many maladies, there are indications that statins can have many benefits.

There is conflicting evidence that shows that statin drugs may help prevent some types disease, including certain forms of cancer (such as colorectal or skin), by working against cellular functions that may be involved in tumor growth, initiation and metastatis. However, there is also a significant amount of research which suggests that statins have no effect on cancer prevention whatsoever. Additionally, while preliminary studies suggest that the onset of Alzheimer’s Disease may be affected by statin drugs and clinical trails are underway, this has yet to be proven. The role of stain drugs in reducing the risks of other health-related issues is a contested topic, but statins have certainly been proven to be effective against fighting high cholesterol.

It has also been suggested that statins could be used in fighting infection, much as antibiotic medications have traditionally been used. Statins help with endothelial functioning. The endothelium is the thin layer of cells inside blood vessels. Endothelial dysfunction often leads to atherosclerosis and can signal other vascular diseases.

More on the science of statins

Side effects