Statins

Statins are medications that effectively reduce blood cholesterol (inhibit cholesterol production in the liver) and thus prevent the occurrence of strokes and heart attacks. They are one of the most commonly prescribed drugs that are regularly taken by over 32 million Americans. A lot of people today have high cholesterol levels due to the modern style of life that consists of a lot of stress, constant rushing and eating unhealthy foods. This is an important risk factor for cardiovascular diseases and stroke as cholesterol accumulates in the vascular walls, narrowing them, which leads to a disturbed blood flow and damage to the brain or the heart. The level of cholesterol can be largely influenced by a proper diet and regular exercise. These precautions, however, are not enough in the case of an inadequate regulation of the formation of cholesterol in the liver cells. If this happens it is necessary to take appropriate medication according to the doctors’ instructions.

The mechanism of statins activity

Statins are medications that inhibit the activity of the liver enzyme HMG-CoA (3-hydroxy-3-methylglutaryl-coenzyme A) reductase, an enzyme which regulates the rate of cholesterol synthesis in the liver cells. After oral ingestion, the liver cells will come to "lack" cholesterol, a necessary component for the formation of bile acids, and will increase the number of cell surface LDL (low-density lipoprotein) receptors. These receptors draw cholesterol from the blood into the liver cells. This is an important factor for atherosclerotic vessels as it diminishes the concentration of cholesterol in the blood.

Statins also reduce the production of VLDL (very low-density lipoprotein) lipoproteins, which are the main carriers of triglycerides in the blood. They also have protective properties on the walls of blood vessels not directly related to controlling the level of blood fats. The actual effectiveness of statins depends largely on the SLCO1B1 gene. The SLCO1B1 product is a trans-membrane protein that regulates the removal of statins from the blood and their uptake in the liver cells. It has been shown that carriers of certain variants of this gene have four times the risk for myopathy (muscle disease), one of the most frequent side effects of taking statins. Symptoms of muscle myopathy usually develop four weeks after the initiation of therapy with statins and manifest in the form of exhaustion, fatigue and muscle aches of limbs. Carriers of the unfavourable forms of the gene should refrain from taking certain drugs from the statin group containing the active ingredients such as simvastatin, pravastatin or atorvastatin and replace them with fluvastatin, which is a safer alternative.