What are Statin Drugs?

Statin drugs are medications used to reduce serum levels of lipids and lipoproteins. Also known as statins, statin drugs work by suppressing HMG-CoA reductase, an enzyme involved in cholesterol production. Blocking this enzyme’s action also stimulates certain protein receptors that reside on the surface of cells to bind with circulating low-density lipoproteins (LDL) so that they may be contained and digested in the liver. Since high levels of LDL cholesterol are associated with promoting arterial plaque buildup, statin drugs are particularly beneficial for people at risk for heart disease. However, there is evidence to suggest that statin drugs may also help to prevent kidney disease, arthritis, osteoporosis, dementia (such as Alzheimer's disease), and certain cancers.

Statin drugs are either made synthetically or are obtained as a substrate of fermentation, or the by-product of oxidizing an organic compound. Yet, one of the statin drugs, compactin, occurs naturally in red yeast rice due to the presence of Penicillium citrinum, a type of mold. However, due to being linked to several unwanted side effects, compactin is not used as a lipid-lowering agent itself. Instead, it is used to produce another statin called pravastatin. In fact, compactin synthesis is the only way that pravastatin can be obtained.

Lovastatin was the first of the statin drugs to be approved by the U.S. Food and Drug Administration (FDA). Like several other drugs in this class, it is obtained by fermentation, in this case from the fungus Aspergillus terreus. In fact, like compactin, it is also found naturally in red yeast rice. Lovastatin is marketed under several brand names, including Mevacor® and Altocor®.

The cholesterol-lowering effects of statin drugs are observed within a very short time, usually within just seven days. However, statin therapy is not necessarily a permanent solution. In fact, unless measurable lifestyle changes are made, it is highly likely that LDL cholesterol levels will become elevated again if therapy is interrupted. Therefore, most patients undergoing treatment with statin drugs must continue their medication for the rest of their lives.

While the health-giving benefits of statin therapy are readily apparent for certain people, these drugs do present risks. For one thing, combining statin drugs with other medications increases the risk of rhabdomyolysis, a condition characterized by the disintegration of muscle cells. This drug interaction may occur with other lipid-lowering drugs, such as gemfibrozil, with certain antibiotics (i.e., erythromycin), or antifungal agents, such as cyclosporine. In addition, statin drugs may produce short-term side effects, most commonly nausea, diarrhea, and pain in the muscles and joints. These drugs can sometimes increase enzyme production in the liver, which increases the risk of liver damage and necessitates regular monitoring of enzyme levels.