Beyond the coronary arteries: Possible benefits of statin drugs Part I: Meet the statins

For a young physician just entering practice today, life before the statins must seem like the dark ages of cardiology. Since the first statin was approved in 1987, these important medications have improved the outlook for millions of Americans with heart disease or cardiac risk factors. All in all, statins can reduce the risk of heart attacks and other major clinical manifestations of coronary artery disease (CAD) by up to 37%, with the greatest benefit going to men at the highest risk. And since heart disease is America's leading cause of death, it's no wonder that the seven statin drugs (see Table 1) are the best-selling prescription medications in the United States.

Targeting cholesterol

All seven statin drugs act in the same way, by inhibiting the activity of 5-hydroxy-3-methylglutaryl coenzyme A reductase, a liver enzyme that's better known by its short name HMG-CoA reductase. By either name, it's the key enzyme responsible for cholesterol production. When the enzyme is blocked, liver cells make less cholesterol, and blood levels of LDL ("bad") cholesterol fall. But these drugs have another benefit: as cholesterol production falls, the liver takes up more cholesterol from the blood, so blood levels fall even further. The statins produce only small elevations in HDL ("good") cholesterol, and only atorvastatin and rosuvastatin lower triglycerides, another potentially "bad" lipid, to an important degree.