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For nearly thirty years have been the mainstay of treatment for high cholesterol and cardiovascular disease. For some people, however, they simply do not work. For people who do not respond to statins, two new drugs may be what the doctor ordered.

There seems to be no end to how low doctors want cholesterol levels to go.

Fifty years ago, high cholesterol was not treated unless total cholesterol levels ran over 300 mg/dl (7.8 mmol/l). Thirty years ago, a total cholesterol level of 200 mg/dl (5.2 mmol/l) was thought to merit treatment, and currently, many people who have a history of heart disease or diabetes are put on statin medications when their LDL cholesterol levels are as low as 100 mg/dl (2.6 mmol/l). Some people, however, suffer truly life-threateningly high cholesterol levels no matter how they diet or whether or not they take statin medications. For them, there have been very few alternatives until extremely recently, although not everyone will benefit from the new medications, either.

Statins Work Well In Most Cases

Most of us have been conditioned to think of high cholesterol as a condition that is caused by consuming too many foods that contain cholesterol, but that is not really the case. The liver makes about 85 percent of the body's total cholesterol from fats and carbohydrates. Since most of the body's cholesterol doesn't come from food, a low-cholesterol diet will make at most about 15 percent difference in bloodstream cholesterol levels, and often not even that much.
However, a class of compounds known as the statins have become a mainstay of medical therapy for cholesterol problems over the last 30 years. These medications, which include Altocor and Mevacor (lovastatin), CRESTOR (rosuvastatin), Lescol (fluvastatin) Lipitor (atorvastatin), Livalo (pitavastatin), and Zoco (simvastatin), among others, have entered the ranks of the best-selling medications of all times. They are so popular that some doctors have even been proposed that they be added to drinking water, like fluoride.
Statin drugs interfere with the action of an enzyme called HMG-Co A reductase. This enzyme is necessary for the production of cholesterol by the liver. Blocking this enzyme makes it possible to lower cholesterol by more than the 10 to 15 percent possible with diet and some earlier cholesterol drugs. That is not all statin drugs can do. They block inflammation. This keeps arteries from narrowing so that they are blocked by cholesterol-laden plaques or clots. The statin drugs help existing cholesterol plaques stabilize, so that they do not rupture and trigger a heart attack. They stimulate the liver to take LDL cholesterol out of the bloodstream. 
They stop a process called prenylation, which makes certain proteins "water-phobic," so they would cause irritation in the bloodstream.

Not Everyone Benefits From Statins

Although statin medications have a number of proven beneficial effects, not everyone benefits from them. A substantial number of people suffer intolerable side effects from statin medications. In a small number of people, statins cause a phenomenon known as rhabodmyolysis. Muscle tissue breaks down. This hurts. It also releases byproducts that are toxic to the kidneys.
In some people, statins cause memory loss. This is particularly a problem with the more potent statins, such as CRESTOR. Statins may increase the anticoagulant effect of warfarin (Coumadin). They possibly increase the risk of diabetes and certain kinds of cancer. The major drawback of statin therapy, however, is that they do not work for the people who most urgently need lower cholesterol, those who have familial hypercholesterolemia.
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