Statins can be effective in lowering harmful cholesterol

June 1, 2006

More than 106 million American adults have borderline or high lipidlevels, which places them at increased risk for heart disease. Whenrecommended changes in diet and exercise do not sufficiently lowerhigh cholesterol levels, national medical guidelines call for theuse of lipid-lowering drugs.

More than 106 million American adults have borderline or high lipid levels, which places them at increased risk for heart disease. When recommended changes in diet and exercise do not sufficiently lower high cholesterol levels, national medical guidelines call for the use of lipid-lowering drugs.

Statins inhibit an enzyme that plays an important role in cholesterol synthesis, leading to lower levels of LDL-cholesterol (the "bad" cholesterol) and also lowering triglycerides. They have a number of other beneficial effects as well. Statin medications include Altoprev (lovastatin); Crestor (rosuvastatin); Lescol (fluvastatin); Lipitor (atorvastatin); Mevacor (lovastatin); Pravachol (pravastatin); Zocor (simvastatin); and generic lovastatin. Pravachol became available as a generic in May, and the generic version of Zocor will be available later this year.

"In patients who have not achieved their goal with a statin, doubling the dose usually achieves only a 6% further reduction of the LDL-cholesterol level, while addition of ezetimibe, for example, provides an additional 17% to 24% reduction."

Statins differ in potency. Many patients require LDL-cholesterol reductions of 30% to 40%, which all the statins can provide. According to Dr. Abramowicz, those requiring maximal lowering should be treated with Lipitor or Zocor. Statins generally are well-tolerated, and patients who cannot tolerate one statin may tolerate another. Mild gastrointestinal disturbances, headache or rash may occur; muscle pains and weakness are common. A rare side effect may occur with any of the statins, called rhabdomyolysis. In this condition, muscle fibers break down, releasing potentially toxic compounds into the bloodstream. The risk and severity of muscle damage is dosage-related, and the compounds in the blood often lead to kidney damage. To monitor this condition, physicians measure blood levels of creatine phosphokinase (CPK), at the start of statin treatment, and again if the patient develops muscle pains. CPK is an enzyme found predominantly in brain and muscle tissue, so elevated CPK levels are a warning sign for statin-related muscle damage.

In 2004, the consumer watchdog group Public Citizen called on the FDA to remove Crestor from the market, claiming it was linked to life-threatening muscle and kidney damage. Crestor's incidence of problems has been similar to the other statins. "However, its safety record is not as long as the other statins and no clinical trial demonstrating Crestor's clinical benefit for cardiovascular disease has been completed," Dr. Abramowicz says.