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Drug treatments: Statins

Statins are considered the most effective drugs for the treatment of high cholesterol. Statins work by inhibiting a liver enzyme used to make cholesterol.

Drugs classified as statins include:

  • Atorvastatin (Lipitor)
  • Fluvastatin (Lescol)
  • Lovastatin (Mevacor)
  • Pravastatin (Pravachol)
  • Rosuvastatin (Crestor)
  • Simvastatin (Zocor)

The benefits of statins

  • They are particularly effective for lowering LDL ("bad" cholesterol) levels. They also reduce triglycerides.
  • Statins raise HDL ("good" cholesterol) levels, but to a lesser extent than other types of cholesterol medications.
  • Statins reduce the risk of first and second heart attacks in women, men, and older people with evidence of heart disease. In addition, they may reduce the risk of stroke.

Patients who may benefit

Statins are strongly recommended as the first choice for almost all patients with high cholesterol levels, particularly:

  • Patients with existing heart disease, diabetes, or both.
  • Postmenopausal women with heart disease or risk factors for heart disease.

Statins may be safe for children and adolescents with unhealthy cholesterol levels, but long-term studies are needed to confirm their value and safety in all children.

Side effects

Statins tend to be better tolerated than other cholesterol-lowering drugs. In many studies, the side effects reported were nearly the same as those taking placebo (inactive agents). The side effects may include upset stomach, nausea, constipation, gas, headaches, skin rashes, muscle aches, insomnia, unusual dreams, daytime drowsiness, and dizziness. Less common side effects include sexual dysfunction, numbness or tingling in the hands and feet, and depression.

Statins can affect the liver, so liver function should be assessed periodically through a blood test. Statins should never be taken by anyone with liver problems or by women who are pregnant or breast-feeding.

In very rare cases, drugs in this class may also lead to muscle tissue breakdown, which can overwhelm the kidneys (called rhabdomyolysis) and lead to kidney failure. Muscle cramps are not in themselves a major concern. If muscle cramps, aches, or pains occur, your doctor will look for signs of muscle tissue breakdown through a blood test that checks the level of an enzyme called creatine kinase (CK). The levels of CK would likely be much higher than normal (at least 10 times), with elevated creatinine (usually causing brown urine) and muscle cramps, before rhabdomyolysis would be diagnosed.

Interactions with drugs and food

Statins may have negative interactions with other drugs, including other cholesterol-lowering drugs. For example, when certain medications are taken with statins, the risk for muscle tissue breakdown increases. Such drugs include:

  • Diltiazem (Cardiem, Tiazac, Dilacor -- used for high blood pressure)
  • Fluvoxamine (for obsessive-compulsive disorder)
  • Protease inhibitors for HIV (such as indinavir, ritonavir, nelfinavir, and saquinavir)
  • Antibiotics classified as macrolides (such as azithromycin, clarithromycin, and erythromycin)
  • Cyclosporine (used following transplant)
  • Drugs for fungal infections (such as fluconazole, itraconazole, and miconazole)
  • Other cholesterol lowering drugs, including niacin and fibrates (for example, fenofibrate and gemfibrozil)

Using statins together with bile acid resins (such as cholestyramine) may improve cholesterol-lowering effects, but the two types of medications should not be taken within 4 hours of one another.

You should tell your doctor about any other medications or supplements you are taking. For example, statins should not be used with red yeast rice, a popular supplement promoted for lowering cholesterol. Also, statins may lower levels of certain antioxidants, including vitamin E, beta-carotene, and coenzyme Q10. However, these nutrients should be replenished from foods, NOT supplements -- one study suggested that taking vitamin E and C tablets may blunt the HDL-enhancing effects of a statin-niacin combination.

Grapefruit juice and Seville oranges (found in marmalades and other condiments, not in juice) may increase blood levels of statins and, therefore, increase the risk of side effects, including potential damage to the liver or muscle tissue.

Withdrawal of cerivastatin (Baycol)

One statin drug, cerivastatin, was withdrawn from the market on August 8, 2001, because of rare reports of death from rhabdomyolysis. This is a condition that causes muscle problems and can lead to kidney failure. People at highest risk for this complication were those taking high doses of Baycol and who also took the fibrate gemfibrozil.

Rhabdomyolysis has occurred with other statins, but even more rarely.

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Review Date: 10/10/2008
Reviewed By: Larry A. Weinrauch, MD, Asst. Prof. of Med., Harvard Medical School, and Private practice specializing in Cardiovascular Disease, Watertown, MA. Review provided by VeriMed Healthcare Network. Previously reviewed by Alan Greene, MD, FAAP, Stanford University School of Medicine (10/31/2006).
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