Statins are the most effective drugs for lowering LDL (“bad” cholesterol) levels and reducing the risk for heart disease and stroke. Statins inhibit the liver enzyme HMG-CoA reductase, which the body uses to manufacturer of cholesterol.
Current guidelines from the American College of Cardiology and American Heart Association recommend a statin drug as the first-line drug treatment for patients at risk for cardiovascular disease. Other cholesterol-lowering medications are not as effective as statins and are not recommended, except in rare cases.
Depending on your LDL cholesterol level, presence of atherosclerotic heart disease, 10-year risk for heart disease, and whether or not you have diabetes, your doctor will recommend either a moderate-intensity or high-intensity statin therapy dosage plan. The exact dosage will depend on the statin drug the doctor prescribes for you.
If a particular statin drug does not work for you, or if you experience significant side effects, your doctor may switch you to a different statin drug.
Brands. Statins approved in the U.S. include:
- Lovastatin (Mevacor, generic)
- Pravastatin (Pravachol, generic)
- Simvastatin (Zocor, generic)
- Atorvastatin (Lipitor, generic)
- Fluvastatin (Lescol)
- Pitavastatin (Livalo)
- Rosuvastatin (Crestor)
Some statins come as fixed-dose combination drugs, which combine two drugs in one pill. Examples include sitagliptin/simvastatin (Juvisync), amlodipine/atorvastatin (Caduet), and ezetimibe/simvastatin (Vytorin).
Side Effects. Statin side effects may include diarrhea, constipation, upset stomach, muscle and joint pain, tendon problems, headache, fatigue, and forgetfulness or memory loss. More serious side effects include liver and muscle damage. Patients should immediately tell their doctor about any unusual muscle discomfort or weakness, fever, nausea or vomiting, or darkening of urine color.
Statins can affect the results of liver tests. Liver enzyme tests should be performed before starting statin therapy. Liver damage is a rare but can occur, particularly at higher doses. Tell your doctor if you have symptoms that indicate liver problems such as unusual fatigue, loss of appetite, upper belly pain, dark-colored urine or yellowing of the skin or whites of the eyes.
A specific safety concern with statins is an uncommon muscle disease called myopathy, in which a patient may experience muscle pains and certain lab tests may be elevated. Severe myopathy called rhabdomyolysis can lead to kidney failure, but fortunately its occurrence is very rare. The risk for myopathy/rhabdomyolysis is highest at higher doses and in older people (over 65 years), those with hyperthyroidism, and those with renal insufficiency (kidney disease).
Rosuvastatin (Crestor) may in particular increase the risk for myopathy, especially when given at the highest dose level (40 mg). The FDA advises that patients should not start therapy at a high dose. In addition, people of Asian heritage appear to metabolize the drug differently and should start treatment at the lowest rosuvastatin dose (5 mg). Maximal doses of simvastatin and lovastatin also appear to increase the risk of myopathy.
Other Safety Concerns. Statins are recommended as the best drugs for improving cholesterol and lipid levels in people with type 1 or type 2 diabetes. However, they may increase blood glucose levels in some patients, especially when taken in high doses. They may also increase the risk for developing type 2 diabetes in patients with risk factors.
There is evidence that statins may increase the risk for developing cataracts.
Interactions with Drugs and Food. Statins may have some adverse interactions with other drugs. Patients should tell their doctors about any other medications they are taking. Medications that should not be taken along with statins include protease inhibitors, telaprevir, cyclosporine, macrolide antibiotics, and certain antifungals. Grapefruit juice and Seville oranges can increase the blood levels of certain statins.
Other Cholesterol-Lowering Drugs
Statins are the primary drugs for treating cholesterol and reducing cardiovascular disease risk. They have replaced the other drugs that were used for lowering cholesterol. For certain patients and in select cases, however, some of these drugs may be used.
Fibrates. Fibrates, also called fenofibrates, are generally reserved for patients with extremely high triglyceride levels or patients with high cholesterol who cannot tolerate a statin drug.
Gemfibrozil (Lopid, generic) is the most commonly prescribed fibrate. Other fibrates include fenofibrate (TriCor, Lofibra) and fenofibric acid (Trilipix). These drugs have many side effects. They can cause gallstones, abnormal heart rhythms, and muscle problems (myopathy), which may lead to kidney damage. A fibrate should only be carefully used in combination with a statin because of increased risk for myopathy.
Click the icon to see an image of gallbladder problems.
Niacin. For many years, high doses of niacin (nicotinic acid or vitamin B3) were considered a treatment option for low HDL cholesterol and high LDL cholesterol and triglyceride levels. Research now suggests that niacin does not add to the benefit of a statin alone for reducing the risk of cardiovascular events, including heart attacks and stroke. In addition, niacin can cause unpleasant and potentially dangerous side effects. Therefore, its use has been declining.
Bile-Acid Binding Drugs. Bile-acid binding drugs are also known as bile acid resins or bile acid sequestrants. They reduce LDL levels. Brands include cholestyramine (generic), colesevelam (Welchol), and colestipol (Colestid, generic).
Bile acid resins commonly cause constipation, heartburn, gas, and other gastrointestinal problems, side effects that many people cannot tolerate. These drugs may increase the risk for osteoporosis, elevate triglyceride levels, and interfere with the absorption of other medications.
Ezetimibe. Ezetimibe (Zetia) blocks absorption of cholesterol that comes from food. It helps reduce LDL cholesterol, but not as well as statin drugs. Unlike statins, it has not been proven to prevent heart disease or stroke. Vytorin is a combination of ezetimibe and the statin simvastatin in a single pill. Liptruzet combines ezetimibe and the statin atorvastatin in a single pill.
Prescription Fish Oil Supplements. Lovaza and Vascepa are prescription forms of omega-3 fish oil, which may be prescribed to help lower triglyceride in people who have very high levels. Recent research has questioned the benefits of fish oil supplements for preventing heart attack and stroke.
Other Drugs. Mipomersen (Kynamro) and lomitapide (Juxtapid) are approved specifically for treatment of homozygous familial hypercholesterolemia, a very rare genetic condition that can cause heart attack and stroke before the age of 30.