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How cholesterol-lowering drugs work Too much of a good thing. That's what you've got if you have high cholesterol — one of the most common health problems. Cholesterol is in every cell of your body, and every cell needs it. But your risk of cardiovascular disease goes up considerably if you have too much of this waxy, fatty substance in your blood. A diet low in fat but rich in phytochemicals, fiber and soy, plus weight loss and other lifestyle changes can help bring your cholesterol down. But sometimes they aren't enough. Your cholesterol level may still put you at risk of a heart attack or stroke. Fortunately an array of powerful drugs are now available that can rapidly reduce your cholesterol and, ultimately, the health risks it poses.
Your liver makes about 80 percent of the cholesterol in your body. You take in the rest when you eat animal products. Like nutrients from digested food, cholesterol is transported throughout your body in your bloodstream. For this to happen, your body coats cholesterol with a protein. The cholesterol-protein package is called a lipoprotein (lip-oh-PRO-teen). Low-density lipoprotein (LDL) is often referred to as bad cholesterol. Over time, it can build up in your blood vessels with other substances to form plaques. That can cause a blockage, resulting in a heart attack or stroke. In contrast, high-density lipoprotein (HDL) cholesterol is often called good cholesterol because it helps clean cholesterol from your blood vessels. Drug therapyIf, despite dietary changes and exercise, you still have too much bad cholesterol or not enough good, your doctor may consider drug therapy. Medications can change your blood levels of cholesterol or triglycerides, another type of fat (lipid) in your blood. By reducing LDL cholesterol or other lipids, the drugs can help prevent plaque buildup or even reduce it. And within a few months of taking them, they can help stabilize plaques already in your blood vessels. This may prevent them from cracking or breaking off, which can cause an obstruction or blood clot. Numerous studies have demonstrated that lowering cholesterol can reduce the risk of heart attack and death in people at high risk of a heart attack. The following types of drugs are used to lower cholesterol. They may be taken alone or in combination. Resins. Cholestyramine (Questran) and colestipol (Colestid), both known as resins, have been in use for about 20 years. They lower cholesterol indirectly by binding with bile acids in your intestinal tract. Bile acids are made in your liver from cholesterol and are needed for food digestion. By tying up bile acids, the drugs prompt your liver to make more bile acids. Since your liver uses cholesterol to make the acids, less cholesterol is available to reach your bloodstream. Fibrates. Gemfibrozil (Lopid) and fenofibrate (Tricor) are triglyceride-lowering drugs that also increase the levels of good cholesterol (HDL). They are also called fibric acid derivatives. They reduce triglyceride production and remove triglycerides from circulation. Niacin. Large doses of niacin, a vitamin, also can lower triglycerides. In addition, niacin can lower LDL cholesterol and increase HDL cholesterol, both beneficial effects. Statins. These drugs, introduced in the late 1980s, are fast becoming the most widely prescribed drugs to lower cholesterol. They are also known as HMG-CoA reductase inhibitors. You may have seen them advertised and already know their names: fluvastatin (Lescol), lovastatin (Mevacor), simvastatin (Zocor), pravastatin (Pravachol) and atorvastatin (Lipitor). Statins work directly in your liver to block a substance your liver needs to manufacture cholesterol. That depletes cholesterol in your liver cells and causes the cells to remove cholesterol from circulating blood. Depending on the dose, statins can reduce your LDL cholesterol by up to 40 percent. That's usually enough to bring your LDL levels within recommended guidelines. Statins may also help your body reabsorb cholesterol from plaques, which slowly unplugs your blood vessels. Statins reduce inflammation around the plaques, which helps stabilize them and reduces your chances of rupture and blockage of the affected artery. Statins are the only type of lipid-lowering drug proved to reduce your risk of death from cardiovascular disease. Along with niacin, statins have also been proved to reduce your risk of having a second heart attack. A word of caution, though: Don't eat any grapefruit or drink grapefruit juice at any time while you are taking this medication. Grapefruit juice interacts with statins, causing blood levels of the medication to rise. This can increase your risk of side effects from the statin.
Do you need medication?If your LDL cholesterol is more than 100 milligrams per deciliter (mg/dL) and your doctor knows you have cardiovascular disease — you've had a heart attack, for example — he or she will likely prescribe medication and lifestyle changes right away. The decision isn't as clear if you have high cholesterol without known cardiovascular disease. It then depends on how high your cholesterol is and whether you have other risk factors for a heart attack, such as:
At first your doctor may recommend exercise, a low-fat diet and other changes. But if these aren't effective, drug therapy in addition to these lifestyle changes is an option, particularly if you have other risk factors for cardiovascular disease. Drug therapy, along with lifestyle changes, is often recommended even in the absence of established cardiovascular disease if:
Weighing your optionsWhich lipid-lowering drug your doctor recommends for you depends on many factors. These include how much good or bad cholesterol you have and whether other lipids in your blood are high. Your age also may be a factor. Sometimes your doctor may recommend a combination of drugs. The effectiveness of lipid-lowering drugs varies from person to person. There isn't one drug that's best for everyone. Nor is it necessary to take the newest drug if your current medication is effective. The bottom line is that all lipid-lowering drugs approved by the Food and Drug Administration can, to different degrees, improve the balance of your good and bad cholesterol as well as your triglycerides, which slows the buildup of plaques in your blood vessels. That helps reduce your risk of cardiovascular disease — the goal of taking any of these medications.
A long-term programThe decision to take any kind of lipid-lowering drug is a serious matter. Once you start, you must typically stay on the drug the rest of your life. That can be expensive. You might also need to have your liver checked regularly. On rare occasions the drugs can cause liver damage, which is why they're not recommended if you have liver disease. Other side effects for most lipid-lowering drugs usually aren't serious, but they may be bothersome enough to keep you from taking the medication. Statins, for example, can cause muscle pain, especially when taken in combination with other drugs, such as gemfibrozil, antifungal medications or the popular antibiotic erythromycin. This side effect is rare, but you should notify your doctor promptly if it occurs. In addition, one study reports a slightly increased rate of nerve damage (neuropathy) for long-term statin users, especially those over age 50. The resins can cause constipation and bloating or decrease the effectiveness of other medications taken at the same time. Niacin sometimes causes irritating skin flushing and can elevate your blood sugar, aggravate a stomach ulcer or trigger an attack of gout. And fibrates can cause gallstones. Because lipid-lowering drugs have only been available for about 20 years, doctors haven't been able to study their safety when used over a lifetime. As with any medication, carefully weigh the advantages of taking a drug against not taking it. But if you have cardiovascular disease or are at high risk of it, lipid-lowering drugs are one of the most important treatment options you have.
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