Medication Treatments for Lowering Cholesterol Levels

In many cases, diet changes and regular physical activity are not enough to lower high LDL-cholesterol to a desirable level.

Medication should be started for people who, despite dietary changes, regular physical activity and weight loss, need further treatment to get to their LDL-cholesterol target. In addition, medication therapy should be initiated immediately for anyone who has high LDL-cholesterol and either cardiovascular disease or diabetes.

Medication can change your levels of 'good' and 'bad' cholesterol and triglycerides. By reducing LDL-cholesterol, certain medications can help prevent plaque build-up inside your arteries.

However, it is important to remember that cholesterol-lowering medication is not a cure, and you will likely need to take it for the rest of your life. In addition, you will also need to exercise regularly, eat enough vegetables and fruit, cut down on saturated and trans fats and maintain a healthy weight.

Currently, there are five main classes of medications available that lower cholesterol. Your doctor can advise which may be appropriate for you. His or her choice will depend on many factors, including how much good (HDL) or bad (LDL) cholesterol you have, and whether other lipids or triglycerides in your blood are high. Your age or medical history may also be a factor. Sometimes a doctor will recommend a combination of medications.

Statins

Statins are the most widely prescribed group of cholesterol-lowering medications. They act by reducing the amount of cholesterol produced by the liver. With lower levels of cholesterol in the bloodstream, less LDL-cholesterol is incorporated into plaque, reducing your risk of cardiovascular disease. Statins are one of the most widely studied medications available.

Statins can lower your 'bad' cholesterol level, and also decrease triglycerides and increase HDL-cholesterol levels. More common side effects of statins may include headaches, nausea, cramps, diarrhea or constipation.

People taking statins have been able to lower their risk of heart attack and stroke. They also need fewer surgeries such as angioplasty and coronary bypass operations.

The statin medications currently available are atorvastatin (Lipitor^®), fluvastatin (Lescol^®), lovastatin (Mevacor^®), pravastatin (Pravachol^®), rosuvastatin (Crestor^®) and simvastatin (Zocor^®). All are available in once-a-day tablet form.

A "fixed dose combination therapy" (Caduet®) is also available, which combines a statin with a calcium channel blocker (a medication to treat high blood pressure). This can ease the process of taking the medication, since it only requires taking one pill instead of two. Ask your healthcare professional for more information on such an alternative.

Fibrates

Fibrates, or fibric acid derivatives, are mainly used for lowering triglycerides and increasing HDL-cholesterol levels. They work by increasing the activity of an enzyme that breaks down some kinds of cholesterol, helping the liver to eliminate cholesterol and blocking the production of triglycerides and cholesterol. Fibrates can significantly reduce triglyceride levels and can increase HDL-cholesterol, but they don't lower LDL-cholesterol levels as effectively. The fibrates currently available are bezafibrate (Bezalip^®), fenofibrate (Lipidil^®) and gemfibrozil (Lopid*). Their most common side effects include nausea, stomach pain, gas, diarrhea, constipation, itching, rash, tiredness and muscle aches.

Prescription niacin

Niaspan^® is an extended-release tablet of nicotinic acid (niacin or vitamin B3) that is available by prescription only. It can affect LDL-cholesterol levels while increasing the blood levels of HDL-cholesterol, and also reducing total cholesterol and triglyceride levels. The most common side effects of Niaspan^® are flushing, nausea, gas, heartburn, diarrhea, itching and low blood pressure. Niaspan^® is available in once-a-day form.

Resins

Resins, also called bile acid sequestrants, are primarily used to lower total cholesterol and LDL-cholesterol. They work by trapping bile acids in the bowels. When there are less bile acids, your body is forced to break down more cholesterol, which will lower the cholesterol level in your blood. The two currently available resins, cholestyramine (Questran^®) and colestipol (Colestid*), can reduce LDL-cholesterol levels but tend to raise triglyceride levels slightly. Side effects may include constipation, stomach pain, gas, heartburn, nausea, diarrhea and loss of appetite.

Cholesterol absorption inhibitors

Used alone or in combination with statins, a cholesterol absorption inhibitor such as ezetimibe (Ezetrol^®) decreases the body's absorption of cholesterol in the intestines. This reduces LDL-cholesterol, triglyceride and total cholesterol levels and raises HDL-cholesterol levels. The most common side effects are fatigue, joint pain, sinus infection, diarrhea, abdominal pain and back pain. Ezetimibe is available in once-a-day form.