A Guide to Cholesterol Drugs

Learn about the different categories of cholesterol-lowering medicines, along with their specific benefits and risks.

Your doctor has decided that a cholesterol-lowering drug is right for you. You may be wondering which drug is best to lower your cholesterol and how the medication will work in your body. You may also have questions about side effects and what you should know about your new medication. Here is some information about different types of cholesterol-lowering medications, how they work, what you can expect and what to be aware of as you begin taking your new medication.

Statins: The Most Effective Cholesterol-Lowering Drugs

Statins are the most frequently prescribed class of cholesterol-lowering drugs and the most effective. Statins work in your liver to lower cholesterol by blocking a key step in the production of cholesterol. Statins are particularly effective at lowering LDL levels. Statins are prescribed to lower LDL and triglyceride levels in the blood, as well as increase HDL levels. Statins should be used in conjunction with a healthy diet and exercise. Serious side effects associated with statins are rare but may include problems with your muscles or liver. You should tell your doctor as soon as possible if you experience muscle pain, weakness or tenderness with fever or flu-like symptoms, dark urine, unexplained tiredness or abdominal pain.

Drugs in this class include:

Zocor (simvastatin)

  • Prescribed for people at risk for heart disease as a result of diabetes, vascular disease or history of stroke, or those with existing heart disease
  • Reduces your risk of heart attack, stroke or death from heart disease
  • Reduces the risk for surgical procedures related to heart disease
  • Can be used in adults and children 10 years of age and older
  • Common side effects may include mild stomach pain, gas, bloating, stomach upset, heartburn, nausea, diarrhea or constipation

Lipitor (atorvastatin)

  • Prescribed to lower the risk of stroke, heart attack or other heart complications in people with diabetes, heart disease or other risk factors
  • Prescribed for adults and children 10 years of age and older
  • Common side effects may include mild stomach pain, gas, bloating, stomach upset, heartburn, nausea, constipation or headache

Crestor (rosuvastatin)

  • Prescribed to reduce the risk for heart attack, stroke and other heart-related problems
  • Prescribed to slow the progression of atherosclerosis in some people
  • Common side effects include headache, muscle pain, abdominal pain, weakness and nausea
  • Prescribed for adults and children 10 years of age and older

Pravachol (pravastatin)

  • Prescribed to lower the risk of stroke, heart attack, death and other heart complications in people with diabetes, heart disease or other risk factors
  • Prescribed for some people to reduce the risk of surgical procedures related to heart disease
  • Prescribed for some people to slow the progression of atherosclerosis
  • Prescribed for adults and children 8 years of age and older
  • Side effects may include abdominal pain, chest pain, constipation, cough, diarrhea, dizziness, fatigue, gas, headache, heartburn, swelling of nasal passages, muscle aching or weakness, nausea, rash, stomach discomfort, urinary problems or vomiting

Mevacor (lovastatin) and Altoprev (lovastatin extended-release)

  • Prescribed to reduce the risk of heart attack, angina (chest pain) and the need for surgical procedures related to heart disease
  • Prescribed to slow the progression of atherosclerosis in people who already have heart disease
  • Can be used in adults and children 10 years of age and older
  • Side effects may include upset stomach, flatulence, headache, nausea, weakness, diarrhea, constipation or stomach pain

Livalo (pitavastatin)

  • Newest statin on the market; approved in 2009
  • Only prescribed to lower cholesterol; effects related to heart disease have not been determined
  • Safety and effectiveness in the pediatric population have not been determined
  • Common side effects may include muscle pain, back pain, diarrhea, constipation or pain in the arms or legs

Lescol (fluvastatin) and Lescol XL (fluvastatin extended-release)

  • Prescribed for people with heart disease to slow the buildup of cholesterol in the arteries of the heart
  • Prescribed to lower the need for procedures to help restore blood flow to the heart
  • Approved for adults and children 10 years of age and older
  • Side effects may include flu-like symptoms, sinus infection, diarrhea, stomach pain, upset stomach, headache, trouble sleeping and feeling tired

Fibrates: Good for Triglyceride Levels

Fibrates, sometimes called fibric acid derivatives, are primarily effective in lowering triglyceride levels and can also raise HDL levels. Your doctor may prescribe a fibrate drug if you have very high triglyceride levels or if you have low HDL levels and high triglyceride levels. Fibrates are not prescribed to lower LDL levels and may actually cause them to increase slightly in some patients. Fibrates should be used in combination with a healthy, low-fat and low-cholesterol diet and exercise program to help lower your cholesterol. Some of the side effects common to this class of cholesterol-lowering drugs may include dyspepsia (upset stomach, indigestion), gallstones and problems with your muscles. Tell your doctor as soon as possible if you experience abdominal pain, nausea, vomiting, unexplained muscle pain, weakness or tenderness.

Drugs in this class include:

Lopid (gemfibrozil)

  • Prescribed to lower your triglyceride levels if you are at risk for pancreatitis (inflammation of the pancreas) and diet and exercise alone have not lowered your triglycerides enough
  • Prescribed to reduce the chances of developing coronary artery disease if you are at risk and have not responded well to diet and exercise or other cholesterol-lowering medications
  • Should not be prescribed if you only have high LDL levels or low HDL levels
  • Common side effects include upset stomach, nausea, vomiting or abdominal pain
  • May slightly increase your risk of gallstones
  • Usually taken twice daily

Fenofibrate

  • Decreases the levels of fatty substances in your blood
  • Has not been shown to decrease the risk of heart problems caused by fatty substances in the blood
  • Available in different formulations including a capsule, a delayed-release capsule and a tablet; some are taken with a meal and others may be taken without regard to food
  • Side effects may include constipation, diarrhea, heartburn, pain in your back, arm or legs or headache
  • May slightly increase your risk of gallstones, hepatitis (inflammation of the liver) or myositis (inflammation of the muscles)
  • Usually taken once daily

Drugs that have fenofibrate as the active ingredient include:

  • Antara
  • Fenoglide
  • Lofibra
  • Lipofen
  • Tricor
  • Triglide
  • Trilipix

Niacin: Increases HDL Levels

Nicotinic acid, commonly referred to as niacin, mainly works in your liver to increase HDL levels and decrease LDL and triglyceride levels. Your doctor may choose to prescribe nicotinic acid if you have low HDL levels. Nicotinic acid raises HDL levels more than other cholesterol-lowering drugs. It is especially beneficial if you have low HDL levels and high triglyceride levels.

Drugs in this class include:

  • Niacin
  • Niacor (immediate-release)
  • Niaspan (extended-release)
  • Slo-Niacin (sustained-release)

Side effects common to this class of cholesterol-lowering drugs include:

  • Sudden blushing or redness of the face (known as flushing); more common with immediate-release forms of nicotinic acid
  • Itching
  • Liver problems; more likely with sustained-release forms of nicotinic acid and less likely with extended-release formulation
  • High blood sugar
  • Increased levels of uric acid in the blood, which may lead to gout
  • Gastrointestinal distress (upset stomach, gas, nausea, vomiting and diarrhea)
  • Dizziness
  • Lightheadedness
  • A fast or slow heartbeat

If you experience flushing and itching when you start taking niacin, there are a few tips that can help you cope with these side effects. These side effects slowly go away over time for most people. Talk to your doctor and make sure you are starting with a low dose and slowly increasing the dose. This usually helps reduce flushing and itching. Also check with your doctor about whether it safe to take aspirin 30 to 60 minutes before your dose of niacin; this also helps. Taking niacin with a snack also helps to decrease some of the side effects. Discuss these options with your doctor to determine which would be best for you.

Cholesterol Absoption Inhibitors: A New Class of Drugs

Cholesterol absorption inhibitors are a newer class of cholesterol-lowering drugs. They are most effective in lowering LDL cholesterol. Cholesterol absorption inhibitors work in your intestines to block the absorption of cholesterol, decreasing the amount your body can absorb. This class of cholesterol-lowering drugs lowers total cholesterol and LDL levels and may help to lower triglycerides and raise HDL levels as well. Common side effects may include upper respiratory infection, diarrhea, joint pain, sinus inflammation, or pain in the arms or legs.

The only drug in this class is:

  • Zetia (ezetimibe)

Bile Acid Sequestrants: Eliminating Cholesterol

Bile acid sequestrants, also referred to as resins, work in your intestines to eliminate cholesterol from your body. They bind to cholesterol-containing bile (a digestive substance produced in your liver) in your intestines, preventing it from being absorbed. Bile acid sequestrants primarily lower LDL levels. These cholesterol-lowering drugs are not absorbed into the body. Side effects common to this class of drugs may include gastrointestinal distress and constipation. A major limitation of this class of drugs is the potential for drug interactions.

Drugs in this class include:

  • Welchol (colesevelam)
  • Questran, Questran Lite, and Prevalite (cholestyramine)
  • Colestid (colestipol)

Combination Therapy: Finding the Right Mix

If you have more than one component of your cholesterol profile that needs improvement, your doctor may prescribe a combination of the above medications. There are several formulations of cholesterol-lowering drugs available as a combination of two treatment options.

Combination drugs include:

  • Vytorin (simvastatin and ezetimibe)
  • Simcor (simvastatin and niacin)
  • Advicor (lovastatin and niacin)

If your doctor prescribes a combination treatment to lower your cholesterol, the potential for side effects may be increased. If you develop anything unusual or bothersome or are unsure if you may be experiencing a side effect, contact your doctor as soon as possible.

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