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High cholesterol affects many people throughout the world. High cholesterol levels can greatly increase the risk of heart disease, including potentially fatal heart attacks. Exercise, weight loss, and a diet low in cholesterol and saturated fats can help lower cholesterol levels. However, when these measures fail, cholesterol-lowering medications are usually needed. In this slideshow we'll discuss cholesterol basics, and review the classes of drugs prescribed to lower cholesterol.
What is cholesterol?
Cholesterol is a waxy, fat-like substance that your body needs to function normally. The cholesterol in a person's blood originates from two major sources; the diet and the liver. Dietary cholesterol comes primarily from meat, poultry, fish, and dairy products. Cholesterol is naturally present in cell walls or membranes everywhere in the body, including the brain, nerves, muscles, skin, liver, intestines, and heart. Your body uses cholesterol to produce many hormones, vitamin D, and the bile acids that help to digest fat. It takes only a small amount of cholesterol in the blood to meet these needs. If you have too much cholesterol in your bloodstream, the excess may be deposited in arteries, including the coronary (heart) arteries, where it contributes to the narrowing and blockages that cause the signs and symptoms of heart disease.
abnormally elevated cholesterol levels, a family history of heart attacks (particularly at a young age), increasing age, diabetes, and high blood pressure.
The next several slides are examples of statins currently prescribed to lower cholesterol.
atorvastatin (Lipitor)
Drug Class: Statins Prescription: Yes Generic: No Preparations: Tablets of 10, 20, 40, and 80 mg. Prescribed for: Atorvastatin (Lipitor) is used for the treatment of elevated total cholesterol, LDL, triglycerides, and to elevate HDL cholesterol. The effectiveness of atorvastatin (Lipitor) in lowering cholesterol is dose-related, meaning that higher doses reduce cholesterol more. Side effects: Atorvastatin (Lipitor) is generally well-tolerated. Minor side effects include constipation, diarrhea, fatigue, gas, heartburn, and headache. Atorvastatin (Lipitor) may cause liver and muscle damage.
rosuvastatin (Crestor)
Drug Class: Statins Prescription: Yes Generic: No Preparations: Tablets of 5, 10, 20, and 40 mg. Prescribed for: Rosuvastatin (Crestor) is used for the reduction of blood total cholesterol, LDL cholesterol and triglyceride levels, and to increase HDL cholesterol levels. Side effects: The most common side effects of rosuvastatin (Crestor) are headache, nausea, vomiting, diarrhea, and muscle pain. The most serious side effects are liver failure, muscle breakdown (rhabdomyolysis) and kidney failure.
simvastatin (Zocor)
Drug Class: Statins Prescription: Yes Generic: Yes Preparations: Tablets of 5, 10, 20, 40, and 80 mg. Prescribed for: Simvastatin (Zocor) is used for reducing total cholesterol, LDL cholesterol, and triglycerides, and for increasing HDL cholesterol. In patients with coronary heart disease, diabetes, peripheral vessel disease, or history of stroke or other cerebrovascular disease. Side effects: The most common side effects of simvastatin (Zocor) are headache, nausea, vomiting, diarrhea, abdominal pain, muscle pain, and abnormal liver tests. Hypersensitivity reactions have also been reported. The most serious potential side effects are liver damage and muscle inflammation or breakdown.
pravastatin (Pravachol)
Drug Class: Statins Prescription: Yes Generic: Yes Preparations: Tablets of 10, 20, 40, and 80 mg. Prescribed for: Pravastatin (Pravachol) is used for the reduction of total and LDL cholesterol as well as triglycerides, and to increase HDL cholesterol. It has been suggested that pravastatin may reduce the occurrence of heart attacks, strokes, and death caused by coronary artery disease. Side Effects: The most common side effects of pravastatin (Pravachol) are headache, nausea, vomiting, diarrhea, muscle pain, and abnormal liver tests. The most serious potential side effects are liver damage and muscle inflammation or breakdown.
lovastatin (Mevacor)
Drug Class: Statins Prescription: Yes Generic: Yes Preparations: Tablets of 10, 20, and 40 mg. Prescribed for: Lovastatin (Mevacor) is used to treat high LDL cholesterol. Effectiveness of the medication in lowering cholesterol is dose-related. Blood cholesterol determinations are performed in regular intervals during treatment so that dosage adjustments can be made. A reduction in LDL cholesterol level can be seen two weeks after starting therapy.
Side Effects: Side effects of lovastatin (Mevacor) are rare. Minor side effects include constipation, diarrhea, gas, heartburn, headache, and insomnia. Major side effects include abdominal pain or cramps, blurred vision, dizziness, itching, muscle pain or cramps, rash, or yellowing of the skin or eyes.
fluvastatin (Lescol)
Drug Class: Statins Prescription: Yes Generic: No Preparations: Tablets of 20 and 40 mg. Prescribed for: Fluvastatin (Lescol) is used to treat high LDL cholesterol. Effectiveness of the medication in lowering cholesterol is dose-related. Blood cholesterol determinations are performed in regular intervals during treatment so that dosage adjustments can be made. Side effects: Side effects of fluvastatin (Lescol) are rare. Minor side effects include constipation, diarrhea, gas, heartburn, headache, and insomnia. Major side effects include abdominal pain or cramps, blurred vision, dizziness, itching, muscle pain or cramps, rash, or yellowing of the skin or eyes.
fenofibrate (Tricor)
Drug Class: Fibrates Prescription: Yes Generic: No Preparations: Tablets of 48 and 145 mg. Prescribed for: Fenofibrate (Tricor) is used along with a non-drug program (including diet changes) to treat elevated cholesterol and triglyceride levels. Side effects: Common side effects of fenofibrate (Tricor) include upset stomach, constipation, headache, dizziness or trouble sleeping. Muscle damage may occur, and muscle pain, tenderness, weakness and fever should be reported promptly to the responsible physician. Decreased sexual drive, yellowing of the eyes or skin (jaundice), and stomach pain may occur and also should be reported.
gemfibrozil (Lopid)
Drug Class: Fibrates Prescription: Yes Generic: No Preparations: Tablet of 600 mg. Prescribed for: Gemfibrozil (Lopid) is used for persons with either low HDL cholesterol and/or high triglyceride concentrations to reduce the risk of heart attacks. It also is used in persons with very high triglyceride levels that may cause pancreatitis (inflammation of the pancreas). Side effects: Side effects of gemfibrozil (Lopid) include upset stomach (1 in 5 patients), diarrhea (1 in 14 patients), tiredness (1 in 30 patients) and nausea or vomiting (1 in 40 patients). Additional patients may experience dizziness, tiredness, tingling in the extremities, headache, decreased sexual drive, impotence, depression, or blurred vision. Less common side effects are muscle aches, pains, weakness or tenderness.
colesevelam (Welchol)
Drug Class: Bile acid sequestrants Prescription: Yes Generic: No Preparations: Tablet of 625 mg. Prescribed for: Colesevelam (Welchol) is used to treat high blood cholesterol levels, especially high levels of LDL cholesterol. It does not lower cholesterol as much as the statin class of drugs, but when used in combination with a statin, it lowers cholesterol levels further than the statin alone. Colesevelam (Welchol) also is used in combination with other drugs for treating type 2 diabetes such as metformin (Glucophage), sulfonylureas, or insulin to further lower blood sugar levels. Side effects: Colesevelam (Welchol) usually is well-tolerated. Patients may experience constipation, upset stomach, indigestion, headache, stomach pain, or diarrhea.
colestipol (Colestid)
Drug Class: Bile acid sequestrants Prescription: Yes Generic: No Preparations: Tablet of 1 gm. Granules in 5gm packets or bulk. Prescribed for: Colestipol (Colestid) is used for the treatment of high cholesterol in conjunction with dietary control; for the treatment of diarrhea due to increased intestinal bile acids after some types of surgery; for the treatment of itching associated with partial obstruction to the flow of bile due to liver disease. Side effects: Side effects of colestipol (Colestid) include constipation, stomach upset, heartburn, belching, gas, nausea, loss of appetite, aggravated hemorrhoids, change of taste, headache, or itching. If patients experience unusual bruising or bleeding, severe stomach aches, or vomiting they should notify their physicians.
cholestyramine (Questran)
Drug Class: Bile acid sequestrants Prescription: Yes Generic: Yes Preparations: Powder Prescribed for: Cholestyramine (Questran) is used for reducing cholesterol levels in the blood, to relieve the itching of liver and biliary disease, and to treat overdoses of digoxin or thyroid hormone. Side effects: The most common side effects are constipation, abdominal pain, bloating, vomiting, diarrhea, weight loss, and excessive passage of gas (flatulence). Long-term use of cholestyramine may cause a deficiency of vitamins A, D, E, and K.
Prescription: Yes and over-the-counter (OTC) Generic: Yes Preparations: Tablets of 50, 100, 250, 500 and 750 mg. Capsules of 125, 250, 400, 500, 750 and 1000 mg. Prescribed for: Nicotinic acid (vitamin B3 or niacin) is used for treating niacin deficiency and elevated blood cholesterol and/or triglyceride levels and for increasing HDL cholesterol. Side effects: The most common side effects of nicotinic acid (vitamin B3 or niacin) are stomach upset, flushing, headache, itching and tingling sensations of the extremities. Rare cases of liver failure or muscle injury have occurred from the use of nicotinic acid.
ezetimibe (Zetia)
Drug Class: Cholesterol absorption inhibitors Prescription: Yes Generic: No Preparations: Tablets of 10 mg. Prescribed for: Ezetimibe (Zetia) lowers blood cholesterol by reducing the absorption of cholesterol from the intestine. Used in combination with statins, it reduces levels of total cholesterol, LDL cholesterol, and triglycerides. It also may raise HDL cholesterol. Combining ezetimibe with a statin is more effective than either drug alone. Side effects: Ezetimibe (Zetia) usually is well-tolerated. Diarrhea, abdominal pain, back pain, joint pain, and sinusitis were the most commonly reported side effects, occurring in one in every 25 to 30 patients. Hypersensitivity reactions, including angioedema (swelling of the skin and underlying tissues of the head and neck that can be life-threatening) and skin rash occur rarely. Nausea, pancreatitis, muscle damage (myopathy or rhabdomyolysis), and hepatitis have been reported.
ezetimibe/simvastatin (Vytorin)
Prescription: Yes Generic: No Preparations: Tablets of 10/10, 10/20, 10/40, 10/80 mg. (ezetimibe/simvastatin) Prescribed for: Ezetimibe/simvastatin (Vytorin) is a combination of ezetimibe (Zetia) and simvastatin (Zocor) that is used for treating high levels of cholesterol in the blood. Vytorin reduces total cholesterol and LDL cholesterol while it increases HDL cholesterol. Side effects: The most common side effects of ezetimibe/simvastatin (Vytorin) are headache, nausea, vomiting, diarrhea, muscle pain, and abnormal liver tests. Hypersensitivity reactions have also been reported. The most serious potential side effects are liver damage and muscle inflammation or breakdown.