Cholesterol and Drugs

High Cholesterol Can Be Controlled The number of people suffering from high cholesterol around the world is staggering. The sad truth is that many people do not even realize they are affected by high cholesterol. High cholesterol greatly increases the risk of heart disease and often leads to potentially fatal heart attacks. Fortunately, lowering your cholesterol is possible. By eating a heart healthy diet that is low in saturated fat and cholesterol, exercising, and portioning your meals, you can often get your cholesterol count down without the help of drugs. However, if these methods are not sufficient, your physician will prescribe medication. But don't give up your healthy lifestyle! Keep up the good habits in conjunction with your medication.

What Exactly Is Cholesterol? A common misconception is that your body does not need cholesterol. The fact is that it does. Cholesterol is a waxy, fat-like substance that your body requires in order to function normally. It is naturally present in cell walls or membranes everywhere in the body, including the brain, nerves, muscles, skin, liver, intestines, and heart. The two major sources of cholesterol are your diet and your liver. The main function of cholesterol is to produce hormones and vitamins that keep your body running properly. Problems with cholesterol start when you have too much in your blood stream and it ends up sticking to artery walls where it can eventually lead to a blockage. This result is frightening to think about but it's something we must address.

Bad Cholesterol, Good Cholesterol, and Triglycerides Bad Cholesterol, scientifically referred to as LDL cholesterol, is the "bad" cholesterol because elevated levels of LDL are associated with an increased risk of heart disease. LDL lipoprotein deposits cholesterol on the artery walls. This causes the formation of a hard, thick, substance called cholesterol plaque. Over time, cholesterol plaque results in thickening of the arterial walls and narrowing of the arteries, a process called atherosclerosis that often leads to potentially fatal heart attacks. Good cholesterol, known around the medical world as HDL, is referred to as “good” because HDL cholesterol particles prevent atherosclerosis by extracting cholesterol from the arterial walls and disposing of it through the liver. In other words, it takes away plaque from the arterial walls, thus allowing arteries to function properly. HDL is your body's best natural defense against plaque and heart disease. Triglycerides are fatty substances composed of three fatty acids. Like cholesterol, triglycerides in the blood comes from the diet or liver.

Types of Cholesterol Drugs There is an array of cholesterol drugs. Several classes are available here in the United States for physicians to prescribe to their patients. The drugs include but are not limited to statins (HMG CoA reductase inhibitors), nicotinic acid (niacin), fibric acid derivatives (fibrates), bile acid sequestrants, and cholesterol absorption inhibitors. Some of these medications can also be combined to lower LDL cholesterol more aggressively and increase HDL cholesterol levels at the same time. In fact, the practice of combining two drugs for better results is very main stream these days. Remember, always consult your physician before taking any medications.

What Are Fibrates? Fibrates are effective medications that lower blood triglyceride levels. Fibrates work by inhibiting production in the liver of VLDL (particles in the blood that carry triglycerides and lipoproteins), and by speeding up the removal of triglycerides from the blood.

Generic Name: (gemfibrozil) Brand Name: (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), fatigue (1 in 30 patients) and nausea or vomiting (1 in 40 patients). Some patients may also experience dizziness, tingling in the extremities, headache, decreased sexual drive, impotence, depression, or blurred vision. Less common side effects are muscle aches, pains, weakness or tenderness.

Generic Name: (fenofibrate) Brand Name (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 prescribing physician. Decreased sexual drive, yellowing of the eyes or skin (jaundice), and stomach pain may occur and also should be reported.

What Are Bile Acid Sequestrants? Bile acid sequestrants bind bile acids in the intestine and cause more of the bile acids to be excreted in the stool. This reduces the amount of bile acids returning to the liver and forces the liver to produce more bile acids to replace the bile acids lost in the stool.

Generic Name: (colesevelam) Brand Name: (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. Side effects: Colesevelam (Welchol) usually is well-tolerated. Patients may experience constipation, upset stomach, indigestion, headache, stomach pain, or diarrhea.

Generic Name: (colestipol) Brand Name: (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.

Generic Name: (cholestyramine) Brand Name: (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.

What Is Nicotinic Acid? Nicotinic acid (vitamin B3 or niacin) is a B vitamin. An average American diet contains 15-30 mg of niacin per day. However, in treating blood cholesterol and triglyceride disorders, high doses (1-3 grams a day) of nicotinic acid are necessary. Nicotinic acid is available in several preparations. Prescription nicotinic acid includes immediate release niacin or sustained release niacin. Over-the-counter (OTC) nicotinic acid is available as sustained release niacin. OTC preparations are not federally regulated, and some OTC preparations may have no active ingredient and are ineffective in lowering LDL or raising HDL cholesterol.

Generic Names: ( niacin, nicotinic acid, vitamin B3) Brand Names (Niacor, Niaspan, Slo-Niacin) 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.

What Are Statins? Statins are a class of drugs that lower the level of cholesterol in the blood by reducing the production of cholesterol by the liver. Statins block the enzyme in the liver that controls the production of cholesterol. Most patients are placed on statins because of high levels of cholesterol. However, statins are also used for preventing and treating atherosclerosis that causes chest pain, heart attacks, strokes, and intermittent claudication in individuals who have or are at risk for atherosclerosis.

Generic Name: (atorvastatin) Brand Name (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.

Generic Name: (rosuvastatin) Brand Name: (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.

Generic Name: (simvastatin) Brand Name: (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.

Generic Name: (pravastatin) Brand Name: (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.

Generic Name: (lovastatin) Brand Name: (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.

Generic Name: (fluvastatin) Brand Name: (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.

What Are Cholesterol Absorption Inhibitors? This relatively new class of cholesterol-lowering medication works by preventing the absorption of cholesterol from the intestine. Selective cholesterol absorption inhibitors are most effective at lowering the LDL (bad) cholesterol but may also have modest effects on lowering triglycerides (blood fats), and raising HDL (good) cholesterol.

Generic Name (ezetimibe) Brand Name (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.

Combining Drugs As noted on the previous slides, some medications are primarily useful in lowering LDL cholesterol, others in lowering triglycerides, and some in elevating HDL cholesterol. Doctors may also prescribe two medications from two different drug classes to lower LDL more aggressively and increase HDL cholesterol levels at the same time.

Generic Names: (ezetimibe/simvastatin) Brand Name (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.

Generic Names: (niacin and lovastatin) Brand Name (Advicor) Prescription: Yes Generic: No Preparations: Tablet of 500/20 and 1000/20 mg (niacin/lovastatin). Prescribed for: Niacin and lovastatin (Advicor) is used for treating elevated blood levels of total cholesterol, LDL cholesterol, and triglycerides, and for raising low levels of HDL cholesterol. Side effects: Please refer to the individual slides for niacin and lovastatin.

Reminder! Always consult a medical professional before taking any kind of medication.