Currently, many classes of cholesterol medications are available to treat high cholesterol, and they all affect the various components of cholesterol differently. The classes of agents are detailed below. HMG CoA reductase inhibitors (commonly known as “statins”) are the most commonly prescribed medications and are the most effective in lowering LDL levels. Bile acid sequestrants also help lower LDL and are usually chosen along with a statin or if a patient cannot take a statin due to side effects or other reasons that make this treatment inadvisable. Bile acid sequestrants may raise triglycerides and should not be used in patients with elevated triglycerides. Fibric acid derivatives are the main class to help lower triglycerides and also help lower LDL levels. Nicotinic acid helps raise HDL and also lowers triglycerides. It has some effect on lowering LDL levels. Ezetimibe is a new drug class that is used mainly to lower LDL. It is usually given along with a statin when a statin alone is not effective in lowering LDL levels to goal. It can also be used alone. Fish oils are available over-the-counter and are also found in certain types of fish. The main effect is lowering triglycerides. It is very important to remember that medications are supplements to the primary treatment, which is lifestyle modifications.
• HMG CoA reductase inhibitors (also known as Statins)
Lipitor (atorvastatin)
Lescol (fluvastatin)
Mevacor (lovastatin)
Pravachol (pravastatin)
Crestor (rosuvastatin)
Zocor (simvastatin)
This is the most effective class of drugs for lowering LDL, the “bad” cholesterol. They inhibit HMG CoA reductase, an enzyme that is the rate-limiting step in making cholesterol. Therefore, they stop the “bad” cholesterol from being made in the liver. The statins are typically most effective when taken at bedtime when most of the cholesterol is made in the liver. They also help decrease triglycerides and increase HDL. Some of the statins have been shown to reduce deaths from cardiovascular events. The main side effects one might experience are stomach discomfort, muscle soreness, tenderness, weakness or pain, and possible abnormal liver function tests. Patients should notify their doctors if they are experiencing any muscle symptoms or have noticed brown urine. One should not be taking a statin if he or she has active or chronic liver disease. After starting a statin, a blood test will need to be done after 12 weeks to make sure liver function is normal.
• Bile Acid Sequestrants
Questran (cholestyramine)
Colestid (colestipol)
Welchol (colesevelam)
The main use of this class of drugs is to lower LDL cholesterol. They act by binding bile acids in the intestine through anion exchange. The binding results in a decrease of cholesterol in the liver, which, in turn, lowers LDL cholesterol. The bile acid sequestrants also increase HDL but have no effect on or may increase triglycerides. This class of medications has been shown to reduce the risk of coronary events. The sequestrants are useful in combination with statins. These medications should be used with caution in patients with high triglycerides because these drugs can increase triglycerides. Patients with triglycerides (higher than 400 mg/dL) should not receive the sequestrants, and it is recommended to avoid them if levels are higher than 250 mg/dL. Cholestyramine and colestipol are administered as powders that have to be mixed with water or juice; colestipol is also available as a tablet. Colesevelam comes only in tablet form, making it more convenient to administer and decreasing the risk of drug interactions. Cholestyramine and colestipol can decrease the absorption of a number of drugs. It is generally recommended to take the other drugs either one hour before or four hours after the cholestryramine and colestipol. Colesevelam can generally be administered with other drugs. The main side effects one might experience are constipation, bloating, indigestion, nausea, abdominal pain, and belching.
• Fibric Acid Derivatives
Tricor (fenofibrate)
Lopid (gemfibrozil)
The fibric acid derivatives lower LDL and triglycerides and increase HDL. Fibric acids inhibit lipolysis (the breakdown of fat) and decrease the amount of fatty acids taken up by the liver. They also inhibit VLDL secretion by the liver, which results in a decrease in circulating VLDL levels. They are most effective at lowering triglyceride levels. This class of medications has been shown to reduce the risk of coronary events. They should not be used in patients with severe liver or renal problems. The main side effects one might experience are heartburn, gallstones, muscle pain, weakness, soreness, and abdominal pain. It is recommended to take fenofibrate with meals and gemfibrozil before meals. Patients should inform their doctors if they are experiencing any type of muscle pain.
• Nicotinic Acid
Niacin (immediate release)
Niaspan (sustained release)
Nicobid (extended release)
Nicotinic acid works by inhibiting the production of VLDL by the liver. It inhibits the peripheral mobilization of free fatty acids, reducing liver secretion of VLDL. This medication is most effective at raising HDL, the “good” cholesterol. It decreases LDL and triglycerides as well. Nicotinic acid is also known as vitamin B3, which is found in many foods including meat, eggs, fish, cereal, milk, and green vegetables. The daily recommended dietary allowance of niacin is 14 to18 mg/day in adults. Small doses often increase HDL and decrease triglycerides, but doses of 2 to 3 grams per day are often needed to lower LDL. Nicotinic acid has been shown to reduce the risk of coronary events. The main side effects one might experience are flushing, itching, an increase in blood sugar, gout due to increased uric acid, abdominal discomfort, heartburn, diarrhea, vomiting, nausea, indigestion, and possible liver toxicity. Patients with liver disease and severe gout should not receive nicotinic acid. Diabetics should be careful taking this medication since it can raise blood sugar levels especially at higher doses. To minimize flushing, the dose is usually started low and increased as one builds tolerance. After extended use, most patients develop tolerance to the flushing. To reduce flushing, take a low dose aspirin 30 minutes to an hour before taking niacin. Niaspan and Nicobid are generally better tolerated and do not cause as much flushing as niacin causes.
• Ezetimibe (Zetia)
This new class of cholesterol medication inhibits absorption of cholesterol from food. This promotes elimination of cholesterol out of the body through the intestines before it can be absorbed. It decreases LDL and triglycerides and increases HDL. It has the most effect when given in combination with a statin. It can be taken with or without meals. The main side effects include abdominal pain, diarrhea, chest pain, dizziness, headache, fatigue, and muscle pain. Patients should tell their doctors if they experience any of these symptoms for a long time. It has not yet been proven to reduce the risk of coronary events.
• Fish Oils
Fish oil capsules can be taken to help lower cholesterol. Fish oil is effective at lowering triglycerides. Eating fish that contains fish oils, including mackerel, herring, tuna, halibut, salmon, cod liver, or whale or seal blubber, can also help lower triglycerides. Fish oils contain omega-3 fatty acids that can help lower cholesterol, blood pressure, and plaque formation. Fish oils also can help reduce cardiac arrhythmia and arthritis pain as well as benefiting some cancer treatments. The most common side effects are fishy taste, bad breath, heartburn, and upset stomach. Patients should talk to their doctors before trying fish oil capsules. Evidence has shown that high intakes of omega-3 fatty acids (1 to 2 grams per day) can reduce the risk of major coronary events in patients who already have coronary heart disease. They may also increase the risk of bleeding when given to patients on medications to prevent or reduce clotting.
Summary
Cholesterol numbers are important to watch, particularly as you age. Although some factors are beyond our control since we are born with them, many factors can be addressed. Fortunately, many effective medication options that will help prevent heart problems are available. The best first defense, however, is to take charge of your own health through education, diet, and exercise.
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