Blood Cholesterol-Lowering Agents
To achieve and retain the LDL-cholesterol goal of less than 100 mg/dL, cholesterol-lowering medications may be required to augment lifestyle changes already adopted. These medicines may be even more important for patients with pre-existing heart disease and those who are deemed to be at high risk for developing heart disease.1
Most patients who have an LDL level of 130 mg/dL or greater will generally need to take a cholestero-lowering medication. If a patient’s level is 100 to 129 mg/dL, their physician will consider all the facts before deciding whether to prescribe medication. Even when medicines are prescribed, it is important to:1
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Follow a cholesterol-lowering diet |
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Be more physically active |
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Lose weight if overweight |
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Control other heart disease risk factors, including smoking, high blood pressure and diabetes |
Cholesterol-Lowering Agents include:
Statins
The major effect of statins is to lower LDL-cholesterol levels and they do this better than other types of drugs available. Statins inhibit an enzyme, HMG-CoA reductase, that controls the rate of cholesterol production in the body. They increase the liver’s ability to remove the LDL-cholesterol (total and LDL-cholesterol) already in the blood. Numerous studies have shown that reducing cholesterol has resulted in large reductions of heart attacks and heart disease deaths. Studies using statins have reported 20% to 60% lower LDL-cholesterol levels. These agents also reduce elevated triglyceride levels and produce a modest increase in HDL-cholesterol.2
Statins are usually given in a single dose in the evening because the body makes more cholesterol at night than during the day. Results of statin therapy are typically observed after several weeks, with a maximum effect at 4 to 6 weeks; therefore, monitoring of LDL levels usually starts at 6 to 8 weeks.2
Statins are well tolerated by most patients and serious side effects are rare. Some patients will experience an upset stomach, gas, constipation and abdominal pain or cramps. These symptoms are usually mild to moderate in severity and generally go away as the patients body adjusts to the statins. Rarely, a patient will develop muscle problems (soreness, pain, weakness) or abnormalities in liver function tests.2
Bile Acid Sequestrants
Bile Acid Sequestrants bind with cholesterol-containing bile acids in the intestines, which are then eliminated in the stool. Typically, these agents can lower LDL-cholesterol by 10% to 20%. Sometimes Bile Acid Sequestrants are prescribed with a statin for patients with heart disease to increase cholesterol reduction. When these two drugs are used together, their effect can decrease LDL levels by more than 40%.3
Bile Acid Sequestrants may produce a variety of symptoms such as constipation, bloating, nausea and gas. Therefore, these sequestrants are not prescribed as the sole medicine if the patient has a history of severe constipation or high triglyceride levels. Further, they may interfere with the absorption of other medicines if taken at the same time.3
Nicotinic Acid
Nicotinic acid or niacin, the water-soluble B vitamin, improves all lipoproteins when given in dose well above the vitamin requirement. Nicotinic acid can reduce LDL-cholesterol levels by 10% to 20%, reduce triglycerides by 20% to 50% and raise HDL-cholesterol by 15% to 35%.4
There are three types of nicotinic acid: immediate release, timed release, and extended release. Most experts recommend starting with the immediate release formulation, but this decision should be made by the patient’s physician.4
Nicotinic acid is inexpensive and widely available without a prescription, but must not be used for cholesterol lowering without the monitoring by a physician because of the potential and serious side effects. The side effects may include flushing or hot flashes and a variety of gastrointestinal symptoms such as nausea, gas, indigestion, vomiting, diarrhea and the activation of peptic ulcers. Other major adverse effects that increase with the dose of nicotinic acid are liver problems, gout and high blood sugar. The effect of high blood pressure medications may also be increased by nicotinic acid.4
Fibrates
Fibrates are primarily effective in lowering triglycerides by 20% to 50% and to a lesser extent, in increasing HDL-cholesterol levels from 10% to 15%. They are not very effective in lowering LDL-cholesterol.5
Fibrates are generally well tolerated by most patients. The most common side effect is gastrointestinal complaints. Fibrates may also increase the likelihood of developing cholesterol gallstones. Further, fibrates can increase the effect of medicines that thin the blood; therefore, this should be monitored closely.5
References
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