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CHAPTER 11

Controlling Cholesterol: Medications

PART 1

Cholesterol-Lowering Medications

Doctors generally recommend lifestyle changes as the first line of defense against atherosclerosis. In addition, one or more drugs may be prescribed.

Cholesterol medications help to lower your LDL-cholesterol levels and raise your HDL levels, which may help to slow or stop the buildup of plaque in your arteries. A number of different types are available:

  • Statins are the most commonly prescribed anticholesterol medications and are generally very effective. They work by blocking the production of cholesterol by the liver and by increasing the capacity of the liver to remove cholesterol from circulating blood. High doses of statins have been shown to actually reduce the volume of plaque in the arteries. However, statins can have serious side effects, including muscle pain and damage, liver damage, and cognitive impairment.

  • Fibric acid derivatives, or fibrates, are primarily effective in lowering triglycerides (types of fat that can lead to heart disease). They do this by reducing the liver’s production of VLDL, which transports triglycerides in the bloodstream. Fibrates also modestly increase HDL-cholesterol levels, but they don’t reduce LDL-cholesterol levels.

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  • Bile-acid sequestrants , also known as bile-acid resins, bind in the intestines with bile acids, which are produced by converting cholesterol. Bile acids are then eliminated in the stool, stimulating the liver to convert more cholesterol into bile acids, thereby lowering LDL-cholesterol levels. Bile-acid sequestrants are most effective when used in combination with niacin or a statin.

  • Niacin, or vitamin B3, raises HDL levels and decreases LDL and triglyceride levels by blocking the release of triglycerides from body fat and by inhibiting the liver from making more triglycerides from blood sugar. For this reason, it is sometimes prescribed along with other medications. Bear in mind, though, that niacin increases levels of homocysteine in the blood, which is associated with an increased risk of heart disease. You should not take high doses of niacin without talking to your doctor about it first.


Other drugs may be prescribed to prevent clotting and to treat high blood pressure.

  • Antiplatelet drugs block platelets from aggregating into clots. They include aspirin, ticlopidine, clopidogrel, tirofiban, and eptifibatide.

  • Anticoagulants, also known as blood-thinning drugs, help keep clots from forming. Heparin and warfarin are two commonly used anticoagulants.

  • Blood pressure medications, or antihypertensives, can help slow the progression of atherosclerosis. Thiazide diuretics, beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), and calcium channel blockers are among the most commonly prescribed types of antihypertensives.

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