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High Cholesterol (cont.)

Medical Treatment: Other Medications

Bile acid sequestrants: These drugs bind with cholesterol-containing bile acids in the intestines and allow them to be eliminated in the stool. Bile acid sequestrants may lower LDL cholesterol by about 10%-20%. Bile acid sequestrants are sometimes prescribed with a statin to enhance cholesterol reduction.

  • Cholestyramine (Questran, Questran Light), colestipol (Colestid), and colesevelam (WelChol) are the three bile acid sequestrants currently available. These three drugs are available as powders or tablets and are are not absorbed from the gastrointestinal tract.
  • Bile acid sequestrant powders must be mixed with water or fruit juice and are taken once or twice daily with meals. Tablets must be taken with large amounts of fluids to avoid stomach and intestinal complaints including constipation, bloating, nausea, and gas.

Cholesterol absorption inhibitors: These drugs inhibit cholesterol absorption in the gut and has few, if any, side effects. Cholesterol absorption inhibitors may be rarely associated with tongue swelling (angioedema). Ezetimibe (Zetia) reduces LDL cholesterol by 18%-20%. It is probably most useful in people who cannot tolerate taking statins. When used in addition to a statin, ezetimibe is equivalent to doubling or tripling the statin dose.

Nicotinic acid or niacin: Nicotinic acid lowers total cholesterol, LDL cholesterol, and triglyceride levels, while raising HDL cholesterol levels.

  • There are two types of nicotinic acid: immediate release and extended release.
  • The immediate-release form of crystalline niacin is inexpensive and widely accessible without a prescription, but, because of potential side effects, it should not be used for cholesterol lowering without monitoring by a health care practitioner. (Nicotinamide, another form of niacin, does not lower cholesterol levels and should not be used in place of nicotinic acid.)
  • Nicotinic acid reduces LDL cholesterol levels by 10%-20%, reduces triglycerides by 20%-50%, and raises HDL cholesterol by 15%-35%.
  • A common and troublesome side effect of nicotinic acid is flushing or hot flashes, which are the result of blood vessels dilating. Most people develop a tolerance to flushing, which can sometimes be decreased by taking the drug during or after meals or by the use of aspirin or other similar medications prescribed by your doctor 30 minutes prior to taking niacin. The extended-release form may cause less flushing than the other forms.
  • The effect of high blood pressure medicines may also be increased while taking niacin causing blood pressure to potentially drop. A variety of gastrointestinal symptoms, including nausea, indigestion, gas, vomiting, diarrhea, and peptic ulcers, have been experienced with the use of nicotinic acid. Other major side effects include liver problems, gout, and high blood sugar.
  • Extended-release niacin is often better tolerated than crystalline niacin. However, its liver toxicity (liver damage) is probably greater. The dose of extended-release niacin is usually limited to 2 grams per day.

Fibrates: These cholesterol-lowering drugs are effective in lowering triglycerides.

  • gemfibrozil (Lopid),
  • fenofibrate (Tricor), which is more effective at lowering triglycerides and LDL cholesterol.

Side effects of fibrates may include stomach or intestinal discomfort, gallstones, and may affect anticoagulation medication effects in thinning blood.

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