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November 22, 2009
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Your Cholesterol Profile - In Depth (cont.)

What is nicotinic acid (niacin)?

Nicotinic acid (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 that include immediate release niacin, sustained release prescription brand Niaspan, and over- the- counter (OTC) sustained release niacin. OTC preparations are not federally regulated, and some OTC preparations may have no active ingredient. Thus, they would be ineffective in either lowering LDL or raising HDL cholesterol. Some formulations of OTC sustained release niacin have been associated with liver toxicity and rare cases of fulminant (usually fatal without liver transplantation) hepatitis have been reported. The prescription brand sustained release Niaspan has been found in clinical trials to cause only minor elevations in blood liver enzymes without causing significant liver disease.

Nicotinic acid is most effective in increasing HDL cholesterol and it is also modestly effective in lowering LDL cholesterol, Lp(a) cholesterol, and triglyceride levels (see below). Nicotinic acid is most suited for individuals whose only problem is low HDL cholesterol. Nicotinic acid used alone can raise HDL cholesterol levels by 30% or more. Nicotinic acid is not as effective as a statin in lowering LDL cholesterol levels. Therefore, when low HDL cholesterol is accompanied by high LDL cholesterol, most doctors use a statin to decrease the LDL cholesterol first. If necessary, nicotinic acid can be added to a statin to further raise HDL cholesterol levels.

Advicor is a combination product approved for use in the United States. It is a combination of sustained release niacin with lovastatin. Advicor is useful in patients who need to both significantly lower their LDL cholesterol and increase HDL cholesterol.

What are the side effects of niacin?

The most common side effect of nicotinic acid is a flushing (which can occur in 80% of patients taking the immediate release crystalline preparations), itching, and upset stomach. Other side effects include liver toxicity, aggravating blood sugar levels in patients with diabetes mellitus, and precipitating painful arthritis attacks in patients with gout.

The itching, flushing, and stomach upset can be partially alleviated by the following measures:

  • Taking nicotinic acid with meals.
  • The sustained release Niaspan capsules release nicotinic acid from the stomach into the blood circulation more gradually than the immediate release preparations. Therefore, Niaspan produces a lower incidence of upset stomach and skin flushing than the niacin immediate release tablets.
  • Pretreatment with aspirin 30 minutes prior to nicotinic acid can reduce flushing.
  • Initiating nicotinic acid treatment at low doses and gradually increasing to the targeted dosage.

Liver toxicity with the immediate release nicotinic acid is usually mild and in the form of abnormal elevation of liver enzymes in the blood, which normalizes when nicotinic acid is stopped. Severe liver diseases, including fulminant hepatitis (see above), have been reported, especially with the use of over-the-counter sustained release formulations. The onset of liver damage with nicotinic acid is unpredictable. Therefore, patients taking any nicotinic acid preparations should have regular liver enzyme blood tests.



Next: What are fibric acid derivatives (fibrates)? »

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