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July 15, 1999

Niacin Therapy

By Chiayu Chen, M.D., F.A.C.C. and Jane Magro, F.N.P.,Riverside Cardiology Associates Medical Group

Niacin (nicotinic acid) has been used for many years to reduce elevated cholesterol and triglycerides. It is a B-vitamin (B-3), but when used in the doses necessary for blood cholesterol control, it is a drug and not a vitamin. It has side effects and should be treated with the same caution as other medications.

How Niacin Works

Niacin works by decreasing the liver's production of very low-density lipoprotein (VLDL), a relatively large particle comprised mainly of triglycerides and cholesterol. This leads to a decrease in the production of low density lipoprotein (LDL), which is the major carrier of cholesterol in your body. Another important and beneficial effect of Niacin is to raise the level of high-density lipoprotein (HDL) by decreasing the degradation rate of HDL. Finally, niacin also lowers triglycerides level.

Clinical Studies and Indications

Niacin is most helpful in persons with LDL-pattern B (small dense LDL), low HDL cholesterol, high triglycerides, elevated Lp(a), and elevation in LDL cholesterol. Niacin has been shown to decrease cardiovascular events and mortality. Some degree of angiographic regression has also being shown with niacin when used with other cholesterol medications.

Major Niacin Outcome Studies*:
Study Name Medication Regimen Summary of Outcome
Coronary Drug Project (CDP) Niacin alone Decreased second infarct over 6 yrs; decreased total mortality at 15 years
Stockholm Ischaemic Heart Disease (IHD) Secondary Prevention Study Niacin, clofibrate Decreased total and cardiac mortality over 5 yrs.
Cholesterol-Lowering Atherosclerosis Study (CLAS I and II) Niacin, colestipol Decreased progression of atherosclerosis; regression in 16% of patients
Familial Atherosclerosis Treatment Study (FATS) Niacin, colestipol Regression of coronary disease; reduction in cardiovascular events
University of California-San Francisco Specialized Center of Research (UCSF-SCOR) Niacin, colestipol, lovastatin Regression of coronary disease
Harvard Atherosclerosis Reversibility Project (HARP) Pravastatin, niacin, colestipol, gemfibrozil 33% reduction in cardiovascular events; however, not statistically significant
* Adapted from Guyton, JR. Effect of Niacin on Atheroscleotic Cardiovascular Disease. Am J Cardiol 1998;82:18U-23U.

How is Niacin Supplied?

Niacin is available in immediate-release and extended-release forms. Immediate-release niacin can be purchased in drug stores and health food stores without a prescription. It is available in 100 mg, 250 mg, 500 mg, and 1000 mg tablets. We do not recommend the "no-flush" niacin.

Sample brand of immediate-release niacin we recommend is:
Twinlab

Extended-release niacin we recommend is:
Niaspan® (KOS Pharmaceuticals, Inc.)- by prescription only

Side Effects

Remember that the use of niacin in high doses can cause serious side effects. Please only take niacin under the direct supervision of a physician. The most common side effect from niacin is flushing of the skin. This reaction is well documented and is mediated by a substance called prostaglandin.

Flushing of the skin is commonly described as a redness or itching and tingling sensations that typically occurs on the face, neck, chest, and back. The flushing sensation can be a nuisance, but there is no cause to worry. The flushing sensation is usually transient and will go away within 10 to 60 minutes. As your body adjust to the niacin, the flushing will become milder and eventually resolve.

The following are some guidelines and tips to minimize the flushing side effects:
  • Do not take niacin with hot beverage, alcohol, or spicy food.
  • Titrate up the dosage VERY SLOWLY, every 3 to 7 days.
  • Take the niacin with breakfast and dinner to avoid stomach upset and promote more even absorption.
  • Take half of a regular adult aspirin twenty minutes before each niacin dose. You may need to take the aspirin for three to four weeks, until your system adjusts.
Other important side effects:
  • Elevation in liver function test.
  • Elevation in uric acid.
  • Possible exacerbation of atrial arrhythmias.
  • Rare occurrence of retinopathy.
  • May exacerbate diabetes.

Sample dosing schedule for immediate-release niacin:
Day # Breakfast
100mg
Dinner
100mg
Total Dose per Day
1 - 3 0 1 100 mg
4 - 6 1 1 200 mg
7 - 9 1 2 300 mg
10 -12 2 2 400 mg
13 - 15 2 3 500 mg
16 - 18 3 3 600 mg
19 - 21 3 4 700 mg
22 - 24 4 4 800 mg **
** Continue the same dose titration gradually until taking 1000 mg to 1500 mg a day total. A repeat blood test should be done at that time.

The extended-release niacin we recommend is Niaspan®. Niaspan® was developed by Kos Pharmaceuticals, Inc., for a Once-a-Night ™ dosing. Niaspan® is available by prescription only up to 2000 mg a day. Niaspan® is much better tolerated as compared to the immediate-release niacin.

Warning

Do not switch between immediate-release niacin and the extended-release Niaspan® without notifying your physician. Serious side effects can result. Dosages of immediate-release and extended-release niacin are not interchangeable.

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