Cholesterol Altering Drugs: Niacin and Niaspan

Statin type medications are known for their powerful effect on lowering LDL. Fibrates are specifically effective in lowering triglycerides. But neither have much an effect on the HDL. Raising HDL is of benefit in lowering the risk of heart disease. The cholesterol lowering effect of niacin, actually vitamin B-3, was first reported in 1955. As a general cholesterol drug, niacin has it all. In doses well above the vitamin requirement (about 50 mg per day), niacin can lower LDL and lower TG, but in particular it increases the HDL more than any other drug. Given in combination with a statin, niacin can lower the LDL more than any other drug combination.
Thus, you may prescribe niacin specifically to help increase HDL as well as lower the LDL (“up with the good and down with the bad”). The mechanism of action for niacin is not well understood but it may inhibit the release of free fatty acids from adipose tissue and thus increase the production of an enzyme called lipoprotein lipase; this in turn likely increases the rate of TG removal from the blood. Niacin has also been shown to reduce the synthesis of LDL in the liver. Indirectly, by increasing the amount of HDL, its action in what is called “reverse cholesterol transport” actually enhances the return of LDL to the liver and out of the circulation.
1. Common Names: there are a number of niacin preparation – so called “slo-niacin” has been questioned to be of any value in lowering cholesterols; however, the other preparations do have the desired therapeutic effect. There is immediate release niacin, extended release niacin, and (in prescription form only and the most effective) sustained release niacin (Niaspan).
2. Effect on Cholesterols: decrease LDL 5%-25%, raise HDL 15%-35%, decrease TG 20%-50% - the effect on TG is enhanced on a low carbohydrate type, weight loss diet; however, be aware that since niacin (except for Niaspan) is available from many sources including the internet and the health food store (actually a “nutraceutical” rather than a “pharmaceutical” and thus not strictly regulated) you may not always get what you pay for – so choose wisely; Niaspan, made by KOS Pharmaceutical on the other hand is strictly regulated as required by law.
3. Side Effects: the most common is flushing (potentially relieved by taking an aspirin 30 minutes before the dose) and gastrointestinal upset (can be reduced by taking dose with a low-fat snack such as yogurt); studies do indicate that niacin may increase blood sugar, but on the other hand it is a very useful medication in diabetics; niacin can increase the potential for gout and has a small risk of causing increases in liver enzymes, especially when combined with statins.
4. Usage: the frequency of dosing depends on the preparation – the immediate release and extended release niacin are taken generally twice per day; Niaspan is taken once per day.
5. Contraindications: an absolute contraindication is chronic liver disease; relative contraindications are gout, diabetes, and ulcer disease; liver blood tests should be monitored especially if also taking statin type medications.