Cardiovascular Institute and Center for Cardiovascular Health

Cholesterol (Lipid) Lowering Drugs

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e acquire cholesterol through some of the foods we eat, but the body also produces this important molecule to use in the synthesis (fabrication) of certain hormones and digestive substances called, "bile acids." Cholesterol is transported through your body via the circulation system in carriers called, " lipoproteins".

If you have elevated levels of low-density lipoprotein cholesterol (LDL), the so-called, "bad cholesterol", this increases the risk for coronary artery and other vascular disease like stroke. Sometimes fat, LDL cholesterol, and other substances combine to form a hard substance known as, "plaque". Plaque may be deposited on the inner lining of your arteries. The build up of plaque may clog the arteries and restrict blood flow. Treatment with cholesterol lowering (lipid lowering) medications can reduce your LDL cholesterol and diminish your risk. If you already have elevated cholesterol, these medications can decrease your chances of having a heart attack or stroke or of dying from one.

Usually, lipid lowering medications can significantly reduce LDL cholesterol without lowering HDL cholesterol (the "good cholesterol").

How do these medications work?
There are various types of lipid-lowering drugs. The main ones are (1) the "statins", (2) the sequestrants or resins, (3) the nicotinic acids or niacins, and (4) the fibrates. They each work somewhat differently.

The Statins (Lovastatin, Pravastatin, Simvastatin, etc.)
Statins are the most widely prescribed lipid lowering medications. A natural enzyme called, "HMG-CoA Reductase" contributes to the synthesis of some of the cholesterol in your body. The statins inhibit the action of the HMG-CoA Reductase enzyme, thereby reducing the production of cholesterol. Statins sometimes raise the level of good cholesterol.

The Sequestrants or Resins
Bile acids are produced by your liver to be used in the digestion process. Your liver uses cholesterol to produce the bile acids. Sequestrants bind with the bile acids in your intestinal tract, thus rendering them unavailable for digestion. The liver responds by making more bile acids. In doing so, it uses up additional cholesterol, thereby leaving less cholesterol to circulate and get deposited in your coronary arteries.

Nicotinic Acid (Niacin)
Nicotinic acid or niacin, is a form of vitamin B which is found in food. You can also obtain it in low doses over-the-counter. In high, prescription doses it lowers LDL cholesterol and raises HDL cholesterol. It has the added benefit of also lowering triglycerides which are combinations of glycerol and fatty acids.

The precise manner in which niacin lowers cholesterol is unknown.

Fibrates
Although fibrates are limited in their efficacy for lowering LDL- cholesterol levels, they are very effective in lowering triglyceride levels and removing them from circulating in the bloodstream.. The may also increase HDL-cholesterol levels.

What are t he potential side effects of these medications?
Statins on rare occasions produce muscle pain, but do not cause muscle weakness. It is rare for the pain to reach a dangerous or life threatening state. The risk of severe muscle problems may increase if you are taking other drugs such as such as erythromycin, antifungal agents, gemfibrozil, or niacin.

Other potential side effects of the statins include: headaches, shortened sleep, gastrointestinal problems, fatigue and joint pains.

Most people tolerate statins very well with no side effects.

The side effects of the sequestrants/resins are bloating and constipation.

The major side effect of niacin is flushing of the skin. You may experience a feeling of warmth on your face, forearms and the backs of your hands. These areas may become red. Usually, the flushing subsides with continued use of the medication. If you take niacin at the end of a meal, the food will delay the absorption. This leads to greater tolerance and less flushing. You also may benefit from taking an aspirin 30 minutes before the niacin.

Niacin may also cause a dark skin discoloration on the back of your neck or groin.

Although this is not a dangerous condition, it does annoy some people.

The side effects associated with the fibrates, include: gastrointestinal problems and muscle pain.

Are there any dangers or risks associated with lipid-lowering drugs?
These medications can cause liver abnormalities. To avoid such problems, have your physician should monitor your response to the medication and change your dose accordingly.

Fibrates increase your risk of having gallstones.

Is there anyone who should not take these medications?
You should not take lipid lowering medications if you have a history of liver abnormalities. If you have diabetes mellitus, you should refrain from taking niacin, as it may exacerbate your condition. Similarly, if you have a history of gout, you should not take niacin because it may precipitate a flare-up. Niacin has also been associated with exacerbation of peptic ulcer disease.

You should refrain from taking Gemfibrozil if you have a history of kidney disease. If you are pregnant or obese, you should take this medication with caution.

Are there other medications which prohibit me from taking lipid-lowering drugs?
If you are taking Warfarin, as well as lipid-lowering medication, the dose of the anti-coagulant may have to be adjusted.

Are there any other medications which can be taken instead of this one which has the same or similar effect as this medication?
No.

Are there any natural remedies which have the same or similar effect as this medication?
Exercise and prudent dietary changes may help. If you increase your intake of dietary fiber (e.g. by eating oat bran), you may lower your cholesterol level. Consult with your physician to determine whether lifestyle changes are sufficient in your situation.

Can I take a generic version of this medication?
No.

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