Lowering Cholesterol When Diet and Exercise Aren’t Enough

March 16, 2011 No Comments by Scott Isaacs MD

What do you do when diet and exercise aren’t enough to lower your cholesterol?

Statin Medications

Statin medications (Atorvastatin-Lipitor, Pravastatin-Pravachol, Simvistatin-Zocor, Fluvastatin- Lescol XL, Lovastatin-Mevacor and Rosuvastatin-Crestor) are considered the best first choice for lowering cholesterol.  That’s because they have a proven track record of decreasing heart attacks and strokes as well as prolonging life.  You can’t watch the evening news anymore without seeing a commercial this class of drugs. Statins work by inhibiting the enzyme HMG CoA reductase which is needed to produce bad cholesterol.

These blockbuster drugs are the most commonly used medications to treat high LDL (bad) cholesterol.  But, the amount of LDL cholesterol is not always the problem in insulin resistance.  Insulin resistance causes the quality of LDL to shift to the dangerous small dense type.  Statins have a small effect in lowering triglycerides and raising HDL (good) cholesterol levels.  Statins help improve the quality of LDL from the dangerous, small dense type to the less dangerous, large fluffy type. Statins have “antioxidant” properties which decrease inflammation and blood clotting.  Statins dramatically reduce the risk of cardiovascular disease and can even reverse it.  This is why statins are being prescribed more and more commonly and in higher doses than ever before.

The most common side effect is muscle problems that can range from mild aches and pains to severe muscle damage can also occur.  Any muscle pain or weakness should be reported to your physician.  A test called CPK or CK can be done to determine if the drug is causing muscle damage. Because statins have such tremendous health benefits, most physicians now recommend that you continue taking it if it is causing only mild muscle pain.   Inflammation of the liver is an infrequent side effect.  Your doctor will need to monitor liver tests periodically.

Other Solutions?

Also known as “fibric acid derivatives” or “fibrates,” are an effective method for lowering cholesterol.  Fibrates are a perfect choice for people who are overweight because they lower triglycerides and LDL cholesterol while raising HDL cholesterol. Side effects are uncommon, but muscle problems or liver problems can occur.

Niacin (also known as nicotinic acid or vitamin B3) in high doses simultaneously treats multiple lipid abnormalities by lowering triglycerides and LDL cholesterol while raising HDL cholesterol.   Regular niacin is available as an over-the-counter supplement, but is very hard to take because the doses needed (usually 1000-2000 mg per day) almost always cause side effects of flushing or tingling or redness of the skin.  To reduce side effects start with a low dose and gradually increasing the dose over several months. The flushing can also be reduced by taking an aspirin and drinking a full glass of water one hour before taking niacin.  The slow release prescription formulation of niacin known as Niaspan is easier to take because there are fewer side effects, but there can still be significant flushing with this product.

A concern with niacin is that it can worsen insulin resistance and can raise blood sugar levels.  For many people, the benefits can outweigh the risks and niacin can be beneficial for an overall plan of health and wellness.  Even though niacin is available without a prescription, it should only be taken under medical supervision.

Lovaza is a prescription formulation of the omega 3 fatty acids approved for the treatment of high triglyceride levels.  This substance, found naturally in cold water fish, also improves insulin resistance.  The prescription formulation is better than over the counter preparations because it is more potent and more pure.

Bile acid sequestrants or “bile acid resins,” lower LDL cholesterol by pulling it out of digestive juices, allowing it to pass in the stool.  Bile acid resins can raise triglyceride levels.   The most common side effect is constipation.  Fiber supplementation and proper hydration helps.

Is Ezetimibe the Answer?

Ezetimibe lowers LDL cholesterol by blocking absorption of cholesterol from the intestines. Ezetimibe doesn’t do much for triglycerides or HDL cholesterol.  Side effects are rare but there can be abdominal pain or diarrhea. Do you remember those Vytorin ads, touting the benefits combining medications to treat high cholesterol?  The commercials displayed an interesting character matched up with plate of food in the same colors and design as the actor’s ensemble.  The benefit, the ad explained, is to treat cholesterol by treating the genetics as well as the food.  The drug’s makers claimed that two drugs were better than one.   Here’s another commercial:


An important study called ENHANCE, which questions the benefits of ezetimibe, one of the components of Vytorin, was a big shock to physicians and patients. In this study, the combination of ezetimibe and simvastatin (sold as Vytorin) was compared to simvastatin alone.  It turned out that cholesterol buildup in the arteries was no different between the two treatments, even though the combination drug was more potent at lowering cholesterol. Researchers are working to understand these results and what they really mean. We don’t really know if ezetimibe actually reduces heart attacks or saves lives.  On the other hand, simvastatin and other statin drugs are well proven to do just this.

A 2008 ezetimibe study published in the New England Journal of Medicine suggested that it may increase the risk for a variety of cancers including prostate, colon, and skin cancers. Death from cancer was more common in patients who took ezetimibe.  We don’t know if the increased cancer is truly an effect of ezetemibe or something else.  One theory is that ezetemibe increases risk because it not only blocks the absorption of cholesterol but it also blocks the absorption of other cancer-fighting substances.

The bottom line?

Most experts including the American College of Cardiology recommend that statin drugs are the best first approach for fighting cholesterol and to use other medications like niacin, fibrates, colesevelam, cholestyramine and omega-3 fatty acids as the next line of defense.  Ezetimibe should be reserved as a last resort.

The bottom line is that most experts recommend using tried and true medications to lower cholesterol.  Unproven medications are just that…unproven.



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