We will discuss in some detail the last category, the statins, because they have become widely recognized as the most effective drugs for the treatment of high cholesterol. But first, we will give a brief description of the other categories.
Bile Acid Resins – Because the liver takes cholesterol out of the blood to make bile, bile acid resins prevent the recycling of bile acids in the intestine. As a result, the liver is forced to remove more cholesterol from the blood in order to manufacture more bile. Bile acid resins are usually taken in powder form or in a chewable bar. Many patients, however, have gastrointestinal discomfort with these drugs.
Fibrates – Fibric acid reduces the production of triglycerides and increases the rate at which existing triglycerides are removed from the bloodstream. Fibrates can significantly lower triglyceride levels and modestly increase HDL (good) cholesterol levels in most patients, but they are less effective at reducing LDL (bad) cholesterol levels. They are most commonly used in patients who have elevated triglyceride levels; usually in conjunction with low HDLs (many diabetics have this type of lipid profile). Simultaneous use of fibrates and statins should be carefully monitored.
Nicotinic Acid (niacin) – a form of vitamin B3. In large doses, nicotinic acid is very effective in lowering triglyceride levels and raising levels of HDL cholesterol. Nicotinic acid can also lower levels of LDL cholesterol, but not as effectively as other cholesterol reducers. When taking nicotinic acid, patients are advised to slowly build up to the high doses needed to treat high cholesterol. Taking too much nicotinic acid too quickly can lead to intense side effects that include flushing, palpitations, nausea, and in extreme cases, liver toxicity (especially when taken in “rapid release” form). Even with proper build-up as many as 50% of patients find the side effects of this medication too difficult to tolerate. Nicotinic acid is available over the counter, but physicians prefer to prescribe it in time-released pills. Because of the potentially intense side effects, patients should never begin taking nicotinic acid without the supervision of a physician.
Ezetimibe – represents a new class of drug that directly blocks cholesterol absorption in the small intestine (in contrast to bile acid resins, which bind with bile acid in the intestine). Ezetimibe is most commonly used in addition to statins, with up to an additional 25% reduction in LDLs. One combination drug is Vytorin which helps block the absorption of cholesterol that comes from food, and reduces the cholesterol your body makes naturally. Ezetimibe can also be used as a single agent, but whether or not it will have the same protective effect as statins when used as a single agent remains inconclusive. Side effects have been similar to a placebo, and there is minimal
increase in liver enzymes when used with statins.
Statins – work by inhibiting a liver enzyme used to manufacture cholesterol. Statins are particularly effective for lowering LDL levels. They also reduce triglycerides. They raise HDL levels, but to a lesser extent than other types of cholesterol medications. Statins reduce the risk of first and second heart attacks in women, men, and older people with evidence of heart disease. In addition, they may reduce the risk of stroke.
Statins are strongly recommended as the first choice for almost all patients with high cholesterol levels, particularly:
• Patients with existing heart disease, diabetes, or both.
• Postmenopausal women with heart disease or risk factors for heart disease.
• Statins may be safe for children and adolescents with unhealthy cholesterol levels,
but long-term studies are needed to confirm their value and safety in all children.
The side effects of statins may include upset stomach, nausea, constipation, gas, headaches, skin rashes, muscle aches, insomnia, unusual dreams, daytime drowsiness, and dizziness. Less common side effects include sexual dysfunction, numbness or tingling in the hands and feet and depression.

Statins can affect the liver, so liver function should be assessed periodically though a blood test. They should never be taken by anyone with liver problems or by women who are pregnant or breastfeeding.
In very rare cases, drugs in this class may also lead to breakdown of muscle tissue, which can overwhelm the kidneys (called rhabdomyolysis) and lead to kidney failure. Muscle cramps are not in themselves a major concern. If muscle cramps, aches, or pains occur, your doctor will look for signs of muscle tissue breakdown through a
blood test that checks the level of an enzyme called creatine kinase (CK). The levels of CK would likely be much higher than normal (at least ten times), with elevated creatinine (usually causing brown urine) and muscle cramps, before rhabdomyolysis would be diagnosed.
Statins may have negative interactions with other drugs, including other cholesterol-lowering drugs. For example, when certain medications are taken with statins, the risk for muscle tissue breakdown increases. Some of the known medications are:
• Danazol – a prescription hormone used to treat endometriosis in women.
• Diltiazem – also known as Cardizem, used to treat high blood pressure.
• Fluvoxamine – brand name Luvox, used to treat obsessive-compulsive disorder.
• Protease inhibitors for HIV, such as indinivir, ritonavir, nelfinavir and
saquinavir.
• Some antibiotics such as erythromycin and clarithromycin.
• Cyclosporine which is a potent immunosuppression medication often used following an organ transplant, such as kidney and heart transplants.
• Drugs for fungal infections, i.e., diflucan, sporanox and monistat or micatin.
• Other cholesterol lowering drugs, including nicotinic acid and fibrates.
• Statins should not be used with red yeast rice, a popular supplement promoted for lowering cholesterol.
• They may also lower levels of certain antioxidants, including vitamin E, betacarotene, and coenzyme Q10.
• Grapefruit juice and Seville oranges (found in marmalades and other condiments, not in juice) may increase blood levels of statins and, therefore, increase the risk of side effects, including potential damage to the liver or muscle tissue.
Using statins together with bile acid resins may improve cholesterol-lowering effects, but the two types of medications should not be taken within 4 hours of one another.
There is definitely a benefit to taking cholesterol-lowering medications, especially statins; but you must be aware of the side effects and the interactions that they have with drugs, over the counter supplements and food. Most importantly, you should tell your doctor about any other medications and supplements you are taking so that they
can be informed before making any recommendations.
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References
The American Heart Association
Heart Center Online for Cardiologists and Their Patients, 2000-2005.
Envision Adam Careguides on Cholesterol, 2004.