Cholesterol Lowering Medications

Types and differences of cholesterol-reducing drugs

Different types of cholesterol reducers affect levels of fats (lipids) in different ways and generally fall into the following categories:

Examples of these medications* include the following:

Investigations continue with a new medication that influences HDL levels. Known as a CETP inhibitor, the drug is thought to block a particular protein responsible for lowering HDL. A recent study of torcetrapib, a CETP inhibitor, in combination with a statin unexpectedly showed an increase in deaths and cardiovascular events compared to a statin alone.

Potential side effects of cholesterol drugs

There are a number of side effects that could occur as a result of taking cholesterol reducers, but fortunately, side effect frequency is low. Muscle aches can occur with statin use and must be immediately reported to a physician. Certain cholesterol-lowering medications can also produce abnormal liver function in approximately 2 percent of the population, which can be diagnosed by periodic liver enzyme testing. In rare cases, this may lead to liver failure. Patients with moderate or severe liver disease should not take statins. For the most part, abnormal liver function is reversible when the statin is discontinued.

A rare, but potentially fatal side effect of some cholesterol-reducing drugs (statins and certain fibrates) is rhabdomyolysis, a severe muscle reaction in which muscle cells break down, releasing their contents into the bloodstream. Physicians can monitor patients for this complication by checking muscle enzyme levels (e.g., creatine phosphokinase [CPK]) in the blood. It most often affects the muscles in the back or lower calves. Some patients report no symptoms and in rare cases rhabdomyolysis can lead to kidney or other organ failure and death. Patients should report any of the following symptoms of rhabdomyolysis to their physicians immediately:

• Muscle cramps, pain, swelling, weakness, stiffness and/or tenderness
• Fever
• Dark urine
• Nausea and/or vomiting
• Malaise (a general feeling of illness or discomfort)

Risk of this severe complication appears to be higher in elderly patients, those taking high doses of statin and those taking statins in conjunction with a fibrate (e.g., fenofibrate, gemfibrozil). In 2001, one type of statin, called cerivastatin (brand name “Baycol”) was voluntarily withdrawn from the market by its manufacturer due to reports that fatal cases of rhabdomyolysis had been significantly more common with cerivastatin than with other approved statin drugs.

Statins carry a very low risk of side effects to the nervous system, including tingling, numbness and burning pain. These manifestations are known as peripheral neuropathy.

Patients on any cholesterol-lowering drugs should also notify their physician if they experience any side effects such as the following:

• Allergic reaction (new onset of wheezing, respiratory congestion, itching or skin rashes)
• Abdominal pain
• Headache
• Constipation
• Heartburn
• Dizziness or lightheadedness
• Flushing of the face or neck
• Bloating
• Blurred vision
• Drowsiness, weakness or fatigue
• Nausea or vomiting
• Hair loss
• Decreased sexual interest or ability

Drug or other interactions

Patients should consult their physician before taking any other medication (either prescription or over-the-counter) or nutritional supplements. Of particular concern to patients taking cholesterol reducers are other cholesterol reducers. Taking more than one cholesterol reducer at a time may worsen side effects, unless physicians have prescribed a specially dosed combination of medications.

It is also important to consider the effects of over-the-counter herbal remedies that claim to lower cholesterol. Because these preparations do not make explicit health claims, they do not undergo the same level of scrutiny by the U.S. Food and Drug Administration as do prescription drugs. For example, the herbal remedy “guggul,” derived from the mukul myrhh tree, has been advertised as a “cholesterol-fighter.” However, researchers found, however, that it actually increased levels of LDL (“bad”) cholesterol.

Other substances that may cause concern for some types of cholesterol-reducing drugs include:

• Inotropes (e.g., digoxin)
• Birth control pills
• Calcium channel blockers
• Protease inhibitors (for treatment of human immunodeficiency virus, HIV)
• Azole antifungals (systemic antifungals)
• Immunosuppressants (reduce the body's immune system)
• Some antibiotics
• Anticoagulants
• Antihypertensives (medications to treat high blood pressure)
• Diuretics (water pills)
• Certain NSAIDs (nonsteroidal anti–inflammatory drugs)
• Certain beta blockers
• Thyroid hormones

Patients taking cholesterol-reducing drugs may also be instructed to avoid grapefruit juice. Grapefruit juice interferes with the liver’s ability to rid the body of some substances. This could lead to a buildup of medications to toxic levels in the body. While the buildup is less likely if the juice is ingested four or more hours prior to the medicine, patients taking cholesterol reducers are usually advised to refrain from drinking grapefruit juice. Patients may also be instructed to avoid eating grapefruit.

Lifestyle considerations with Cholesterol Blocker

Some cholesterol reducers can cause liver inflammation, which tends to resolve on its own after patients stop taking the medication. To monitor this and other complications, patients will undergo regular blood tests and liver function tests.

Women taking cholesterol-reducing drugs should inform their physicians at once if they are or plan to become pregnant. Although it has been found that statins do not have a negative effect on female reproductive hormone levels, cholesterol is an important contributor to the development of the fetus. In addition, some cholesterol reducers are excreted in breastmilk. Nursing mothers, therefore, should consult with their physician before taking or discontinuing these drugs. Patients should not abruptly stop taking their medications without first consulting their physicians. It is also important that patients notify all physicians (including dentists) that they are taking statins before undergoing any surgical procedure. And all patients taking statins should inform their physician immediately of any side effects or concerns.

Most patients on medication to treat high cholesterol (hypercholesterolemia) will be taking it for the rest of their lives, provided no serious side effects occur. Patients should remember that medications may control high cholesterol, but they do not cure it. Even if all their symptoms are relieved, patients should continue to take their medication exactly as directed, eat a heart-healthy diet that is low in saturated fats and keep all scheduled follow-up appointments with their physician. Numerous studies have shown the dangers associated with noncompliance, or people not taking their cholesterol-lowering medications exactly as prescribed. Even if the medications do not appear to make you "feel better," there is a significantly higher risk of heart attack among people who simply stop taking their medications.