When a patient without heart disease is first diagnosed with elevated blood cholesterol, doctors often prescribe a program of diet, exercise, and weight loss to bring levels down. National Cholesterol Education Program guidelines suggest at least a six-month program of reduced dietary saturated fat and cholesterol, together with physical activity and weight control, as the primary treatment before resorting to drug therapy. Typically, doctors prescribe the Step I/Step II diet (see “Food for Thought”) to lower dietary fat, especially saturated fat. Many patients respond well to this diet and end up sufficiently reducing blood cholesterol levels. Study data reinforce these benefits. For example, a 1998 Columbia University study examined 103 male and female patients of diverse ages and ethnic backgrounds and found that reducing dietary saturated fat directly affected blood cholesterol. For every 1 percent drop in saturated fat, the study showed a 1 percent lowering of LDL in patients.
But sometimes diet and exercise alone are not enough to reduce cholesterol to goal levels. Perhaps a patient is genetically predisposed to high blood cholesterol. In these cases, doctors often prescribe drugs. The National Cholesterol Education Program estimates that as many as 9 million Americans take some form of cholesterol-lowering drug therapy. The most prominent cholesterol drugs are in the statin family, an array of powerful treatments that includes Mevacor (lovastatin), Lescol (fluvastatin), Pravachol (pravastatin), Zocor (simvastatin), Baycol (cervastatin), and Lipitor (atorvastatin). Many doctors say statin drugs have revolutionized patient care.

Description of Cholesterol Reducing Drugs

Cholesterol-reducing drugs are medications that lower the levels of fats (lipids) in the blood, including cholesterol and triglycerides. Besides lowering total cholesterol and LDL (“bad”) cholesterol levels, some cholesterol-lowering medications may also modestly increase levels of HDL (“good”) cholesterol. High LDL cholesterol levels and low HDL cholesterol levels are associated with heart attack, stroke and coronary artery disease.
Cholesterol-reducing drugs work on lipids in the bloodstream. Some work by reducing the amount of cholesterol or triglycerides produced or absorbed in the body. Others remove cholesterol that has built up in the arteries. The mechanisms and strengths of each type of cholesterol-reducing drug varies.

Types of Cholesterol Reducing Drugs

There are several types of drugs that can help reduce blood cholesterol levels, including:

Staitins

Statins lower low-density lipoprotein cholesterol levels more than other types of drugs. Statins inhibit an enzyme, HMG-CoA reductase, that controls the rate of cholesterol production in the body. These drugs lower cholesterol by slowing down the production of cholesterol and by increasing the liver’s ability to remove the low-density lipoprotein cholesterol already in the blood.
Statins were used to lower cholesterol levels in many of the clinical trials discussed previously. The large reductions in total and LDL cholesterol produced by these drugs resulted in significant reductions in heart attacks and coronary heart disease deaths. Thanks to their safety and to their ability to lower low-density lipoprotein cholesterol the number of coronary heart attacks and heart disease deaths, statins have become the drugs most often prescribed for lowering cholesterol.
Studies using statins have reported 20-60% lower LDL cholesterol levels in people taking them. Statins also reduce high triglyceride levels modestly and produce a mild increase in HDL cholesterol. The statins are most often given in a single dose at the evening meal or at bedtime. It is important that these medications be given in the evening to take advantage of the fact that the body makes more cholesterol at night than during the day. Newer, long-acting statins, such as atorvastatin (Lipitor), may be administered in the morning.
You should begin to see results from the statins after several weeks, with a maximum effect in 4-6 weeks. After about 6-8 weeks, your doctor can do the first check of your LDL cholesterol while you are on the medication. A second measurement of your low-density lipoprotein cholesterol level must be averaged with the first for your doctor to decide whether your dose of medicine should be changed to help you meet your goal.
The statins are well tolerated, and serious side effects are rare (liver problems, muscle soreness, pain, weakness). If this happens, or if you have brown urine, contact your doctor right away to get blood tests for possible muscle problems. Rarely, widespread muscle breakdown, known as rhabdomyolysis, can occur, usually in people who are taking other drugs that interfere with the breakdown of the statin and in people with advanced kidney problems. This is a medical emergency. So, if you have diffuse muscle pain and weakness, or brown urine (a possible sign of muscle breakdown), contact your doctor immediately and stop taking the statin medication. Some people experience an upset stomach, gas, constipation, and abdominal pain or cramps. These symptoms are usually mild to moderate and generally go away as your body adjusts. Monitoring of liver function tests is usually done in patients taking statins.

Niacin

The B vitamin Niacin, in high doses, can lower triglycerides and low-density lipoprotein levels and increase HDL levels. Niacin has been proven to reduce a person’s risk of having a second heart attack.
Nicotinic acid or niacin: This water-soluble B vitamin improves all lipoproteins when given in doses well above the vitamin requirement. Nicotinic acid lowers total cholesterol, low-density lipoprotein cholesterol, and triglyceride levels, while raising HDL cholesterol levels.
There are 2 types of nicotinic acid: immediate release and extended release. The immediate-release form of crystalline niacin is inexpensive and widely accessible without a prescription, but, because of potential side effects, it must not be used for cholesterol lowering without the monitoring of a doctor. (Nicotinamide, another form of niacin, does not lower cholesterol levels and should not be used in place of nicotinic acid.) If you take nicotinic acid to lower cholesterol, your doctor will closely monitor you to avoid complications from this medication. You should not take this medication on your own. You may miss important side effects. Nicotinic acid reduces LDL cholesterol levels by 10-20%, reduces triglycerides by 20-50%, and raises HDL cholesterol by 15-35%.
A common and troublesome side effect of nicotinic acid is flushing or hot flashes, which are the result of blood vessels opening wide. Most people develop a tolerance to flushing, which can sometimes be decreased by taking the drug during or after meals or by the use of aspirin or other similar medications prescribed by your doctor 30 minutes prior to taking niacin. The extended-release form may cause less flushing than the other forms.
The effect of high blood pressure medicines may also be increased while you are on niacin. If you are taking high blood pressure medication, it is important to set up a blood pressure monitoring system while you are getting used to your new niacin regimen. A variety of gastrointestinal symptoms, including nausea, indigestion, gas, vomiting, diarrhea, and the activation of peptic ulcers, has been seen with the use of nicotinic acid. Three other major adverse effects include liver problems, gout, and high blood sugar. Risk of the latter 3 complications increases as the dose of nicotinic acid is increased. Your doctor may not prescribe this medicine for you if you have diabetes because of the effect on your blood sugar.
Extended-release niacin is often better tolerated than crystalline niacin. However, its liver toxicity (liver damage) is probably greater. Therefore, the dose of extended-release niacin is usually limited to 2 grams per day.

Bile acid sequestrants

These drugs bind with cholesterol-containing bile acids in the intestines and are then eliminated in the stool. The usual effect of bile acid sequestrants is to lower low-density lipoprotein cholesterol by about 10-20%. Small doses of sequestrants can produce useful reductions in low-density lipoprotein cholesterol.
Bile acid sequestrants are sometimes prescribed with a statin to enhance cholesterol reduction. When these drugs are combined, their effects are added together to lower low-density lipoprotein cholesterol by more than 40%.
Cholestyramine (Questran, Questran Light), colestipol (Colestid), and colesevelam (Welchol) are the 3 main bile acid sequestrants currently available. These 3 drugs are available as powders or tablets. They are not absorbed from the gastrointestinal tract, and 30 years of experience with these drugs indicates that long-term use is safe.
Bile acid sequestrant powders must be mixed with water or fruit juice and must be taken once or twice (rarely, 3 times) daily with meals. Tablets must be taken with large amounts of fluids to avoid stomach and intestinal problems. Sequestrant therapy may produce a variety of symptoms, including constipation, bloating, nausea, and gas. The bile acid sequestrants are not prescribed as the sole medicine to lower your cholesterol if you have high triglycerides or a history of severe constipation. Although sequestrants are not absorbed, they may interfere with the absorption of other medicines if taken at the same time. You must take other medications at least 1 hour before or 4-6 hours after the sequestrant. You should talk to your doctor about the best time to take this medicine, especially if you take other medications.

Cholesterol absorption inhibitors

This new class of drugs was approved in late 2002. The drug inhibits cholesterol absorption in the gut and has few, if any, side effects. Cholesterol absorption inhibitors may rarely be associated with tongue swelling (angioedema). Ezetimibe (Zetia) is the first drug in this class. Ezetimibe reduces LDL cholesterol by 18-20%. It is probably most useful in people who cannot take statins or as an additional drug for people who take statins but who notice side effects when the statin dose is increased. Adding ezetimibe to a statin is equivalent to doubling or tripling the statin dose.

Fibrates

These cholesterol-lowering drugs are primarily effective in lowering triglycerides and, to a lesser extent, increasing HDL cholesterol levels. Gemfibrozil (Lopid), the fibrate most widely used in the United States, can be effective for people with high triglyceride levels. However, gemfibrozil is not very effective for lowering LDL cholesterol. It is used in some people with heart disease for whom a goal of treatment is lowering triglycerides or raising HDL. Another fibrate is fenofibrate (Tricor), which is more effective at lowering triglycerides and low-density lipoprotein cholesterol. Some people taking fibrates may have side effects such as stomach or intestinal discomfort. Fibrates may increase the likelihood of your developing gallstones and can increase the effect of medications that thin the blood. Your doctor will monitor you. The dose of fibrates should be reduced if your kidney function declines.

Hormone replacement therapy

The risk of heart disease is increased in women after menopause. The increasing risk may be related to loss of estrogen that comes with menopause. Previously, women might have been treated with hormone replacement therapy (replacing the estrogen and perhaps progestin). Recent studies have found that women on hormone replacement therapy did not benefit by having a lower rate of heart-related events compared with women treated with placebo.
Therefore, postmenopausal women who are judged by their doctor to need drug treatment to reduce their risk for heart disease should consider cholesterol-lowering drugs instead of hormones because cholesterol-lowering drugs have been shown to be safe and effective in lowering cholesterol and reducing coronary heart disease risk.

Examples of these medications* include the following:

Statins

Bile acid resins

Nicotinic acid

Fibrates
  • Atorvastatin
  • Fluvastatin
  • Rovastatin
  • Pravastatin
  • Rosuvastatin
  • Simvastatin
  • Cholestyramine
  • Colestipol
  • Colesevelam
  • Niacin (vitamin B3)
  • Clofibrate
  • Fenofibrate
  • Gemfibrozil

*Note: Ezetimibe (not listed above) is the first of a new class of cholesterol reducing drugs that directly blocks cholesterol absorption.

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.

Recommended dosage

The recommended dosage depends on the type of cholesterol-reducing drug used. The prescribing physician or the pharmacist who filled the prescription can advise about the correct dosage.
Cholesterol-reducing drugs should be taken exactly as directed and doses should not be missed. Double doses should not be taken to make up for a missed dose.
Physicians may prescribe a combination of cholesterol-reducing drugs, such as pravastatin and colestipol. Following the directions for how and when to take the drugs is very important. The medicine may not work properly if both drugs are taken at the same time of day.
Niacin should not be taken at the same time as an HMG-CoA inhibitor, as this combination may cause severe muscle problems. If niacin is taken in an over-the-counter form, both the prescribing physician and pharmacist should be informed. There are no problems when the niacin is taken in normal doses as a vitamin.
The prescription should not be stopped without first checking with the physician who prescribed it. Cholesterol levels may increase when the medicine is stopped, and the physician may prescribe a special diet to make this less likely.

Precautions

Seeing a physician regularly while taking cholesterol-reducing drugs is important. The physician will check to make sure the medicine is working as it should and will decide whether it is still needed. Blood tests and other medical tests may be ordered to help the physician monitor the drug’s effectiveness and check for side effects.
For most people, cholesterol-reducing drugs are just one part of a whole program for lowering cholesterol levels. Other important elements of the program may include weight loss, exercise, special diets, and changes in other habits. The medication should never be viewed as a substitute for other measures ordered by the physician. Cholesterol-reducing drugs will not cure problems that cause high cholesterol; they will only help control cholesterol levels.
People over 60 years of age may be unusually sensitive to the effects of some cholesterol-reducing drugs. This may increase the chance of side effects.
Anyone who is taking an HMG-CoA reductase inhibitor should notify the health care professional in charge before having any surgical or dental procedures or receiving emergency treatment.

Special conditions

People who have certain medical conditions or who are taking certain other medications may have problems if they take cholesterol-reducing drugs. Before taking these drugs, the prescribing physician should be informed of any of the following conditions:

ALLERGIES
Anyone who has had unusual reactions to cholesterol-reducing drugs in the past should inform the prescribing physician before taking the drugs again. The physician also should be told about any allergies to foods, dyes, preservatives, or other substances.

PREGNANCY
Studies of laboratory animals have shown that giving high doses of gemfibrozil during pregnancy increases the risk of birth defects and other problems, including death of the unborn baby. The effects of this drug have not been studied in pregnant women. Women who are pregnant or who may become pregnant should check with their physicians before using gemfibrozil.
Cholesterol-reducing drugs in the group known as HMG-CoA reductase inhibitors (such as lovastatin, fluvastatin, pravastatin and simvastatin) should not be taken by women who are pregnant or who plan to become pregnant soon. By blocking the production of cholesterol, these drugs prevent a fetus from developing properly. Women who are able to bear children should use an effective birth control method while taking these drugs. Any woman who becomes pregnant while taking these drugs should check with her physician immediately.
Cholestyramine and colestipol will not directly harm an unborn baby, because these drugs are not taken into the body. However, the drugs may keep the mother’s body from absorbing vitamins that she and the baby need. Pregnant women who take these drugs should ask their physicians whether they need to take extra vitamins.

BREASTFEEDING
Because cholestyramine and colestipol interfere with the absorption of vitamins, women who use these drugs while breastfeeding should ask their physicians if they need to take extra vitamins.
Women who are breastfeeding should talk to their physicians before using gemfibrozil. Whether this drug passes into breast milk is not known. But because animal studies suggest that it may increase the risk of some types of cancer, women should carefully consider the safety of using it while breastfeeding.
HMG-CoA reductase inhibitors (such as lovastatin, pravastatin, fluvastatin and simvastatin) should not be used by women who are breastfeeding their babies.

OTHER MEDICAL CONDITIONS
Cholesterol-reducing drugs may make some medical problems worse. Before using these drugs, people with any of these medical conditions should make sure their physicians are aware of their conditions:

  • stomach problems, including stomach ulcer
  • constipation
  • hemorrhoids
  • gallstones or gallbladder disease
  • bleeding problems
  • underactive thyroid
  • heart or blood vessel disease

In addition, people with kidney or liver disease may be more likely to have blood problems or other side effects when they take certain cholesterol-reducing drugs. And some drugs of this type may actually raise cholesterol levels in people with liver disease.
Patients with any of the following medical conditions may develop problems that could lead to kidney failure if they take HMG-CoA reductase inhibitors:

  • treatments to prevent rejection after an organ transplant
  • recent major surgery
  • seizures (convulsions) that are not well controlled

People with phenylketonuria (PKU) should be aware that sugar-free formulations of some cholesterol-reducing drugs contain phenylalanine in aspartame. This ingredient can cause problems in people who have phenylketonuria.

Use of certain medicines

Cholesterol-reducing drugs may change the effects of other medicines. Patients should not take any other medicine that has not been prescribed or approved by a physician who knows they are taking cholesterol-reducing drugs.

Side effects

Gemfibrozil

Studies in animals and humans suggest that gemfibrozil increases the risk of some types of cancer. The drug may also cause gallstones or muscle problems. Patients who need to take this medicine should ask their physicians for the latest information on its benefits and risks.
Patients taking gemfibrozil should check with a physician immediately if any of these side effects occur:

  • fever or chills
  • severe stomach pain with nausea and vomiting
  • pain in the lower back or side
  • pain or difficulty when urinating
  • cough or hoarseness

HMG-CoA reductase inhibitors

These drugs may damage the liver or muscles. Patients who take the drugs should have blood tests to check for liver damage as often as their physician recommends. Any unexplained pain, tenderness or weakness in the muscles should be reported to the physician at once.

All cholesterol-reducing drugs

Minor side effects such as heartburn, indigestion, belching, bloating, gas, nausea or vomiting, stomach pain, dizziness and headache usually go away as the body adjusts to the drug and do not require medical treatment unless they continue or they interfere with normal activities.
Patients who have constipation while taking cholesterol-reducing drugs should bring the problem to a physician’s attention as soon as possible.
Additional side effects are possible. Anyone who has unusual symptoms while taking cholesterol-reducing drugs should get in touch with his or her physician.

Interactions

Cholesterol-reducing drugs may interact with other medicines. When this happens, the effects of one or both of the drugs may change or the risk of side effects may be greater. Anyone who takes cholesterol-reducing drugs should let the physician know all other medicines he or she is taking and should ask whether the possible interactions can interfere with drug therapy. Examples of possible interactions are listed below.
Some cholesterol-reducing drugs may prevent the following medicines from working properly:

  • thyroid hormones
  • water pills (diuretics)
  • certain antibiotics taken by mouth, such as tetracyclines, penicillin G and vancomycin
  • the beta-blocker Inderal, used to treat high blood pressure
  • digitalis heart medicines
  • phenylbutazone, a nonsteroidal anti-inflammatory drug

Taking some cholesterol-reducing drugs with blood thinners (anticoagulants) may increase the chance of bleeding.
Combining HMG-CoA reductase inhibitors with gemfibrozil, cyclosporine (Sandimmune) or niacin may cause or worsen problems with the kidneys or muscles.

Lifestyle considerations with cholesterol drugs

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.

For other cholesterol-improving strategies, read: “HDL – Good Cholesterol, natural ways to increase it” or “LDL – Bad Cholesterol, Natural ways to reduce it”

Sources: ivillage, mens-health, healthatoz, fda

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