Ezetimibe chemical structure
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Zetia

Ezetimibe (Zetia®, Ezemibe®, Ezetrol®) is an anti-hyperlipidemic medication. It acts by decreasing cholesterol absorption in the intestine. It is used together with statins (Vytorin®, Inegy®) to help lower cholesterol in patients who cannot be controlled on statins alone.

Ezetimibe binds to Niemann-Pick C1 like 1 protein on the gastrointestinal tract epithelium. This protein is required to transport cholesterol into the cells; hence ezetimibe blocks absorption.

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continuing challenge of cholesterol, The
From Electrical Apparatus, 12/1/04 by Elsberry, Richard B

The wax-like fat can clog arteries and is a major cause of heart disease

CONTROLLING THE AMOUNT of cholesterol in your bloodstream has become a never-ending battle for one in five American adults. Some are able to improve their cholesterol levels with diet and exercise, but two out of three adults need to supplement a healthy lifestyle with cholesterol-fighting medications.

And once the first prescription is written, chances are you have embarked on a lifetime program of managing your cholesterol level with pills.

Why control cholesterol? Because many physicians are convinced the wax-like fat can clog arteries and is a major cause of heart disease. But some researchers have recently started to question the accuracy of those conclusions. The reason: although Americans have been spending millions of dollars on cholesterol "maintenance" prescriptions, cardiovascular disease statistics in the U.S. have not declined in recent years but have skyrocketed to 930,000 deaths annually.

No one wants to refill an expensive prescription on a monthly basis if it is proving ineffective. But until medical professionals reach agreement on its true value in the fight against cholesterol then you and your internist ought to develop ground rules on how many resources you should invest in the fight. You should monitor progress in reducing cholesterol levels by laboratory testing every six months and adjust your program accordingly.

Cholesterol comes from two sources. It is produced naturally in your body, and it also is found in the foods you eat, such as eggs, meat, and dairy products. It is a bodily requirement; it is needed to produce vitamin D and to help develop adrenaline. But too much cholesterol also can clog up arteries and is a major risk factor for coronary heart disease and strokes.

To control cholesterol levels, physicians have been prescribing a combination of a low-fat diet, exercise, and cholesterol-fighting statin drugs. Over the past five years, the number of prescriptions issued to reduce cholesterol levels in the bloodstream have increased from 35 million to 125 million. One out of two adult Americans now pops at least one anti-cholesterol pill daily.

For the past several years, physicians have set the recommended level for cholesterol in the blood stream at 100 milligrams per 1,000 calories of food-or under 300 milligrams daily. But having a total cholesterol level under 200 mgs. does not mean you are home free. That is because cholesterol travels through the blood in different packages, called lipoproteins. Lowdensity lipoproteins (LDL)-also known as the "bad cholesterol"-originate in your liver and digestive tract and are delivered throughout to the body. High-density lipoproteins (HDL) remove it from the bloodstream.

The recommended level for LDL is less than 130 mgs., unless you are diabetic; then your LDL should be 100 mgs. or less. An LDL level between 130 and 160 is considered borderline high for most of the population. HDL levels less than 40 are considered at higher risk for heart disease; physicians would prefer them to be 60 or higher.

Triglycerides are a third type of fat in the blood. High levels of this fat, however, do not cause clogged arteries. Individuals with higher levels of triglycerides tend also to have higher levels of total cholesterol and LDL.

In order to keep a finger on patient cholesterol levels, most family physicians opt for regular blood tests and urge their patients to follow a diet that avoids sausage, bacon, whole milk, egg yolks, fried foods, saturated fats, potato chips, and pastries. Americans, however, do not have a good track record following low-fat and sugarfree diets. And some weight loss physicians, such as Dr. Atkins, have encouraged patients to gorge on fatty foods while eschewing carbohydrates.

Nationally, 60% of those being treated for high cholesterol with a combination of medication, diet, and exercise have not been able to reduce their cholesterol level to recommended limits.

However, a new drug is now available that works in conjunction with a statin to reduce the amount of LDL cholesterol absorbed from the digestive tract, and to regulate cholesterol in the liver. It is called Zetia (generically, ezetimibe) and is now available as a K) mg tablet. Zetia is designed to be taken by itself, or with a statin or lopid medication as part of a low fat diet. It was developed by Merck, which acknowledges that it may be weeks or months before beneficial effects are seen from this medication. Zetia works in the digestive tract to reduce the absorption of cholesterol. When added to a treatment plan that includes a statin and a healthy diet, zetia significantly reduces LDL. In the study group, it reduced LDL levels averaging 139 mg. by 25%.

In another study with the goal of increasing HDL levels, an experimental drug called torcetrapib was used in a dosage 120 mgs. in combination with Lipitor to double HDL in a group described as having "worrisomely low levels." This drug is said to still be a few years away from reaching the market.

For more information, contact the National Cholesterol Education Program at the National Heart, Lung, and Blood Institute Information Center, P.O. Box 30105, Bethesda, Md. 20824; 301592-8573; www.nhlhl.gov.

By Richard B. Elsberry, EA Contributing Editor

Copyright Barks Publications Dec 2004
Provided by ProQuest Information and Learning Company. All rights Reserved

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