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Pantethine: a Critical Player in a Heart-Healthy Lifestyle PDF Print E-mail


Heart disease is the number one killer of Americans, accounting for more than 40 percent of all deaths in the United States. While heart disease is a broad term, it is used by doctors to describe atherosclerosis, the main cause of heart attacks and strokes. The National Cholesterol Education Program (NCEP), a division of the National Heart, Lung and Blood Institute (NHLBI) of the National Institutes of Health (NIH) has just released the latest guidelines for identifying and managing risks for coronary heart disease (CHD).

If you are like many health-conscious individuals, you may be willing to take several steps to prevent heart disease. You make healthy food choices, you exercise and you probably take several supplements for your general health. However, you may be confused about what other steps you can take. You may wonder what role cholesterol and blood lipids play in cardiovascular health. You may wonder if you have any risk factors for heart disease and what you can do in terms of prevention. If you have already been diagnosed with heart disease, you may be wondering how you can supplement the program your doctor has given you.

Atherosclerosis results from the buildup of plaque along the walls of blood vessels. It begins when the lining of the vessel is damaged. Fat carrying proteins, called lipoproteins, attach themselves to the damaged surface, causing cholesterol to build up. The low density lipoproteins (LDL) start to break down or oxidize, releasing free radicals, damaging nearby cells. The more LDL-cholesterol (LDL-C) in your blood, the more it can build up on the blood vessels. This whole process sets off the immune system to try to repair the damaged site, sending in specialized white blood cells, called macrophages, which eat the LDL-C. However when they become full of LDL-C, they become useless foam cells which contribute to the plaque formation. Chemical signals called growth factors are released, which cause fibrinogen (a sticky substance) to adhere to the plaque, attracting platelets. All these things together form a stiff plaque on the artery wall and ultimately block the artery. Your blood flow can be reduced by 90 percent before you feel any symptoms, but then it is too late; CHD has occurred.

These plaques have the unfortunate propensity to break loose, causing strokes, heart attacks and other ischemic conditions such as angina, poor kidney function, reduced eyesight, poor circulation in the legs (claudication). If in addition to poor lipids levels, someone has other risk factors such as hypertension (high blood pressure) or diabetes, then these events are accelerated. A heart attack (also called a myocardial infarction) is when something blocks the flow of blood to your heart—a clot, a spasm or an accumulation of plaque. A stroke is brain damage that occurs when blood flow to the brain is interrupted, either by a clot or when a blood vessel bursts. High blood pressure plays a crucial role in the development of heart disease and stroke. The higher the pressure the greater the stress on arteries and the more rapid the buildup of plaque. For reasons that are not entirely known, diabetes also increases plaque formation.

Blood Lipid Profile
When doctors order a lipid profile, they are measuring the levels of all the cholesterol in your blood, both good and bad. These include: Total cholesterol (TC), Low density lipoprotein (LDL-C—also known as the bad cholesterol), Very low density lipoprotein (VLDL-C—another bad player, very bad), High density lipoprotein (HDL-C—the good “healthy” cholesterol) and triglycerides (TG—yet another bad player). They may order additional tests such as glucose, to test for diabetes and homocysteine levels, as elevations of homocysteine are also implicated in heart disease.

When people talk about their “cholesterol level” they are usually referring to their total cholesterol. The assumption that many people make is simply “the lower, the better.” In reality, a healthy lipid profile is more complicated than simply low cholesterol. Cholesterol is a natural substance found in the body. The cells need a certain amount of cholesterol to make flexible, permeable membranes. The liver usually makes all the cholesterol the body needs. The cholesterol one ingests in the diet provides excess amounts. Cholesterol travels from the liver into the circulation by hitching a ride on LDL. It is carried away from tissues and back to the liver aboard HDL.

Perhaps even more important than the total cholesterol level is the ratio of good to bad cholesterol. High levels of HDL-C are cardioprotective. One well-known way to increase the level of HDL-C in the blood is to increase one’s activity level. Conversely, elevated levels of LDL-C are associated with an increased risk of heart disease, as are elevated triglycerides.

We need a certain amount of HDL-C because as discovered in the 1970s, it actually protects against the buildup of cholesterol plaques. It acts as a scavenger preventing plaques from adhering to vessel walls. Without these scavengers, or when the ratio of HDL-C to LDL-C is off, plaques can build causing atherosclerosis (or hardening of the arteries). An appropriate heart-healthy goal, then, goes beyond “low cholesterol.” Instead, we need to focus on a healthy lipid profile, with appropriate ratios of HDL-C, LDL-C and TG. Just as we should want to keep LDL-C and TG down to appropriate levels, we should also want to keep HDL-C up to an adequate level. The new definitions of normal, borderline and elevated cholesterol are more stringent than previously, which means that many more Americans will fall into “at risk” categories, with physicians recommending treatment. (For appropriate HDL and LDL levels, see “New Recommendations” .)

New Recommendations
Because heart disease claims more lives than any other condition in the United States (as well as other industrialized countries), the NHLBI is continually reviewing risk factors for heart disease in order to find more effective

COMPARISON OF EARLIER AND NEW CHOLESTEROL GUIDELINES
Lipid   Earlier NCEP* Guidelines   New NCEP* Guidelines
LDL-cholesterol
  • <130 mg/dl=optimal
  • 130–159 mg/dl=borderline high
  • 160 mg/dl=high
  • <100 mg/dl=optimal
  • 100–129 mg/dl=above optimal
  • 130–159 mg/dl=borderline high
  • 160–189 mg/dl=high
  • >190 mg/dl=very high
  • HDL-cholesterol
  • >35 mg/dl=optimal
  • >40 mg/dl=optimal
  • *National Cholesterol Education Program


    ways to prevent it. In this spirit, the NHLBI’S National Cholesterol Education Program (NCEP) has established new guidelines for a healthy lipid profile. These guidelines establish LDL-C as the target for therapy and define as normal an LDL-C level of 100 mg/dl or less (milligrams per deciliter of blood serum). The new guidelines identify levels of 100–129 mg/dl as “above optimal.” Those of 130–159 mg/dl are still defined as “borderline high,” and those at 160–189 mg/dl as “high.” Those above 190 mg/dl are considered “very high.” A healthy HDL-C level is defined as at least 40 mg/dl. Previous guidelines had identified 130 mg/dl as a borderline LDL-C level and 160 mg/dl as a high level. A desirable level of HDL-C was previously defined as at least 35 mg/dl. (See accompanying table.) For more information on the new NCEP cholesterol guidelines you may want to visit this section of the NHLBI Web site:
    http://www.nhlbi.nih.gov/guidelines/cholesterol/atp_iii.htm.

    The NCEP guidelines also call for more aggressive monitoring of people with “borderline” LDL-C levels. A physician’s initial intervention for a person in the borderline category would typically be lifestyle modification. The number of Americans receiving recommendations increases from 52 to 65 million with the new guidelines. Lifestyle modifications designed to promote a healthy lipid profile include reduction of dietary fat, increase of soluble dietary fiber and increase in physical activity, as well as weight loss and smoking cessation, if indicated.

    As a result of the new recommendations, more people with borderline profiles may find their physicians recommending that they begin taking a cholesterol-lowering medication, in addition to lifestyle modifications. The new recommendations increase this number from 13 to 36 million Americans. The medications typically used to lower cholesterol belong to a drug category known as HMG-CoA reductase inhibitors, or “statins,” because they end with the suffix “-statin.” Commonly used drugs in this category include atorvastatin (Lipitor), cerivastatin (Baycol), lovastatin (Mevacor), pravastatin (Pravachol), and simvastatin ( Zocor). Statins are typically prescribed with the goal of lowering LDL-C. They work by inhibiting cholesterol synthesis and increasing the number of LDL receptors in the liver. They also have a modest effect of increasing HDL-C and lowering triglycerides (TC).

    While statins have a clear benefit, they can also have adverse effects, a risk with any effective therapy. Common side effects include myositis (muscle inflammation), arthralgias (joint pains), GI upset and elevated liver function tests. Physicians typically obtain liver enzyme levels before starting a patient on a statin medication and monitor those levels throughout therapy. Because animal studies have shown an increase in birth defects, statins are not appropriate medications to take during pregnancy.

    Additionally there is some concern that statin medications deplete levels of certain natural substances that are beneficial, such as coenzyme Q-10 (CoQ10), a heart protective substance that is made in the liver. For this reason many people on statin therapy often take supplements of CoQ10 as well.

    What Else Can You Do?
    If your physician is concerned about your lipid profile, you should be too. There are several steps you may want to take before beginning statin therapy or in addition. Anyone with an elevated LDL-C and an HDL-C that is less than optimal would be wise to make any and all lifestyle modifications that apply. As mentioned earlier, these include increasing fiber and reducing dietary fat, which would lower LDL-C, and increasing physical activity, which is known to raise HDL-C. If you smoke, you need to quit. If you have diabetes, tight glucose control can also aid your lipid profile. While you will certainly benefit from a heart-healthy meal plan, it is wise to be skeptical of fad diets. They are often designed more for the benefit of the developer’s pocketbook than for your health and they often are too stringent for a reasonable person to follow for long. When perusing a diet ask yourself, “Could I stay on this plan for the next five or ten years?” If the answer is “no,” keep looking. In avoiding bad fats (animal fat and saturated plant fats—i.e. palm oil and trans fatty acids—margarine) don’t be afraid of the good fats: nuts, fish and other sources of omega-3 fatty acids. These can help you to achieve a good lipid profile. Red wine is protective, as is red grape juice, because the flavinoids protect against the oxidative damage from LDL-C. Soy protein has also been shown to lower LDL-C.

    Some supplements can lower cholesterol, too. As you probably know, niacin supplements (vitamin B3) have been used since the 1950s, particularly for lowering triglycerides. While immediate-release niacin is associated with flushing, the likelihood of flushing is much less with sustained-release formulations. However the risk of liver toxicity increases with sustained release formulations. Other side effects are nausea and difficulty with blood sugar control, making it less attractive for diabetics.

    Whether vitamin E supplementation is beneficial is in question. Several recent studies have shown no relationship between vitamin E supplementation and the prevention of cardiovascular mortality. However, future studies that take into account the bioavailability of vitamin E and appropriate dosages may yield different results. It works because of its antioxidant protection. Since it is fat soluble it is incorporated directly into the LDL-C molecule, helping prevent oxidative damage at the site of plaque formation.

    Folic acid (vitamin B9) is known to lower homocysteine levels, as does vitamin B12, vitamin B6 and betaine. Since elevated homocysteine levels are associated with heart disease and increased rate of atherosclerosis, it would be wise to include these in any heart healthy plan.

    Garlic has also been shown to lower LDL-C and increase HDL-C. The sulfur-containing substances in garlic help inhibit HMG-CoA reductase. Garlic is best used as fresh garlic, as the preparations are somewhat ineffective. Prolonged cooking and drying destroys the sulfur-containing compounds that are thought to be beneficial. The equivalent of one clove per day is sufficient. Since garlic has some antithrombotic activity, it is not recommended for patients taking anticoagulants (i.e. Coumadin).

    Pantethine: Known to Increase HDL-Cholesterol
    If you want to improve your lipid profile, you may want to consider supplements of pantethine. Remember the goal is not just lower cholesterol but a healthy profile overall. This includes LDL-C levels of 100 mg/dl or lower, TG of 150 mg/dl or lower and HDL-C levels of at least 40 mg/dl.

    Pantethine has been used for the past 30 years in Japan, where it is approved as a pharmaceutical agent for the purpose of increasing HDL-C. Pantethine is sold as a supplement in the United States. This water-soluble component of coenzyme A is a derivative of pantothenic acid (vitamin B5). Pantethine has a greater capacity to lower cholesterol than the vitamin itself. It is a colorless or light yellow substance that is soluble in water and alcohol and is usually taken as a tablet. Pantethine works by slowing production of cholesterol in the liver and boosting the rate at which one’s metabolism uses fats. It significantly reduces levels of TC and LDL-C while raising HDL-C. It is the most effective natural product against serum TG levels. Pantethine is not known to cause significant side effects, has no known drug interactions and may be the best choice for diabetics. It has not been known to cause birth defects.

    In a recent multicenter study daily doses of 600 mg pantethine were associated with increases averaging approximately 7 mg/dl in HDL-C, as well as moderate decreases in LDL-C and TG. In addition to taking several other heart-healthy steps, you may want to add pantethine to the tools you use for improving your lipid profile.

    Where to Get Quality Pantethine
    In order to get the best results from pantethine supplements you need to take a total of 600 to 900 mg daily, in two to three separate doses. Since the supplement industry is self-regulated, as a consumer you need to be cautious about how supplements are manufactured and whether they are what they claim to be. Daiichi Pharmaceutical Co., based in Japan, is the largest producer of pantethine in the world. They sell their own pantethine product here in North America as an ingredient to the dietary supplement industry under the name Pantesin™. Pantesin is manufactured by Daiichi’s own proprietary process.

    The result is a consistent, high-quality product. If a pantethine-based dietary supplement product includes the name Pantesin, you can be assured that you are buying a supplement made with the highest quality, pharmaceuticalgrade pantethine available in the market today. Supplements are just that. They do not replace adequate exercise and a healthy diet. To learn more about the role of fat in the body, visit the NCEP Web site (listed earlier). Ask your doctor if cholesterol screening is appropriate for you and use the knowledge you gain to live a heart-healthy lifestyle, adding supplements, and if needed, medication.

    Cathleen London, M.D. is a board certified family physician. Dr. London is a clinical instructor at Boston University in the Department of Family Medicine. She is also an assistant professor at Tufts University School of Medicine. She earned her medical degree from Yale University and completed her residency in family practice at Oregon Health Sciences University. Her premedical requirements were completed at Stanford University.

    Dr. London believes in a holistic approach to health care which utilizes a combination of Western, allopathic medicines, diet and lifestyle modification and herbal medicines when appropriate.
     
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