Disease, Illness and Condition Library
Cholesterol
cells of the body. It plays an important role in the production of bile secretions, and is used by the body to make such steroid hormones as the sex and adrenal hormones. The liver makes the majority of the cholesterol needed by the body, and most of the rest comes from the intestines. Only about 5 percent of the cholesterol in the blood comes from the foods we eat. Cholesterol levels in the body are determined by measuring the lipoproteins in the blood. Lipoproteins are the proteins that carry fat in the bloodstream, as the fat is not water soluble and can not travel alone. The serum lipoproteins are known collectively as cholesterol and include the following types: Low-density lipoproteins (LDL) transport cholesterol to the tissue. LDLs may stick to the blood vessel walls, and are thus considered bad cholesterol. They are only harmful after being oxidized by free radicals. Very low density lipoproteins (VLDL) are made in the liver to carry fats to other parts of the body. When they shed their fat they are LDLs. VLDL levels reflect triglyceride levels, and are high when the diet contains a lot of sugar and pastry. High density lipoproteins return cholesterol to the liver to be metabolized into VLDLs and waste products. HDLs protect against atherosclerosis and are consider good cholesterol. Cholesterol and Diet Modern western medicine attempts to control cholesterol and triglyceride levels through diet and prescription medications. Diet itself is important but may not be the main factor in controlling cholesterol levels. Some researchers believe controlling stress levels could be the x factor in the fight against high cholesterol. Dietary factors affecting cholesterol not only include total calorie intake but also the percentage from different food groups and well as the type of fat ingested. Fat will also tend to boost calorie intake and fast food restaurants provide the most concentrated sources of fat. So eating a steady diet from fast food restaurants will certainly put you at risk of higher cholesterol levels and cholesterol related diseases. Ultimately it is the type of fat you eat that is the most important. Saturated fats are found in butter, coconut and palm oil, and hydrogenated oils. Monounsaturated fats include olive and canola oils. Polyunsaturated fats include safflower, sunflower, and corn oils. Lowering the intake of saturated fats does lower cholesterol levels in most people, as is strongly recommended by doctors. Not only does a diet high in polyunsaturated fats help with cholesterol levels it can reduce the propensity to form blood clots, which sometimes play a role in initiating heart attacks and strokes. In addition to affecting cholesterol levels, fats cause the cell membranes to become too rigid, so that the cell itself cannot function properly. This leads to insulin resistance and hyperinsulinemia. An interesting note: Eating some fat signals the body to stop eating, thus helps to reduce obesity by overeating.
The majority medical experts agree that the best approach to lowering high cholesterol levels is through positive changes in diet and lifestyle. The dietary guidelines are straightforward: * Eat less saturated fat and cholesterol by reducing or limiting the amount of animal products in the diet. * Eat more fiber rich plant foods (fruits, vegetables, grains, and legumes) * Lose weight if necessary The lifestyle guidelines are * Get regular cardiovascular exercise * Don’t smoke * Reduce or eliminate consumption of coffee (both with caffeine and decaffeinated) In a lot of cases, dietary therapy alone is not sufficient to get lipid levels into the desired ranges. Fortunately, there are several natural compounds that can lower cholesterol levels and other significant risk factors for coronary artery disease. In fact, when all factors are considered (cost, safety, effectiveness, etc.), the natural alternatives presented below offer significant advantages over standard drug therapy. The natural products are best utilized in a comprehensive program that stresses a healthy diet and lifestyle. Conventional Drug Therapy Conventional drug therapy designed to lower cholesterol levels is prescribed at an alarming rate – nearly thirty million prescriptions per year – due to aggressive marketing by drug companies. The main problem is that these drugs have not yet shown, in long term studies, to lengthen a person’s life span. Several of the drugs are, in point of fact, associated with an increase in non-vascular mortality. In other words, while these drugs reduced the number of deaths from heart attacks and strokes, they increased the overall death rate. One of the reasons why cholesterol lowering drugs may add to overall mortality is that they are toxic to the liver and exceedingly carcinogenic (cancer causing). An article published in Journal of the American Medical Association (JAMA) summarized the carcinogenicity studies of cholesterol lowering drugs and clearly demonstrated that the risk of carcinogenicity for these drugs is far above recently issued FDA guidelines. The article asked several questions and provided answers that were extremely interesting. Here is an example: How did it happen that cholesterol lowering drugs were approved by the FDA for long term use in spite of their animal carcinogenicity? To address the question, the Encyclopedia of Natural Medicine obtained minutes of the Endocrinologic and Metabolic Advisory Committee meeting (under the freedom of Information Act) at which lovastatin and gemfibrozil – the most popular cholesterol lowering drugs – were discussed… The only reported discussion of animal carcinogenicity studies at the FDA advisory committee meeting on lovastatin (February 19 and 20, 1987) was by a representative of Merck Sharp & Dohme (makers of he Mevacor brand of lovastatin), who downplayed the importance of the studies. The minutes from the meeting on gemfibrozil (October 17, 1988) are particularly revealing. The committee did discuss the carcinogenicity of the drug. The minutes state: Dr. Troendle [deputy director, Division of Metabolism and Endocrine Drug Products for the FDA] noted that gemfibrozil belongs to a class of drugs that has been shown to increase total mortality. It has been shown to have animal carcinogenicity, and she does not believe that the FDA has ever approved a drug for ling term prophylactic use that was carcinogenic at such low multiples of the human doses of gemfibrozil. When asked to vote at the end of the meeting, only three of the nine members for the advisory committee believed the potential benefit of gemfibrozil outweighed the risk. However, the FDA ignored the committee’s recommendation and decided to grant gemfibrozil drug approval. Lopid (gemfibrozil) is now the second most popular lipid lowering drug, behind Mevacor (lovastatin). The bottom line is that thee drugs have been shown to be extremely carcinogenic in animal studies. Although extrapolation of animal data to humans is an uncertain process, there is enough evidence of carcinogenicity to warrant concern. The authors of the interview advised that lipid lowering drug treatment be avoided except in patients at high risk for an immediate heart attack or stroke. Yet the widespread use of these drugs defies this recommendation.
Niacin Even though niacin has demonstrated better overall results than other cholesterol lowering agents in reducing the risk of coronary heart disease, physicians are often hesitant to prescribe niacin. The reason is a widespread perception that niacin is a difficult and somewhat dangerous medicine. There is a great deal confusion about the benefits versus the risks for patients who take niacin. In contrast, most physicians are unacquainted with the considerable risks and limited benefits of commonly used prescription cholesterol lowering agents. In addition, since niacin is a widely available generic agent, no pharmaceutical company stands to generate the enormous profits that the other cholesterol lowering drugs have enjoyed. As a result, niacin is not intensively advertised like the other drugs. Despite the advantages of niacin over the cholesterol lowering drugs, niacin accounts for only 7.9 percent of all lipid lowering prescriptions. The cholesterol lowering activity of niacin was first described in the 1950s. It is now know that niacin does much more than lower the total cholesterol levels. Specifically, niacin has been shown to lower LDL cholesterol, Lp(a), triglyceride, and fibrinogen (a blood protein that causes clot formation) levels, while raising HDL cholesterol levels. An extensive evaluation of cholesterol lowering drugs (The Coronary Drug Project) demonstrated that niacin was the only cholesterol lowering agent to actually reduce overall mortality. Its effects are long lasting, as demonstrated in a fifteen year follow up study to the Coronary Drug Project. The follow up study showed that the long term death rate for patients treated with niacin was actually 11% lower than that of the placebo group, even though the treatment has been discontinued in most patients many years earlier. In other words, even though the patients were no longer taking the niacin, they still had al lower death rate. In contrast, patients being treated with cholesterol lowering drugs (clofibrate and/or cholestyramine) actually showed an increased death rate. Clofibrate was associated with a 36% higher mortality rate. Presumably both clofibrate and cholestyramine lowered cholesterol levels and reduced the mortality rate for coronary artery disease but increased the risk of dying prematurely form cancer, complications of gallbladder surgery (clofibrate causes gallstones), and other conditions. Clofibrate and, to a lesser extent, cholestyramine have been replaced by drugs such as lovastatin (Mevacor), pravastatin (Pravochol), simvastatin (Zocor), and gemfibrozil (Lopid). Are these new drugs effective at reducing mortality? The jury is still out. Preliminary studies are showing some benefits. For example, a five year safety and efficacy study of lovastatin involved 745 patients with severe hypercholesterolemia (total cholesterol levels greater than 360 mg/dl). The study demonstrated that the efficacy of lovastatin was maintained over time, there was no increase in mortality, and lovastatin was by and large well tolerated. Longer term studies with larger patient populations are now in progress with all of the statin drugs, but these results will not be presented for several years. In the meantime, millions of Americans are being placed on these drugs. Comparative Studies: Lovastatin vs Niacin To evaluate how niacin compares in safety and efficacy to the new lipid lowering drugs, one need only examine the results of several recent head to head comparison studies. In 1994, the Annals of Internal Medicine published the first clinical study that directly compared niacin and lovastatin. The twenty six week study was performed at five clinics and involved 136 patients who had coronary heart disease and LDL cholesterol levels greater than 160 mg/dl, and/or more than two coronary heart disease risk factors, or an LDL cholesterol level greater than 190 mg/dl without coronary heart disease or with few coronary heart disease risk factors. Patients were first placed on a four week diet, after which suitable patients were randomly assigned to receive treatment with either lovastatin (20 mg/day) or niacin (1.5 g/day). On the basis of the LDL cholesterol response and patients tolerance, the doses were sequentially increased after ten and eighteen weeks of treatment, to 40 and 80 mg/day of niacin, respectively. In the two patient groups, 66% of patients treated with lovastatin, and 54% of patients treated with niacin. Here were the results on lipoprotein levels: Group Week 10 Week 18 Week 26 LDL Cholesterol Reduction Lovastatin 26% 28% 32% Niacin 5% 16% 23% HDL Cholesterol Increase Lovastatin 6% 8% 7% Niacin 20% 29% 33% Lp(a) Lipoprotein Reduction Lovastatin 0% 0% 0% Niacin 14% 30% 35% These results show that, while lovastatin produced greater reduction in LDL cholesterol levels, niacin provided overall results despite the fact that fewer patients were able to endure a full dosage of niacin because of skin flushing. The percentage increase in HDL cholesterol, a more significant indicator for coronary heart disease, was dramatically in favor of niacin (thirty percent versus seven percent). Equally as impressive was the percentage decrease in Lp(a) level with niacin treatment. While niacin produced a 35% reduction in Lp(a) levels, lovastatin did not produce any effect. Niacin’s effect on Lp(a) in this study confirmed a previous study that showed that niacin (4 grams/day) reduced Lp(a) levels by 38%. Another comparative study focused on determining the lipoprotein responses to niacin, gemfibrozil, and lovastatin in patients with normal total cholesterol levels but low levels of HDL cholesterol. The first phase of the study compared lipoprotein responses to lovastatin and gemfibrozil in sixty one middle aged men with low HDL levels. In the second phase, thirty seven patients agreed to take niacin; twenty seven patients finished this phase at a dose of 4.5 g/day. In the first phase, gemfibrozil therapy increased HDL cholesterol levels by 10% and lovastatin by 6%. In the second phase, niacin therapy was shown to raise HDL cholesterol levels by 30%. Dealing with the Side Effects of Niacin The side effects of niacin are fairly common knowledge. The most common and bothersome side effect is the skin flushing that characteristically occurs twenty to thirty minutes after the niacin is taken. Other sporadic side effects of niacin include gastric irritation, nausea, and liver damage. In an attempt to combat the acute reaction of skin flushing, several manufacturers began marketing “sustained release,” “timed release,” or “slow release” niacin products. These formulations allow the niacin to be absorbed gradually, thereby reducing the flushing reaction. However, while these forms of niacin reduce skin flushing, they actually have proven to be more toxic to the liver. In a recent study published in JAMA, it was strongly recommended that sustained released niacin be restricted from use because of the high percentage (seventy eight percent) of patient withdrawal due to side effects; 52% of patients who took the sustained release niacin developed liver toxicity, while none of the patients who took regular niacin developed liver toxicity. Because niacin can impair blood sugar control, it should be used with close observation in patients with diabetes. Niacin should not be used by patients with preexisting liver disease or elevated levels of liver enzymes. For these patient groups, gugulipid (an extract of Commiphora mukul), garlic, or pantethine recommended. The safest form of niacin currently is known as inositol hexaniacinate. This form of niacin has long been used in Europe to lower cholesterol levels and to improve blood flow in cases of intermittent claudication. It produces slightly better results than standard niacin but is much better tolerated, both in terms of flushing and, more important, long term side effects. Niacin: Practical Ideas Regardless of the form of niacin being used, periodic checking (every three months, minimum) for cholesterol and liver enzyme levels in the blood is important. Please tell your physician that you are taking niacin and that you wish to be monitored. Because of its low cost and proven efficacy, niacin should be considered the first cholesterol lowering agent to try. The problems with niacin (skin flushing and other side effects) can be avoided by using inositol hexaniacinate. Sustained release niacin should not be used. If pure crystalline niacin is being used, start with a dose of 100 mg three times per day, and carefully increase the dosage over a period of four to six weeks to the full therapeutic dose of 1.5 g to 3 g daily in divided doses. If inositol hexaniacinate is being used, begin with 500 mg three times per day for two weeks, then increase to 1,000 mg. It is best to take either crystalline niacin or inositol hexaniacinate with meals. Pantethine Pantethine is the stable form of pantetheine, the active form of vitamin B5, or pantothenic acid. Pantetheine is the most important component of coenzyme A (CoA). This enzyme is involved in the transport of fats to and from cells, as well as to the energy producing compartments within the cell. Without coenzyme A, the cells of our body would not be able to utilize fats as energy. For some reason, pantethine has significant lipid lowering activity, while pantothenic acid has very little (if any) effect in lowering cholesterol and triglyceride levels. Pantethine administration (standard dose: 900 mg per day) has been shown to appreciably reduce serum triglyceride levels (by 32%), while increasing HDL cholesterol levels (by 23%). These effects are most striking when the toxicity of pantethine (virtually none) is compared to that of conventional lipid lowering drugs. Pantethine acts by inhibiting cholesterol synthesis and accelerating the utilization of fat as an energy source. There appears to be no toxicity or side effects from taking pantethine. Of the natural lipid lowering agents discussed, pantethine has the best effect on blood triglyceride levels. Therefore, it is quite helpful for individuals who primarily have elevated triglyceride levels. Pantethine is also appropriate for treating diabetics, since niacin is associated with impairment of insulin action. Several clinical studies have shown that pantethine produces impressive lipid lowering effects without side effects in diabetics. The dosage for pantethine is 300 mg three times per day. It has an excellent safety profile, and no significant side effects have been reported in the clinical trials. Vitamin C and Cholesterol Numerous population based and clinical studies have shown that vitamin C levels correspond with total cholesterol and HDL cholesterol levels. In one of the best designed studies, it was shown that the higher the vitamin C content of the blood, the lower the total cholesterol and triglyceride levels and the higher the HDL cholesterol level. The beneficial effects on HDL levels were particularly impressive. For each 0.5 mg/dl increase in vitamin C content of the blood, there was an increase in HDL cholesterol of 14.9 mg/dl in women and 2.1 mg/dl in men. Remember, for every one percent in crease in HDL cholesterol levels, the risk of heart disease drops four percent. This study and others demonstrate that vitamin C supplementation increases HDL levels even in well nourished individuals with normal levels of vitamin C in their blood. The most important effect of high dosage vitamin C therapy in reducing the risk of heart disease may turn out to be a reduction in Lp(a) and its antioxidant activity. Garlic Although garlic exerts a wide-ranging spectrum of beneficial effects, the modern use of garlic has focused on its ability to lower blood pressure and cholesterol levels, in the attempt to reduce the risk of dying prematurely from a heart attack or stroke. The volatile compounds of garlic are by and large considered to be responsible for most of the pharmacological properties. Fresh garlic contains 0.1 to 0.36 percent of a volatile oil composed of sulfur containing compounds: allicin, diallyl disulfide, diallyltrisulfide, and others. Allicin is mainly responsible for the pungent odor of garlic, as well as its pharmacology. Allicin is formed by the action of the enzyme alliinase on the compound allin. The essential oil of garlic yields approximately 60% of its weight in allicin after exposure to alliinase. The enzyme alliinase is inactivated by heat, which accounts for the fact that cooked garlic produces neither as strong an odor as raw garlic nor nearly as powerful physiological effects. Commercial Garlic Preparations The bulk of studies that showed a positive effect from administering garlic and garlic preparation used a form of garlic that delivers a ample dosage of allicin. Since allicin is the component of garlic that is responsible for its easily identifiable odor, some manufacturers have developed highly sophisticated methods of providing the full benefits of garlic; they provide odorless garlic products concentrated for alliin because alliin is relatively odorless until it is converted to allicin in the body. Products concentrated for alliin and other sulfur components provide all of the benefits of fresh garlic but are more publicly acceptable. Based on a great deal of clinical research, the recommendation is that a commercial garlic product should provide a daily dose of at least 10 mg of alliin, or a total allicin potential of 4,000 mcg. The German Commission E, and expert panel that sets dosage requirements to allow for therapeutic claims in Germany, requires that products deliver the equivalent of 4,000 mg of fresh garlic – roughly one to four cloves. Manufacturers of garlic products all publicize their preparation as being the best. How do you know who to believe? First of all, preparations standardized for alliin content are viewed by most garlic experts as the most favorable. However, there are other compounds in garlic that exert beneficial effects, including S-allylcysteines and gamma-glutamylpeptides. Therefore, the best product would be one that is rich in all garlic compounds and most resembles fresh garlic. What about aged garlic? It is notible that the expert panel of the German Commission E specified that the daily dose of garlic be equivalent to fresh, raw garlic. Since aged garlic preparations do not contain the beneficial compounds found in fresh garlic, they do not meet the Commission E monograph guidelines and cannot be marketed in Germany with the claims allowed for garlic. The Commission E was very specific: the daily dosage recommended to achieve the benefits associated with garlic requires the equivalent of 4,000 mg of fresh garlic. To highlight the superiority of fresh garlic preparations over aged garlic, let’s examine the results of the effects of both on blood pressure and cholesterol and triglyceride levels. AGED GARLIC FRESH GARLIC PREPARATIONS Total Cholesterol 7% reduction 10-12% reduction LDL cholesterol 4% reduction 15% reduction HDL cholesterol no effect 10% increase Systolic blood 5 mm Hg 11 mm Hg pressure reduction reduction Diastolic blood no effect 5 mm Hg Pressure reduction Daily dosage 7.2 grams >4,000 mcg of allicin The data for aged garlic in the preceding table are based on a recently completed double blind study of forty one men with beginning cholesterol levels in the 220 to 290 mg/dl range. The men received either aged garlic (7.2 grams per day) or a placebo for six months and then were switched to the other supplement for an additional four months. The results demonstrated a reduction of total cholesterol by 7%, and LDL cholesterol by 4%, but no changes in HDL cholesterol or triglyceride levels were noted. The systolic blood pressure dropped an average of 5.5% during the aged garlic period, but there was no change in diastolic blood pressure. Now let’s take a look at the effect of fresh garlic preparations in similar patient populations. A large number of double blind placebo controlled studies have been preformed on patients with initial cholesterol levels greater than 200 mg/dl. Supplementation with commercial preparations that provided a daily dose of at least 10 mg of alliin, or a total allicin potential of 4,00 mcg, were found to lower total serum cholesterol levels by about 10 to 12%. LDL cholesterol levels decreased by about 15%, HDL cholesterol levels usually increased by about 10%, and triglyceride, levels typically dropped 15%. These results were generally achieved within one to three months; significantly better results are typically achieved in a shorter amount of time with the fresh garlic preparations compared to aged garlic. Reduction of blood pressure has also proved greater when using fresh garlic preparations than when using aged garlic. With fresh garlic preparations, typical reduction of 11mm Hg for the systolic and 5.0 in the diastolic are usually achieved within a one to three month period. It has been concluded in expert reviews that the anti atherosclerotic effects of garlic are derived from alliin and allicin. The bottom line is that preparations standardized for alliin content provide the greatest assurance of quality. Garlic and Heart Disease A garlic supplement may not be necessary if the dietary intake of garlic and onion can be increased. In a 1979 population study, researchers studies three populations of vegetarians in the Jain community of India who consumed differing amounts of garlic and onions. Numerous favorable effects on blood lipids were observed in the group that consumed the largest amounts of both. Blood fibrinogen levels were highest in the group that ate no onions or garlic. This study is quite significant because the subjects had nearly the same diets, except in their levels of garlic and onion intake. Gugulipid Gugulipid is the standardized extract of the mukul myrrh tree, which is native to India. The active components of gugulipid are two compounds: Z-guggulsterone and E-guggulsterone. Several clinical studies have established that gugulipid has an ability to lower both cholesterol and triglyceride levels. Characteristically, total cholesterol levels dropped 14 to 27% in a four to twelve week period, while LDL cholesterol and triglyceride levels dropped from 25 to 35% and 22 to 30%, respectively. HDL cholesterol levels on average showed and increase of 16 to 20%. The effect of gugulipid on cholesterol and triglyceride levels is similar to that of lipid lowering drugs. While those drugs are associated with some degree of toxicity, gugulipid is without side effects. Safety studies in rats, rabbits, and monkeys have demonstrated it to be nontoxic. It is also considered safe to use during pregnancy. The mechanism of gugulipid’s cholesterol lowering action is its ability to boost the liver’s metabolism of LDL cholesterol. In addition to lowering lipid levels, gugulipid has been shown in animals to prevent atherosclerosis and aid in the regression of preexisting atherosclerotic plaques. This implies that it may have a similar effect in humans. Gugulipid also has a mild effect in inhibiting platelet aggregation and promoting fibrinolysis, suggesting that it may also prevent the development of a stroke or embolism. The dosage of gugulipid is based on its guggulsterone content. Clinical studies have demonstrated that gugulipid extract, standardized to contain to 25 mg of guggulsterone per 500 mg tablet, given three times daily is an effective treatment for elevated cholesterol levels, elevated triglyceride levels, or both. No significant side effects have been reported with purified gugulipid preparations, but crude guggul preparations such as gum guggul are associated with side effects (skin rashes, diarrhea, etc.)
Research has shown that consuming policosanol, a nutrient found in raw sugar cane and beeswax, significantly decreases LDL cholesterol levels, increases HDL levels and lowers total triglycerides, without raising blood sugar levels. Lecithin oil is high in nutrients. It helps to raise HDL levels and inhibits the absorption of cholesterol from foods. Two of the nutrients found in lecithin help to cleanse the liver, so that it can function more effectively, removing more fats from the bloodstream. Pumpkin seed oil contains nutrients we refer to as essential fatty acids. They are also used by the body to create hormones. Consuming the essential, polyunsaturated fatty acids may help to reduce the amount of cholesterol produced by the liver. The oil has also been shown to enhance the cholesterol-lowering ability of policosanol and other nutrients. D-limonene is a nutrient found in orange peel oil. It has been used to successfully dissolve gallstones, which are composed of cholesterol. It reduces blood cholesterol levels, additionally. Phytosterols, which are compounds found in plants that are similar in structure to cholesterol, have been shown to decrease cholesterol absorption in the gut by competing for absorption. Beta-sitosterol, for example, has been shown to inhibit cholesterol absorption by about 50% and lower blood cholesterol levels.
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