What is Cholesterol? Cholesterol is described by most medical textbooks as a waxy fat-like substance found in some foods and also made by the liver.  Although cholesterol gets a lot of bad press, cholesterol is absolutely necessary for life.  Cholesterol is used by all living cells.  A Few of the Important Roles Of Cholesterol All cells need cholesterol to maintain the structure of their cell membranes.  Some important hormones are derived from cholesterol.  Cholesterol is essential for brain function and protects against depression.  Cholesterol is so important that the body actually manufactures cholesterol.  The body has a beautiful way of handling cholesterol to keep everything in balance.  If there is not enough cholesterol it makes more.  If there is too much cholesterol the body removes it. However when our diet contains too much saturated fat our system becomes overwhelmed with cholesterol and the elaborate system that the body uses for keeping cholesterol in check breaks down. Some of you may be old enough to remember “The I Love Lucy” episode where Lucy and Ethel are working in a chocolate factory.  They are responsible for boxing up the chocolate as it comes down the conveyor belt.  Every thing is fine and fun when the belt is moving at the right speed.  However when the conveyor belt goes too fast they can’t keep up with all the chocolate. They start stuffing the chocolate in their mouths, aprons and pants to try to keep the chocolate from falling on the floor. This is what happens when we overload our diet with saturated fats.  The cholesterol conveyor belt in our body starts moving too fast.  The body is unable to package the cholesterol properly and the body starts looking to places to put the excess.  One of the places the body put the excess cholesterol is on the blood vessel walls. Let’s take a little closer look at what goes on in liver which is the cholesterol processing plant of the body.  When we eat fats, the fats are absorbed in the intestinal wall.  Here the fats are packaged up in little transport submarines called chylomicrons (ky-low-my-crons).  The fats cannot travel in the blood stream without these submarines because of the simple fact that oil and water do not mix.  The fats are oil and the blood is primarily water.  So in order for the fats to travel in the blood stream they have to be transported in submarines.  Once in the blood stream the submarines take the fats to the tissues where they are needed.  The fats are a good source of energy so if they travel by a muscle that is actively working and in need of energy the muscle snatches up the fats from the submarine.  If there is not much activity going on the submarine transports the fats to the fat cells for storage.  The fat and muscle cells are interested in unloading only the portion of the fat that they can use.  After the muscle and fat tissue takes off what they can use the sub goes to the liver for repackaging.   The empty sub is reloaded with repackaged as a lipoprotein particles. The lipoprotein particles are a combination of lipid and protein.  The submarines are then sent back into the circulation.  This transport system allows fat molecules to be transported from the place where they are made (the liver) to the place where that are used, namely, fat and muscle tissue.  Each time the submarine goes back to the liver to get repackaged, the lipoprotein contains less and less triglyceride.  Eventually the LDL (low density lipoprotein, also know as the “bad” cholesterol) gets sent out for delivery.  The LDL cholesterol contains very little triglyceride and is mostly cholesterol. Why is cholesterol important? Please keep in mind that the LDL particles are necessary for health and serve an important purpose.  However the problems arise when the system gets overloaded with the LDL particles.  If the liver is unable to process all the fats that show up at its door, the orphaned fats are free to roam the streets (blood vessels) looking for trouble.  When the roaming LDL particles reach a certain concentration, the LDL starts to stick onto blood vessel walls.  This then sets off a whole cascade of bad events that may eventually lead to heart attack and stroke. Once the LDL binds to the blood vessel wall they are susceptible to be oxidized.  The oxidized LDL then starts to attract more LDL particles and the LDL cluster gets bigger and bigger.  The next event that happens in this sequence of bad events is that the growing LDL cluster which I will call a lesion, sets off the inflammation alarms.  The inflammation alarm causes the body to send in the soldier cells to try to take care of the situation.  You know as well as I when the soldiers are sent into battle, even though they are well-meaning, the process of the battle causes damage to the area where the battle took place.  The soldier cells that are sent in are called macrophages meaning large eating cells ("macro" = large; "phage" = to eat).  The macrophages start eating the LDL but because there is so much LDL in these lesions the macrophages become what are know as lipid-laden foam cells.  Thus these cells that were initially sent in to help the situation actually make the situation much worse.  The growing lesion with the LDL and the foam cells becomes what is sometimes described as a pimple on the blood vessel wall.  This gives a wrong picture because these plaques generally do not occur in one little area.  These lesions occur more in streaks and cover long areas of the blood vessels. As the lesions get worse and worse they develop areas of calcification and develop into what are know as plaques.  These calcium containing plaques make it possible for doctors to detect the presence of the plaques with some of the newer imagining techniques.  The plaques are what cause narrowing of the blood vessel and start to cause blood flow problems as the artery becomes smaller and smaller.  For many years doctors thought that the blood vessel continued to narrow until it was completely closed and this was what caused the heart attacks and strokes.  We know now that these plaques grow slowly enough to allow the body to remodel the blood vessel (the blood vessel bulges out) or grows new blood vessels to by pass the narrow area to maintain blood flow.   The greatest cause of heart attacks and stroke is when the blood vessel suddenly gets blocked. This occurs when plaques that are unstable suddenly burst.  The contents of the lesion then attracts platelets and other chemicals that rapidly forms a clot which blocks the blood vessels.  In summary the stable plaques that narrow the blood vessel wall are not as worrisome as the fragile unstable plaques.  The body can compensate for the stable plaques but the fragile clots break off, clots form that break off and suddenly close off the blood vessel. before This is what is know as a heart attack.  What IS HDL? (Good Cholesterol) The HDL cholesterol is known as the good cholesterol.  These lipid particles contain little or no cholesterol.  They contain the apolipoproten A. These particles actually serve to remove the cholesterol from the plaques and bring it back to the liver for processing or excretion.    What should my cholesterol levels be? When your cholesterol is checked by your doctor the cholesterol that is measured is the total cholesterol, HDL and the triglyceride.  The LDL cholesterol is calculated from these values from the formula LDL = TC – HDL – (TG/5).  LDL is LDL cholesterol (“bad cholesterol”) HDL is HDL cholesterol (“good cholesterol”) TG = triglyceride TC is total cholesterol LDL Cholesterol (mg/dL) Opitmal  < 100 Near optimal/above optimal  100-129 Borderline High  130-159 High  160-189 Very High > 90 HDL Cholesterol  (mg/dl) Low  <40 High >60 Total Cholesterol (mg/dl) Desirable  <200 Borderline High 200-239 High >240 The LDL cholesterol is the cholesterol that attaches itself to the blood vessel walls and can cause heart disease.  The LDL cholesterol is what we want to lower.  The HDL is the “good cholesterol”.  The HDL cholesterol attaches itself to the LDL cholesterol and brings it back to the liver for processing.  Triglycerides are the chemical form in which most fat exists in food as well as in the body. Triglycerides in the blood come from the fats eaten in foods or made in the body from carbohydrates.  If carbohydrates are not used immediately for energy, the carbohydrates are converted to triglycerides and transported to fat cells to be stored.  Hormones regulate the release of triglycerides from fat tissue so they meet the body's needs for energy between meals.  How can I normalize my cholesterol? By far the best way to reduce your cholesterol is through lifestyle modifications.  Modest amounts of exercise make a huge impact on cholesterol.  In terms of diet you really have to read the labels and avoid saturated fats. What I have found most effective is education about what cholesterol is and why it is important to reduce cholesterol.  I have also found it effective to discuss small, simple changes that can be made in the diet and lifestyle to improve cholesterol.  Prescription Medications to Lower LDL, Raise HDL, Lower TG Bile Acid Sequestrants There are some medications called bile acid sequestrants which prevent the cholesterol from being absorbed from the intestines.  Some of the brand names include Questran® (Cholestyramine) Welchol® (Colesevalam) Colestid® (Colestipol).  These medications bind bile acid to form a substance which cannot be absorbed by the body and therefore is eliminated via feces. The side effects include gastrointestinal problems such as constipation; they may also decrease the absorption of other medications the patient may be taking. Ezetimibe Zetia (ezetimibe) also helps block the absorption of cholesterol in the intestine but by a different mechanism from the bile acid sequestrants. Fibrates Fibrates are useful for lowering triglycerides and raising HDL but are not as effective in lowering LDL.  A couple of the brand names include Gemfibrozil® (lopid) and Tricor® (fenofibrate).  Fibrates increase cholesterol excretion in bile.  Therefore the fibrates may predispose patients to the formation of cholesterol gallstones. Niacin Niacin (Nicotinic acid) is a natural supplement.  It is one of the B vitamins and is useful for lowering cholesterol if taken in doses that are much higher than the doses when used as a vitamin.  Niacin can be purchased without a prescription but the high doses required for cholesterol lowering can cause significant side effects. The side effects range from unpleasant to dangerous.  The unpleasant side effects include facial flushing similar to a hot flash, nausea, vomiting, indigestion and diarrhea.  The dangerous side effects include liver problems, gout, and high blood sugar. The risk of these complications increase as the dose of nicotinic acid is increased.  Therefore Niacin should not be used at the doses required to lower cholesterol without the supervision of a physician.   HMG CoA Reductase Inhibitors (statins) The most common medications that are used to treat cholesterol are the so called “statin” drugs.  The brand names include Zocor® (simvastatin), Lipitor® (atorvastatin), Pravachol® (pravastatin), and Crestor® (rosuvastatin), and Mevacor® (lovastatin).  The statins work mainly with your liver to decrease production of cholesterol and reduce cholesterol in your bloodstream.  The statin medications are in the class of medications known as HMG CoA Reductase Inhibitors.  To explain how the statins (HMG CoA Reductase Inhibitors) work let’s first take a look at how cholesterol is manufactured in the liver.  I am going to start with molecule called mevalonic acid, or mevalonate.  There are many steps that take place in the liver take lead up to the formation of mevalonate but for our discussions we can start with the mevalonate.  Just like bread dough can be used to form either a loaf of bread or a pizza crust, mevalonate can be used to make either cholesterol or another important molecule called CoQ10.  However in order for the mevalonate to be made into either cholesterol or CoQ10 it needs the enzyme called HMG CoA Reductase to make the reaction happen.  If there is no HMG CoA Reductase then there is no cholesterol and no Co-Q10.  The statin drugs work by interfering with the HMG CoA Reductase.  The statin drugs are therefore called HMG CoA Reductase inhibitors.  The statin drugs prevent mevalonate from becoming either cholesterol or CoQ10.  Many researchers believe that one of the reasons that statins are associated with the side effects like muscle cramps is because they interfere with the production of Co-Q10as well as with the cholesterol.  For this reason anyone taking statin medications should also be supplementing with Co-Q10.  Because the statin drugs work in the liver they can cause liver problems and should definitely not be used by anyone with existing liver problems.  For this reason you should have a blood test to check for liver problems before starting statin medications and every 3-6 months after starting statin medications. Natural Supplements to Lower LDL, Raise HDL, Lower TG As a family doctor not a day goes by when I don’t hear a patient say “Doc I just cannot take the cholesterol drugs”.  Despite what the prescribing label and the medical literature says about the “very rare side effect s” many patients do have side effects from the statin drugs and refuse to take them.  I often try some of the other medications but none are effective as the statin drugs in lowering cholesterol.  This is why I am so excited about discovering natural supplements that can effectively normalize cholesterol for some patients without causing troublesome side effects.   Fish oil (omega 3 fatty acids) Omega -3 fatty acids have receive a great deal of attention recently because research has shown that omega-3 fatty acids reduce inflammation and appear to be very important for preventing a growing list of diseases that include heart disease and arthritis.  Although the Omega-3 fatty acids are essential for good health they are not capable of being manufactured by the body.  The omega-3 fatty acids must obtained from food.  Omega-3 fatty acids can be found primarily in fish but some plants also contain omega-3 fatty acids.  Omega-6 is another important fatty acid that must be obtained from food (meats).  Omega-3 and Omega-6 work in concert with each other.  The omega-3 fatty acids reduce inflammation and the omega-6 fatty acids promote inflammation.  These two fatty acids keep each other in check and therefore our diets must contain a balance between the omega-3 and omega-6 fatty acids.  It is okay for our diets to contain more omega-6 than omega-3 but we should not eat more than 4 times the amount of mega-6 than omega-3.  However the typical American diet tends to contain 10 to 30 times more omega-6 fatty acids than omega-3 fatty acids.  This imbalance may be the reason that we are seeing an increasing rate of inflammatory diseases in the United States. By eating a diet high in omega-3 fatty acids or by taking omega-3 supplements to balance out the over abundance of omega-6 in our diet we can increase the HDL (“good cholesterol) decrease triglycerides and decrease LDL (‘bad cholesterol”).  In addition to improving cholesterol, research has indicated that by increasing our intake of omega-3 fatty acids either through diet or supplements we may also improve blood pressure, reduce the risk of heart disease and stroke, and improve or prevent some forms of arthritis.  There have also been interesting studies that indicate that omega-3 fatty acids help psychiatric disorders such as depression, bipolar disorder, schizophrenia and ADHD. There are a staggering number of potential benefits and the relative lack of side effects and risks associated with supplementing omega-3 fatty acids   CoQ10 CoQ10 does not specifically normalize cholesterol but it is such an important coenzyme that I wanted to include CoQ10 in this discussion. You may remember from biology class that the mitochondria is the “powerhouse of the cell”  Coenzyme Q10 is an important enzyme involved in the chemical reactions in the mitochondria to produce the cellular fuel known as ATP.  It seems that the more we learn about CoQ10 the more important it becomes.  CoQ10 is current being studied in the treatment of heart disease and the early results are very promising.  CoQ10 is also a powerful antioxidant.  CoQ10 inhibits the oxidation of LDL cholesterol.  Remember from the discussion above that the oxidized LDL attracts more LDL to the blood vessel walls and leads to heart disease and stroke.  Both cholesterol and CoQ10 require an enzyme known as HMG CoA Reductase to be made.  The statin drugs inhibit the HMG CoA Reductase.  Therefore, while the statin drugs lower cholesterol, they also lower CoQ10 levels.  Many researchers believe that the lowered Q Q10 levels is one of the causes of the muscle aches that are some times associated with the statin drugs.  Red Yeast Rice Fermented red yeast rice is a natural form of lovastatin.  Lovastatin is marketed by the brand name Mevacor.  In fact red yeast rice is so similar to the prescription medication, lovastatin that the FDA, until recently, has banned the over-the-counter sale of red yeast rice.  For me, red yeast rice offers the best of both worlds.  It is a natural compound that works like a statin drug.  Because it is a natural compound and not synthesized in a laboratory, the body has the mechanisms in place to process it correctly with a reduced risk of side effects. There have been a number of recent studies that show that red yeast rice significantly lowers cholesterol levels without reported side effects (Click here to read to this study). Red yeast rice is has been a food staple for thousands of years in Asian countries without reports of toxicity. They attribute the safety of red yeast rice products to the process of preparation that does not involve the isolation and concentration of a single ingredient as is done when the statin drugs are industrially manufactured Precautions when starting red yeast rice products One of the problems with natural supplements is that different products contain different concentrations of melavolin, the ingredient in red yeast rice that lowers cholesterol.  In addition it is important to keep the level of citrinic acid to a minimum.  For these reasons it is important to buy from a company that has strict control of quality. Who are suitable candidates for red yeast rice products? There is no universal agreement among doctors about who are the best candidates for the red yeast rice.  There is agreement however that the decision to start red yeast rice should be made in conjunction with the patients own doctor familiar with the patients medical condition and family history.  In general red yeast rice is recommended for patients with mild elevation of cholesterol when diet, weight loss, and exercise are insufficient in lowering cholesterol to optimal levels.  Red yeast rice may also be effective for patients that have had their cholesterol lowered with a statin drug and would like to maintain their cholesterol in the normal range.  I also recommend red yeast rice to my patients that will not take a statin drug or who cannot tolerate a statin drug.  Who are not suitable candidates for red yeast rice? Patients that have moderate to severely elevated cholesterol or those at risk for heart attacks or stroke (patients with a prior heart attack or stroke or patients with diabetes) should probably take more aggressive measures to lower cholesterol before starting red yeast rice.     The following is a statement from the American College of Cardiology Foundation on the use of red yeast rice. Click here to link to the entire article “Red yeast is the rice fermentation product of a mixture of several species of Monascus fungi, principally Monascus purpureas. It contains monacolin K (lovastatin, mevinolin) and other HMG-CoA reductase inhibiting compounds. Red yeast has been used to reduce cholesterol levels. In a 12-week placebo-controlled study conducted in the U.S. in 83 healthy subjects with hyperlipidemia (Click here to link to this study), 2.4 g of red yeast rice significantly reduced total cholesterol by 16%, LDL cholesterol levels by 22%, and total triglycerides by 7% compared with placebo. No serious side effects were reported, but additional longer-term studies are needed. Red yeast should be treated as an HMG-CoA reductase inhibitor, with all the possible side effects, drug interactions, and precautions associated with this class of drugs. Red yeast rice is no longer marketed with standardized lovastatin levels in U.S. owing to legal issues, and it is now sold without lovastatin levels declared. Because of the availability of statins, its use is not recommended.” The way I read this statement is that red yeast rice does seem to be effective but because the prescription medication is available patients should use the prescription medication.  It is difficult for me to read this without calling to mind how much influence the pharmaceutical companies have on conventional medicine but this is just my opinion. Cholestsure I wanted to find a supplement containing both red yeast rice and CoQ10.  I also wanted to find a manufacturer that assured that their products were of the highest quality and would deliver the same quantity and concentration of ingredients in each dose.  Finally I wanted to find a product that contained no artificial flavorings, preservatives, colors or sweeteners. The product that we found, Cholestesure, meets all these criteria.  In addition the Cholestsure contains other ingredients that have been found to be helpful in lowering cholesterol. Chromium Polynicotinate Chromium is used for increasing high-density lipoprotein (HDL) cholesterol levels. Chromium is also used also for improving glucose control in diabetics and in patients with prediabetes.  . It is also used orally for weight loss, to increase muscle mass and fat-free mass, and decrease body fat. Chromium is also used orally to enhance athletic performance, to increase energy and vigor, and to treat some mild forms of depression. Policosanols Policosanol is used for treating high cholesterol and as an anti-plaque agent. Octacosanol Octacosanol is used for treating hyperlipidemia; and atherosclerosis.  It is also used for exercise performance including strength, stamina and reaction time. Guggul lipids Guggul gum resin is used for arthritis, lowering high cholesterol, atherosclerosis, and weight loss. Artichoke (leaf) Extract Artichoke has many other uses in addition to helping treat high cholesterol.  It is used for nausea, alcohol-induced hangover, and irritable bowel syndrome (IBS). Artichoke is also used orally for treating, anemia, edema, arthritis, bladder infections, liver dysfunction, preventing gallstones, and lowering blood pressure. Eicosapentaenoic Acid Eicosapentaenoic acid (EPA) also has many uses. EPA is used for cystic fibrosis, treating depression, pregnancy-induced hypertension in high-risk pregnancies, age-related macular degeneration (AMD), coronary artery disease, schizophrenia, personality disorder, Alzheimer's disease, and diabetes.  EPA has been found most effective when used in combination with docosahexaenoic acid (DHA) in fish oil preparations for a variety of conditions, including preventing and reversing heart disease, asthma, cancer, dysmenorrhea, hay fever and lung diseases.