The current understanding of statin drugs

Statin drugs have been considered as medications to lower cholesterol levels in the clinic. An enzyme called HMG-CoA reductase is responsible for the production of cholesterol in liver and statins inhibit the enzyme and thus reduce the production of cholesterol in the body.^[1] As a result, statin medications are presently one of the most prescribed drugs in the United States and in the world. According to Bloomberg, the 2010 sales of the two top selling statin drugs, Lipitor and Crestor, were $16 billion in the USA alone and worldwide sales of all statins drugs are in the upper range of $300 billion. Statin drugs like Lipitor, Mevacor, Pravacol, Zocor and others do interfere with the enzyme reductase to inhibit cholesterol production which is normally produced by liver, cholesterol is also derived from dietary sources.

Statin drugs are reported effective in lowering cholesterol and reducing cholesterol related heart attack. But the question is, why are we not seeing remarkable drop in heart attack rates? An ongoing debate in the medical field is whether statins are effective in segments of population with high cholesterol but without health problems,^[2] and negative evidences OF WHAT were found from clinical data. Some published reviews suggest that there are mortality and morbidity benefits from statin,^[3][4] but there is concern about the quality of the evidence supporting these claims.^[5] Another review did not find a mortality benefit in populations with high risk for, but without prior, cardiovascular disease.^[2] With respect to quality of life, there is limited evidence of improvement when statins are used for primary prevention purpose.^[5] As of 2010, no study shows improved clinical outcomes in children with high cholesterol even though statins decreased their cholesterol levels.^[6] In the meantime, millions of prescriptions are written every year with little attention paid to statin’s possible or even severe adverse effects – a problem encountered with many drugs- like cognitive loss, neuropathy, muscle wasting, pancreatic and hepatic dysfunction, and sexual dysfunction.^[7]

Lovastatin was the first approved statin drug, which was isolated by Merck from the fungus Aspergillus terreus in 1978, and marketed in 1987 as Mevacor and then lovastatin.^[8] Individuals on statin drugs are supposed to continue with these medications for the rest of their lives to control cholesterol within so called healthy levels. Some studies have shown that long-term use of statin medications reduces the risk of recurrent heart attack, stroke and hospitalization of unstable angina. In fact, a regression of established atherosclerotic plaque will not benefit from the use of statins, but it is thought that there may be benefit derived from the stabilization of lipid levels which may reduce further progression. Therapies to reduce thrombotic episode associated atherosclerosis which is responsible for myocardial infarction and unstable angina are urgently needed.

The adverse effects of statin drugs

According to an article by Dr. Beatrice Golomb (MD, PhD, and Associate Professor of medicine at UC San Diego) published in the October 2008 issue of the journal of Pulse of Health Freedom, there is little or no evidence that statin drugs could benefit women.^[9] In that regard, a study published in the Journal of Empirical Legal Studies found that ads for Lipitor (atorvastatin) falsely stated the drugs’ potential benefits for women. The ads failed to make clear that research to date has proven that statin drugs could only help to prevent heart-related deaths among women with existing heart disease.

In theoretical model, statin medications should decrease cardiac mortality by about 2% for every 1% decrease in cholesterol levels. This was initially hailed as a major victory over heart disease and death from heart attack. However, the deaths rates from prolonged use of the medications due to suicide, homicide and accidents in patients who took statins were 3 times higher than those in patients who did not take statins.^[9] Importantly, the use of 80 mg of statins has been banned by FDA recently due to the risk of muscle injury, and it indicates that the dose has more side effects than benefits.^[10]

Is it really necessary to take statins to reduce heart attack? While there has been somewhat of a decrease in deaths attributed to myocardial infarction by statins, much of this can be attributed to changes in diet and the addition of fish oils and antioxidants. Importantly, there has been no correlation between the uses of statins and the decreasing of the incidence of first time heart attack.

Furthermore, there are warning signs that since the introduction of statins, episodes of congestive heart failure have been increasing. This is thought to be due to their propensity to deplete Coenzyme Q10 (Co-Q10) levels, an essential nutrient for the production of energy in muscle and other tissues. As a consequence, lowering of Co-Q10 levels translates to muscle weakness which is thought to be one of the factors in the formation of congestive heart failure.^[11] Are we really helping the heart, or we are making it more vulnerable to disease?

Cholesterol is an important nutrient necessary for life

Over the last 32 years, I was made to believe that cholesterol is the cause of heart disease. Now after seeing thousands of patients, cholesterol story does not match up. I have patients who have high cholesterol and no trace of heart disease, I have patients on statin drugs for 10+ years with extensive diseases but with low cholesterol, and I also have patients with high cholesterol and heart diseases. In fact, dietary cholesterol is not very absorbable by the body, but factors like lipid peroxidation, HCRP, homocysteine, inflammation, other dietary factors, nutritional deficiency due to MTHFR gene, other genetic factors, emotional factors, chemicals in food and environment and more, are the aggravating factors in heart disease, but not simply cholesterol.It needs to be emphasized that cholesterol is not that bad as we think, it is very important nutrient that the body make up to 3,000 mg daily because each of more than 33 trillion cells needs cholesterol. Cholesterol is an essential nutrient for the formation of important components like Vitamin D and cortisol, and the production of critical hormones like estrogen and testosterone.[12,13] Higher concentrations of cholesterol are found in brain and nerve tissue as it is an essential component for nerve system function. Cholesterol is generally insoluble in water and acts as a protective barrier in addition to being a vital component of the cell wall. Soluble forms of cholesterol are lipoproteins such as Low Density Cholesterol (LDL), Very Low Density Cholesterol (VLDL), and High Density Cholesterol (HDL). The solubility of cholesterols make them more mobile so they can be transported to areas where they are needed, and removed from areas where they aren’t.

In addition, cholesterol is dependent on the production of ubiquinone and dilochol. Ubiquinone or Co-Q10 is a critical cellular nutrient produced in the mitochondria where it plays a role in ATP production in the cells and functions as an electron carrier to cytochrome oxidase, one of our main respiratory enzymes. Because of its high energy requirements, the heart requires higher levels of Co-Q10 to be produced. Furthermore, another form of Co-Q10 is found in all cell membranes where it plays a role in maintaining membrane integrity and active transport of nutrients. Co-Q10 is also vital to the formation of elastin and collagen, components in higher amounts in cardiac and skeletal muscle. As a result, Co-Q10 deficiency may cause muscle wasting and even congestive heart failure, which could be the cause of the commonly reported adverse effect of statin drug use.

The synthesis of cholesterol occurs mainly at night in the liver, and there is an increase in liver activity between the hours of 1 to 3 am, according to Ayuvedic and Chinese medicine. This is also the time when the liver does toxin cleansing from blood stream, and patients who are awake during this time of night can be liver deficient. In other words, they wake up probably because their livers are not capable of adequately processing cholesterol or cleaning toxins.

It has been hypothesized that there is an association between blood type and higher cholesterol levels.^[14] People with blood types A and AB have an increased susceptibility to develop coronary artery disease (CAD) and atherosclerosis compared with types O and B. A person’s secretor type also plays a role with respect to inflammation and the ability to modulate it once it has occurred.^[15] Inflammation is mentioned here because there has been an explosion of knowledge about inflammation and the development of CAD In the past ten years. The most direct factor of inflammation tested in cardiovascular laboratories is the Cardiac C-reactive protein. The knowledge of Cardiac C-reactive protein allows physicians to develop treatments to control inflammation in order to decrease the deposition of plaque in the cardiovascular system, and thus to reduce CAD.

There are some comprehensive tests available in the clinic to make sure that what kind of treatment strategy is needed for a specific patient, as listed here:

• Routine lipid panel, including total cholesterol, LDL, HDL, TG
• LDL particle size
• HDL particle size
• Apo B – LDL particle number
• Lp(a): high levels can cause blood to clot easily, inherited, can be altered with medications
• Homocysteine:
• marker for inflammation and may have genetic component
• Lp-PLA2:
• measures imminent stroke risk
• CRP: highly sensitive, measures inflammation
• Fibrinogen:
• measures inflammation
• NT-proBNP:
• determines cardiac stress level
• Insulin and A1C : measures early insulin resistance and diabetic risk
• Vitamin D, B12, and folic acid
• Calcium scoring is a cat scan of the heart, which shows how much calcium deposits you have on your major blood vessels supplying circulation to your heart. This is very inexpensive test and can really tell us which direction we need to go with our treatment strategy.

Genetic tests to evaluate the risk of heart diseases:

• Apo E Genotype – identifies how people respond to dietary fat
• Kif6 Genotype – identifies if certain medications would be helpful
• LPA Genotype – identifies if taking aspirin would reduce heart disease risk
• 9p21 Genotype – identifies people with a risk of early onset heart attack

In addition, abdominal aortic aneurysm can be a heart disease risk factor, which can be easily detected with abdominal ultrasound.

Ayurvedic and Naturopathic medicine to regulate cholesterol level

Naturopathic medicine views lipids such as cholesterol and its various components as being essential to the normal development and maintenance of cellular function in support of homeostasis.^[16] To support this vital need, we have developed therapies to control not only the manufacture of cholesterol, but also the absorbance from dietary sources in a healthy way.

Each of the single components of cholesterol like LDL, VLDL and HDL, plays a role in maintaining healthy cellular growth and function, as well as being precursors in the formation of hormones, cortisol and mineral corticoids.^[12] To this end, the human organism has developed numerous mechanisms to regulate the intake and elimination of fats and cholesterol so that a balance is maintained. Most of the dietary fats we eat are cooked or fried at very high temperature, and the worst one are deep-fried. The temperature of deep-fried can reach in upper ranges of 400-500°F, and the food absorbs so much heat that when taken into the body, the heat is released and causes damages like heart burn, indigestion, inflammation, etc., and may help atherosclerotic plaque formation. I usually tell my patients that since there are no deep fryer in Mother Nature, our body’s millions years old genetic set-up does not fit to fried foods. Furthermore, deep-fried foods also adds chemicals like preservatives, pesticides, insecticide, hormones, plastics and even make harmful hydrocarbons, to the food which may increase the risk. This could become problematic when excessive cholesterols and fats are derived from dietary sources, and the body’s processing and cleaning capability is skewed or impaired. If there is inflammation as an additional factor, these factors together will cause the deposition of excessive cholesterol in the walls of arteries and veins, and result health problems.

Under normal body conditions, in addition to the functions mentioned above, cholesterol is functioning as a reparative substance to disrupt the glycosaminoglycan layer and protect arteries from being damaged. When there is an excessive amount and in the presence of inflammation, cholesterol will cause the formation of free radicals, oxidants, immune complexes and inflammatory mediators. Under these circumstances, excessive cholesterol will deposit on the inner surface of arteries to form atherosclerotic plaque, and lead to a narrowed and weaken artery. The plaque development occurs when the normal oxidation balance of cholesterol and lipid is disrupted, which will enable additional lipid deposition. The severe consequence is coronary artery disease and arteriosclerosis which are the predisposing factors to heart attack and stroke. Furthermore, genetic disposition factor of arteriosclerosis tendency, such as certain body types and blood types, will work together with the habit of taking cholesterol laden fast foods to cause further damage to the heart.

Naturopathic medicine views heart disease as primarily a disease due to problematic lipid oxidation, but not necessarily due to the elevated cholesterol level. Cholesterol level is elevated normally after ingestion of a meal, so do the triglycerides, since cholesterol and triglycerides are packaged and absorbed together in the intestine. How the body processes these will decide whether one will be healthy or if it will lead to the formation of plaque and deposition of lipid in the body. On the other hand, too low a level of cholesterol from either the use of statins, the lack of dietary source, or a liver disease, can be problematic to the body as well. The use of natural treatments of Ayurvedic and Naturopathic medicine together with well controlled dietary and living habits are the best ways to go for controlling cholesterol level healthily and permanently.

Natural treatments to lower cholesterol and triglyceride levels and reduce the risk of CAD include modifications of diet, monitor of dietary fat, addition of antioxidants to counter free radical formation, and decrease the chance of inflammation.^[16] A typical program to combat high cholesterol levels may also include liver support to not only clear excessive cholesterol, but to produce the proper combination of bile acids in order to eliminate excessive lipids, and as an additional impact, to reduce the incidence of gallbladder disease. There are several wonderful liver herbs in Ayurvedic Medicine for the regulation and normalization of liver function. Herbs like Guggul (Comiphora mukul), Amla (Emblica officinalis) and Turmeric, Red Rice Yeast has been shown to provide the same benefits as statin drugs but without the side effects. A number of natural treatment products combine it with niacin, phosphatidyl choline, fatty acids such as EPA and DHA, garlic, other known cholesterol and lipid lowering substances in order to enhance their effectiveness. As a matter of fact, Niacin has shown more plaque regression than statin drugs.^[17]

It is now common knowledge that a combination of treatments can bring higher cholesterol and lipid levels under control, and that normal levels can be maintained by diet alone. In those patients with genetic predispositions of higher lipid tendency, a current on-going program can be applied based upon individual body conditions and its needs. The following nutritional plan and routines will help the patient in general:

• Cut down red meat consumption to minimum like once a month, or eliminate completely. Studies show people who consume more red meat have a higher risk of death.
• Add healthy meat proportions like fish, chicken breast, or other seafood only two times per week.
• Add 7-8 servings of variety of vegetables daily, one serve is one 8 ounce cup of cut raw vegetables or ½ cup of cooked.
• Add 1-2 handfuls of nuts and seeds like walnuts, pecans, pumpkins, cashews, sesame, chia seeds, flax seeds, Brazil nuts, etc., per day. These should be non-roasted and non-salted.
• Add 1-2 tablespoon of good quality oils like olive oil, flax seed oil, mustard oil, safflower oil, coconut oil, even Ghee and grape seed oil. But do not cook with these oils, because most of them are mono or poly unsaturated oils and will go rancid with cooking. Add oil to your salads, beans, soups and rice. If you need to cook with oil, which I do not recommend, use Ghee or Coconut oils, these are saturated oils and on low heat will not go rancid.
• Even if you sautéing vegetables, put vegetable first in pan and then add oil to the pan. This way oil will temperature will stay below 100 degree Celsius.
• Add 1-2 bean-dishes per day, there are 700 different types of beans in the world.
• Add 2-3 fresh seasonal fruits per day.
• Walk 45 minutes per day and do light weight bearing exercises per day.
• Do stress reduction like yoga, breathing exercises, mediation, Tai chi, etc.
• Spend quality time with your friends, family, laugh and have fun, life is too short.

Adverse effects of statin medications

The adverse effects can be found from the NIH database web Pubmed, the highest authority of scientific and medical research. Please click Reference #18, and click the upper corner link on the webpage to access the free PDF article.^[18]