Statins | How They Work | The Problems | Who Needs 'Em? | Natural Alternatives | Recommendations | References

What Are Statins?

So you had some blood work, and were told your cholesterol is too high. Now what??? If you have a regular family doctor, chances are you’ve been given a prescription for a medication to lower your cholesterol. The most common of these are “statin” medications including: Lipitor, Zocor, Crestor, and Mevacor. The first of these medications, Mevacor, came into the market in the late 1970’s.

As I’ve noted in earlier articles in this series, Statins are one of the most frequently prescribed classes of medication in the US. Spending on statin drugs increased by 156% from 2000-2005, with 2005 spending topping $20 billion. In Britain, 1 in 3 people over the age of 45 is on a statin medication. (13) These medications are widely prescribed, and believed to be completely safe for pretty much anyone to take. In fact, as reported by the Philadelphia Examiner in August 2010, a British researcher has suggested that these medications become available “over the counter”, and be handed out in fast food establishments alongside the condiments as a means to overcome the damage to our cardiovascular systems from consuming a fast-food meal. (3)

But are they REALLY that safe?  As with so many medical things, the answer depends on whom you ask. back to top

How do they Work?

Statin medications inhibit the enzyme HMG-CoA reductase. This enzyme is crucial in the production of one of the precursors to cholesterol. When the enzyme is inhibited, the cholesterol precursor can’t be produced, so the body is unable to produce cholesterol. The degree of inhibition is dose dependent – these medications at therapeutic doses reduce the production of cholesterol but do not block it completely. back to top

The Problems with Statin Medications

Unfortunately for the person taking statin medications, the precursor to cholesterol is also the precursor for Coenzyme Q10 (Co-Q10). Co-Q10 (also called ubiquinone), is a potent antioxidant which is present in all cell membranes. It is essential for production of ATP, the “fuel” for all cellular functions. Over 15 studies have documented reduction in Co-Q10 levels as a result of taking statin medications. (9)

Co-Q10 is required for cell membrane integrity, ATP production, nerve conductivity, muscle integrity, and formation of elastin and collagen. Side effects of Co-Q10 deficiency include muscle wasting, weakness, severe back pain, heart failure, neuropathy, and inflammation of tendons and ligaments with increased risk of rupture. (4)

The more fuel a cell requires, the more ATP it requires. Muscle cells, including the muscle cells in the heart, have a particularly high demand for energy. With reduced Co-Q10, these cells are unable to make sufficient ATP, and their ability to fully function declines.

One of the most common adverse affects of statin medications is muscle pain which can be mild to severe. Although most doctors will tell you that  muscle pain is a rare side effect, a study by Beatrice Golomb found that 98% of patients taking Lipitor and 1/3 of patients taking Mevachor suffered from muscle problems. “Muscle problems are the best known of statin drugs’ adverse side effects,” said Golomb. “But cognitive problems and peripheral neuropathy, or pain or numbness in the extremities like fingers and toes, are also widely reported.” A spectrum of other problems, ranging from blood glucose elevations to tendon problems, can also occur as side effects from statins. (5)

Deficiency of CoQ10 has also been documented in the blood and heart muscle of patients with congestive heart failure. (7, 8) In fact, while patients taking statin medications have been shown to have fewer fatal heart attacks, there is an increase in congestive heart failure in these patients. (9)

Statin medications have also been demonstrated to have negative affects on immune system functioning. In one study, macrophages (the white blood cells which provide “front-line” immune defense) were treated with Zocor at a relevant physiologic dose and others were not. They were then exposed to a common bacterial infection. The Zocor-treated macrophages were unable to properly engulf the bacteria and they generated excessive inappropriate inflammatory signals. (11) Not only were the cells unable to do their protective job of engulfing the bacteria, they contributed to a strong inflammatory response. This study, of course, was conducted in a laboratory and not in a human body. The implication of the results is that a human taking this medication is likely to experience a slower immune response to a bacterial threat, with more inflammation than a person not taking this medication. back to top

Who Should Take Statin Medications?

With the very real risks associated with these medications, I am firmly against making them available over the counter. Only a physician can advise you of whether the benefits of taking a statin medication outweigh the risks for your particular case.

Elevated blood cholesterol levels are not, in and of themselves, a reason to use these medications. If the total cholesterol is high, but the LDL/HDL ratio is good, the risks probably outweigh the benefits. Even if the cholesterol is high and the LDL/HDL ratio is marginal, if certain inflammatory markers are low (such as homocysteine), it is unlikely that statin medications will help to prolong your life.

Recent research has led to even further breakdown of types of cholesterol molecules. Some of these have been found to be pro-inflammatory and others have been found to be anti-inflammatory. A VAP or LPP test can determine these cholesterol fractions, and give you a better sense of whether you can truly benefit from using statin medications. I’ll talk more about these tests in my next newsletter! back to top

What About “Natural” Cholesterol Reducers Like Red Yeast Rice?

Natural cholesterol-lowering substances work through the same pathway as statin medications. They are less potent, and contain other alkaloids which may moderate their effects more than the concentrated, purified versions manufactured in a laboratory. The same cautions apply to these substances as to the statin medications because they can also lead to depletion of Co-Q10. back to top

What Should I do?

If it is determined that you truly need to take a statin medication, don’t go against your doctor’s orders. However, make sure you protect yourself against the side effects of the medication! It is critical that you replenish your Co-Q10. Dietary sources for Co-Q10 include oily fish, whole grains, and organ meats such as liver. Because it is very difficult to get enough Co-Q10 from your diet, especially if you are on a medication which blocks its production, supplementing is strongly recommended. A standard dose of CoQ10 is 200mg, and it is most easily absorbed when taken with a meal which contains some fat. (14)

One of the most important things you can do to manage your heart health is to manage your inflammation. Watch for information about the role of inflammation in heart disease and suggestions for how to measure and reduce inflammation in my next newsletter! If you want more information sooner, call me and set up an appointment for a consultation. back to top

References

1. Benati, Daniela, et al. Opposite effects of simvastatin on the bactericidal and inflammatory response of macrophages to opsonized S. aureus. Journal of Leukocyte Biology 2010 March.

2. Deambrosis P, Terrazzani G, Walley T, Bader G, Giusti P, Debetto P, Chinellato A. Benefit of statins in daily practice? A six-year retrospective observational study. Pharmacol Res. 2009 June.

3. Examiner.com, Philadelphia. Should McDonald's dispense free cholesterol drugs with your Quarter Pounder? August 15, 2010.

4. Fallon, Sally & Enig, MaryDangers of Statin Drugs: What You Haven’t Been Told About Popular Cholesterol-Lowering Medicines.

5. Golomb BA, Evans MA. Statin adverse effects : a review of the literature and evidence for a mitochondrial mechanism. Am J Cardiovasc Drugs. 2008 December 8(6):373-418.

6. Hippisley-Cox, J, et. al.. Unintended effects of statins in men and women in England and Wales: population based cohort study using the QResearch database. BMJ. 2010 May.

7. Kitamura, N., et al. Myocardial tissue level of coenzyme Q10 in patients with cardiac failure. In: Folkers K, Yamamura Y, (eds) Biomedical and Clinical Aspects of Coenzyme Q. Elsevier, Amsterdam 1984;4:243-252.

8. Folkers K., et al. Biochemical rationale and myocardial tissue data on the effective therapy of cardiomyopathy with coenzyme Q10. Proc Natl Acad Sci USA, 1985Feb,82:3, 901-4.

9. Langsjoen, P. The clinical use of HMG CoA-reductase inhibitors (statins) and the associated depletion of the essential co-factor coenzyme Q10; a review of tpertinent human and animal data. BioFactors. 18 (2003) 101–111.

10. Mercola.com. New Bombshell of Disastrous Side Effects from Statins… June 12 2010.

11. Richards, Byron. Statins Impair Immune System Function. March 20, 2010.

12. Sinatra, Stephen MD, FACC, FACN. Clearing Up the Cholesterol Confusion. The Townsend Letter, June 2009.

13. The Ledger.com. Spending Soars for Cholesterol-Fighting Statins. June 29th, 2008.

14. University of Maryland Medical Center website: http://www.umm.edu/altmed/articles/coenzyme-q10-000295.htm
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