|Side Effects of Lipitor®, Zocor® and Other Statin Drugs
[Statin Drug Overview | CoQ10 Use in Conjunction with Statin Drugs]
[Drug Patents Explain CoQ10 Supplementation | Recommendation]
[Other Side Effects of Statin Drugs | Label Warnings for Select Statin Drugs]
[Possible Interactions With Other Medicines | References]Side Effects of Lipitor®, Zocor® and Other Statin Drugs
While statin drugs such as Lipitor®, Zocor® and Lovastatin® are beneficial to lower high blood cholesterol, they also have the effect of blocking the body’s natural production of Coenzyme Q10. Supplementation with CoQ10 is necessary to avoid the very heart disease that Lipitor®, Zocor® and Lovastatin® seek to avoid by reducing cholesterol. In a small number of other cases, the statin drugs depletion of CoenzymeQ10 led to liver disease.
Statin drugs such as Zocor®, Lipitor® and Lovastatin® block cholesterol production in the body by inhibiting the enzyme called HMG-CoA reductase in the early steps of its synthesis in the mevalonate pathway. This same biosynthetic pathway is also shared by CoQ10. Therefore, one unfortunate consequence of statin drugs is the unintentional inhibition of CoQ10 synthesis. Thus, in the long run, Lovastatin®, Zocor® and Lipitor® could predispose the patients to heart disease by lowering their Coenzyme Q10 status, the very condition that these drugs are intended to prevent.
The most common statin drugs include:
- Lescol Fluvastatin (FLOO-va-sta-tin)
- Lipitor Atorvastatin (a-TOR-va-sta-tin)
- Mevacor Lovastatin (LOE-va-sta-tin)
- Pravachol Pravastatin (PRA-va-stat-in)
- Zocor Simvastatin (SIM-va-stat-in)
Reporting in the Italian Journal of Respiratory Science in 1999, researchers said that the reduction of CoenzymeQ10 levels is associated with myopathy, an infrequent adverse effect associated with statin drugs. This metabolic myopathy is related to Coenzyme Q10 deficiency in muscle cell mitochondria, disturbing normal cellular respiration and causing adverse effects such as rhabdomyolysis, exercise intolerance, and recurrent myoglobinuria.1
It is important to note that Coenzyme Q10 supplementation does not interfere with the very important cholesterol-lowering effect of statin drugs such as Lovastatin®, Lipitor® and Zocor®. Therefore, if you are taking a statin drug, (especially for an extended period of time), you may want to consider discussing CoQ10 supplementation with your health care professional.
Common supplementation of Coenzyme Q10 is 50 mg to 100 mg per day for someone who is not taking statin drugs. A dosage of 100 mg to 200 mg per day may be considered for a person taking Lipitor® or Zocor® or other statins based on the recommendation of Dr. Julian Whitaker, M.D.8
In his 2002 petition to the FDA to mandate a warning be included in the package inserts of all statin drugs, Dr. Whitaker recommended the following text: “Warning: HMG CoA reductase inhibitors (statin drugs) block the endogenous biosynthesis of an essential cofactor, coenzyme Q10, required for energy production. A deficiency of coenzyme Q10 is associated with impairment of myocardial function, with liver dysfunction and with myopathies (including cardiomyopathy and congestive heart failure). All patients taking HMG CoA reductase inhibitors should therefore be advised to take 100 to 200 mg per day of supplemental coenzyme Q10.“8
It is interesting that the statin drug manufacturers have patented the combination of statin drug and Coenzyme Q10. We do not know of any formulations being marketed which actually use these patents. Unfortunately, the addition of Coenzyme Q10 to the pharmaceutical statin drugs would significantly increase the cost of these drugs. From patent #4,933,165 awarded to Merck & Co, in 1989, makers of lovastatin, the reasons for the combination of statin drug plus CoenzymeQ10 are as follows:
Coenzyme Q10 is a redox component in the respiratory chain and is found in all cells having mitochondria. It is thus an essential co-factor in the generation of metabolic energy and is particularly important in muscle function. Researchers, led by Dr Karl Folkers, have measured the levels of Coenzyme Q10 in endomyocardial biopsy samples taken from patients with varying stages of cardiomyopathy. These researchers observed decreasing tissue levels of CoQ10 with increasing severity of the symptoms of cardiac disease.2 In subsequent studies, this same research team, in a double-blind study, have reported improved cardiac output for some patients upon receiving an oral administration of CoQ10.3
Relatively low doses of Statin drugs such as Lipitor and Zocor effectively reduce plasma cholesterol levels. These drugs function by inhibiting the chemical transformation HMG-CoA to mevalonate, which is an early and rate-limiting step in the biosynthesis of cholesterol. A branch of the mevalonate cholesterol biosynthetic pathway in mammalian cells leads to the formation of CoQ10.4 Furthermore, high levels of statin drugs can reduce CoQ10 in the liver5 and compactin reduces LDL-bound CoQ10 at doses employed in humans6.
The Physician’s Desk Reference7 states that myalgia has been associated with lovastatin therapy. The myopathy is reversible upon discontinuance of lovastatin therapy. Since CoQ10 is of benefit in congestive heart failure patients, the combination with HMG-CoA reductase inhibitors should be of value in such patients who also have the added risk of high cholesterol levels.
Patent #4,929,437, also filed by Merck & Co describes the benefit of CoenzymeQ10 supplementation in the prevention of liver disease.
“In its application to the counteraction of liver damage (caused by statin drugs) and, in particular, elevated transaminase levels, the present invention (CoenzymeQ10 supplementation in combination with the statin drug) is accordingly to be understood as providing for the avoidance of liver damage and elevated transaminase levels where this may otherwise occur as well as the amelioration of said damage and elevated transaminase. The term counteracting is accordingly to be understood as connecting both a precautionary or prophylactic as well as curative or treatmental function.”