It is estimated that 30 million people worldwide are taking statins. Statins are a pharmaceutical prescription drug used to lower cholesterol. It was in 1784 that cholesterol was first isolated from gallstones, since then many scientists have dedicated their life’s work to understanding cholesterol and discovering the medicines that would control cholesterol levels in humans. In 1982 Lovastatin was the first statin drug to be commercially available.
Today there are a number of other statins on the market with the most popular being Pfizer’s Lipitor. Statins have been trialled and tested in lots of large scale clinical trials over long periods of time, the results of these trials have consistently shown that statins will lower plasma LDL levels by 25-35% and reduce the frequency of heart attacks.
But what are the effects of statins on the body?
The liver is the main processing centre for cholesterol. The liver produces an enzyme called HMG-CoA, it is this enzyme that is involved in the pathway that produces cholesterol.
Cholesterol is carried around the bloodstream by proteins. Low density lipoproteins (LDL’s) are one of those types of proteins. LDL’s are commonly referred to as the bad cholesterol because they deposit cholesterol in the walls of the arteries, once in the arteries LDL cholesterol oxidizes forming plaques and damaging the lining of the arteries. This can potentially lead to heart attack and stroke.
So how do statins work?
Statins inhibit the enzyme HMG CoA this puts a stop to the pathway that produces cholesterol. Statins also increase the number of low-density lipoprotein (LDL) receptors on the surface of liver cells, this results in more cholesterol being removed from the bloodstream. As well as lowering LDL levels statins are known to raise HDL levels by 5% - 15%.
Studies have also shown that statin drugs can help the body reabsorb cholesterol that has accumulated on the artery walls. Inside the blood vessels there is a thin layer of cells called the endothelium. Statins also help with endothelial functioning. Endothelial dysfunction often leads to atherosclerosis and this can cause other vascular diseases.
Statins are highly effective lipid lowering agents but common side effects of taking this drug are muscle pain, digestive problems, mental fuzziness or potentially liver damage. Statin side effects can be uncomfortable, making it seem like the risks outweigh the benefits.
Memory. Mental fuzziness, memory loss or an inability to concentrate are cognitive defects that can occur for some individuals taking statins. In half of the cases reported to the FDA in the USA, memory loss occurred within the first 60 days of starting to take statins.
Energy. At the University of California researchers found that patients on statins felt decreased energy when exercising. This seems to be worse in women than men. The effect statins have on muscle fibres and the tendency to cause fatigue made the researchers wonder whether statins make it more difficult to be motivated to exercise.
A recently published study showed that rats on statins couldn’t run as far as rats without the drug. On further inspection the muscle tissue in the rats on statins had less glycogen and there was evidence of mitochondrial damage. Glycogen converts to glucose in the body for energy use and the mitochondria are the powerhouses of our cells that burn this glucose for energy.
If statin use makes exercise more difficult and patients more sedentary this is the opposite effect of what someone with high cholesterol should be doing.
Increasing concerns about muscle-related problems are leading to the idea that lower doses of statins should be prescribed than what is currently recommended.
Diabetes. Researchers in Finland found that statin drugs can increase a person’s risk of developing type 2 diabetes. Statins increase a person’s insulin resistance by 24% and can impair the pancreas’s ability to secrete insulin. The concern is more for patients who are prediabetic with high cholesterol and on statins.
Serious side-effects
The following side-effect is very serious and potentially deadly.
Rhabdomyolysis, this is characterised by severe muscle aching and weakness throughout the entire body. The pain indicates that the muscle is breaking down, when this happens the body must eliminate the waste products, one of these waste products is creatine kinase. This is a marker that can be picked up in the patients’ blood test or discovered if the patient has dark cola coloured urine.
Patients taking higher doses of statins, are at a higher the risk of developing rhabdomyolysis. The risk is also increased if the patient is on other medications like cyclosporine and gemfibrozil while taking statins. The risk of developing rhabdomyolysis from statin therapy alone is very low, about 1.5 for each 100,000 people taking statins. Severe rhabdomyolysis can result in death from acute kidney failure due to overload of the kidneys with deteriorated muscle tissue.
In Australia in February and March 2012 the therapeutic Goods Act (TGA) reviewed the current product information given to patients on statins.
Memory loss. While it is noted that memory loss is a potential side effect the product information generally doesn’t mention that cognitive impairment and confusion are a possible side effect while taking statins.
The TGA are also reviewing the association between diabetes, increased blood sugar levels and statin use. At the moment there are varying recommendations for liver function blood tests when taking statins.
Periodic monitoring is recommended for most but not all statins.
Despite the uncomfortable side effects it is still the recommendation by the Australian heart foundation that statin therapy be prescribed for all patients with coronary heart disease / hyperlipidaemia. This therapy will be started in hospital as a treatment after any coronary episode and the patient is recommended to remain on statins even if there cholesterol lowers to a normal level as statins are thought to be beneficial in improving their overall health.
CoQ10 and statins
Coenzyme Q10 is important for mitochondrial biochemistry and is involved in the production of ATP. When statins inhibit the enzyme HMG Co-A they also inhibit one of the key steps in the production of Co Q10. It is known that this will then play a role in statin induced myopathy. It is recommended that individuals taking statins should also take 200-300mg of Co enzyme Q10 every day.
References
- https://www.ncbi.nlm.nih.gov/pmc/articles/Pmc3108295/#_ffn_sectitle Akira Endo, et al. A historical perspective on the discovery of statins. Biopharm Research Laboratories. 2010 May; 86 (5):484-493
Crean Daniel, Create Space Independent Publishing Platform, (2016)
Statin Answers Straight Facts about Cholesterol Drugs
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2849981/ Beatrice A. Golomb, MD., Ph.D. A review of the literature and evidence for a mitochondrial mechanism. Am J Cardiovasc Drugs. 2008;8(6):373-418
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4006404/ Polyana Mendes, et al. Statin- Induced Rhabdomyolysis: A Comprehensive Review of Case Reports.2014 April; 66(2):124-132
- https://www.betterhealth.vic.gov.au/health/conditionsandtreatments/cholesterol
- https://www.heartfoundation.org.au/
- https://www.tga.gov.au/alert/statins
- https://www.healthdirect.gov.au/statins
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