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General Overview of Statin Drugs
Ever since the health professionals learned how to measure cholesterol levels in the blood the problem of high level of ‘bad’ cholesterol started to be the health issue of the 21st century. Almost any middle-aged man, especially who is overweight or smokes suffers from hypercholesterolemia. All of them are advised to take cholesterol-lowering drugs, mostly statins, so it is extremely important to be educated on this issue.
The statins (or HMG-CoA reductase inhibitors) are a powerful group of drugs used as pharmaceutical agents to lower LDL (‘bad’) cholesterol levels.
Common statins are:
  • Atorvastatin calcium (Lipitor) made by Parke-Davis and Pfizer
  • Lovastatin (Mevacor) made by Merck
  • Pravastatin sodium (Pravachol) made by Bristol-Myers Squibb
  • Simvastatin (Zocor) made by Merck
  • Fluvastatin sodium (Lescol) made by Novartis
  • Rosuvastatins ( Crestor)
Mode of action of statins:
  1. Statins bind to the active site of HGM-CoA reductase - competitive inhibitor.
  2. As the result for the inhibitor cells in liver begin to produce more HMG Co-A
  3. Inhibition of this enzyme in the liver stimulates LDL receptors
  4. Since the liver is responsible for removing LDL’s from plasma by the LDL receptors, blood cholesterol levels fall dramatically.
  5. These drugs considered to be very effective as they not only bind to active site, but also change it.
  6. Synthetic statins (the above mentioned list) are larger molecules and form more interactions with the active site, that’s why are better inhibitors.
If taken only after the prescription, mixed with special diet, physical exercises and lifestyle changes and alone with constant regular blood tests (to make sure the medication is working and not causing side effects) statins give promising benefits. Most common benefits are:
  • Statins lower your ‘bad’ cholesterol
  • They are very effective in preventing strokes
  • They reduce risk of heart disease and give primary prevention of heart attack
  • When combined with fixed diet statins give secondary prevention to those patients who have already suffered a heart attack
  • They reduce coronary artery inflammation
  • Statins affect blood vessel growth
  • They reduce risk of osteoporosis
  • Reduce the risk of colon cancer when combined with non-steroid anti-inflammatory drugs
  • Reduce risk of Alzheimer’s Disease
  • Reduce MS symptoms
  • Statins have some immune system expression
  • Statins have comparatively small and affordable price
  • The first results can be seen after one week of use – that is rather fast
  • Statins have a moderate ability to reduce triglyceride levels, and increase levels of HDL cholesterol ("good" cholesterol)
All the statins have some differences. Some of them reduce ‘bad’ cholesterol levels to a greater extent than others, and some differs in the level of increasing the ‘good’ cholesterol level. Some of them are cheaper than others (the most expensive are atorvastatin and simvastatin). The newest statins are even called ‘superstatins’ as they appear to reduce LDL cholesterol to a greater degree than the other approved statin drugs. Some of them are not in use now because of their side effects.
By the way, the question of side effects is rather tricky. Either side effects are really dangerous or they are exaggerated. However, in most references statins are considered to be safe and well tolerated.
Side effects of the statins and other demerits:
  • Most common side effects of the statins are gastrointestinal - nausea, gas, upset stomach. 
  • Others are headache, dizziness, rash, and sleep disturbances (s more common with atorvastatin and simvastatin.)
  • Statins cause elevations in liver enzymes in 1 of 100 patients.
  • Statins cause a muscle disorder producing muscle weakness, and occasionally pain, in 1 of 1000 patients.
  • Some statistics say that it is rather dangerous for your brain, especially when taken statins for a long period of time.
  • Statins inhibit the production of healthy cholesterol in your body, that means they interfere with sex hormones and the normal healthy functioning of the endocrine system.
Some of the statins were removed from the market for their drastically dangerous side effects. In August 2001, Bayer Pharmaceuticals voluntarily withdrew Baycol (cerivastatin) following the deaths of 31 patients in the U.S. over a four year period. The reason of deaths was rhabdomyolysis, which destroys muscle cells and causes severe muscle pain. This condition is a side effect of all statin drugs and lots of non-fatal cases of rhabdomyolysis were already reported in the US.
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Important note is that side effects are increased by some other drugs, including some other class of cholesterol lowering drugs; and by some other factors (for example grapefruit juice increases the side effects).
In the way to a strong healthy body we should always remember the most important thing – medicines are the tool ONLY if there is no other way to treat the disease. Every nutritionist has known for a long time that if you want to have healthy biochemistry and healthy cholesterol levels, you have to turn to natural foods, to a healthy active lifestyle and adopt the strategies of natural health. Taking it more than for a month seems to be like overdosing for our body (as many doctors think). Of course, the choice is yours. But maybe it’s the time for you to begin living in harmony with your body in natural way.


Valentyna Ant.

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