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The Effect of Statins on Bile Formation

According to 2008 data from the American Heart Association, 106.7 million Americans aged 20 or older have elevated blood cholesterol levels. When lifestyle changes fail, lipid-lowering drugs, such as statins, are often used help reduce high cholesterol levels.

  1. History

    • In 1976, Endo and colleagues isolated the first statin from the mold Penicillium citrinum. In 1979, Alberts and colleagues at Merck patented a different statin, lovastatin, from the fungus Aspergillus terreus. Lovastatin later became the first statin approved for use in humans.

    Types

    • The original statin (mevastatin) and the six currently prescribed statins have similar chemical structures. Statin medications have similar effects on bile formation, and include:

      * Crestor (rosuvastatin)
      * Lescol (fluvastatin)
      * Lipitor (atorvastatin)
      * Mevacor or Altoprev (lovastatin)
      * Pravachol (pravastatin)
      * Zocor (simvastatin)

    Bile Formation

    • Bile is a watery mixture of different compounds. In humans, the liver uses cholesterol to synthesize bile acids, which are then converted into bile salts. Bile salts are a major component of bile. Bile is important for the proper digestion of fats.

    Mechanism of Action of Statins

    • Statins slow bile formation by interfering with the liver's production of a major component of bile acids: cholesterol. More specifically, statins block a key enzyme in cholesterol synthesis called hydroxymethylglutaryl CoA (HMG-CoA) reductase, and keep excess cholesterol from entering the bloodstream.

    Therapeutic Effects

    • Although statins' main effect is to lower low-density lipoprotein (LDL or "bad") cholesterol, they can also help increase high-density lipoprotein (HDL or "good") cholesterol. Additionally, they have anti-inflammatory effects and slow the formation of plaque in a person's arteries, thereby reducing the risk of a heart attack or stroke.

    Side Effects

    • Although statins are generally safe, side effects may include back pain, chest pain, diarrhea, headache, joint pain, muscle pain, upper respiratory tract infection, sinus inflammation, tiredness, constipation and kidney or liver problems.

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