Fibrates

3237

Summary

Fenofibrate, Bezafibrate and Gemfibrozil are fibrate drugs, a class of drugs primarily used to lower triglyceride levels. Fibrates lower triglyceride levels by activating PPAR-alpha, a transcription factor that upregulates or increases the expression of lipoprotein lipase. Lipoprotein lipase is an enzyme that then goes around cutting up triglycerides, breaking them down into free fatty acids. Fibrates also work to decrease production of VLDL and increase production of HDL, both of which help reduce triglyceride and cholesterol levels in your bloodstream. Fibrates are particularly potent for reducing triglyceride levels, which makes them first-line agents in treating hypertriglyceridemia. Important side effects to look out for include myopathy, hepatotoxicity, and gallstone formation, which is caused by the inhibition of 7-alpha-hydroxylase.

Key Points

  • Fibrates
    • Drug Names
      • Gemfibrozil
      • Bezafibrate
      • Fenofibrate
    • Mechanism
      • Activates PPAR-alpha
        • ↓↓↓ triglycerides
          • Induce lipoprotein lipase
        • Decrease VLDL
        • Increase HDL
        • Decrease LDL (usually)
    • Clinical Use
      • Most effective drug for lowering triglycerides
      • Prevents acute pancreatitis
        • Hypertriglyceridemia is an important cause of acute pancreatitis
    • Adverse Effects
      • Myopathy
        • ↑ risk with statins
      • Hepatotoxicity
        • ↑ risk with statins
      • Cholesterol gallstones
        • Via inhibition of cholesterol 7-alpha-hydroxylase