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Pharmacology Lipid Lowering Agents (Antilipidemics)

Fibrates

Topic overview

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Fibrates—including gemfibrozil, fenofibrate, bezafibrate, and ciprofibrate—activate PPAR-α. This increases lipoprotein lipase activity, reduces apoC-III, and promotes fatty-acid β-oxidation. The resulting lipid changes include lower triglycerides and higher HDL, while LDL reduction is variable and limited. Their main clinical role is severe hypertriglyceridemia, including types III, IV, and V, and mixed dyslipidemia; reducing pancreatitis risk is a key outcome. Important risks include myopathy, cholestatic hepatotoxicity, and gallstones. Muscle toxicity is more concerning with statin combinations, particularly gemfibrozil, while fenofibrate is preferred when a fibrate is used with a statin. The lesson also covers interactions, renal dose considerations, contraindications, and monitoring of liver enzymes, CK, renal function, and lipids.

Learning objectives

What you'll learn

  • Identify prototype fibrates and explain their PPAR-α mechanism of action.
  • Describe fibrates’ effects on triglycerides, HDL, and LDL.
  • Recognize the principal clinical uses and outcomes of fibrate therapy.
  • Identify major adverse effects, contraindications, and clinically important interactions.
  • Outline monitoring and renal dose-adjustment considerations, including statin co-therapy.
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