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Second-line lipid-lowering agents

Last updated: February 15, 2021

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Second-line lipid-lowering agents include fibrates, bile acid resins, niacin, and cholesterol absorption inhibitors. These drugs are used concurrently with statins for patients who have hypercholesterolemia that is inadequately controlled with statin monotherapy. They are also used as second-line agents for patients who experience persistent side effects from statins (e.g., myositis, myalgias, and/or myopathy). Each drug targets different steps in the cholesterol and lipid metabolism pathways to treat hypercholesterolemia and, therefore, vary in their effectiveness at decreasing low-density lipoprotein (LDL), increasing high-density lipoprotein (HDL), and decreasing triglycerides. Second-line lipid-lowering agents are rarely indicated for primary prevention of cardiovascular disease because they do not improve cardiovascular outcomes or mortality.

Overview of lipid-lowering agents
Agent Lipids

Adverse effects

HDL LDL Triglycerides
HMG-CoA reductase inhibitors
  • Increased
  • Very greatly decreased
  • Decreased
Bile acid sequestrants
  • Slightly increased
  • Greatly decreased
  • Slightly increased
Ezetimibe
  • Increased/normal
  • Greatly decreased
  • Decreased/normal
Fibrates
  • Increased
  • Decreased
  • Very greatly decreased
Niacin
  • Greatly increased
  • Greatly decreased
  • Decreased
PCSK9 inhibitors
  • Increased
  • Very greatly decreased
  • Decreased

Marine omega-3 fatty acids (fish oil)

  • Slightly increased
  • Slightly increased
  • Decreased at high doses

Marine omega-3 fatty acids (fish oil)

Lomitapide

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