Safety of statins: focus on clinical pharmacokinetics and drug interactions

Circulation. 2004 Jun 15;109(23 Suppl 1):III50-7. doi: 10.1161/01.CIR.0000131519.15067.1f.


Statin monotherapy is generally well tolerated, with a low frequency of adverse events. The most important adverse effects associated with statins are myopathy and an asymptomatic increase in hepatic transaminases, both of which occur infrequently. Because statins are prescribed on a long-term basis, however, possible interactions with other drugs deserve particular attention, as many patients will typically receive pharmacological therapy for concomitant conditions during the course of statin treatment. This review summarizes the pharmacokinetic properties of statins and emphasizes their clinically relevant drug interactions.

Publication types

  • Review

MeSH terms

  • Binding, Competitive
  • Biological Availability
  • Calcium Channel Blockers / pharmacokinetics
  • Chemical and Drug Induced Liver Injury
  • Citrus
  • Cytochrome P-450 CYP2D6 / genetics
  • Cytochrome P-450 CYP3A
  • Cytochrome P-450 Enzyme Inhibitors
  • Cytochrome P-450 Enzyme System / physiology
  • Drug Interactions
  • Fenofibrate / pharmacokinetics
  • Gemfibrozil / pharmacokinetics
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects*
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics
  • Liver Function Tests
  • Polymorphism, Genetic
  • Polymyositis / chemically induced
  • Rhabdomyolysis / chemically induced


  • Calcium Channel Blockers
  • Cytochrome P-450 Enzyme Inhibitors
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Cytochrome P-450 Enzyme System
  • CYP3A protein, human
  • Cytochrome P-450 CYP2D6
  • Cytochrome P-450 CYP3A
  • Gemfibrozil
  • Fenofibrate