A clinician's guide to statin drug-drug interactions

J Clin Lipidol. 2014 May-Jun;8(3 Suppl):S30-46. doi: 10.1016/j.jacl.2014.02.010.


The statins are widely used worldwide to reduce risk for cardiovascular events in both the primary and secondary prevention settings. Although generally quite safe, the statins can be associated with a variety of serious side adverse effects, including myalgia, myopathy, and changes in plasma enzymes of hepatic origin. Although rare, the most serious of these is rhabdomyolysis. Several drugs can interfere with the metabolism and disposal of the statins, thereby increasing risk for adverse events. It is important that clinicians treating patients with statins be aware of the potential for drug-drug interactions between each statin and specific other drugs and take measures to prevent them. The prediction of potential drug-drug interactions derives from basic pharmacokinetic principles. Certain drug interactions are predicted by measuring the effect of interacting drugs on blood plasma concentrations of the statin. Individual patient variations resulting in part from polymorphisms in the metabolizing enzymes confound some of these predictions. Based on these known effects, a new classification for predicting statin drug interactions is proposed. This report discusses likely prescription and nonprescription interactions as well as potential alternatives for special populations.

Keywords: Cytochrome; Drug-drug interactions; Glucuronidation; Pharmacogenetics; Pharmacokinetics; Statins.

Publication types

  • Practice Guideline

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters / genetics
  • Age Factors
  • Alleles
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacokinetics
  • Area Under Curve
  • Asian People / ethnology
  • Cardiovascular Diseases / drug therapy
  • Cardiovascular Diseases / prevention & control*
  • Cytochrome P-450 Enzyme System / chemistry
  • Cytochrome P-450 Enzyme System / metabolism
  • Drug Interactions
  • Evidence-Based Medicine
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / pharmacokinetics
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / therapeutic use*
  • Liver-Specific Organic Anion Transporter 1
  • Muscular Diseases / etiology
  • Myalgia / etiology
  • Neoplasm Proteins / genetics
  • Nonprescription Drugs / chemistry
  • Nonprescription Drugs / pharmacokinetics
  • Organic Anion Transporters / genetics
  • ROC Curve


  • ABCG2 protein, human
  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters
  • Antiviral Agents
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Liver-Specific Organic Anion Transporter 1
  • Neoplasm Proteins
  • Nonprescription Drugs
  • Organic Anion Transporters
  • SLCO1B1 protein, human
  • Cytochrome P-450 Enzyme System