Pharmacological interactions of statins

Rodolfo Paoletti, Alberto Corsini, Stefano Bellosta

Research output: Contribution to journalArticlepeer-review

Abstract

The 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) are effective in reducing the risk of coronary events, and are generally very well tolerated. However, simvastatin, lovastatin, cerivastatin and atorvastatin are biotransformed in the liver primarily by cytochrome P450 (CYP) 3A4, and clinical experience has shown that the risk of adverse effect, such as myopathy, increases with concomitant use of statins with drugs that substantially inhibit CYP 3A4 at therapeutic doses. Indeed, pharmacokinetic interactions (e.g. increased bioavailability), myositis, and rhabdomyolysis have been reported following concurrent use of atorvastatin, cerivastatin, simvastatin or lovastatin and cyclosporine A, mibefradil or nefazodone. In contrast, fluvastatin (mainly metabolized by CYP 2C9) and pravastatin (eliminated by other metabolic routes) are less subject to this interaction. Nevertheless, an increase in pravastatin bioavailability has been reported in the presence of cyclosporine A, possibly because of an interaction at the level of biliary excretion. In summary, some statins may have lower adverse drug interaction potential than others, which is an important determinant of safety during long-term therapy.

Original languageEnglish
Pages (from-to)35-40
Number of pages6
JournalAtherosclerosis Supplements
Volume3
Issue number1
DOIs
Publication statusPublished - May 2002

Keywords

  • Cytochrome P450
  • Drug interaction
  • Fibrate
  • HMG-CoA reductase inhibitors
  • Rhabdomyolysis

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine

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