Decreased ubiquinone availability and impaired mitochondrial cytochrome oxidase activity associated with statin treatment

Toxicol Mech Methods. 2009 Jan;19(1):44-50. doi: 10.1080/15376510802305047.

Abstract

In order to investigate the potential involvement of mitochondrial electron transport chain (ETC) dysfunction in myotoxicity associated with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor (statin) treatment, assessment was made of ETC activity and ubiquinone status in two patients experiencing myopathy following treatment with simvastatin (40 mg/day) and cyclosporin (patient 1) and simvastatin (40 mg/day) and itraconazole (patient 2). Analysis of skeletal muscle biopsies revealed a decreased ubiquinone status (77 and 132; reference range: 140-580 pmol/mg) and cytochrome oxidase (complex IV) activity (0.006 and 0.007 reference range: 0.014-0.034). To assess statin treatment in the absence of possible pharmacological interference from cyclosporin or itraconazole, primary astrocytes were cultured with lovastatin (100 microM). Lovastatin treatment resulted in a decrease in ubiquinone (97.9 +/- 14.9; control: 202.9 +/- 18.4 pmol/mg; p < 0.05), and complex IV activity (0.008 +/- 0.001; control: 0.011 +/- 0.001; p < 0.05) relative to control. These data, coupled with the patient findings, indicate a possible association between statin treatment, decreased ubiquinone status, and loss of complex IV activity.

Publication types

  • Case Reports
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Animals
  • Astrocytes / drug effects
  • Astrocytes / enzymology
  • Astrocytes / metabolism
  • Cells, Cultured
  • Cyclosporine / administration & dosage
  • Cyclosporine / pharmacology
  • Cyclosporine / therapeutic use
  • Drug Interactions
  • Drug Therapy, Combination
  • Electron Transport Complex IV / metabolism*
  • Female
  • Humans
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / administration & dosage
  • Hydroxymethylglutaryl-CoA Reductase Inhibitors / adverse effects*
  • Itraconazole / administration & dosage
  • Itraconazole / pharmacology
  • Itraconazole / therapeutic use
  • Male
  • Middle Aged
  • Muscle, Skeletal / drug effects*
  • Muscle, Skeletal / enzymology
  • Muscle, Skeletal / metabolism
  • Muscle, Skeletal / pathology
  • Muscular Diseases / chemically induced*
  • Muscular Diseases / enzymology
  • Muscular Diseases / metabolism
  • Muscular Diseases / pathology
  • Rats
  • Rhabdomyolysis / chemically induced
  • Rhabdomyolysis / enzymology
  • Rhabdomyolysis / metabolism
  • Rhabdomyolysis / pathology
  • Simvastatin / administration & dosage
  • Simvastatin / adverse effects*
  • Ubiquinone / metabolism*

Substances

  • Hydroxymethylglutaryl-CoA Reductase Inhibitors
  • Ubiquinone
  • Itraconazole
  • Cyclosporine
  • Simvastatin
  • Electron Transport Complex IV