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Pitavastatin: an overview
Statin metabolism and its implication for side effects and drug–drug interactions: pitavastatin for the treatment of hypercholesterolemia
Michel Farnier
Correspondence to:
Michel Farnier - MD, PhD
Lipid Clinic
Point Medical
Dijon, France
E-mail: michelfarnier@nerim.net
DOI: 10.4147/HTCD-110407

Abstract


Statins, inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, powerfully lower total cholesterol and low-density lipoprotein cholesterol (LDL-C). Stereochemical similarities in the primary mechanisms of action, competitive inhibition of the HMG-CoA reductase active site, and results of early large-scale clinical trials over the last two decades helped to reinforce a widespread concept of the class effects of statins as generally similar agents. Development of ever-more potent second- and third-generation statins have offset this initial uniform statin class-effect concept, perhaps fuelled by cerivastatin’s withdrawal from the market due to an exceptionally high incidence of severe muscle toxicity, especially in combination with gemfibrozil. At the same time, the notion that statins may not differ in terms of safety has also persisted. A comparative review of metabolism and drug–drug-interactions of pitavastatin, the most recent addition to the class, and other statins may help further differentiate different agents, with special reference to safety.

Summary


  • STATIN CLASS-EFFECT PARADIGM
  • Weaknesses revealed
  • PITAVASTATIN METABOLISM
  • CLINICAL RELEVANCE OF DRUG INTERACTIONS WITH LIPID-LOWERING MEDICATIONS
  • Statin interactions mediated by CYP enzymes
  • Role of CYP3A4 inhibitors
  • Role of CYP2C9 and CYP2C8 inhibitors
  • Statin interactions mediated by membrane transporters
  • CONCLUSION
  • REFERENCES


     
Michel Farnier
     
Michel Farnier