Pharmacology of 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors (statins), including rosuvastatin and pitavastatin

J Clin Pharmacol. 2002 Aug;42(8):835-45. doi: 10.1177/009127002401102731.


Coronary heart disease (CHD) is the leading cause of morbidity and mortality in the Western world, with hypercholesterolemia as the major risk factor. The 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors represent the most efficient drugsfor the treatment of hypercholesterolemia. They lower plasma cholesterol due to the inhibition of endogenous cholesterol synthesis in the liverand subsequent increased expression of low-density lipoprotein (LDL) receptors, resulting in an up-regulated catabolic rate for plasma LDL. The beneficial effect of statins on the incidence of CHD was clearly demonstrated in several large-scale clinical trials. Currently, five statins (atorvastatin, fluvastatin, lovastatin, pravastatin, and simvastatin) are available, and two novel compounds (pitavastatin, rosuvastatin) are undergoing clinical investigation. To point out potential mechanisms leading to increased toxicity and to compare the novel statins with the established ones, this article summarizes their pharmacological data since the prevalence of adverse events can be explained at least in part by their pharmacokinetic differences.

Publication types

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

MeSH terms

  • Acyl Coenzyme A / antagonists & inhibitors*
  • Acyl Coenzyme A / metabolism
  • Coronary Disease / drug therapy
  • Enzyme Inhibitors / adverse effects
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • Enzyme Inhibitors / therapeutic use
  • Fluorobenzenes / adverse effects
  • Fluorobenzenes / pharmacokinetics
  • Fluorobenzenes / pharmacology*
  • Fluorobenzenes / therapeutic use
  • Hypolipidemic Agents / adverse effects
  • Hypolipidemic Agents / pharmacokinetics
  • Hypolipidemic Agents / pharmacology
  • Hypolipidemic Agents / therapeutic use
  • Pyrimidines*
  • Quinolines / adverse effects
  • Quinolines / pharmacokinetics
  • Quinolines / pharmacology*
  • Quinolines / therapeutic use
  • Rosuvastatin Calcium
  • Sulfonamides*


  • Acyl Coenzyme A
  • Enzyme Inhibitors
  • Fluorobenzenes
  • Hypolipidemic Agents
  • Pyrimidines
  • Quinolines
  • Sulfonamides
  • 3-hydroxy-3-methylglutaryl-coenzyme A
  • Rosuvastatin Calcium
  • pitavastatin