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HMG CoA reductase inhibitors

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HMG CoA reductase inhibitors (statins) include:

  • simvastatin
  • lovastatin
  • pravastatin
  • cerivastatin - marketing and distribution has been suspended in the UK and in all other countries where gemfibrozil is available because of concerns regarding the risk of rhabdomyolysis when these drugs are co-prescribed (1)
  • fluvastatin
  • atorvastatin
  • rosuvastatin

Actions:

  • inhibition of hydroxymethylglutaryl coenzyme A (HMG CoA) in the liver - the rate limiting step in cholesterol synthesis (approximately 50% of circulating cholesterol is endogenously synthesised, the remainder being derived directly or indirectly from the diet
  • reduction in plasma cholesterol and LDL (statins alter the balance of cholesterol and cholesteryl ester within the hepatocyte and increase the removal of IDL and LDL, and decrease the production of VLDL and LDL)
  • increase in LDL receptors
  • small reduction in plasma triglyceride and VLDL
  • modest increase in HDL (mechanism unknown)

Statins are the most potent drugs available for treating hypercholesterolaemia.

Statins are appropriately prescribed in the evening since the synthesis of cholesterol appears most active overnight (2).

The summary of product characteristics should be consulted before prescribing a particular statin.

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