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Statins are a class of pharmacological agents that are competitive inhibitors of HMG-CoA reductase, which is the rate-limiting enzyme in cholesterol biosynthesis. They are most effective in reducing LDL, though it has become standard practice to initiate reductase inhibitor therapy immediately after a myocardial infarction, irrespective of lipid levels.

Because of a marked first pass effect, the major effect of statins is on the liver, which compensates by increasing LDL receptors and decreasing VLDL production. The net effect is a decrease of 15-60% in LDL cholesterol, and an increase of 8-10% in HDL cholesterol, as well as a decrease of 10-40% in triglycerides.

Reductase inhibitors (statins) are useful alone or with resins, niacin, or ezetimibe in reducing levels of LDL. Pregnancy is a contraindication, as is lactation.

Side effects are rare, but include gastrointestinal tract upset, liver enzyme elevations, myopathy, or rhabdomyolysis. They may also interact with fibrates, niacin, cyclosporin or erythromycin.