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October 1, 2001Journal of Cellular and Molecular Medicine907 citationsOpen Access

Statins: mechanism of action and effects

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CSCamelia S. StancuASAnca V. Sima

Key Points

  • To summarize the pharmacological mechanisms of statins, including their inhibition of cholesterol biosynthesis and pleiotropic antiatherosclerotic effects.
  • Narrative review of statin pharmacodynamics focusing on hepatic HMG-CoA reductase inhibition.
  • Evaluation of mevalonate pathway modulation, isoprenoid synthesis, lipid profiles, and cardiovascular outcomes.
  • Statins selectively inhibit hepatic HMG-CoA reductase, suppressing cholesterol biosynthesis and lowering LDL cholesterol in proportion to their antiatherosclerotic benefits.
  • Inhibition of mevalonate metabolism alters isoprenoid generation, mediating pleiotropic effects that significantly reduce coronary event incidence and mortality in both primary and secondary prevention.
  • Independent of lipid lowering, statin activity influences bone formation mechanisms and impedes tumor cell proliferation.

Abstract

The beneficial effects of statins are the result of their capacity to reduce cholesterol biosyntesis, mainly in the liver, where they are selectively distributed, as well as to the modulation of lipid metabolism, derived from their effect of inhibition upon HMG-CoA reductase. Statins have antiatherosclerotic effects, that positively correlate with the percent decrease in LDL cholesterol. In addition, they can exert antiatherosclerotic effects independently of their hypolipidemic action. Because the mevalonate metabolism generates a series of isoprenoids vital for different cellular functions, from cholesterol synthesis to the control of cell growth and differentiation, HMG-CoA reductase inhibition has beneficial pleiotropic effects. Consequently, statins reduce significantly the incidence of coronary events, both in primary and secondary prevention, being the most efficient hypolipidemic compounds that have reduced the rate of mortality in coronary patients. Independent of their hypolipidemic properties, statins interfere with events involved in bone formation and impede tumor cell growth.

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Cite This Study

Stancu et al. (2001) studied this question.

synapsesocial.com/papers/69dba0ddc9a120f055a3c2c3https://doi.org/10.1111/j.1582-4934.2001.tb00172.x
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