An overview on the mechanism of action of statins:

HMG CoA reductase inhibitors,or statins are widely prescribed drugs. They are indicated for the treatment of hipercholesterolemia, a condition that increases cardiovascular risk. Currently, the drugs of this group that are available are:









Mechanism of action. Animation explained

HMG CoA reductase inhibitors competitively inhibit the activity of HMG CoA reductase, the rate-limiting enzyme in cholesterol synthesis. Inhibition of this enzyme results in a transient, modest decrease in cellular cholesterol concentration . The decrease in cholesterol concentration activates a cellular signaling cascade culminating in the activation of sterol regulatory element binding protein (SREBP), a transcription factor that up-regulates expression of the gene encoding the LDL receptor. Increased LDL receptor expression causes increased uptake of plasma LDL, and consequently decreases plasma LDL-cholesterol concentration. Approximately 70% of LDL receptors are expressed by hepatocytes, with the remainder expressed by a variety of cell types in the body.

Clinical uses

Adverse effects and contraindications


[1] Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy, Second Edition
by David E. Golan.
[2] Modern Pharmacology with Clinical Applications, Sixth Edition by Charles Craig.[3] Basic & Clinical Pharmacology, 10th Edition by Bertram G. Katzung.

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