Pharmacology · Class
Statins !
The main cholesterol-lowering drugs: they slow the liver's cholesterol production, lower LDL and prevent heart attacks and strokes.
Updated 2026-11-01
What they are
Competitive inhibitors of HMG-CoA reductase. They are the base of drug treatment for high LDL cholesterol and atherosclerotic disease.
Mechanism of action
Statins mimic the HMG part of HMG-CoA and occupy the active site of HMG-CoA reductase, the rate-limiting step of the mevalonate pathway. With less cholesterol inside the hepatocyte, SREBP-2 increases the production of LDL receptors, and the liver clears more LDL from blood. They also modestly lower triglycerides and slightly raise HDL.
Target: HMG-CoA reductase
Drugs in this class
- AtorvastatinA potent statin: it blocks the liver's cholesterol-making enzyme, lowers LDL cholesterol and reduces heart attacks and…HMG-CoA reductase
- SimvastatinAn older, widely used statin swallowed as an inactive lactone that the liver turns into the active drug; prone to…HMG-CoA reductase
- RosuvastatinA potent, long-acting statin that relies little on CYP3A4. It lowers LDL cholesterol strongly and reduces heart…HMG-CoA reductase
- PravastatinA water-soluble statin that is not metabolized by CYP enzymes, so it has fewer drug interactions. It lowers LDL and…HMG-CoA reductase
- FluvastatinA lower-potency statin metabolized mainly by CYP2C9 rather than CYP3A4. It lowers LDL moderately.HMG-CoA reductase
- LovastatinA statin derived from a fungus. A lactone prodrug metabolized by CYP3A4, so strong CYP3A4 inhibitors are…HMG-CoA reductase
Others in the class
- rosuvastatin
- pravastatin
- lovastatin
- fluvastatin
- pitavastatin
Test yourself
Think of the answer, then tap the question to see it.
How does blocking cholesterol synthesis lower LDL in the blood?
Lower cholesterol in the hepatocyte activates SREBP-2, which increases LDL receptor expression; the liver then takes up more LDL particles from the blood.
Which statins are least affected by CYP3A4 inhibitors?
Pravastatin and rosuvastatin, which rely little on CYP3A4. Simvastatin, lovastatin and, to a lesser degree, atorvastatin are most affected.
A patient on a statin has muscle pain, weakness and dark urine. What must be ruled out?
Rhabdomyolysis: creatine kinase, kidney function and urine myoglobin are checked, and interacting drugs are reviewed.
What effect on blood glucose has been reported with statins?
Rises in HbA1c and fasting glucose; the risk of developing type 2 diabetes goes up slightly, mainly in people already at high risk.
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Statins: MedlinePlus (MedlinePlus (U.S. National Library of Medicine), 2025); COMPLEX OF THE CATALYTIC PORTION OF HUMAN HMG-COA REDUCTASE WITH ATORVASTATIN (RCSB Protein Data Bank, 2001); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.