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[Pharmacology](https://durgical.com/en/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

## Key points

- They lower LDL most among standard lipid drugs and reduce heart attacks, strokes and cardiovascular deaths.
- High-intensity regimens (atorvastatin or rosuvastatin at high doses) give the largest LDL falls.
- Atorvastatin, simvastatin and lovastatin are CYP3A4 substrates; pravastatin and rosuvastatin depend much less on it.
- Muscle symptoms are the classic adverse effect; rhabdomyolysis is rare but serious and more likely with interacting drugs.
- Not recommended in pregnancy or breastfeeding.

## Drugs in this class

- [**Atorvastatin** A potent statin: it blocks the liver's cholesterol-making enzyme, lowers LDL cholesterol and reduces heart attacks and… HMG-CoA reductase](https://durgical.com/en/pharmacology/atorvastatin/)
- [**Simvastatin** An older, widely used statin swallowed as an inactive lactone that the liver turns into the active drug; prone to… HMG-CoA reductase](https://durgical.com/en/pharmacology/simvastatin/)
- [**Rosuvastatin** A potent, long-acting statin that relies little on CYP3A4. It lowers LDL cholesterol strongly and reduces heart… HMG-CoA reductase](https://durgical.com/en/pharmacology/rosuvastatin/)
- [**Pravastatin** A water-soluble statin that is not metabolized by CYP enzymes, so it has fewer drug interactions. It lowers LDL and… HMG-CoA reductase](https://durgical.com/en/pharmacology/pravastatin/)
- [**Fluvastatin** A lower-potency statin metabolized mainly by CYP2C9 rather than CYP3A4. It lowers LDL moderately. HMG-CoA reductase](https://durgical.com/en/pharmacology/fluvastatin/)
- [**Lovastatin** A statin derived from a fungus. A lactone prodrug metabolized by CYP3A4, so strong CYP3A4 inhibitors are… HMG-CoA reductase](https://durgical.com/en/pharmacology/lovastatin/)

## 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.

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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](https://medlineplus.gov/statins.html) (MedlinePlus (U.S. National Library of Medicine), 2025); [COMPLEX OF THE CATALYTIC PORTION OF HUMAN HMG-COA REDUCTASE WITH ATORVASTATIN](https://www.rcsb.org/structure/1HWK) (RCSB Protein Data Bank, 2001); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=C10AA) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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