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Life Science Dictionary

Statin

Pharmacology · Medicine

Say it: STAT-in

A statin is a cholesterol-lowering drug that blocks HMG-CoA reductase, the liver enzyme that controls how fast the body makes its own cholesterol.

Also: statins, HMG-CoA reductase inhibitor

Definition

What is a statin?

A statin is a drug that lowers blood cholesterol by inhibiting HMG-CoA reductase, the enzyme that runs the slowest, rate-limiting step of the pathway cells use to make cholesterol. Statins carry names ending in -statin, such as atorvastatin, simvastatin and rosuvastatin. The first ones were found in fungi in the 1970s.

When liver cells make less cholesterol of their own, they respond by placing more LDL receptors on their surface, and these pull low-density lipoprotein, the so-called bad cholesterol, out of the blood. LDL levels fall substantially, triglycerides drop a little and HDL may rise slightly. Lower LDL slows the growth of fatty plaques in artery walls, the process called atherosclerosis, and large trials show that statins prevent many heart attacks and strokes. They are usually taken long term by people with high cholesterol or a high overall cardiovascular risk and by those who already have heart or blood vessel disease.

Most people take statins without trouble. Muscle aches are the best-known complaint, serious muscle breakdown is rare, and a slightly higher chance of developing type 2 diabetes is seen mainly in people already close to it. Some statins are broken down by the liver enzyme CYP3A4, so grapefruit juice and certain other drugs can push their blood levels up. Statins are not used in pregnancy.

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