HMG-CoA-reductase-inhibitors

Erik Berg Schmidt, Mogens Lytken Larsen

Department of Preventive Cardiology, Aalborg Hospital, Denmark; Department of Cardiology, Aarhus University Hospital, Aarhus, Denmark

ebs@dadlnet.dk, mogenslytkenlarsen@dadlnet.dk

Synonyms

Statins

Definition

A class of important pharmacological compounds that are the most effective drugs for lowering plasma levels of total cholesterol and in particular low-density-lipoprotein (LDL)-cholesterol.

Mechanism of Action

HMG-CoA-reductase-inhibitors (statins) inhibit the enzyme HMG-CoA-reductase that catalyzes the conversion of acetyl coenzyme A to mevalonate, which through several further biochemical steps is metabolized to cholesterol (Fig. 1). HMG-CoA-reductase is the rate-limiting enzyme for the endogenous formation of cholesterol in the human body, which takes place primarily in the liver. The reduced production of cholesterol leads to an increased formation (upregulation) of so-called LDL-receptorson the surface of hepatic cells that remove...