The Sound of Evolution
Rosuvastatin
Mechanism of action:
Rosuvastatin is an HMG-CoA reductase inhibitor. Rosuvastatin binds to HMG-CoA reductase and inhibits the conversion of HMG-CoA into mevalonate, thereby reducing cholesterol synthesis in the liver. This lowers intracellular cholesterol levels in hepatocytes, which subsequently upregulates LDL receptor expression on liver cells and enhances the uptake and breakdown of low-density lipoprotein cholesterol, or LDL-C, from the blood. As a result, plasma LDL-C, total cholesterol, very-low-density lipoprotein, or VLDL, and triglyceride levels decrease, while high-density lipoprotein cholesterol, or HDL-C, may increase slightly.
Reference(s):
1. Di Napoli P et al. (2005). Chronic treatment with rosuvastatin modulates nitric oxide synthase expression and reduces ischemia-reperfusion injury in rat hearts. Cardiovasc Res.
2. Everett BM et al. (2010). Rosuvastatin in the prevention of stroke among men and women with elevated levels of C-reactive protein: justification for the Use of Statins in Prevention: an Intervention Trial Evaluating Rosuvastatin (JUPITER). Circulation.
3. Jones SP et al. (2002). Direct vascular and cardioprotective effects of rosuvastatin, a new HMG-CoA reductase inhibitor. J Am Coll Cardiol.