General Information

Crestor (rosuvastatin calcium) is a synthetic lipid-lowering agent approved as a treatment for hypercholesterolemia. The drug is classified as a Statin, a type of agent that inhibits cholesterol production in the liver.

Crestor is indicated as an adjunct to diet to reduce elevated cholesterol levels in the blood. It is indicated for primary hypercholesterolemia (heterozygous familial and nonfamilial) and mixed dyslipidemia (Fredrickson Type IIa and IIb).

It is also indicated as an adjunct to diet for the treatment of patients with elevated serum TG levels (Fredrickson Type IV) and in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid-lowering treatments.

The dose range for Crestor is 5 to 40 mg once daily. Therapy should be individualized according to goal of therapy and response.

Clinical Results

FDA approval of Crestor was based a double-blind, placebo-controlled, dose-ranging study and a open-label study of 2,240 subjects with type IIa and IIb hypercholesterolemia. Results demonstrated that Crestor reduced total-C, LDL-C, ApoB, nonHDL-C, and TG, and increases HDL-C, in patients with hypercholesterolemia and mixed dyslipidemia.

Side Effects

Adverse events associated with the use of Crestor may include (but are not limited to) the following:

• 
  
• Pharyngitis
• Headache
• Diarrhea
• Dyspepsia
• Myalgia
• Asthenia
• Back Pain
• Flu syndrome
• Urinary tract infection

Mechanism of Action

Rosuvastatin is an inhibitor of HMG-CoA reductase, an enzyme that catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.

Rosuvastatin reduces cholesterol by increasing the number of low-density lipoprotein (LDL) receptors on the cell-surface to enhance uptake and catabolism of LDL. It also inhibits hepatic synthesis of hepatic very-low-density lipoprotein (VLDL), which reduces the total number of VLDL and LDL particles. The treatment reduces triglycerides (TG) and produces increases in high-density lipoprotein cholesterol (HDL-C.)

Literature References

Davidson MH.. Rosuvastatin: a highly efficacious statin for the treatment of dyslipidaemia. Expert Opin Investig Drugs. 2002 Mar;11(3):125-41. Review.

McTaggart F. Comparative pharmacology of rosuvastatin. Atheroscler Suppl.. 2003 Mar; 4(1): 9-14.

Nezasa K, Higaki K, Takeuchi M, Nakano M, Koike M. Uptake of rosuvastatin by isolated rat hepatocytes: comparison with pravastatin. Xenobiotica. 2003 Apr; 33(4): 379-88.

Stein EA. The power of statins: aggressive lipid lowering. Clin Cardiol. 2003 Apr; 26(4 Suppl 3): III25-31. Review.

Additional Information

For additional information on Hypercholesterolemia or Crestor, please visit The Crestor Home Page