Efficacy and safety of rosuvastatin in treatment of dyslipidemia.
OBJECTIVE
The chemistry, pharmacology, pharmacokinetics, drug interactions, clinical efficacy, adverse effects, dosage and administration, and place in therapy of rosuvastatin are reviewed.


CONCLUSIONS
Rosuvastatin, the latest statin to receive approved labeling by the Food and Drug Administration, has shown superior efficacy in lowering low-density-lipoprotein (LDL) cholesterol. At daily doses of 5-40 mg, rosuvastatin produces mean reductions in plasma LDL cholesterol of 45-63%, statistically greater than those achieved with equivalent doses of atorvastatin, simvastatin, and pravastatin. Rosuvastatin also improves triglyceride, non-high-density lipoprotein (HDL)-cholesterol, and HDL cholesterol levels to produce a more favorable lipid profile. Rosuvastatin's safety was studied in more than 10,000 patients, exceeding the number of patients evaluated before the launch of any other statin. Many of these patients took the drug for up to 96 weeks. With regard to muscle, renal, and hepatic toxicity and the withdrawal rate due to adverse events, rosuvastatin demonstrates a safety profile similar to that of the other marketed statins. Rosuvastatin undergoes only minor metabolism (10% of the administered dose) by the cytochrome P-450 2C9 isoenzyme. Significant drug interactions were reported with cyclosporine, gemfibrozil, warfarin, and antacids. Evidence suggests that rosuvastatin will be a valuable addition to the choices for treatment of patients with dyslipidemia.


CONCLUSIONS
Rosuvastatin has greater efficacy in lowering LDL cholesterol and non-HDL-cholesterol concentrations than the other statins. It has been shown to enable more patients to reach their LDL cholesterol goals than other statins and to do so with an acceptable safety profile.
McKenney
James M
JM
School of Pharmacy, Medical College of Virginia, Virginia Commonwealth University, Richmond, USA. jmckenney@ncrinc.net
D008076:Cholesterol, HDL / Q000097:blood; D008078:Cholesterol, LDL / Q000097:blood; D003404:Creatinine / Q000097:blood; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D005464:Fluorobenzenes / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D005919:Glomerular Filtration Rate; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006949:Hyperlipidemias / Q000097:blood / Q000188:drug therapy*; D011507:Proteinuria; D011743:Pyrimidines / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D000068718:Rosuvastatin Calcium; D013449:Sulfonamides / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D016896:Treatment Outcome; D014481:United States
D008076:Cholesterol, HDL; D008078:Cholesterol, LDL; D005464:Fluorobenzenes; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011743:Pyrimidines; D013449:Sulfonamides; D000068718:Rosuvastatin Calcium; D003404:Creatinine