Rosuvastatin: profile and news

Rosuvastatin Helped More Patients Reach Goal in MERCURY II Study  May 15, 2006
WILMINGTON, DE -- May 15, 2006 -- Results from the MERCURY II (Measuring Effective Reductions in Cholesterol Using Rosuvastatin therapY) trial, published ... - DG News

Generic Pravachol Approved  May 10, 2006
...heart disease. Other drugs in this class include atorvastatin (Lipitor), rosuvastatin (Crestor), and simvastatin (Zocor). One other ... - Diabetes Self Management

Reactive oxygen species production by circulating monocytes ...  May 10, 2006
Rosuvastatin in the primary prevention of cardiovascular disease among patients with low levels of low-density lipoprotein cholesterol and elevated high ... - Nature.com (subscription),

Endocrinology & Metabolism News May 2006  May 5, 2006
In patients with known coronary artery disease, two years of high-intensity statin therapy (rosuvastatin 40 mg/d) achieved significant regression of ... - Journal of Clinical Endocrinology and Metabolism,

Statin Alternatives  May 8, 2006
...are approved by the FDA: atorvastatin (Lipitor®), fluvastatin (Lescol®), lovastatin (Mevacor®), pravastatin (Pravachol®), rosuvastatin (Crestor®) and ... - WHOI,

Scientists uncover gene mutation key to cholesterol control  Apr 20, 2006
...cerivastatin); Lescol (fluvastatin); Mevacor (lovastatin); Pravachol (pravastatin); Zocor (simvastatin); and the newest approved drug Crestor (rosuvastatin). ... - DrugResearcher.com,

AstraZeneca's profits leap ahead of sales growth  Apr 27, 2006
Second-rank product Seroquel came to the fore with a 27% increase in turnover to $807 million, while Crestor (rosuvastatin) surged 42% to $387 million. ... - Pharma Times (subscription),

Cyclosporine: When rosuvastatin 10 mg was co-administered with cyclosporine in cardiac transplant patients, rosuvastatin mean c_max and mean AUC were increased 11-fold and 7-fold, respectively, compared with healthy volunteers. These increases are considered to be clinically significant and require special consideration in the dosing of rosuvastatin to patients taking concomitant cyclosporine .

Warfarin: Coadministration of rosuvastatin to patients on stable warfarin therapy resulted in clinically significant rises in INR (>4, baseline 2-3). In patients taking coumarin anticoagulants and rosuvastatin concomitantly, INR should be determined before starting rosuvastatin and frequently enough during early therapy to ensure that no significant alteration of INR occurs. Once a stable INR time has been documented, INR can be monitored at the intervals usually recommended for patients on coumarin anticoagulants. If the dose of rosuvastatin is changed, the same procedure should be repeated. Rosuvastatin therapy has not been associated with bleeding or with changes in INR in patients not taking anticoagulants.

Gemfibrozil: Coadministration of a single rosuvastatin dose to healthy volunteers on gemfibrozil (600 mg twice daily) resulted in 2.2- and 1.9-fold, respectively, increase in mean c_max and mean AUC of rosuvastatin .

Endocrine Function

Although clinical studies have shown that rosuvastatin alone does not reduce basal plasma cortisol concentration or impair adrenal reserve, caution should be exercised if any HMG-CoA reductase inhibitor or other agent used to lower cholesterol levels is administered concomitantly with drugs that may decrease the levels or activity of endogenous steroid hormones such as ketoconazole, spironolactone, and cimetidine.

CNS Toxicity

CNS vascular lesions, characterized by perivascular hemorrhages, edema, and mononuclear cell infiltration of perivascular spaces, have been observed in dogs treated with several other members of this drug class. A chemically similar drug in this class produced dose-dependent optic nerve degeneration (Wallerian degeneration of retinogeniculate fibers) in dogs, at a dose that produced plasma drug levels about 30 times higher than the mean drug level in humans taking the highest recommended dose. Edema, hemorrhage, and partial necrosis in the interstitium of the choroid plexus was observed in a female dog sacrificed moribund at day 24 at 90 mg/kg/day by oral gavage (systemic exposures 100 times the human exposure at 40 mg/day based on AUC comparisons). Corneal opacity was seen in dogs treated for 52 weeks at 6 mg/kg/day by oral gavage (systemic exposures 20 times the human exposure at 40 mg/day based on AUC comparisons). Cataracts were seen in dogs treated for 12 weeks by oral gavage at 30 mg/kg/day (systemic exposures 60 times the human exposure at 40 mg/day based on AUC comparisons). Retinal dysplasia and retinal loss were seen in dogs treated for 4 weeks by oral gavage at 90 mg/kg/day (systemic exposures 100 times the human exposure at 40 mg/day based on AUC). Doses ≤30 mg/kg/day (systemic exposures ≤60 times the human exposure at 40 mg/day based on AUC comparisons) following treatment up to one year, did not reveal retinal findings.