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CRESTOR® (rosuvastatin calcium)



 

Pharmacokinetics

In normal volunteers and in vitro — not metabolized by CYP450 3A4 to a clinically significant extent.1

CRESTOR Pharmacokinetics Chart 1 2 3 4 5

 

 

CRESTOR® (rosuvastatin calcium) has no clinically significant drug interaction with1

  • Erythromycin
  • Azole antifungals
  • Fenofibrate
  • Digoxin

The risk of myopathy during treatment with CRESTOR may be increased with concurrent administration of some lipid-lowering therapies (fibrates or niacin), gemfibrozil, cyclosporine, or lopinavir/ritonavir. The benefit of further alterations in lipid levels by the combined use of CRESTOR with fibrates should be carefully weighed against the potential risks of this combination. Gemfibrozil significantly increased rosuvastatin exposure. Therefore, combination therapy with CRESTOR and gemfibrozil should be avoided. If used, do not exceed CRESTOR 10 mg once daily.1

Caution should be exercised when anticoagulants are given in conjunction with CRESTOR because of the potentiation of coumarin-type anticoagulants in prolonging the prothrombin time/INR. In patients taking coumarin anticoagulants and CRESTOR concomitantly, INR should be determined before starting CRESTOR and frequently enough during early therapy to ensure that no significant alteration of INR occurs.1

Pharmacokinetic studies have demonstrated an approximate 2-fold increase in median exposure in Asian subjects compared to Caucasian controls. CRESTOR dosage should be adjusted in Asian patients.1

Learn more about the efficacy of CRESTOR based on clinical trial data by reviewing our clinical experience.

Defined as covered without prior authorization on commercial, Medicare Part D, and Medicaid formularies. Patients without prior authorization means covered lives at Tiers 1 to 7 calculated by Fingertip Formulary as of June 2009 that do not require additional information to the health plan in order for CRESTOR to be covered. Data include covered lives whose prescriptions may be subject to step-therapy requirements.6