Rhea Rosuvastatin Drug Interactions

Effect of co-administered medicinal products on rosuvastatin: In vitro and in vivo data indicate that rosuvastatin has no clinically significant cytochrome P450 interactions (as a substrate, inhibitor or inducer). Rosuvastatin is a substrate for certain transporter proteins including the hepatic uptake transporter OATP1B1 and efflux transporter BCRP. Concomitant administration of Rosuvastatin with medicinal products that are inhibitors of these transporter proteins may result in increased rosuvastatin plasma concentrations and an increased risk of myopathy (see Table 7, and Dosage & Administration and Precautions).

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Interactions requiring rosuvastatin dose adjustments (see also Table 7): When it is necessary to co-administer Rosuvastatin with other medicinal products known to increase exposure to rosuvastatin, doses of Rosuvastatin should be adjusted. It is recommended that prescribers consult the relevant product information when considering administration of such products together with Rosuvastatin. Start with a 5 mg once daily dose of Rosuvastatin if the expected increase in exposure (AUC) is approximately 2‑fold or higher. The maximum daily dose of Rosuvastatin should be adjusted so that the expected rosuvastatin exposure would not likely exceed that of a 40 mg daily dose of Rosuvastatin taken without interacting medicinal products, for example a 5 mg dose of Rosuvastatin with ciclosporin (7.1-fold increase in exposure), a 10 mg dose of Rosuvastatin with ritonavir/atazanavir combination (3.1-fold increase) and a 20 mg dose of Rosuvastatin with gemfibrozil (1.9-fold increase).
Other interacting medicinal products: Antacid: The simultaneous dosing of Rosuvastatin with an antacid suspension containing aluminium and magnesium hydroxide resulted in a decrease in rosuvastatin plasma concentration of approximately 50%. This effect was mitigated when the antacid was dosed 2 hours after Rosuvastatin. The clinical relevance of this interaction has not been studied.
Fusidic Acid: Interaction studies with rosuvastatin and fusidic acid have not been conducted. As with other statins, muscle related events, including rhabdomyolysis, have been reported in post-marketing experience with rosuvastatin and fusidic acid given concurrently. Patients should be closely monitored and temporary suspension of rosuvastatin treatment may be appropriate.
Effect of rosuvastatin on co-administered medicinal products: Warfarin: The pharmacokinetics of warfarin are not significantly affected following co-administration with Rosuvastatin. However, as with other HMG-CoA reductase inhibitors, co-administration of Rosuvastatin and warfarin may result in a rise in INR compared to warfarin alone. In patients taking vitamin K antagonists monitoring of INR is recommended both at initiation or cessation of therapy with Rosuvastatin or following dose adjustment.
Fenofibrates/fibric acid derivatives: Although no pharmacokinetic interaction between rosuvastatin and fenofibrate was observed; a pharmacodynamic interaction may occur. Gemfibrozil, fenofibrate and other fibric acids, including nicotinic acid, may increase the risk of myopathy when given concomitantly with HMG-CoA reductase inhibitors (see Precautions).
Ciclosporin: Co-administration of Rosuvastatin with ciclosporin resulted in no significant changes in ciclosporin plasma concentration.
Other medications: There were no clinically significant interactions with an oral contraceptive, digoxin, ezetimibe or fenofibrate.
In clinical studies Rosuvastatin was co-administered with antihypertensive agents, antidiabetic agents and hormone replacement therapy. These studies did not produce any evidence of clinically significant adverse interactions.