rosuvastatin and cyclosporine

Cyclosporine inhibits the hepatic uptake transporters OATP1B1 and OATP1B3, which are responsible for the clearance of rosuvastatin. This inhibition increases rosuvastatin plasma concentrations, significantly raising the risk of dose-dependent skeletal muscle toxicity.

Co-administration can lead to markedly elevated rosuvastatin exposure, increasing the risk of myopathy and rhabdomyolysis, which may manifest as unexplained muscle pain, tenderness, weakness, and dark urine. The risk is greatest with higher rosuvastatin doses and in patients with renal impairment.

Avoid concomitant use where possible. If co-administration is essential, use the lowest effective rosuvastatin dose (not exceeding 5 mg daily) and monitor the patient for muscle symptoms and for creatine kinase elevations at baseline and periodically thereafter. Reassess renal function and consider an alternative statin with less interaction potential.

The interaction is well established in human pharmacokinetic studies and supported by case reports of rhabdomyolysis. Product labels for rosuvastatin specify a dose limit with cyclosporine. The evidence is considered strong, though the precise magnitude of exposure increase varies between studies.