Pitavastatin is a substrate of organic anion transport polypeptide (OATP) 1B1 (OATP2). Drugs that inhibit OATP1B1 (e.g., cyclosporine, erythromycin, rifampin) can increase bioavailability of pitavastatin.
Cyclosporine substantially increases pitavastatin exposure; such effects were considered clinically important. Concomitant use of pitavastatin with cyclosporine is contraindicated.
Concomitant use of pitavastatin and digoxin decreased pitavastatin peak plasma concentration, increased pitavastatin area under the curve (AUC) and decreased digoxin peak plasma concentration and AUC.
Concomitant use of pitavastatin and extended-release diltiazem hydrochloride increased pitavastatin peak plasma concentration and AUC and decreased diltiazem peak plasma concentration and AUC.
Erythromycin substantially increases pitavastatin exposure; such effects were considered clinically important. If used concomitantly with erythromycin, dosage of pitavastatin should not exceed 1 mg once daily.
Concomitant use of statins and gemfibrozil increases the risk of myopathy or rhabdomyolysis. Concomitant use of pitavastatin and gemfibrozil should be avoided. Caution is advised when pitavastatin is used concomitantly with other fibric acid derivatives (e.g., fenofibrate).
Concomitant use of pitavastatin and grapefruit juice decreased pitavastatin peak plasma concentration and increased pitavastatin AUC.
Concomitant use of pitavastatin and HIV protease inhibitors such as atazanavir, ritonavir-boosted darunavir, and lopinavir/ritonavir may disturb peak plasma concentration and AUC of pitavastatin and HIV protease inhibitors. Dosage adjustment are not necessary when pitavastatin is used concomitantly with HIV protease inhibitors.
Concomitant use of pitavastatin and itraconazole decreased pitavastatin peak plasma concentration and AUC.
Concomitant use of pitavastatin and antilipemic dosages (1 g daily or higher) of niacin increased the risk of myopathy. If used concomitantly with antilipemic dosage of niacin, caution is advised, and reduction in pitavastatin dosage should be considered.
Rifampin substantially increases pitavastatin exposure. If used concomitantly with rifampin, dosage of pitavastatin should not exceed 2 mg once daily.
Pitavastatin had no clinically important pharmacokinetic interaction with warfarin. In addition, pitavastatin had no clinically important effect on prothrombin time (PT) and international normalized ratio (INR) in patients receiving long-term warfarin therapy.
However, PT and INR should be monitored when pitavastatin is initiated in patients receiving warfarin.
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