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Effects of cyclosporin A and itraconazole on the pharmacokinetics of atorvastatin in rats

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Aim: To evaluate the effects of cyclosporin A and itraconazole, which were used as inhibitors of P-glycoprotein (P-gp) and/or cytochrome P450 (CYP) 3A4 on the pharmacokinetics of atorvastatin in rats. Methods: The pharmacokinetic parameters of atorvastatin were measured after intravenous (2 mg/kg) and intra-gastric (10 mg/kg) administration of atorvastatin in rats, which were pretreated with cyclosporin A (5, 10, and 20 mg/kg) or itraconazole (5, 10, and 20 mg/kg). Results: Compared with the control rats, cyclosporin A and itraconazole altered the pharmacokinetics of atorvastatin significantly. The AUC0-t values of atorvastatin after intragastric administration, pretreated with cyclosporin A (5–20 mg/kg), increased by 32.3%, 61.8%, and 187.2%, respectively, but the CLbile values decreased (P<0.01, 5–20 mg/kg). With pretreatment of itraconazole (5–20 mg/kg), the AUC0-t values of atorvastatin increased by 88.2%, 102%, and 123%, respectively, but the CLbile values decreased (P<0.01, 5–20 mg/kg). Conclusion: These data indicated that cyclosporin A could be effective in inhibiting the efflux of atorvastatin, and itraconazole could be effective in inhibiting both the metabolism and biliary excretion of atorvastatin.

Keywords: P-glycoprotein; atorvastatin; cyclosporin A; cytochrome P450 (CYP) 3A4; itraconazole; pharamcokinetics

Document Type: Research Article


Affiliations: Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, China

Publication date: 2008-10-01

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