Related Experiment Video
Updated: Aug 16, 2026

Quantification of the Immunosuppressant Tacrolimus on Dried Blood Spots Using LC-MS/MS
Published on: November 8, 2015
Bilateral pharmacokinetic interaction between cyclosporine A and atorvastatin in renal transplant recipients
A Asberg1, A Hartmann, E Fjeldså
1Medical Department, The National Hospital, Oslo, Norway. anderas@klinmed.uio.no
Insights
This study examined the interaction between atorvastatin and cyclosporine A (CsA) in kidney transplant patients. Atorvastatin increased CsA
Area of Science:
- Pharmacology
- Nephrology
- Immunosuppression
Background:
- Atorvastatin is commonly prescribed for cholesterol management in organ transplant recipients on cyclosporine A (CsA).
- The pharmacokinetic interaction between atorvastatin and CsA in renal transplant recipients remains largely uncharacterized.
Purpose of the Study:
- To investigate the bilateral pharmacokinetic interaction between atorvastatin and CsA in renal transplant recipients.
- To assess the impact of atorvastatin on CsA exposure and lipid levels.
Main Methods:
- A pharmacokinetic study was conducted in 21 renal transplant recipients over 4 weeks.
- Patients received atorvastatin (10 mg/day) alongside their standard CsA and prednisolone immunosuppression.
- Cyclosporine A (CsA) and atorvastatin pharmacokinetics were measured at baseline and after 4 weeks of atorvastatin treatment.
Main Results:
- Atorvastatin treatment led to a sixfold increase in plasma HMG-CoA reductase inhibitory activity in CsA-treated patients.
- Atorvastatin moderately reduced CsA's area under the curve (AUC0-12) by 9.5% and Cmax by 13.5%.
- Total cholesterol and LDL cholesterol significantly decreased by 26.8% and 41.5%, respectively.
Conclusions:
- A significant bilateral pharmacokinetic interaction exists between atorvastatin and CsA in renal transplant recipients.
- While atorvastatin enhances CsA's inhibitory activity, its effect on CsA systemic exposure is moderate.
- Atorvastatin effectively reduces cholesterol levels in this patient population.
Abstract:
Atorvastatin is increasingly used as a cholesterol-lowering agent in solid organ transplant recipients receiving cyclosporine A (CsA). However, the potential bilateral pharmacokinetic interaction between atorvastatin and CsA in renal transplant recipients has not previously been examined. Baseline 12-h CsA pharmacokinetic investigation was performed in 21 renal transplant recipients and repeated after 4 weeks of atorvastatin treatment (10 mg/ d). At week 4, 24-h pharmacokinetics of atorvastatin was also performed. All patients received basiliximab induction followed by CsA and prednisolone immunosuppression. Compared with historic controls, CsA-treated patients showed, on average, sixfold higher plasma HMG-CoA reductase inhibitory activity after 4 weeks of atorvastatin treatment (p < 0.05). Atorvastatin had a moderate effect on the pharmacokinetics of CsA and reduced the AUC0-12 (area under curve, 0-12h) by 9.5 +/- 18% (p = 0.013) and Cmax (maximal concentration) by 13.5 +/- 24% (p =0.009), while C12 (trough level) was unchanged (p =0.42). Total and LDL cholesterol decreased by 26.8 +/- 8.4% (p < 0.0001) and 41.5 +/- 11.0% (p < 0.0001), respectively. Bilateral pharmacokinetic interaction between atorvastatin and CsA resulted in sixfold higher plasma HMG-CoA reductase inhibitory activity, but only a moderate decrease in systemic exposure of CsA.
More Related Videos
Related Concept Videos
Renal Drug Excretion: Tubular Secretion
Factors Affecting Renal Clearance: Drug Distribution and Drug Interactions
One important factor is the relationship between renal clearance and the apparent volume of distribution. Renal clearance tends to be inversely proportional to the apparent volume of distribution. Drugs with an extensive distribution volume or those...
Pharmacokinetics: Drug–Drug Interactions
Pharmacokinetics: Drug–Food and Drug–Viral Interactions
Pharmacokinetics in Geriatric Patients: Effect of Age on Drug Metabolism
Drug Dosing in Renal Diseases: Dose Adjustments Based on Drug Clearance and Elimination Rate Constant

