Cyclosporine (CsA) is considered to be a potential treatment for steroid-resistant nephrotic patients.The purpose of our study was to compare the pharmacokinetics and pharmacodynamics of CsA (microemulsion formulation,Neoral) between preprandial and postprandial dosing regimens in patients with refractory nephrotic syndrome.Twenty seven patients,who received Neoral once in the morning,were enrolled in this study.Neoral was administered to twelve and fifteen patients after (postprandial group) and 30 minutes before breakfast (preprandial group),respectively.Blood CsA concentrations were measured before (C0) and 1,2,3 and 4 hours after administration of CsA (C1-C4).The value of C1 in the preprandial group was higher than that in the postprandial group but the area under the concentration-time curve from 0-4 hours (AUC0-4) was not higher.While the values of C0,C1,C2,C3 and C4 were correlated with those of AUC0-4 in the preprandial group,only the value of C2 was correlated with AUC0-4 in the postprandial group.In the preprandial group,the rate of increase in serum albumin concentrations was significantly higher than in the postprandial group.However,the incidences of nausea and/or vomiting in the preprandial group were higher than those in the postprandial group.
In conclusion,our results suggest that preprandial dosing regimens of CsA are more efficient than postprandial dosing regimens,although gastrointestinal symptoms have to be considered.