Cyclosporin pharmacokinetics following administration of capsules and Neoral in paediatric patients with lupus nephritis

Abstract

Aims: Neoral is a new microemulsion form of cyclosporin. Pharmacokinetic reports in children are scarce. Therefore, we performed a pharmacokinetic study between Cyclosporin A (CsA) capsules and Neoral in paediatric patients with lupus nephritis.

Methods: A single 5 mg kg(-1) dose orally of either CsA capsules or Neoral was given to 10 paediatric patients (serum creatinine < 1.5 mg dl(-1)). CsA whole blood levels were measured for 24 h post-dose by h.p.l.c.

Results: Neoral had a higher C(max) and AUC(C(max): 943 +/- 176 ng ml(-1); AUC: 4612 +/- 785 ng ml(-1) h) than those of the CsA capsules (C(max): 697 +/- 187 ng ml(-1); AUC: 3483 +/- 873 ng ml(-1) h; P < 0.05). There was no difference in t(max) and t(1/2,z) between the two groups.

Conclusions: CsA Neoral had improved absorption and bioavailability, which is similar to what is reported in adults. However, interpatient variability still existed. Careful drug monitoring and dose adjustment should be performed during treatment to avoid nephrotoxicity, especially in lupus nephritis.