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Pharmacokinetics of oral cyclosporin A in diabetic children and adolescents

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Summary

Cyclosporin A (CsA) pharmacokinetics was studied in 19 diabetic children (mean age: 10.6 y). They were divided into prepubertal (I) and pubertal (II) groups according to plasma oestradiol or testosterone concentrations. The kinetic study was performed after a 72 h wash out period and a single oral dose of 7.5 mg/kg CsA. CsA in blood was measured by HPLC. The kinetic parameters: Cmax, tmax, t1/2, AUC, CL/f, Vz/f and tss were calculated.

No significant difference was found between the two groups. A significant negative correlation was found between Vz and both total cholesterol (r=0.46), VLDL+LDL−cholesterol (r=−0.49) and VLDL+LDL−phospholipids (r=−0.58). CsA kinetics at steady-state were simulated by superimposition of single dose kinetics derived from each single dose. Measured steady-state blood concentrations were correlated (r=0.80) with the values predicted by the simulation. The results suggest that CsA adjustment dosage of the CsA may be performed after a single oral dose using blood levels measured by HPLC. This procedure requires validation in further studies.

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Misteli, C., Rey, E., Pons, G. et al. Pharmacokinetics of oral cyclosporin A in diabetic children and adolescents. Eur J Clin Pharmacol 38, 181–184 (1990). https://doi.org/10.1007/BF00265981

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