Open AccessPharmacokinetics of cyclosporine in pediatric long‐term liver transplant recipients converted from Sandimmun to Neoral
Author(s) -
Melter M.,
Rodeck B.,
Kardorff R.,
Hoyer P.F.,
Brodehl J.
Publication year - 1997
Publication title -
transplant international
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.998
H-Index - 82
eISSN - 1432-2277
pISSN - 0934-0874
DOI - 10.1111/j.1432-2277.1997.tb00718.x
Subject(s) - cmin , medicine , pharmacokinetics , cmax , area under the curve , urology , ciclosporin , therapeutic drug monitoring , trough level , trough concentration , pharmacology , transplantation , tacrolimus
. Absorption of cyclosporin from the microemulsion formulation Neoral is less variable than from Sandimmun. Because of a lack of data in pediatric liver transplant recipients, the pharmacokinetic profiles with Sandimmun and Neoral were compared in a conversion study. Thirty‐eight children with stable graft function were converted 2–12.3 years post‐transplant at a 1:1 ratio. The trough‐level (C min ) with Neoral was 123 ± 39 ng/ml versus 134 ± 29 ng/ml with Sandimmun ( P = NS), the area under the time‐concentration curve (AUC) was 3325 ± 1125 ng * h/ml versus 2423 ± 846 ng * h/ml ( P < 0.001), the peak concentration (C max ) was 650 ± 280 ng/ml versus 337 ± 142 ng/ ml ( P < 0.001), and the median time to C max was 2 h (range 0.5‐3 h) versus 4 h (range 1–8 h; P < 0.05). The weak correlation between C min and AUC with Sandimmun ( r = 0.5; P = NS) was improved by using Neoral (r = 0.7; P < 0.001). The best predictor of AUC was the 2‐h concentration (C 2h ) of Neoral ( r = 0.9; P < 0.001). Increased absorption and a more predictable pharmacokinetic profile with Neoral permit safer therapeutic monitoring in children. The exclusive measurement of Neoral‐C 2h allows one to estimate drug exposure with high precision (>90%).