Table 2.
Mean (± SD) pharmacokinetic and pharmacodynamic parameters throughout the study period
| CsA 15 patients | Tac 25 patients | Sir 14 patients | |
|---|---|---|---|
| 102 total obs | 166 total obs | 56 total obs | |
| mean 6.8/pt | mean 6.65/pt | mean 4/pt | |
| Dose (mg kg−1 day−1) | 2.8 ± 1.1 | 0.071 ± 0.038 | 0.050 ± 0.022 |
| Trough conc. (ng ml−1) | 142 ± 46 | 9.6 ± 3.1 | 13.0 ± 3.9 |
| MMF dose (mg kg−1 day−1) | 23.0 ± 9.1 | 17.4 ± 4.3 | 16.7 ± 6.7 |
| C0 MPAtot (µg ml−1) | 2.3 ± 1.9 | 2.6 ± 2.1 | 3.0 ± 1.9 |
| C2 MPAtot (µg ml−1) | 7.7 ± 4.8 | 5.5 ± 3.0 | 6.2 ± 4.3 |
| C0 fMPA (µg ml−1) | 0.035 ± 0.017 | 0.033 ± 0.028 | 0.036 ± 0.019 |
| C2 fMPA (µg ml−1) | 0.105 ± 0.048* | 0.068 ± 0.054 | 0.072 ± 0.048 |
| MPA AUC0–12 h (µg h ml−1) | 42.0 ± 17.5 | 44.6 ± 19.2 | NA |
| CL/F (l h−1 kg−1) | 0.47 ± 0.30 | 0.33 ± 0.13 | NA |
| t0 IMPDH activity (nmol h−1 mg−1) | 7.8 ± 5.5 | 8.0 ± 5.1 | 7.6 ± 4.8 |
| t2 IMPDH activity (nmol h−1 mg−1) | 5.1 ± 5.6 | 5.7 ± 4.6 | 5.9 ± 3.9 |
| IMPDH inhibition (% of residual activity) | 68.5 ± 33.6 | 77.5 ± 55.0 | 80.9 ± 43.5 |
NA, not applicable;
*
P= 0.001 vs. Tac and P= 0.021 vs. Sir. CsA, ciclosporin; Tac, tacrolimus; Sir, sirolimus; MMF, mycophenolate mofetil; MPA, mycophenolic acid; IMPDH, inosine 5′-monophosphate dehydrogenase.