Table 2.
Pharmacodynamic parameters of the relationship between perindoprilat concentrations and effects on plasma converting enzyme activity in healthy volunteers (HV) and in congestive heart failure (CHF) patients.
| Subject number | CE50 (ng ml−1) | Asymptotic s.d. CE50 (ng ml−1) | γ | ke0 (h−1) | r2 |
|---|---|---|---|---|---|
| HV | |||||
| 1 | 1.91 | 0.25 | 1.00 | NH | 0.7019 |
| 2 | 1.82 | 0.14 | 1.00 | NH | 0.8353 |
| 3 | 2.32 | 0.19 | 1.00 | NH | 0.8492 |
| 4 | 2.28 | 0.28 | 0.80 | NH | 0.7093 |
| 5 | 2.15 | 0.26 | 0.90 | NH | 0.5890 |
| 6 | 0.71 | 0.10 | 0.70 | NH | 0.7887 |
| Mean±s.d. | 1.87 ± 0.60 | 0.90 ± 0.13 | |||
| CHF patients | |||||
| 1 | 0.41 | 0.06 | 0.75 | 0.06 | 0.8800 |
| 2 | 0.86 | 0.08 | 1.50 | 0.05 | 0.8730 |
| 3 | 2.41 | 0.24 | 1.50 | 0.55 | 0.8935 |
| 4 | 0.45 | 0.06 | 0.75 | 0.20 | 0.8723 |
| 5 | 4.16 | 0.32 | 1.00 | 0.06 | 0.7470 |
| 6 | 0.51 | 0.08 | 1.00 | 0.06 | 0.9157 |
| 7 | 0.33 | 0.07 | 1.00 | 0.07 | 0.8550 |
| 8 | 0.73 | 0.13 | 0.50 | 0.08 | 0.8716 |
| 10 | 2.41 | 0.15 | 2.00 | 0.04 | 0.7840 |
| Mean±s.d. | 1.36 ± 1.33 | 1.11 ± 0.47 | 0.13 ± 0.16 | ||
| P value | 0.3424 | 0.2302 | |||
CE50: concentration of perindoprilat which induces an effect of 50% of maximum theoretical effect, γ: Hill coefficient, ke0: first order rate constant which governs the kinetics of the drug in the effect compartment, r2: determination coefficient. NH: no hysteresis. Maximum theoretical effect (Emax) and baseline value of the variable of effect (E0) set to −100% and 0, respectively. The P values correspond to comparisons between HV and CHF patients groups (Student's t-test). In HV: model fitted to the data of the three doses simultaneously.