Table 2.
Noncompartmental pharmacokinetic–pharmacodynamic analysis of single dose 24‐h plasma concentration curves
| Subject ID | Dose (mg) | Tlag (h) | Tmax (h) | Cmax (ng ml–1) | AUC (h ng ml–1) | T1/2 (h) | Pre‐treatment PRL (ng ml–1) | Nadir (%PRL) | Time of Nadir (h) | Desensitizationa | %Inhibition/AUCb |
|---|---|---|---|---|---|---|---|---|---|---|---|
| 1A | 0.5 | 2.0 | 8 | 0.7 | 6.5 | 3.8 | 85 | 85 | 5.0 | 1 | 2.3 |
| 1B | 2.0 | 1.5 | 5 | 2.6 | 34 | 5.6 | 109 | 43 | 4.5 | 1 | 1.7 |
| 2 | 1.0 | 0 | 2.5 | 2.1 | 15 | 3.9 | 39 | 61 | 5.5 | 0 | 2.6 |
| 3 | 2.0 | 0.5 | 8 | 3.4 | 52 | 7.6 | 523 | 56 | 5.5 | 1 | 0.9 |
| 4A | 1.0 | 0.5 | 2 | 1.4 | 14 | 6.7 | 107 | 43 | 3.0 | 0 | 4.0 |
| 4B | 2.0 | 0.5 | 1.5 | 2.8 | 25 | 4.8 | 82 | 26 | 4.5 | 0 | 2.9 |
| 5 | 1.0 | 0.5 | 4 | 3.2 | 36 | 7.9 | 264 | 58 | 2.5 | 1 | 1.2 |
| Mean ± SD | N/a | 0.8 ± 0.7 | 4.4 ± 2.7 | N/a | N/a | 5.8 ± 1.7 | 173 ± 170 | N/a | 4.4 ± 1.2 | N/a | 2.2 ± 1.0 |
a
The subject will be marked as desensitization = 1, if its time of nadir < Tmax. Otherwise, desensitization = 0.
b
%Inhibition/AUC is calculated as (100 – nadir)/AUC
PKPD data are reported for each study visit (n = 7) and mean ± standard deviation is reported when applicable. N/a indicates not applicable
AUC, area under the serum concentration time curve; Cmax, maximum drug concentration; Tlag, lag time for absorption; Tmax, time at maximum drug concentration; T1/2, terminal half‐life