Table 1: Steady-State Pharmacokinetic Parameters of Gepirone, 3´-OH-Gepirone, and 1-PP in 24 Healthy Subjects on Day 7 of Gepirone Treatment, with or without Concurrent Rifampin 600 mg Daily
|
Without Rifampin |
With Rifampin |
P-Value |
| Gepirone |
| AUC0-24 (ng.hr/mL) |
138 ± 65.7 |
6.7 ± 7.1 |
< .001 |
| Clapp (L/hr) |
332 ± 174 |
13619 ± 14046 |
< .001 |
| t1/2 (hr) |
6.1 ± 3.7 |
12.3 ± 8.5+
|
< .01 |
| Cmax (ng/mL) |
10.6 ± 4.8 |
0.7 ± 0.8 |
< .001 |
| Tmax (hr) |
4.2 ± 1.8 |
4.9 ± 4.7 |
NS |
| 3´-OH-Gepirone |
| AUC0-24 (ng.hr/mL) |
388 ± 125 |
135 ± 55.3 |
< .001 |
| Clapp (L/hr) |
103 ± 33.4 |
307 ± 106 |
< .001 |
| t1/2 (hr) |
10.0 ± 4.7 |
6.2 ± 2.4 |
< .001 |
| Cmax (ng/mL) |
24.2 ± 8.7 |
10.0 ± 3.8 |
< .001 |
| Tmax (hr) |
5.8 ± 2.2 |
4.1 ± 2.0 |
< .01 |
| 1-PP |
| AUC0-24 (ng.hr/mL) |
102 ± 47.4 |
93.3 ± 50.5 |
NS |
| Clapp (L/hr) |
432 ± 191 |
514 ± 274 |
NS |
| t1/2 (hr) |
7.2 ± 3.2 |
7.2 ± 2.8 |
NS |
| Cmax (ng/mL) |
6.8 ± 2.5 |
6.7 ± 2.9 |
NS |
| Tmax (hr) |
4.4 ± 1.7 |
4.0 ± 1.8 |
NS |