TABLE 3.
Demographic and medication data for subjects included in population PK analysis. Data are expressed as mean values ± standard deviation (ranges)
| PICME I: Healthy volunteer | PICME II: Autoinduction group | PICME II: Maintenance group | |
|---|---|---|---|
| Numbers of subjects | 8 | 3 | 69 |
| Sets of drug/metabolite assays | 96 | 75 | 77 |
| Gender (%): | |||
| Male | 8 (100%) | 1 (33.3%) | 37 (53.6%) |
| Female | 0 | 2 (66.6%) | 32 (46.4%) |
| Age (y) | 27.4 ± 3.5 (21.7–32.8) | 46.7 ± 4.4 (43.5–51.7) | 47 ± 14.3 (25.9–75.8) |
| Total body weight (kg) | 84.6 ± 11.2 (69.8–99.4) | 95.2 ± 26.4 (73.1–124.5) | 79.7 ± 18.8 (39.0–140.5) |
| Smoker (%): | |||
| Yes | 0 (0%) | 0 (0%) | 20 (29.0%) |
| No | 8 (100%) | 3 (100%) | 49 (71.0%) |
| Sparse PK sampling time points (minutes) | NA | NA | 337.5 ± 230.9 (70–1030) |
| CBZ dose (mg/d) | 400‐mg single dose | 200 mg once daily (days 1–14) | 819 mg ± 367 (range: 200–1600 mg) |
| 200 mg twice daily (days 15–28) | |||
| 200 mg AM and 400 mg PM (days 29–42) | |||
| CBZ therapy without concomitant AEDs or CYP3A4 inducer/inhibitor (%) | 8 (100%) | 2 (66.6%) | 16 (23.2%) |
| Concomitant with 1 AED (%) | 0 | 0 | 26 (37.7%) |
| Concomitant with 2 AEDs (%) | 0 | 0 | 16 (23.2%) |
| Concomitant with 3 AEDs (%) | 0 | 0 | 5 (7.2%) |
| Concomitant with 1 CYP3A4 inducer/inhibitor (%) | 0 | 1 (33.3%) | 12 (17.4%) |
| Concomitant with 2 CYP3A4 inducer/inhibitors (%) | 0 | 0 | 3 (4.3%) |
| Number of subjects for each AED: | |||
| Levetiracetam | 0 | 0 | 26 |
| Clobazam | 0 | 0 | 18 |
| Lamotrigine | 0 | 0 | 5 |
| Zonisamide | 0 | 0 | 5 |
| Phenytoin | 0 | 0 | 4 |
| Topirmate | 0 | 0 | 4 |
| Pregabalin | 0 | 0 | 4 |
| Valproate | 0 | 0 | 3 |
| Lacosamide | 0 | 0 | 3 |
| Perampanel | 0 | 0 | 1 |
| Phenobarbital | 0 | 0 | 1 |
| Number of subjects for each CYP3A4 | |||
| Inducer/inhibitor: | |||
| Statin | 0 | 1 | 12 |
| Omeprazole | 0 | 0 | 6 |
*
time points applicable only to sparse PK sampling group; AED: antiepileptic drug; CBZ: carbamazepine, PK: pharmacokinetic.