Table 3.
Pharmacokinetic Parameters for Loxapine and Metabolites Across Dose Groups. All subjects receiving loxapine (72 doses in 24 subjects receiving 3 doses each)
| Parameter | Observations | All 3 Doses |
|---|---|---|
| Tmax (min)a | 72 | 2 [2, 120] |
| Cmax (Dose 1) b (ng/mL)c | 24 | 69.3 ± 55.0 |
| Cmax (Dose 2)(ng/mL)c | 24 | 101 ± 78.5 |
| Cmax (Dose 3)(ng/mL)c | 24 | 107 ± 82.6 |
| AUCinf 7‐OH‐loxapine (%)cd | 24 | 15.0 ± 7.7 |
| AUCinf 8‐OH‐loxapine (%)cd | 24 | 103 ± 45.0 |
| AUCinf Amoxapine(%)cd | 24 | 6.1 ± 3.5 |
| Half‐life (h)c | 24 | 7.1 ± 1.9 |
| CL/F (mL/h)c | 24 | 103 ± 51.7 |
| C2 hr – C4 hr (% of Cmax)ce | 9 | 7.6 ± 1.9% |
| Thalf‐max (min) ae | 9 | 6.8 [4.9, 8.4] |
| Thalf‐max ‐ Tmax (min) ae | 9 | 4.8 [2.9, 6.4] |
a = Median [Min, Max]
b = Normalized to 10 mg dose
c = Arithmetic mean ± standard deviation
d = As a percent of the loxapine AUCinf
e = From mean concentration profiles (3 doses in each of the 3 dose groups)