Table 1.
Parametera | Adults 125 mg single-dose (n = 26)43,44 | Adults 250 mg single-dose (n = 29)45,46 | Adults 125 mg steady-state (n = 10)43 | Adults 250 mg steady-state (n = 22)46,47 | Children 125 mg single-dose (n = 28)43,44 | Children 125 mg steady-state (n = 16)43 |
---|---|---|---|---|---|---|
Tmax (h) | 1.3–1.5 | 1.4–1.5 | 1.6 | 1.2 | 1.7–2.1 | 1.8 |
Cmax (ng/mL) | 506–565 | 1340–1656 | 646 | 1700b | 706–909 | 1059 |
AUC (h*ng/mL) | 1624–2135 | 4740–6762 | 3720 | 10481 | 2967–4104 | 5851 |
Cl/F (L/h/kg) | 1.2 | 0.55 | 0.4 | 1.9 | 1.7 | |
Vss/F (L/kg) | 19.2 | 19.5 | ||||
t1/2α (h) | 0.7 | 0.35 | 1.2 | |||
t1/2β (h) | 26.7 | 12.6–14.2 | 14.7 | |||
t1/2γ (h) | 396 | 156 |
Notes: Values represent the mean reported values from the referenced studies (when more than one study is referenced, values represent the range of reported mean values).
Corresponding peak tissue concentrations: hair, 2.4 μg/g; stratum corneum, 14.4 μg/g; sebum, 56.1 μg/g.
Abbreviations: Tmax, time at maximum plasma concentration; Cmax, maximum plasma concentration; AUC, area under the plasma concentration vs time curve; Cl/F, apparent oral clearance; Vss/F, steady-state volume of distribution; t1/2α, alpha-phase half-life; t1/2β, beta-phase half-life, t1/2γ, gamma-phase or terminal half-life.