TABLE 2.
Dose (mg [no. of subjects]) | AUC (mg · h/liter) | AUCnorm (kg · h/liter) | Cmax (mg/liter) | Cmax,norm (kg/liter) | Tmax (h)b |
---|---|---|---|---|---|
50 (6) | 3.88/1.13 (3.30–4.42) | 6.53/1.18 (5.34–8.10) | 0.29/1.25 (0.22–0.42) | 0.48/1.30 (0.35–0.78) | 1.75 (0.50–4.00) |
100 (6) | 8.51/1.21 (8.06–11.3) | 6.18/1.18 (5.08–7.80) | 0.59/1.21 (0.46–0.79) | 0.43/1.23 (0.31–0.54) | 2.00 (1.00–4.00) |
200 (6) | 15.4/1.20 (12.1–20.8) | 6.13/1.13 (5.44–7.57) | 1.16/1.35 (0.72–1.54) | 0.46/1.27 (0.32–0.57) | 2.50 (1.00–3.00) |
400 (7) | 26.9/1.18 (20.7–33.2) | 5.33/1.18 (4.14–6.39) | 2.50/1.31 (1.62–3.64) | 0.50/1.25 (0.32–0.65) | 1.50 (0.50–2.57) |
600 (7) | 39.9/1.11 (34.1–45.6) | 5.45/1.24 (3.75–6.72) | 3.19/1.19 (2.41–3.99) | 0.44/1.29 (0.31–0.63) | 2.50 (0.50–3.00) |
800 (7) | 59.9/1.24 (42.2–78.1) | 6.39/1.22 (4.64–7.76) | 4.73/1.16 (3.98–5.61) | 0.51/1.16 (0.44–0.68) | 3.00 (2.00–4.00) |
Mean residence time (h) | t1/2 (h) | V/F (liters/kg)c | CL/F (liters/h) | CLR (liters/h)d | Aeur (%) |
---|---|---|---|---|---|
16.2/1.17 (12.5–19.9) | 11.4/1.11 (9.3–12.4) | 2.52/1.15 (2.17–3.22) | 12.9/1.13 (11.3–15.2) | 2.77/1.22 (0.06–3.38) | 20.4/1.15 (17.2–23.7) |
17.8/1.13 (15.7–22.2) | 12.2/1.11 (11.0–14.6) | 2.85/1.13 (2.32–3.11) | 11.8/1.21 (8.9–15.3) | 2.38/1.25 (1.72–3.26) | 18.9/1.34 (10.7–24.6) |
17.0/1.11 (14.8–19.9) | 14.0/1.14 (12.2–16.7) | 3.30/1.14 (2.77–3.87) | 13.0/1.20 (9.6–16.6) | 2.64/1.25 (2.01–3.52) | 19.8/1.16 (16.3–24.0) |
14.9/1.14 (11.8–17.9) | 13.1/1.06 (12.2–14.6) | 3.55/1.23 (2.76–5.10) | 14.9/1.18 (12.1–19.3) | 3.03/1.17 (2.45–3.75) | 20.1/1.20 (15.7–24.7) |
14.6/1.18 (12.0–19.0) | 12.5/1.14 (10.3–15.0) | 3.30/1.12 (2.90–3.95) | 15.0/1.11 (13.2–17.6) | 2.67/1.10 (2.35–3.08) | 17.5/1.16 (14.4–21.8) |
14.7/1.13 (12.0–17.3) | 12.3/1.13 (9.3–14.3) | 2.77/1.19 (2.23–3.41) | 13.4/1.24 (10.3–19.0) | 2.50/1.28 (1.98–4.14) | 18.7/1.25 (13.3–24.7) |
Values are geometric mean/SD (range) unless indicated otherwise.
Values are median (range).
V/F, volume of distribution during the terminal phase.
CLR, renal clearance.