Table 3.
Reference | n | Regimen | Cmax (mg/L) | Tmax (h) | t 1/2 (h) | CL/F (L/h) | CLR (L/h) | Fe (%) |
---|---|---|---|---|---|---|---|---|
(1) | 11 | 400 mg PO × 1 | 2.53 ± 1.31 | 1.0a | 14.6 ± 1.18 | 13.7 ± 1.16 | 3.17 ± 1.12 | 23.2 ± 2.7 |
(2) | 12 | 400 mg PO qd | ||||||
dose 1 | 3.10 ± 0.60b | 1.67 ± 0.96 | 10.6a,b | 11.6 ± 2.1 | ——— | ——— | ||
dose 7 | 3.98 ± 1.10b | 1.59 ± 0.79 | 14.9a,b | 10.4 ± 2.0 | ——— | ——— | ||
(3) | 12 | 400 mg PO × 1 | 2.50 ± 1.29 | 2 .0a | 15.6 ± 1.15 | 11.6 ± 1.21 | 2.58 ± 1.25 | 19.3 ± 2.8 |
(4) | 8 | 400 mg PO × 1 | 4.38 ± 1.4 | 0.77a | 14.9 ± 1.5 | 9.2 ± 1.4 | 2.3 ± 1.3 | 24.2 ± 1.4 |
(5) | 16 | 400 mg PO × 1 | 2.8 (31.7%)c | 1.0a | 11.5 (12.8%)c | ——— | ——— | ——— |
(6) | 8d | 200 mg PO × 1 | 1.31 | 1.28 | 13.16 | 10.61 | 2.25 | 19.63 |
8e | 1.55 | 0.97 | 12.42 | 10.38b | 1.84 | 16.60 | ||
8f | 1.92 | 1.50 | 11.47 | 8.05b | 1.74 | 20.55 | ||
(7) | 8 | 100 mg PO bid × 5 days | ||||||
day 1 | 0.63 ± 1.47 | 2.0a | 9.39 ± 1.08 | 13.1 ± 1.25 | 2.54 ± 1.28 | 15.8 ± 1.21 | ||
day 5 | 0.90 ± 1.28 | 1.5a | 13.7 ± 1.20 | 13.8 ± 1.22 | 3.32 ± 1.31 | 24.0 ± 1.24 | ||
8 | 200 mg PO bid × 5 days | |||||||
day 1 | 1.16 ± 1.96 | 1.5a | 10.4 ± 1.26 | 14.0 ± 1.33 | 3.24 ± 1.36 | 18.2 ± 1.24 | ||
day 5 | 1.96 ± 1.23 | 1.3a | 15.0 ± 1.18 | 13.1 ± 1.26 | 3.08 ± 1.29 | 23.5 ± 1.34 | ||
7 | 400 mg PO qd × 5 days | |||||||
day 1 | 3.10 ± 1.34 | 0.5a | 9.6 ± 1.12 | 12.9 ± 1.12 | 2.33 ± 1.27 | 14.7 ± 1.25 | ||
day 5 | 3.24 ± 1.19 | 1.5a | 15.1 ± 1.05 | 11.8 ± 1.22 | 2.51 ± 1.14 | 21.3 ± 1.19 | ||
7 | 600 mg PO qd × 10 days | |||||||
day 1 | 4.21 ± 1.18 | 1.0a | 9.11 ± 1.16 | 11.9 ± 1.26 | 3.30 ± 1.62 | 23.0 ± 1.46 | ||
day 10 | 5.67 ± 1.19 | 1.5a | 13.7 ± 1.06 | 10.0 ± 1.23 | 2.41 ± 1.15 | 24.2 ± 1.18 | ||
(8) | 12 | 400mg PO × 1 | 4.34 ± 1.61 | 1.02 ± 0.72 | 9.15 ± 1.62 | ——— | 30.5 ± 6.18g | 19.9 ± 4.55 |
(9) | 7 | 400 mg PO × 1 | 4.98 ± 1.01 | 1.0 ± 0.91 | 8.32 ± 1.70 | 147.8h | 22.3h | 15.10 ± 3.61 |
400 mg IV × 1 | 5.09 ± 1.11 | ——— | 8.17 ± 1.58 | 151.5h | 23.0h | 15.2 ± 3.40 | ||
(10) | 10 | 100 mg PO × 1 | 1.15 | 0.86 | 13.5 | ——— | ——— | 24.4 |
100 mg IV × 1 | 1.34 | ——— | 12.7 | ——— | ——— | 25.3 | ||
(11) | 7i | 400 mg PO qd | ||||||
3j | × 10 days | |||||||
day 1 | 3.36 (21.5%)c | 1.49 (62.2%)c | 9.30 (12.1%)c | ——— | ——— | ——— | ||
day 10 | 4.52 (12.2%)c | 1.24 (48.0%)c | 11.95 (10.8%)c | ——— | ——— | ——— | ||
400 mg PO × 1 | 2.53 ± 1.31 | 1.0a | 14.6 ± 1.18 | 13.7 ± 1.16 | 3.17 ± 1.12 | 23.2 ± 2.7 | ||
(12) | 6 | 50 mg PO × 1 | 0.29 ± 1.25 | 1.75a | 11.4 ± 1.11 | 12.9 ± 1.13 | 2.77 ± 1.22 | 20.4 ± 1.15 |
6 | 100 mg PO × 1 | 0.59 ± 1.21 | 2.0a | 12.2 ± 1.11 | 11.8 ± 1.21 | 2.38 ± 1.25 | 18.9 ± 1.34 | |
6 | 200 mg PO × 1 | 1.16 ± 1.35 | 2.50a | 14.0 ± 1.14 | 13.0 ± 1.20 | 2.64 ± 1.25 | 19.8 ± 1.16 | |
7 | 400 mg PO × 1 | 2.50 ± 1.31 | 1.5a | 13.1 ± 1.06 | 14.9 ± 1.18 | 3.03 ± 1.17 | 20.1 ± 1.20 | |
7 | 600 mg PO × 1 | 3.19 ± 1.19 | 2.5a | 12.5 ± 1.14 | 15.0 ± 1.11 | 2.67 ± 1.10 | 17.5 ± 1.16 | |
7 | 800 mg PO × 1 | 4.73 ± 1.16 | 3.0a | 12.3 ± 1.13 | 13.4 ± 1.24 | 2.50 ± 1.28 | 18.7 ± 1.25 |
Abbreviations: bid, twice daily; Cmax, peak serum concentration; CL/F, total body clearance; CLR, renal clearance; Fe, fractional elimination in urine as unchanged parent compound; IV, intravenous; Tmax, time to Cmax; t½, terminal disposition half-life; PO, oral; qd, once daily.
Notes: Median;
Links parameters that are significantly different (p ≤ 0.05);
% coefficient of variation;
Young males (mean age, 32);
Older males (mean age, 74);
Older females (mean age, 74);
mL/min/1.73m2;
Mean values in mL/min;
Male;
Female.
References:1, Stass et al 2004; 2, Burkhardt et al 2002; 3, Stass and Kubitza 1999; 4, Stass et al 2002; 5, Lettieri et al 2001; 6, Sullivan et al 2001; 7, Stass et al 2001; 8, Lubasch et al 2000; 9,Wise et al 1999; 10, Ballow et al 1999; 11, Sullivan et al 1999; 12, Stass et al 1998.