Table 2.
Summary of serum alosetron pharmacokinetic parametersa following a 2 mg dose.
| Young males | Young females | Elderly males | Elderly females | |
|---|---|---|---|---|
| Intravenous | ||||
| Cmax (ng ml−1) | 40.2 (34.2, 47.4) | 43.1 (35.5, 52.3) | 51.0 (42.5, 61.1) | 63.7 (54.3, 74.8) |
| AUC(0, ∞) (ng ml−1 h) | 49.3 (40.5, 59.9) | 66.1 (52.4, 83.4) | 49.7 (40.0, 61.8) | 72.2 (59.6, 87.6) |
| t1/2 (h) | 1.52 (1.36, 1.69) | 1.65 (1.45, 1.88) | 1.69 (1.49, 1.90) | 1.79 (1.61, 1.99) |
| CL (ml min−1) | 677 (556, 823) | 504 (400, 636) | 670 (539, 833) | 461 (381, 559) |
| Vss (l) | 82.6 (72.3, 94.2) | 63.1 (53.9, 73.8) | 84.5 (73.0, 97.8) | 62.4 (54.8, 71.1) |
| Oral | ||||
| Cmax (ng ml−1) | 9.35 (6.85, 12.8) | 14.6 (10.1, 21.1) | 8.67 (6.13, 12.2) | 16.1 (11.9, 21.9) |
| tmax (h) | 1.00 (0.75, 2.00) | 1.00 (0.50, 2.00) | 0.75 (0.50, 2.00) | 0.75 (0.50, 1.50) |
| AUC(0, ∞) (ng ml−1 h) | 24.6 (17.5, 34.7) | 36.6 (24.4, 55.0) | 23.6 (16.1, 34.5) | 44.2 (31.6, 61.9) |
| t1/2 (h) | 1.45 (1.28, 1.64) | 1.44 (1.24, 1.68) | 1.58 (1.37, 1.82) | 1.67 (1.48, 1.89) |
| F | 0.50 (0.41, 0.62) | 0.49 (0.40, 0.61) | 0.51 (0.41, 0.63) | 0.63 (0.51, 0.79) |
a
Geometric least-square mean (95% confidence interval), except tmax: median (range); all groups n = 12.