TABLE II.
Patient Number |
Mean ± SD |
|||||||||
---|---|---|---|---|---|---|---|---|---|---|
1 | 2 | 3 | 4 | 5 | 6 | 7 | Mean ± SD | Normal Subjects* | ||
I. | Protein Binding | |||||||||
nP, mM × 104 | 1.64 | 3.45 | 2.47 | 2.95 | 1.26 | 1.04 | 4.22 | 2.43 ± 1.19 | 4.33 ± 0.87 | |
Ka, mM−1 × 10−4 | 5.92 | 1.74 | 5.90 | 1.76 | 1.48 | 9.83 | 0.56 | 3.89 ± 3.40 | 6.49 ± 1.15 | |
II. | Total Drug | |||||||||
Cmax, μg/mL | 290 | 218 | 306 | 315 | 245 | 560 | 293 | 318 ± 112 | 257 ± 17 | |
C12, μg/mL | 61 | 84 | 90 | 33 | 48 | 54 | 117 | 70 ± 29 | 46 ± 7 | |
C24, μg/ml | 21 | 68 | 81 | 13 | 28 | 19 | 104 | 48 ± 36 | 15 ± 4 | |
TBC, mL/hr | 994 | 368 | 311 | 1706 | 945 | 1059 | 260 | 806 ± 526 | 1190 ± 150 | |
mL/hr/kg | 12.0 | 4.1 | 4.5 | 24.4 | 13.5 | 16.5 | 3.3 | 11.2 ± 7.8 | ||
MRT, hr | 12.5 | 58.8 | 44.6 | 8.5 | 25.8 | 10.7 | 48.5 | 29.9 ± 20.6 | ||
Vss, L | 12.4 | 21.7 | 13.9 | 14.5 | 24.4 | 11.4 | 12.6 | 15.8 ± 5.1 | ||
mL/kg | 150 | 241 | 201 | 207 | 349 | 178 | 159 | 212 ± 68 | ||
Varea, L | 13.1 | 20.9 | 16.3 | 14.7 | 26.7 | 12.7 | 12.1 | 16.6 ± 5.3 | 10.1 ± 1.0 | |
mL/kg | 158 | 232 | 236 | 210 | 381 | 199 | 153 | 224 ± 76 | ||
β, hr−1 | 0.076 | 0.018 | 0.019 | 0.116 | 0.035 | 0.083 | 0.021 | 0.053 ± 0.039 | ||
t1/2, hr | 9.2 | 39.4 | 36.3 | 6.0 | 19.6 | 8.3 | 32.4 | 13.1b | 5.8(4.7–6.8)‡ | |
III. | Unbound Drug | |||||||||
Cmax, μg/mL | 187 | 70 | 154 | 157 | 178 | 492 | 140 | 197 ± 136 | ||
C12, μg/mL | 10 | 16 | 11 | 6 | 21 | 11 | 42 | 17 ± 12 | ||
C24, μg/mL | 2 | 12 | 9 | 2 | 11 | 2 | 37 | 11 ± 12 | ||
TBC, mL/hr | 4322 | 2318 | 3085 | 7163 | 2245 | 2980 | 794 | 3272 ± 2019 | 14940 ± 2160 | |
mL/hr/kg | 52.1 | 25.8 | 44.7 | 102.3 | 32.1 | 46.6 | 10.0 | 44.8 ± 29.1 | ||
MRT, hr | 6.6 | 44.9 | 25.0 | 6.2 | 21.0 | 4.7 | 40.7 | 21.3 ± 16.7 | ||
Vss, L | 28.6 | 104.1 | 77.2 | 44.3 | 47.2 | 14.0 | 32.3 | 49.7 ± 31.0 | ||
mL/kg | 345 | 1156 | 1119 | 634 | 674 | 218 | 409 | 651 ± 368 | ||
Varea, L | 38.8 | 102.7 | 104.0 | 54.3 | 54.0 | 20.2 | 31.1 | 57.9 ± 33.3 | 162 ± 18 | |
mL/kg | 467 | 1141 | 1507 | 776 | 771 | 315 | 394 | 767 ± 432 | ||
β, hr−1 | 0.111 | 0.023 | 0.030 | 0.132 | 0.042 | 0.148 | 0.026 | 0.073 ± 0.055 | ||
t1/2, hr | 6.2 | 30.7 | 23.4 | 5.3 | 16.7 | 4.7 | 27.2 | 9.5† | 7.6 |