Table 5:
In silico pharmacokinetic analysis for compound 19 and linezolid (simulated at 600 mg).
| Oral | Intravenous | |||||
|---|---|---|---|---|---|---|
| 19 (Simulated) | Linezolid (Simulated) | Linezolid (Experimental)1 | 19 (Simulated) | Linezolid (Simulated) | Linezolid (Experimental) | |
| Cmax2 (µg/mL) | 0.17 | 5.33 | 12.7 | - | - | 13.4 |
| tmax3 (hours) | 3 | 2.75 | 1.33 | - | - | 0.5 |
| Fraction absorbed (FAlast) | 0.80 | 0.92 | 1.03 | - | - | - |
| CL4 (mL/min-kg) | - | - | - | 12.58 | 1.09 | 1.749 |
| t1/25 (hours) | - | - | - | 22.90 | 12.31 | 4.40 |
| MRT6 (hours) | - | - | - | 12.82 | 17.04 | - |
| Vd7 (L/kg) | - | - | - | 24.94 | 1.11 | 0.5810 |
| Vss8 (L/kg) | - | - | - | 9.68 | 1.12 | - |
1
(adapted from Stalker DJ et al. J Antimicrob Chemother 2003, 51: 1239–46 (Table 2, 625 mg dose))
2
Cmax = maximum concentration of drug in plasma/blood
3
tmax = time required to reach Cmax
4
CL = rate of clearance
5
t1/2 = half-life
6
MRT = mean residence time
7
Vd = volume of distribution
8
Vss = volume of distribution at steady-state
9
Clearance for linezolid (experimental) obtained by dividing the mean clearance value by the mean weight of patients
10
Volume of distribution for linezolid (experimental) obtained by dividing the mean Vd by the mean weight of patients