Table 6.
Plasma and epithelial lining fluid concentrations of tedizolid and dalbavancin
| Antibacterial agent | Dosage regimen | Subjects [n] | Sampling time [h]a | ELF to plasma ratio based on AUC | Plasma concentration [µg/mL]b | ELF concentration [µg/mL]b | References |
|---|---|---|---|---|---|---|---|
| Tedizolid | 300 mg PO q24h × 3 doses | 5 | 2 | 40c | 2.01 ± 0.55 | 9.05 ± 3.83 | [87] |
| 5 | 6 | 1.51 ± 0.33 | 4.45 ± 2.18 | ||||
| 5 | 12 | 0.946 ± 0.31 | 5.62 ± 1.99 | ||||
| 5 | 24 | 0.398 ± 0.17 | 1.33 ± 0.59 | ||||
| Dalbavancin | 1500 mg IV infused over 30 min × 1 dose | 5 | 4 | 0.36d | 279 ± 32e | 1.9 ± 1.0 | [91] |
| 5 | 8 | 222 ± 27e | 3.1 ± 1.9 | ||||
| 5 | 12 | 194 ± 24e | 3.6 ± 2.1 | ||||
| 5 | 24 | 169 ± 20e | 2.7 ± 0.5 | ||||
| 5 | 72 | 120 ± 14e | 7.3 ± 8.2 | ||||
| 5 | 120 | 94 ± 11e | 11.9 ± 20.1 | ||||
| 5 | 168 | 79 ± 9e | 2.0 ± 0.6 |
ELF epithelial lining fluid, AUC area under the concentration-time curve, PO by mouth, IV intravenously, q24h every 24 h, SD standard deviation
aSampling time after the last dose
bTotal plasma and ELF concentrations expressed as mean ± SD
cBased on the ratio of AUC24 in ELF to AUC24 in unbound plasma, calculated using each participant’s derived unbound fraction
dBased on the ratio of AUC168 in ELF to AUC168 in unbound plasma, assuming 93% protein binding in plasma
eThirty-seven plasma concentrations were reported at each sampling time; values expressed as median ± SD