TABLE 1.
Pharmacokinetics and pharmacodynamics of linezolid and telavancina
| Parameter | Median value for drug (IQR) |
|
|---|---|---|
| Linezolid (n = 6; 10 mg/kg) | Telavancin (n = 3; 22.5 mg/kg) | |
| Pharmacokinetic parameters | ||
| CL (liters/h) | 1.55 (0.70–3.25) | 1.34 (1.13–2.08) |
| Vc (liters) | 11.76 (8.33–14.76) | 6.73 (5.66–7.59) |
| VELF (liters) | 10.19 (6.80–20.65) | 40.95 (29.63–153.93) |
| Kcp (h−1) | 27.37 (23.65–40.51) | 0.12 (0.10–0.15) |
| Kpc (h−1) | 32.47 (29.97–43.88) | 0.19 (0.05–0.28) |
| Plasma Cmax (mg/liter) | 14.58 (13.21–17.16) | 93.63 (84.49–96.10) |
| Plasma Ctrough (mg/liter) | 6.17 (3.14–9.14) | 3.73 (1.55–5.96) |
| Pharmacodynamic indices | ||
| Plasma fAUC0–24 (mg · h/liter) | 208.96 (177.49–312.95) | 515.57 (316.93–539.78) |
| ELF fAUC0–24 (mg · h/liter) | 202.70 (111.70–366.77) | 42.45 (23.51–60.34) |
| % penetration | 92.12 (50.97–170.42) | 7.96 (4.56–21.53) |
| Plasma fAUC0–24/MIC ratio | 208.96 (177.49–312.95) | 4,296.46 (2,641.11–4,498.19) |
| ELF fAUC0–24/MIC ratio | 202.70 (111.70–366.77) | 353.74 (195.92–503.60) |
a
Data are reported as the medians and interquartile ranges (IQR) (25th to 75th percentiles). CL, clearance; Vc, volume of distribution of the central compartment; VELF, volume of distribution of the peripheral epithelial lining fluid (ELF) compartment; Kcp, transfer rate constant from the central compartment to the peripheral ELF compartment; Kpc, transfer rate constant from the peripheral ELF compartment to the central compartment; Cmax, peak concentration; Ctrough, lowest concentration; fAUC0–24/MIC ratio, ratio of the free area under the curve to the MIC over the first 24 h. The linezolid MIC is 1 μg/ml, and the telavancin MIC is 0.12 μg/ml.