TABLE 5.
Pharmacokinetic parameters of linezolid, vancomycin and quinupristin/dalfopristin following a single oral dose
| Dose Adjustment* | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Drug | Dosage (mg) | %F | Cmax(µg/mL) | Tmax(h) | AUC24 (µg x h/mL) | T1/2(h) | Vd L (L/kg) | % Protein binding | Renal | Hepatic |
| Linezolid | 375 | 100 | 8.2 | 1.67 | 65.5 | 4.98 | 44.3 (0.6) | 31 | No | No |
| 500 | 100 | 10.4 | 1.38 | 74.3 | 4.59 | 45.0 (0.6) | 32 | No | No | |
| 625 | 100 | 12.7 | 1.33 | 102.0 | 4.87 | 45.0 (0.6) | NA | No | No | |
| Vancomycin | 500 | <5 | 10-25 | 1.0 | N/A | 7.0 | 10.5 (0.15) | 44-82 | Yes | No |
| 1000 | <5 | 20-50 | 1.0 | N/A | 7.0 | 10.5 (0.15) | 44-82 | Yes | No | |
| Quinupristin | 7.5 mg/kg | <5 | 2.7 | 0.92 | 3.2 | 0.91 | 70 (1.0) | 55-78 | No | † |
| Dalfopristin | <5 | 8.1 | 0.92 | 8.5 | 0.91 | 70 (1.0) | 11-26 | No | † | |
Linezolid: Single oral dose; Vancomycin and quinupristin/dalfopristin: Single intravenous dose.
*
Dose adjustment refers to whether the antimicrobial requires any dosage adjustments in patients with impaired renal or hepatic function (see text for details). Dosage only applies to peak concentration reached in the plasma/serum (Cmax) and the area under the plasma concentration time curve (AUC) after a single dose. The other parameters represent an average of the values available in the literature irrespective of dosage.
†
Dosage adjustment may be necessary although precise recommendations have not been validated.