TABLE 1.
Pharmacokinetic parameters for six fluoroquinolones tested in 12 volunteers eacha
| Drug (mg) | Cmax (μg/ml/70 kg) | Cmax (μg/ml/70 kg), dose normalized | Tmax (h) | Tlag (h) | Half-life (h) | MRT (h) | AUCtot (μg · h/ml/70 kg) | AUCtot (μg · h/ml/70 kg), dose normalized | Total urinary recovery (% of dose) | Renal clearance (ml/min/1.73 m2) | Vss (liters/70 kg) |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Ciprofloxacin (250) | 1.5 ± 0.43 | 1.2 ± 0.34 | 0.78 ± 0.33 | 0.27 ± 0.17 | 5.37 ± 0.82 | 5.8 ± 0.94 | 5.75 ± 1.25 | 4.6 ± 1.0 | 40.8 ± 7.48 | 266 ± 40.6 | 231 ± 61.8 |
| Gatifloxacin (400) | 3.42 ± 0.74* | 1.71 ± 0.37 | 1.49 ± 0.65 | 0.21 ± 0.19 | 6.52 ± 0.87 | 9.28 ± 1.12* | 30 ± 3.8* | 15 ± 1.9* | 76.9 ± 5.6 | 153 ± 21 | 110 ± 20 |
| Grepafloxacin (600) | 1.98 ± 0.52* | 0.66 ± 0.17 | 2.77 ± 1.11 | 0.34 ± 0.06 | 12.12 ± 3.92* | 14.15 ± 2.67* | 23.5 ± 4.73* | 7.85 ± 1.58* | 9.36 ± 2.91 | 35.2 ± 6.9 | 306 ± 54.3 |
| Levofloxacin (500) | 6.21 ± 1.34* | 2.48 ± 0.53* | 0.8 ± 0.38 | 0.33 ± 0.15 | 6.95 ± 0.81 | 8.65 ± 0.8** | 44.8 ± 4.4* | 17.9 ± 1.76* | 75.9 ± 11.6 | 124 ± 19.1 | 88 ± 9.92 |
| Moxifloxacin (400) | 4.34 ± 1.61* | 2.17 ± 0.81* | 1.02 ± 0.72 | 0.18 ± 0.16 | 9.15 ± 1.62* | 12.5 ± 2.03* | 39.3 ± 5.35* | 19.7 ± 2.67* | 19.9 ± 4.55 | 30.5 ± 6.18 | 122 ± 19.6 |
| Trovafloxacin (200) | 2.09 ± 0.58 | 2.09 ± 0.58* | 0.95 ± 0.61 | 0.12 ± 0.16 | 10.3 ± 3.4* | 13.2 ± 5.37* | 19.5 ± 3.1* | 19.5 ± 3.1* | 9.27 ± 2.47 | 14.2 ± 3.5 | 129 ± 58 |
a
Drugs were given orally. Data were determined by HPLC for original doses and for normalized doses (200 mg) and are reported as means and standard deviations. P values for results that were statistically significant compared to those for ciprofloxacin were <0.01 (*) and <0.05 (**).