Table 2.
Pharmacokinetic characteristics of FQ and its active main metabolite, DMFQ, after a single dose
| PK parameter and compound | Value for the parameter at the indicated FQ dose (mean ± SD [CV])a |
||||
|---|---|---|---|---|---|
| 400 mg | 800 mg | 1,200 mg | 1,400 mg | 1,600 mg | |
| tmax (h)b | |||||
| FQ | 6.00 (1.08–48.00) | 6.50 (1.00–16.00) | 5.52 (1.00–12.00) | 4.01 (1.00–8.00) | 3.50 (2.00–10.00) |
| DMFQ | 9.00 (3.00–36.03) | 8.00 (2.00–36.00) | 5.52 (2.00–12.00) | 4.01 (1.07–36.05) | 5.01 (2.00–16.00) |
| Cmax (ng/ml) | |||||
| FQ | 81.7 ± 38.4 (47) | 151 ± 61.6 (41) | 270 ± 189 (70) | 406 ± 189 (47) | 487 ± 115 (24) |
| DMFQ | 38.3 ± 24 (63) | 69.3 ± 32.9 (47) | 171 ± 167 (97) | 233 ± 107 (46) | 250 ± 80.7 (32) |
| AUC0–24 (ng · h/ml) | |||||
| FQ | 1,290 ± 556 (43) | 2,420 ± 848 (35) | 3,890 ± 2,190 (56) | 5,590 ± 2,130 (38) | 6,550 ± 1,360 (21) |
| DMFQ | 657 ± 436 (66) | 1,250 ± 660 (53) | 2,810 ± 2,540 (90) | 3,910 ± 1,680 (43) | 3,860 ± 944 (24) |
| AUC (ng · h/ml) | |||||
| FQ | 13,100 ± 2,740 (21) | 19,200 ± 5,950 (31) | 29,300 ± 11,300 (39) | 44,200 ± 17,900 (40) | 49,200 ± 13,900 (28) |
| DMFQ | 25,400 ± 358 (1) | 28,500 ± 10,000 (35) | 69,600 ± 59,800 (86) | 84,500 ± 27,100 (32) | 83,700 ± 18,000 (22) |
| t1/2z (days) | |||||
| FQ | 16.5 ± 3.47 (21) | 16.0 ± 2.03 (13) | 17.7 ± 5.06 (29) | 15.8 ± 2.58 (16) | 14.7 ± 2.81 (19) |
| DMFQ | 42.1 ± 28.6 (68) | 34.4 ± 20.3 (59) | 38.7 ± 16.8 (43) | 31.8 ± 8.41 (26) | 25.0 ± 3.51 (14) |
a
CV, coefficient of variation expressed as a percentage. Values were tabulated simultaneously.
b
Values for tmax are median (range).