TABLE 2.
Levofloxacin pharmacokinetic parametersa
| Group,b dose, and day | Maximum concn in serum (mg/ml) | Tmax (h) | AUC (mg · h/ml)c | CL/F (ml/min) | t1/2 (h) | Maximum concn in urine (mg/ml) | Ae (% of dose)d | CLR (mg/ml) |
|---|---|---|---|---|---|---|---|---|
| A | ||||||||
| 750 mg | ||||||||
| 1 | 8.89 (2.64) | 1.5 (0.7) | 71.1 (17.3) | 151 (22) | 7.91 (1.50) | 563 (288) | 60.8 (22.2) | 115 (52) |
| 14 | 11.4 (2.4) | 1.4 (0.4) | 97.7 (28.6) | 139 (45) | 9.22 (2.06) | 718 (444) | 74.0 (29.0) | 103 (59) |
| 15 | 10.4 (3.3) | 1.9 (1.2) | 91.4 (28.9) | 153 (64) | 9.41 (1.94) | 825 (422) | 79.3 (27.3) | 120 (54) |
| 26 | 8.94 (1.29) | 1.6 (0.9) | 73.9 (14.0) | 142 (33) | 9.98 (4.32) | 856 (241) | 86.0 (32.4) | 139 (65) |
| 1 g | ||||||||
| 15 | 15.7 (4.5) | 1.2 (0.3) | 122 (28) | 133 (28) | 10.5 (1.9) | 1,156 (601) | 61.9 (9.7) | 89 (23) |
| 26 | 12.1 (1.8) | 1.4 (0.5) | 101 (28) | 151 (49) | 10.2 (4.2) | 826 (666) | 69.2 (8.4) | 103 (40) |
| B | ||||||||
| 750 mg | ||||||||
| 1 | 8.70 (2.37) | 1.4 (0.6) | 56.3 (8.0) | 208 (31) | 6.63 (1.17) | 393 (259) | 60.6 (17.2) | 135 (39) |
| 14 | 9.88 (2.38) | 1.5 (0.4) | 60.7 (8.5) | 210 (35) | 6.69 (0.68) | 684 (405) | 72.9 (23.4) | 150 (59) |
| 15 | 11.2 (3.5) | 1.3 (0.3) | 68.5 (8.7) | 185 (23) | 6.10 (0.88) | 725 (209) | 69.9 (22.6) | 124 (32) |
| 26 | 10.1 (1.4) | 1.4 (0.4) | 55.8 (8.6) | 207 (43) | 7.47 (1.86) | 517 (201) | 72.5 (24.1) | 162 (77) |
| 1 g | ||||||||
| 15 | 10.6 (1.9) | 1.4 (0.4) | 74.6 (19.9) | 224 (73) | 7.30 (2.36) | 902 (416) | 60.9 (35.5) | 144 (110) |
| 26 | 9.61 (1.55) | 2.2 (0.8) | 76.7 (17.2) | 194 (51) | 8.30 (1.08) | 839 (486) | 66.0 (11.9) | 135 (42) |
| All (A plus B) | ||||||||
| 750 mg | ||||||||
| 1 | 8.79 (2.45) | 1.4 (0.6) | 63.7 (15.2) | 184 (39) | 7.17 (1.43) | 475 (280) | 60.7 (19.4) | 125 (46) |
| 14 | 10.7 (2.4) | 1.4 (0.4) | 79.2 (28.0) | 175 (53) | 8.10 (2.03) | 701 (414) | 73.4 (25.1) | 130 (62) |
| 15 | 10.8 (3.2) | 1.6 (0.9) | 80.0 (23.4) | 169 (49) | 7.94 (2.28) | 775 (318) | 75.1 (24.3) | 122 (43) |
| 26 | 9.50 (1.41) | 1.5 (0.7) | 64.8 (14.5) | 178 (50) | 8.59 (3.24) | 686 (275) | 77.6 (26.1) | 152 (68) |
| 1 g | ||||||||
| 15 | 13.1 (4.2) | 1.3 (0.4) | 98.1 (33.7) | 174 (68) | 9.06 (2.57) | 1,029 (505) | 61.5 (22.8) | 113 (75) |
| 26 | 10.9 (2.1) | 1.8 (0.8) | 88.9 (25.5) | 170 (51) | 9.37 (3.21) | 833 (550) | 67.6 (9.9) | 119 (42) |
a
Values are means (standard deviations). HIV-seropositive subjects received 750-mg q.d. oral doses of levofloxacin for 2 weeks, followed by 750-mg or 1-g t.i.w. oral doses of levofloxacin for 2 weeks.
b
Group A, subjects with a CD4 count of <250 cells/mm3; group B, subjects with a CD4 count of >250 cells/mm3.
c
AUC values were calculated from 0 to 24 h.
d
Data for days 1, 14, and 15 are based on 24-h urine recovery values, and data for day 26 are based on 72-h urine recovery values.