TABLE 1.
Pharmacokinetics and dose proportionality of telithromycin following a single oral dosea
| Dose (mg) | Cmax (mg/liter) | tmax (h)bc | C24 (mg/liter) | AUC0–24 (mg · h/liter) | AUC0–∞ (mg · h/liter) | CLR(0–24) (liters/h)c | t1/2λ1 (h)c | t1/2λz (h)d | Ae0–24 (%) | Cmax/dose (mg/liter) | AUC0–z/dose (mg · h/liter) | C24/dosec (mg/liter) |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 400 | 0.80 (57) | 1.0 (0.5–4.0) | 0.0069 (72) | 2.57 (40) | 3.09 (35) | 12.17 (26) | 2.13 (37) | 6.68 (24) | 7.42 (32)f | 1.59 (57) | 5.14 (40)f | 0.0141 (72) |
| 800 | 1.90 (42) | 1.0 (0.5–4.0) | 0.0296 (45) | 8.25 (31) | 8.96 (32) | 12.32 (17) | 2.43 (41) | 7.16 (19) | 12.66 (33)f | 1.90 (42) | 8.40 (32)f | 0.0296 (45) |
| 1,600 | 4.07 (30) | 1.0 (0.5–4.0 | 0.103 (53) | 23.1 (34) | 25.4 (35) | 13.28 (23) | 2.81 (31) | 10.13 (27)e | 18.4 (27)f | 2.04 (30)g | 12.4 (36)f | 0.0512 (53) |
a
Data are means, with percent CV in parentheses, except where indicated otherwise. Statistical significance was determined by ANOVA and Tukey's test. Elimination half-lives were calculated by a compartmental analysis.
b
Values are medians with ranges in parentheses.
c
None of the values are significantly different from each other.
d
For 400-, 800-, and 1,600-mg doses, n = 10, 12, and 15, respectively.
e
Significantly different from values at 400 and 800 mg (P < 0.001).
f
Significantly different from values for other doses (P < 0.001).
g
Significantly different from value for 400-mg dose (P < 0.01).