Skip to main content
. 2017 Aug 8;57(3):267–286. doi: 10.1007/s40262-017-0578-5

Table 3.

Adult populations

Population Dose (mg) No. of subjects, SD or SS Mean pharmacokinetic parameters (% coefficient of variation) [range]
Weight (kg) C max (mg/L) C max at SS (mg/L) C 24h (mg/L) C 24h at SS (mg/L) AUC24 (mg h/L)
Moderate hepatic dysfunction 100 8 SD 98 (19) 7.0 (27) [4.5–9.6] NR NR NR NR
Severe hepatic dysfunction 100 8 SD 73.2 (28) 7.3 (33) NR 1.5e NR 71.6 (34)
Renal dysfunction <30 mL/min 100 9 SD 84 (29) 8.7 (33) [4.9–13.4] NR NR NR NR
CVVH 100 10 SSa 69.6 (9) 7.3 (13) 9.15 (21)a 2.2 (42) 2.46 (30)a 71.31 (22) [49.3–92.2]
HIV 50 20 SS 55.3 (21)b 4.1 (34) 5.1 (22) 1e 1.5e 35.7 (25)
100 20 SS 55.3 (21)b 8.0 (30) 10.1 (26) 1.6e 3e 74.5 (25)
150 14 SS 55.3 (21)b 11.6 (27) 16.4 (40) 2.2e 4e 104.3 (25)
Hematology 12.5 8 SS 82.6 (23)b 0.9 1.1 0.2e 0.2e 9.0
25 8 SS 82.6 (23)b 1.6 g 4.1 0.5e,g 0.5e 16.6g
50 9 SS 82.6 (23)b 3.6 4.4 0.7e 1.5e 33.9
50 5 SS NR NR NR NR 2 (42) [1.2–3.5] NR
75 7 SS NR NR NR NR 4.2 (54) [2.2–9.0] NR
75 8 SS 82.6 (23)b 5.4 g 8.3 1e,g 1.5e 47.0g
100 14 SS NR NR NR NR 4.5 (51) [2.5–11.3] NR
100 8 SS 82.6 (23)b 7.1 g 22 1.5e,g 2e 59.9g
100 20 SS 67.1 (21) 5.69 (38) 10.05 (43) 1.2e 2e 56.6 (53)
150 8 SS 82.6 (23)b 11.7 h 17.6 1.9e,h 3.6e 103.6h
150 10 SS [41–67] NR 21.91 (39) NR 5.62 (60) NR
150 6 SS 60.2 (20) [47.6–82.2] NR 27.3 NR 9.4 NR
150 10 SS NR NR NR NR 4.9 (40) [2.8–10.1] NR
200 8 SS 82.6 (23)b 13.1 22.6 2.5e 5e 118.1
225 8 SS NR NR 21.1 (13) NR NR NR
300 2 SS NR NR NR NR 14.5 (6) [13.9–15.1] NR
300 10 SS NR NR 29.2 (21) NR NR NR
450 8 SS NR NR 38.4 (18) NR NR NR
600 8 SS NR NR 60.8 (44) NR NR NR
ICU 100 20 SS 76.5 [50–134]c NR 6.2 [5.1–9.2]c NR 1.6 [1.3–2.4]c NR
100 99 SD 84.5 [48–141] NR NR NR NR NR
Burn 100 10 SS NR 4.6 [3.9–7.5]c 6.4 [4.5–9.1]c 0.7 [0.5–1.1]c 1.0 [0.9–1.4]c NR
100–150 15 SS 80 [75–87.5]c NR NR NR NR 48.3 [37.7–55.8]c
200 3 SS 46.9 (19) [40–56.7] 8.81 (32) [5.55–10.79] 12.9 (11) [11.3–13.7] 2.59 (26) [1.81–3.07] 5.8 (57) [2.34–8.91] NR
300 5 SS 77.5 (9) [66.8–87] 18.82 (27) [13.6–24.2] 22.8 (18) [18.10–27.9] 4.65 (28) [3.5–6.1] 5.78 (31) [3–7.9] NR
Intra-abdominal infection 100–150 10 SS 65 [60.3–73.8]c NR NR NR NR 51.4 [44.6–56.4]c
Healthy adult subjects (Table 1) 100 mg 9.1
150 mg 16 ~4.5
Population Dose (mg) No. of subjects, SD or SS Mean pharmacokinetic parameters (% coefficient of variation) [range] References
AUC (mg h/L) t ½ (h) CL (mL/h/kg) V d (L/kg)
Moderate hepatic dysfunction 100 8 SD 97.5 (19) [74.8–130.1]d 14.3 (10) [12.2–16.1] 10.9 (16) 0.212 (18) [0.17–0.28] [21]
Severe hepatic dysfunction 100 8 SD 100.1 (34)d 13.7 (15) 15 (32) 0.291 (27) [24]
Renal dysfunction <30 mL/min 100 9 SD 116.2 (28) [72.9–169.2]d 14.8 (11) [11.6–16.5] 11.1 (17) 0.215 (14) [0.16–0.26] [21]
CVVH 100 10 SSa 104.54 (21) [62–136.7]a NR 12.69 (27) [7.47–18.25] 0.31 (16) [0.23–0.39] [63]
HIV 50 20 SS 54.3 (24) 14.9 (29) 19.3 (31) 0.401 (31) [26]
100 20 SS 115.3 (22)d 13.8 (22) 19.8 (27) 0.388 (29) [26]
150 14 SS 166.5 (24)d 14.1 (18) 20.4 (27) 0.407 (25) [26]
Hematology 12.5 8 SS 11.9 11.5 13.4 0.199 [18]
25 8 SS 23.8 12.4 12.7 0.199 [18]
50 9 SS 44.3 12.2 12.8 0.218 [18]
50 5 SS NR NR NR NR [68]
75 7 SS NR NR NR NR [68]
75 8 SS 63 13.4 17.8 0.290 [18]
100 14 SS NR NR NR NR [68]
100 8 SS 101.6 12.0 13.1 0.209 [18]
100 20 SS 97.11 (30) 13.4 (15) 16.9 (48) NR [25]
150 8 SS 166.7 12.9 11.9 0.202 [18]
150 10 SS NR NR NR NR [95]
150 6 SS 367.2 (42) [217.3–617.1] 17.7 (12) [14.5–20.0] 8 (50) [4–12] 0.209 (48) [0.09–0.31] [67]
150 10 SS NR NR NR NR [68]
200 8 SS 210.6 20.1 11.6 0.283 [18]
225 8 SS 234 (15) 14.0 (10) 12.8 (14) 0.243 (8) [15]
300 2 SS NR NR NR NR [68]
300 10 SS 339 (21) 14.2 (23) 12.2 (18) 0.240 (20) [15]
450 8 SS 479 (33) 14.9 (17) 13.4 (29) 0.278 (22) [15]
600 8 SS 663 (32) 17.2 (13) 13.4 (36) 0.307 (37) [15]
ICU 100 20 SS 65.7 [55.9–88.7]c 14.4 [12.8–16.3]c 19.6 [15.7–23.5]c 0.375 [0.22–0.42]c [77]
100 99 SD [65.5–99.5]d,f NR NR 0.231 (9) [61]
Burn 100 10 SS NR NR NR NR [40]
100–150 15 SS NR NR NR NR [41]
200 3 SS NR NR NR NR [43]
300 5 SS NR NR NR NR [42]
Intra-abdominal infection 100–150 10 SS NR NR NR NR [41]
Healthy adult subjects (Table 1) 133 15.4 10.4 0.2
181.4

NR not reported, C max maximum plasma concentration, SD single dose, SS steady state, C 24h trough plasma concentration 24 h after dosing, AUC 24, area under the plasma concentration-time curve after a single dose from zero to 24 h, AUC area under the plasma concentration-time curve at steady state from zero to 24 h, or, when indicated, from zero to infinity after a single dose, t ½ terminal half-life, CL clearance, V d volume of distribution; average is weighted by the number of patients reported, ICU intensive care unit, CVVH continuous venovenous hemofiltration, SOFA Sequential Organ Failure Assessment Score

a Values on day 2 of treatment

b Mean group weight of all groups

c Median value [interquartile range]

d AUC∞ after a single dose

e Values not reported but extracted from figures with concentration versus time curves

f AUC dependent on SOFA score and albumin concentration. SOFA <10: albumin ≤25 = 87.3 and albumin >25 = 99.5 mg*h/L; SOFA ≥10: albumin ≤25 = 65.5 and albumin >25 = 74.6 mg*h/L

g n = 9

h n = 10