TABLE 2.

Mean pharmacokinetic parameters (%CV) of tigecycline after various single i.v. doses in SAD study

ParameterMean valuea (% CV) after:P
1-h infusion (group no., tigecycline [mg], fasting or fed)4-h infusion (group no., tigecycline [mg], fasting or fed)
1, 12.5 fasting2, 25, fasting3, 50, fasting4, 75, fasting5, 100, fasting6, 200, fasting8, 200, fed11, 200, fastingb9, 300, fed7, 200, fasting10, 300, fed
Cmax (ng/ml)108.5 (10)252 (25)383 (17)566 (14)911 (29)1,643 (18)1,528 (22)2,189 (30)2,817 (17)680 (22)960 (10)0.001
AUC (ng h/ml)753 (68)2,255 (45)2,558 (21)3,658 (27)6,396 (10)12,426 (23)11,719 (19)14,462 (17)17,856 (10)14,237 (22)16,732 (16)0.06
CL (l/h/kg)0.29 (67)0.20 (50)0.28 (14)0.29 (16)0.20 (13)0.25 (22)0.22 (12)0.20 (19)0.25 (11)0.24 (11)0.26 (13)0.27
Vss (l/kg)2.8* (34)6.4* (20)6.4* (31)7.5* (10)8.6 (18)11 (25)13 (18)12 (43)12 (20)14 (11)12 (24)0.001
t1/2 (h)11* (84)32* (64)18* (21)21* (25)38 (14)42 (28)54 (28)53 (20)46 (13)58 (14)42 (23)0.001
CLR (l/h)NDNDNDND2.6 (26)3 (50)2.2 (22)1.8 (24)2.7 (23)NA2 (28)0.13
fe (%)2.1 (113)6.5 (39)1.9 (72)8 (37)11 (25)12 (31)7.8 (25)8.5 (38)10.4 (22)NA8 (39)0.001
  • a ND, could not be determined accurately because of low concentrations in urine and serum; NA, not available. Values marked with an asterisk may not be reliably estimated due to the limit of quantification.

  • b Received ondansetron.