TY - JOUR
T1 - In vitro and in vivo activities of sparfloxacin (AT-4140) against Mycobacterium tuberculosis
AU - Ji, B.
AU - Truffot-Pernot, C.
AU - Grosset, J.
PY - 1991/9
Y1 - 1991/9
N2 - The in vitro and in vivo activities of sparfloxacin (AT-4140) against M. tubercubsis are reported. The MICs of sparfloxacin for 50% and 90% of 18 clinical isolates were, respectively, 0.25 and 0.5 mg/l, one or two dilutions lower than that of ciprofklxacin and ofloxacin. In mice infected intravenously with 0.1 mg M. tuberculosis H37Rv strain, the minimal effective dosage of sparfloxacin, as assessed by survival rate, spleen enlargement and gross lung lesidns, was 12.5 mg/kg. The activities of various regimens were in the following rank order: INH 25 mg/kg = sparfloxacin 50-100 mg/kg > ofloxacin 300 mg/kg > (or =) sparfloxacin 25 mg/kg > spartloxacin 12.5 mg/kg > (or =) ofloxacin 200 mg/kg > ofloxacin 100 mg/kg > (or =) negative control. Therefore, on a weight to weight basis, sparfloxacin was six to eight-fold more active against M. tuberculosis infection in mice than ofloxacin. In addition, WIN 57273, a new broad-spectrum fluoroquinolone, at a dosage of 100 mg/kg daily, was inactive against M. tuberculosis infection.
AB - The in vitro and in vivo activities of sparfloxacin (AT-4140) against M. tubercubsis are reported. The MICs of sparfloxacin for 50% and 90% of 18 clinical isolates were, respectively, 0.25 and 0.5 mg/l, one or two dilutions lower than that of ciprofklxacin and ofloxacin. In mice infected intravenously with 0.1 mg M. tuberculosis H37Rv strain, the minimal effective dosage of sparfloxacin, as assessed by survival rate, spleen enlargement and gross lung lesidns, was 12.5 mg/kg. The activities of various regimens were in the following rank order: INH 25 mg/kg = sparfloxacin 50-100 mg/kg > ofloxacin 300 mg/kg > (or =) sparfloxacin 25 mg/kg > spartloxacin 12.5 mg/kg > (or =) ofloxacin 200 mg/kg > ofloxacin 100 mg/kg > (or =) negative control. Therefore, on a weight to weight basis, sparfloxacin was six to eight-fold more active against M. tuberculosis infection in mice than ofloxacin. In addition, WIN 57273, a new broad-spectrum fluoroquinolone, at a dosage of 100 mg/kg daily, was inactive against M. tuberculosis infection.
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U2 - 10.1016/0041-3879(91)90004-C
DO - 10.1016/0041-3879(91)90004-C
M3 - Article
C2 - 1663283
AN - SCOPUS:0025997583
SN - 0041-3879
VL - 72
SP - 181
EP - 186
JO - Tubercle
JF - Tubercle
IS - 3
ER -