[Biliary excretion and clinical efficacy of T-3262 (tosufloxacin tosilate) administered in the treatment of cholecystitis].
T-3262 (tosufloxacin tosilate), a new oral pyridone carboxylic acid agent, was investigated for its biliary excretion and clinical efficacy and safety to evaluate its usefulness in the treatment of cholecystitis. T-3262 was administered to a total of 4 healthy volunteers for 2 days at a dose of 150 mg every 8 hours, and A-, B- or C-bile were collected using the MELTZER-LYON method at 10-11 hours after the final administration. Bile concentrations of T-3262 in 3 cases were 0.33-2.05 micrograms/ml (A-bile), 6.13-9.50 micrograms/ml (B-bile) and 1.11-2.70 micrograms/ml (C-bile). Thus, T-3262 levels in B-bile were 15-34 times higher than serum levels (0.28-0.41 micrograms/ml). Only a trace of serum concentration of T-3262 was detected in another case with the concentration in B-bile was 0.132 micrograms/ml. A total of 10 patients with cholecystitis were treated with T-3262 at a dose level of 150 mg per dose 3 times daily for 1 to 20 days. The clinical efficacy was excellent in 1 case, good in 5 cases and fair in 2 cases and unevaluable in 2 cases, thus the clinical efficacy rate was 75%. Bacteriologically, Klebsiella pneumoniae, Enterococcus faecalis and Haemophilus parahaemolyticus were isolated from biles of 3 patients before treatment. Upon the treatment, E. faecalis was eradicated and K. pneumoniae was unchanged. The fate of H. parahaemolyticus was not known because of examination was not done after treatment. Side effects were observed in 2 cases with diarrhea in 1 case and epigastric pain in another case. But those symptoms disappeared after cessation of administration of T-3262. Abnormal laboratory test values were not observed.
Sugata
F
F
Department of Internal Medicine, Showa University, Fujigaoka Hospital.
Ohguri
S
S
Takamura
Y
Y
Tominaga
S
S
Iwamura
K
K
Yamada
T
T
Shibata
H
H
Yamada
N
N
Okabe
K
K
Kato
Y
Y
D042462:4-Quinolones; D000328:Adult; D000368:Aged; D000890:Anti-Infective Agents / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001646:Bile / Q000378:metabolism*; D002764:Cholecystitis / Q000188:drug therapy*; D004341:Drug Evaluation; D005260:Female; D024841:Fluoroquinolones; D006801:Humans; D008297:Male; D008875:Middle Aged; D009287:Naphthyridines
D042462:4-Quinolones; D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; C055185:tosufloxacin