[Chemotherapy of biliary tract infections (XXXVII). Excretion into bile and gallbladder tissue levels of levofloxacin and its clinical effect in biliary tract infections].
Evaluations were made on biliary excretion and penetration into the gallbladder tissue of levofloxacin (LVFX, DR-3355), a new quinolone antibacterial agent, and its clinical efficacy in biliary tract infections. 1. Gallbladder tissue concentrations and biliary concentrations of LVFX at 2-6 hours at oral administration of 100 mg were 0.58-1.99 micrograms/g and 0.49-5.63 micrograms/ml, respectively. These tissue and biliary levels are almost equal or somewhat higher than the serum levels (0.55-1.63 micrograms/ml) of the compound. 2. The concentrations of LVFX and optical isomer DR-3354 in the serum, gallbladder tissue, and bile were determined after a single or a concomitant administration of LVFX 100 mg and/or ofloxacin (OFLX) 100 to 200 mg. The concentration ratio of LVFX to DR-3354 paralleled with the ratio of the 2 compounds administrated. 3. At a dose of 100 mg, the glucuronide of LVFX in the common duct bile was detected at proportions between 0.9 and 36.0%. 4. A total of 11 patients with biliary tract infections, including 6 cholecystitis 3 cholangitis, and 1 each of cholecystocholangitis and liver abscess was treated with LVFX at 100-200 mg t.i.d. for 3-14 days. Clinical results were excellent or good in 8 cases and fair in 3 cases, resulting in an efficacy rate of 72.7%. 5. A side effect and an abnormal change in laboratory findings were observed in both 1 case each and they were both mild. It was concluded that LVFX showed good penetration to the biliary tract as does OFLX, and that it would be a useful oral agent for the treatment of biliary tract infections.
Tanimura
H
H
Department of Gastroenterological Surgery, Wakayama Medical College.
Ohnishi
H
H
Okamura
T
T
Uenishi
M
M
Ichimiya
G
G
Kobayashi
Y
Y
Aoki
Y
Y
Oka
S
S
Yamamoto
S
S
Shimada
K
K
D000328:Adult; D000368:Aged; D001646:Bile / Q000378:metabolism*; D002761:Cholangitis / Q000188:drug therapy* / Q000378:metabolism; D002764:Cholecystitis / Q000188:drug therapy* / Q000378:metabolism; D004341:Drug Evaluation; D005260:Female; D005704:Gallbladder / Q000378:metabolism*; D006801:Humans; D064704:Levofloxacin; D008297:Male; D008875:Middle Aged; D015242:Ofloxacin / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use
D064704:Levofloxacin; D015242:Ofloxacin