[Transfer of cadrofloxacin, a novel fluoroquinolone antibacterial, into the gallbladder tissue and bile].
Clinical pharmacological studies of a novel fluoroquinolone antibacterial drug, cadrofloxacin, were performed in 12 surgical patients by investigating the transfer of cadrofloxacin into the gallbladder tissue and bile. They were scheduled for cholecystectomy (n = 6) or had undergone a percutaneous transhepatic biliary drainage (n = 5) or gallbladder drainage (n = 1) at the Second Department of Surgery, Wakayama Medical University. A single dose of cadrofloxacin was orally administered to all patients at a dose of 200 mg. The results were as follows: 1) Serum and gallbladder tissue levels of cadrofloxacin after 2.9-5.7 hours were 0.6-2.5 micrograms/ml and 0.6-8.6 micrograms/ml, respectively. The gallbladder/serum ratios of drug concentration were 0.6-3.4. 2) Levels of cadrofloxacin in bile reached a peak of 2.5-12.9 micrograms/ml after individually different period of time. Cumulative bile recoverlies of cadrofloxacin (unchanged compound + glucuronide conjugate) within the first 6 hours were 0.02-0.49%, and 0.08-0.75% within 0-12 hours. The mean value of [glucuronide conjugate/unchanged compound] in bile was 37%, although the values depended on the patients.
Tanimura
Hiroshi
H
Wakayama Rosai Hospital, 435 Koya, Wakayama-shi, Wakayama 640-8505, Japan.
Ohnishi
Hironobu
H
D000284:Administration, Oral; D000328:Adult; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D001646:Bile / Q000378:metabolism*; D005260:Female; D024841:Fluoroquinolones / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D005704:Gallbladder / Q000378:metabolism*; D020719:Glucuronides / Q000378:metabolism; D006801:Humans; D008297:Male; D008875:Middle Aged; D013997:Time Factors
D000890:Anti-Infective Agents; D024841:Fluoroquinolones; D020719:Glucuronides; C487845:cadrofloxacin