Hepatobiliary elimination of temafloxacin.
Clin Pharmacokinet
; 22 Suppl 1: 33-42, 1992.
Article
em En
| MEDLINE
| ID: mdl-1319869
ABSTRACT
The biliary excretion of temafloxacin and temafloxacin glucuronide was characterised in this study after administration of a single oral temafloxacin 600mg dose to 8 patients with T-tube drainage of the common bile duct inserted after cholecystectomy or choledochotomy. High performance liquid chromatographic analyses of plasma, urine and bile samples collected during the 72h after temafloxacin administration showed that biliary concentrations of unchanged temafloxacin followed a time-course parallel to plasma concentrations but were 5- to 10-fold higher. Biliary temafloxacin peak concentrations ranged from 18.74 to 64.35 mg/L and time to peak concentrations from 0.71 to 10.23h. Mean hepatobiliary clearance of temafloxacin was 3.10 ml/min (0.19 L/h) when calculated for the unchanged drug and 1.43 ml/min (0.09 L/h) when calculated for its biliary excretion as glucuronic acid conjugates. Patients with higher bile production had markedly higher clearance of both temafloxacin and temafloxacin glucuronide. The elimination time-course of the conjugate in bile generally paralleled those of temafloxacin in bile and plasma, although there was a lag in the rate of appearance of the conjugate in bile. Biliary excretion of unchanged temafloxacin and temafloxacin glucuronide accounted for approximately 2.2 and 1% of the administered dose, respectively. Thus, it appears that hepatobiliary elimination of temafloxacin and its glucuronide acid accounts for only a small fraction of total temafloxacin clearance. Nonetheless, concentrations attained in the bile are far above the minimum inhibitory concentration values of pathogens relevant in biliary tract infections.
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Base de dados:
MEDLINE
Assunto principal:
Bile
/
Quinolonas
/
Fluoroquinolonas
/
Fígado
/
Anti-Infecciosos
Limite:
Adult
/
Aged
/
Female
/
Humans
/
Male
/
Middle aged
Idioma:
En
Revista:
Clin Pharmacokinet
Ano de publicação:
1992
Tipo de documento:
Article
País de afiliação:
Alemanha