Orlando R, Sawadogo A, Miglioli P A, Cappellazzo M G, Palatini P
Institute of Internal Medicine, Department of Pharmacology, University of Padua, Italy.
Chemotherapy. 1992;38(1):1-6. doi: 10.1159/000238934.
The disposition kinetics of ofloxacin, a quinolone antibacterial agent excreted essentially unmodified by the kidney, was studied after single oral administration in 8 patients with compensated liver cirrhosis and in 8 control subjects. Mean elimination half-life and apparent volume of distribution were significantly increased in the cirrhotic group (7.6 vs. 4.9 h and 1.6 vs. 1.2 liters kg-1, respectively). A reduction in the renal clearance of ofloxacin was also observed in the cirrhotic patients, in spite of an apparently normal renal function. These observations indicate that also the pharmacokinetics of unmetabolized drugs may be altered in compensated liver cirrhosis. The serum concentration-time profiles of nearly all subjects exhibited a secondary peak 4-6 h after dosing. This double-peak behavior was interpreted as either enterohepatic circulation or biphasic gastric emptying of ofloxacin.
在8例代偿期肝硬化患者和8例对照受试者单次口服给药后,对基本上未经代谢即由肾脏排泄的喹诺酮类抗菌剂氧氟沙星的处置动力学进行了研究。肝硬化组的平均消除半衰期和表观分布容积显著增加(分别为7.6对4.9小时和1.6对1.2升·千克⁻¹)。尽管肝硬化患者的肾功能看似正常,但也观察到其氧氟沙星肾清除率降低。这些观察结果表明,代偿期肝硬化患者未代谢药物的药代动力学也可能发生改变。几乎所有受试者的血清浓度-时间曲线在给药后4-6小时出现第二个峰值。这种双峰行为被解释为氧氟沙星的肠肝循环或双相胃排空。