Montay G, Goueffon Y, Roquet F
Antimicrob Agents Chemother. 1984 Apr;25(4):463-72. doi: 10.1128/AAC.25.4.463.
Pefloxacin mesylate is well absorbed by the oral route. The antimicrobial activity in dog, cynomolgus monkey, and human plasma was essentially due to unchanged drug which respectively accounted for 64, 94, and 84% of the total activity (ratios derived from relative area under the curve [AUC] values). Half-lives ranged from 1.9 h in mice to 8.6 h in humans. Protein binding was weak, about 20% in plasma. Except in brain, concentrations in most of the organs and tissues tested in rats and dogs were higher than the plasma levels. Microbiological activity in urine was mainly due to pefloxacin and norfloxacin, the N-desmethyl metabolite. The norfloxacin/pefloxacin ratios were 0 in mice, ca. 1 in rats and dogs, 1.6 in cynomolgus monkeys, and 2.3 in humans. The principal urinary compounds were unchanged drug in mice, pefloxacin glucuronide and pefloxacin N-oxide in rats and dogs, norfloxacin and pefloxacin in monkeys, and pefloxacin N-oxide and norfloxacin in humans. The urinary recovery of identified metabolites was 29.5% of the dose in mice, 37.8% in rats, 36.3% in dogs, 26.5% in monkeys, and 58.9% in humans. Biliary excretion occurred and was extensive in rats and dogs, mainly as a glucuronide conjugate of the drug. In rat and human bile, the main active compound was unchanged pefloxacin.
甲磺酸培氟沙星口服吸收良好。在犬、食蟹猴和人血浆中的抗菌活性主要归因于原形药物，其分别占总活性的64%、94%和84%（该比例由相对曲线下面积[AUC]值得出）。半衰期范围从小鼠的1.9小时至人的8.6小时。蛋白结合较弱，血浆中约为20%。除脑外，在大鼠和犬中所检测的大多数器官和组织中的浓度均高于血浆水平。尿液中的微生物活性主要归因于培氟沙星和N -去甲基代谢产物诺氟沙星。诺氟沙星/培氟沙星的比例在小鼠中为0，在大鼠和犬中约为1，在食蟹猴中为1.6，在人中为2.3。主要的尿中化合物在小鼠中为原形药物，在大鼠和犬中为培氟沙星葡萄糖醛酸苷和培氟沙星N -氧化物，在猴中为诺氟沙星和培氟沙星，在人中为培氟沙星N -氧化物和诺氟沙星。所鉴定代谢产物的尿回收率在小鼠中为剂量的29.5%，在大鼠中为37.8%，在犬中为36.3%，在猴中为26.5%，在人中为58.9%。胆汁排泄存在，且在大鼠和犬中广泛，主要以药物的葡萄糖醛酸苷缀合物形式存在。在大鼠和人胆汁中，主要的活性化合物为原形培氟沙星。
