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硫糖铝对诺氟沙星和氧氟沙星吸收的影响。

Effect of sucralfate on absorption of norfloxacin and ofloxacin.

作者信息

Lehto P, Kivistö K T

机构信息

Department of Pharmacology, University of Turku, Finland.

出版信息

Antimicrob Agents Chemother. 1994 Feb;38(2):248-51. doi: 10.1128/AAC.38.2.248.

Abstract

The effect of sucralfate on the pharmacokinetics of norfloxacin and ofloxacin was assessed in two separate crossover studies with healthy volunteers. In both studies, eight subjects were randomized to one of the following three regimens: a 400-mg dose of norfloxacin or ofloxacin alone, norfloxacin or ofloxacin given simultaneously with sucralfate (1 g), or norfloxacin or ofloxacin given 2 h before sucralfate. Coadministration of sucralfate reduced the bioavailability of norfloxacin and ofloxacin by 91% (P < 0.001) and 61% (P < 0.001), respectively. However, when norfloxacin and ofloxacin were given 2 h before sucralfate, there were no significant alterations in the pharmacokinetics of either fluoroquinolone. Similar results were obtained when the cumulative amount of each fluoroquinolone recovered in the urine was used to calculate bioavailability. To avoid these interactions and potential therapeutic failures, norfloxacin and ofloxacin should not be used concurrently with sucralfate. The interaction can be minimized by maximizing the time between the fluoroquinolone dose and the previous sucralfate dose and giving the fluoroquinolone at least 2 h before another sucralfate dose.

摘要

在两项针对健康志愿者的独立交叉研究中,评估了硫糖铝对诺氟沙星和氧氟沙星药代动力学的影响。在这两项研究中,八名受试者被随机分配到以下三种治疗方案之一:单独服用400毫克诺氟沙星或氧氟沙星,诺氟沙星或氧氟沙星与硫糖铝(1克)同时服用,或在服用硫糖铝前2小时服用诺氟沙星或氧氟沙星。硫糖铝的共同给药分别使诺氟沙星和氧氟沙星的生物利用度降低了91%(P<0.001)和61%(P<0.001)。然而,当在服用硫糖铝前2小时给予诺氟沙星和氧氟沙星时,两种氟喹诺酮类药物的药代动力学均无显著改变。当用尿液中回收的每种氟喹诺酮类药物的累积量来计算生物利用度时,也得到了类似的结果。为避免这些相互作用和潜在的治疗失败,诺氟沙星和氧氟沙星不应与硫糖铝同时使用。通过使氟喹诺酮类药物剂量与上一次硫糖铝剂量之间的时间间隔最大化,并在下次硫糖铝剂量前至少2小时给予氟喹诺酮类药物,可将这种相互作用降至最低。

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Rev Infect Dis. 1988 Jan-Feb;10 Suppl 1:S132-6. doi: 10.1093/clinids/10.supplement_1.s132.
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