EFFECT OF SUCRALFATE ON ABSORPTION OF NORFLOXACIN AND OFLOXACIN

EFFECT OF SUCRALFATE ON ABSORPTION OF NORFLOXACIN AND OFLOXACIN
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DOI:
10.1128/aac.38.2.248
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发表时间:
1994-02-01
影响因子:
4.9
通讯作者:
KIVISTO, KT
KIVISTO, KT
中科院分区:
医学2区
文献类型:
--
作者:
LEHTO, P;KIVISTO, KT

文献摘要

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在两项独立的健康志愿者交叉研究中,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,8名受试者被随机分配到以下三种方案中的一种: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酸钠同时服用(1 g),或在服用硫糖酸钠前2小时服用诺氟沙星或氧氟沙星。同时使用硫糖酸钠可使诺氟沙星和氧氟沙星的生物利用度分别降低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,氟喹诺酮类药物的药代动力学均无明显变化。用从尿液中回收的每种氟喹诺酮类药物的累积量计算生物利用度,也得到了类似的结果。为了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。通过延长氟喹诺酮与前一次硫糖酸盐剂量之间的间隔时间,并在另一次硫糖酸盐剂量前至少2小时给予氟喹诺酮,可将相互作用降至最低。
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.