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分别静脉注射4克阿莫西林和1克氟氯西林后的药代动力学。

Pharmacokinetics of amoxicillin and flucloxacillin following the simultaneous intravenous administration of 4 g and 1 g, respectively.

作者信息

Adam D, Koeppe P, Heilmann H D

出版信息

Infection. 1983 May-Jun;11(3):150-4. doi: 10.1007/BF01641294.

DOI:10.1007/BF01641294
PMID:6885174
Abstract

The combination of amoxicillin and flucloxacillin not only widens the spectrum of pathogenic organisms covered by either of the substances alone; synergy has also been observed, particularly against beta-lactamase-producing organisms. For this reason, the possible interaction of these two penicillins regarding their pharmacokinetics was investigated with respect to therapeutic application. The parameters were calculated on the basis of an open two-compartment model. The highest serum levels of amoxicillin from 551 to 1074 mg/l when 4 g were administered alone, and from 403 to 1133 mg/l when administered together with 1 g flucloxacillin. Flucloxacillin concentrations ranged from 118 to 357 mg/l when administered alone, and from 151 to 226 mg/l in the presence of amoxicillin. Thus, there is no significant difference in the peak levels of either substance when given alone or in combination. The pharmacokinetic parameters of both substances basically do not depend on the presence of the other. A slight decrease was observed in the distribution rate of amoxicillin from the central to the peripheral compartment in the presence of flucloxacillin. Its relevance is questionable, however, since the effect was only minor.

摘要

阿莫西林和氟氯西林联合使用不仅拓宽了单一药物所覆盖的致病生物体谱;还观察到了协同作用,尤其是针对产生β-内酰胺酶的生物体。因此,针对治疗应用,研究了这两种青霉素在药代动力学方面可能的相互作用。这些参数是基于开放的二室模型计算得出的。单独给予4g阿莫西林时,血清最高水平为551至1074mg/l,与1g氟氯西林合用时为403至1133mg/l。单独给予氟氯西林时,其浓度范围为118至357mg/l,在有阿莫西林存在时为151至226mg/l。因此,单独给药或联合给药时,两种药物的峰值水平均无显著差异。两种药物的药代动力学参数基本上不依赖于另一种药物的存在。在有氟氯西林存在的情况下,观察到阿莫西林从中央室到外周室的分布速率略有下降。然而,其相关性值得怀疑,因为这种影响很小。

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The in vitro and in vivo antibacterial activity of amoxicillin-flucloxacillin combination (1:1 ratio).阿莫西林-氟氯西林组合(1:1比例)的体外和体内抗菌活性。
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β-内酰胺类抗菌药物药代动力学在婴幼儿到老年人的年龄阶段的变化。
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Penicillinase-resistant antibiotics induce non-immune-mediated cholestasis through HSP27 activation associated with PKC/P38 and PI3K/AKT signaling pathways.青霉素酶抗性抗生素通过 HSP27 激活诱导非免疫介导的胆汁淤积,该激活与 PKC/P38 和 PI3K/AKT 信号通路有关。
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Minerva Med. 1977 Mar 24;68(14):917-28.
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Chemotherapy. 1979;25(1):30-9. doi: 10.1159/000237819.