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所选吩噻嗪类镇静剂和抗组胺药对细菌细胞的比较作用以及与抗生素的可能相互作用。

Comparative effects of selected phenothiazine tranquilizers and antihistaminics on bacterial cells and possible interactions with antibiotics.

作者信息

Shibl A M, Hammouda Y, Al-Sowaygh I

出版信息

J Pharm Sci. 1984 Jun;73(6):841-3. doi: 10.1002/jps.2600730638.

DOI:10.1002/jps.2600730638
PMID:6145789
Abstract

Evaluation of the antibacterial effect of phenothiazine antihistaminics (trimeprazine, promethazine, and fonazine) and phenothiazine tranquilizers (promazine, chlorpromazine, triflupromazine, and propiomazine) on Staphylococcus aureus showed that tranquilizers were more active [minimum inhibitory concentration (MIC) 0.5-1.6 micrograms/mL] than antihistaminics (MIC greater than 1.6 micrograms/mL). The antibacterial activity was found to correlate with both the rate of adsorption of these drugs on the bacterial cells and the surface tension of their solutions. Phenothiazine tranquilizers caused rapid and extensive leakage of potassium ions from bacterial cells, while phenothiazine antihistaminics produced relatively slower leakage of these ions. A study of the effect of the phenothiazines on the antibacterial activity of some antibiotics showed that all phenothiazines produced a synergistic effect with erythromycin and an antagonistic effect with tobramycin. Variable effects were observed with chloramphenicol, and no effect was observed with penicillin. Results were explained on the basis of structural characteristics of the phenothiazines.

摘要

对吩噻嗪类抗组胺药(曲美苄嗪、异丙嗪和福那嗪)及吩噻嗪类镇静剂(丙嗪、氯丙嗪、三氟拉嗪和丙酰马嗪)对金黄色葡萄球菌的抗菌效果评估显示,镇静剂比抗组胺药更具活性[最低抑菌浓度(MIC)为0.5 - 1.6微克/毫升],而抗组胺药的MIC大于1.6微克/毫升。研究发现抗菌活性与这些药物在细菌细胞上的吸附速率及其溶液的表面张力均相关。吩噻嗪类镇静剂可导致细菌细胞快速且大量地泄漏钾离子,而吩噻嗪类抗组胺药使这些离子泄漏的速度相对较慢。对吩噻嗪类药物对某些抗生素抗菌活性影响的研究表明,所有吩噻嗪类药物与红霉素产生协同效应,与妥布霉素产生拮抗效应。对氯霉素观察到了不同的效应,对青霉素则未观察到效应。研究结果基于吩噻嗪类药物的结构特征进行了解释。

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Comparative effects of selected phenothiazine tranquilizers and antihistaminics on bacterial cells and possible interactions with antibiotics.所选吩噻嗪类镇静剂和抗组胺药对细菌细胞的比较作用以及与抗生素的可能相互作用。
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