In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates
In vitro antibacterial activity of some antihistaminics belonging to different groups against multi-drug resistant clinical isolates
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DOI：
10.1590/s1517-83822011000300018
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发表时间：
2011-09-01
影响因子：
2.2
通讯作者：
El-Halfawy, Omar M
中科院分区：
文献类型：
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作者：
El-Nakeeb, Moustafa A;Abou-Shleib, Hamida M;El-Halfawy, Omar M
抗组胺药广泛用于微生物感染期间的各种适应症。因此，本文研究了10个抗组胺药属于老一代和新一代使用多重耐药革兰氏阳性和革兰氏阴性临床分离株的抗菌活性。采用肉汤稀释法和琼脂稀释法测定了抗组胺药对29株细菌的最低抑菌浓度（MIC）。氮卓斯汀、赛庚啶、美奎他嗪和异丙嗪是测试药物中活性最高的。苯海拉明和西替利嗪具有较弱的活性，而多西拉敏、非索非那定和氯雷他定即使在最高测试浓度（1 mg/ml）下也无活性。无法测定美克洛嗪的MIC，因为其与所用培养基发生沉淀。抗组胺药的MBC值与相应的MIC值几乎相同。抗组胺药的杀菌活性也进行了研究，在无菌生理盐水溶液中的活菌计数技术。美喹他嗪、美克洛嗪、氮卓斯汀和赛庚啶对小鼠有明显的杀伤作用。采用活菌计数法研究了氮卓斯汀在营养肉汤中的杀菌动力学。发现该活性具有浓度依赖性。增加接种量会降低这种效应，而增加pH值则会增加这种效应。还测定了100 μ g/ml氮卓斯汀的抗菌后效应，并达到3.36 h。
Antihistaminics are widely used for various indications during microbial infection. Hence, this paper investigates the antimicrobial activities of 10 antihistaminics belonging to both old and new generations using multiresistant Gram-positive and Gram-negative clinical isolates. The bacteriostatic activity of antihistaminics was investigated by determining their MIC both by broth and agar dilution techniques against 29 bacterial strains. Azelastine, cyproheptadine, mequitazine and promethazine were the most active among the tested drugs. Diphenhydramine and cetirizine possessed weaker activity whereas doxylamine, fexofenadine and loratadine were inactive even at the highest tested concentration (1 mg/ml). The MIC of meclozine could not be determined as it precipitated with the used culture media. The MBC values of antihistaminics were almost identical to the corresponding MIC values. The bactericidal activity of antihistaminics was also studied by the viable count technique in sterile saline solution. Evident killing effects were exerted by mequitazine, meclozine, azelastine and cyproheptadine. Moreover, the dynamics of bactericidal activity of azelastine were studied by the viable count technique in nutrient broth. This activity was found to be concentration-dependant. This effect was reduced on increasing the inoculum size while it was increased on raising the pH. The post-antimicrobial effect of 100 mu g/ml azelastine was also determined and reached up to 3.36 h.