注射用帕珠沙星的药理研究和临床应用

被引：58

作者：

杨信怡

游雪甫

机构：

[1] 中国医学科学院中国协和医科大学医药生物技术研究所

来源：

国外医药(抗生素分册) | 2003年 / 02期

关键词：

合成抗菌药; 帕珠沙星; 药效学研究;

D O I：

10.13461/j.cnki.wna.003840

中图分类号：

R96 [药理学];

学科分类号：

100602 ; 100706 ;

摘要：

注射用帕珠沙星为日本富山化学公司研制的一种新型喹诺酮类抗菌药制剂 ,属III型喹诺酮类药 ,作用靶位为细菌DNA促旋酶和拓扑异构酶VI。体内外研究表明帕珠沙星抗菌谱广 ,与受试的环丙沙星、头孢他啶、亚胺培南、庆大霉素等相比 ,对MRSA抗菌活性突出 ,抗革兰氏阴性菌活性优于头孢他啶、亚胺培南及庆大霉素 ,与环丙沙星相似 ,对部分厌氧菌亦有很强抗菌活性。对机体呼吸、循环、消化及神经各系统功能无明显影响 ,帕珠沙星对受试小鼠、大鼠、狗及猴的LD50 大于 2 60mg/kg体重 ,研究中所采用剂量下无长期毒性及生殖毒性表现。实验动物及人体内代谢研究表明帕珠沙星具有分布迅速 ,组织穿透力强 ,肾代谢为主 ,无蓄积作用等特点。临床研究表明 ,帕珠沙星对接受治疗的各科感染共 10 0 2例总有效率为 82 75 % ,总细菌清除率为 77 68%。不良反应及实验室检测异常发生率低 ,停药后恢复正常。

引用

页码：80 / 87

页数：8

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