氟喹诺酮类与氨茶碱相互作用的基础与临床研究  

Experimental and Clinical Studies on Drug Interactions between Fluoroquinolones and Aminophylline

作　　者：王建刚[1] 李艳[1] 吴银屏 岳苏华 路西明[1] 李转珍[1] 谢秀娟[1] 

机构地区：[1]洛阳医学高等专科学校药理学教研室

出　　处：《河南医学研究》1998年第2期107-110,共4页Henan Medical Research

基　　金：河南省医学科学院科研基金

摘　　要：目的：系统研究氟喹诺酮类抗菌药物与氨茶碱在动物及健康人体内产生相互作用的程度及其机制。方法：用６０只小鼠进行氟喹诺酮类对小鼠异戊巴比妥催眠作用的影响实验；在家兔和健康人体内氟喹诺酮类对氨茶碱动力学影响的实验。结果：氟哌酸、氟嗪酸能缩短异戊巴比妥诱导小鼠睡眠的时间；丙氟哌酸、氟啶酸能延长睡眠时间，且丙氟哌酸的抑制作用较强。在家兔的实验结果显示氟哌酸、氟嗪酸、氟啶酸可缩短氨茶碱的血浆半衰期。结论：氟喹诺酮类抗菌药物对氨茶碱在肝药酶的代谢性质不同且程度不同。Objective: We study systematically the drug interaction between fluoroquinolones and aminophylling.Methods: The effect of fluoquinolones on the sleeping time of mice caused by amobarbital,and the effect of four fluoroquinolone on pharmacokinetics of aminophylline in rabbits,as well as the effect of three fluoroquinolones on pharmacokinetics of aminophylline in healthy volunteers.Results: Norfloxacin and ofloxacin shortened the sleeping time of mice caused by amobarbital by 44.1% (P<0.05) and 25.6% (P>0.05),respectively,while ciproxacin and enoxain prolonged the time by 92.7%(P<0.01) and 25.6%(P>0.05),respectively.The results in rabbits showed that norfloxacin,ofloxacin and enoxacin decreased half time (T1/2) of aminophylline by 22.2%,37.7%,and 14.4%,respectively,but ciprofloxacin increased T1/2 of aminophylline by 15.6%.It suggested that norfloxacin and ofloxacin may induced hepatic microsomal enzyme,but enoxain also induced the enzyme,which differ in experiment result in mice.In healthy human,the results showed ofloxacin decreased T1/2 of aminophylline by 5% (P>0.05),but ciproxacin and enoxacin increased T1/2 by 151%(P>0.05) and 38% (P>0.05),respectively.We also found that in healthy human ciprofloxacin decreased peak concentration of aminophylline by 53% when given orally and simultaeously.Conclusion: The effect of fluoroxacins on hepatic microsomal enzyme differ not only in quality but also in quantity.As results,it was necessary to adjust the dosage of aminophylline given with fluoroquinolones.

关 键 词：氟哌酸 氟嗪酸 丙氟哌酸 氟啶酸 药物相互作用 

分 类 号：R978.1[医药卫生—药品] R969.2[医药卫生—药学]