甲磺酸培氟沙星和氧氟沙星对氨茶碱药动学的影响

EFFECTS OF PEFLOXACIN AND OFLOXACIN ON THE PHARMACOKINETICS OF THEOPHYLLINE

本文量化研究,12例患者口服Theo100mg/8h,d4起Ⅰ组(6例)加服PFLX400mg/12h,Ⅱ组(6例)加服OFLX400mg/12h,至d9,以高效液相色谱法平行监测伍用前后Theo的经时浓度,拟合Theo药动学参数并做统计学处理。结果:Ⅰ组血清中Theo浓度显著增高(P<0.05),消除t_(1/2)非常显著性延长(P<0.01),清除率显著下降(P<O.05);Ⅱ组血清中Theo浓度也相应增加,消除t_(1/2)及清除率均相应减少,但无统计学意义(P>0.05)。实验证明,PFLX对Theo的消除动力学有显著性影响,临床伍用时应对Theo血药浓度作监测,防止Theo因代谢减慢而引起中毒。OFLX与Theo伍用相对安全。

The effects of pefloxacin(PFLX) and ofloxacin(OFLX) on the pharmacokinetics of theo-phylline and their clinical significance were studied quantitatively. 12 patients were orally given theo-phylline 100mg per 8 hours for 9 days. And then the group I ( n =6) received PFLX 400mg per 12hours, while groupⅡ( n=6) added OFLX 400mg per 12 hours from the fourthday to the ninth day. The serum concentrations of theophylline were determined by HPLC. The pharmacokinetic parameters and statistical analysis were performed with computer. The results showed that the serum concentrations of theophylline of group I were increased, the elimination ratio was significantly decreased ( P < 0.05) , and the elimination half- life was markedly prolonged ( P < 0.01) .The serum concentrations of theo-phylline of group Ⅱ were increased, the elimination ratio and elimination half - life were not decreased ( P > 0.05). Conclusion: The effects of PFLX on the pharmacokinetics of elimination phase of theophylline are prominent in human, and the monitoring of the serum concen - tration of theophylline is critical while administered concomitantly with PFLX in order to prevent poisoning due to the slowdown of metabolism of theophylline. The combination of OFLX and theophylline is relatively safe.