Mikamo Hiroshige, Tanaka Kaori, Watanabe Kunitomo
Life Science Research Center, Gifu University.
Jpn J Antibiot. 2006 Dec;59(6):468-73.
We investigated the efficacies of various administration methods for levofloxacin (LVFX) and tosufloxacin (TFLX) against 161 isolates of Streptococcus pneumoniae and 309 isolates of Haemophilus influenzae isolated in Gifu prefecture, using Monte Carlo simulation. The pharmacokinetic parameters of the fluoroquinolones were calculated from changes in blood concentration in healthy adults. Monte Carlo simulation was performed for 1,000 times to determine the AUC/MIC target attainment rates for various administration methods for fluoroquinolones (LVFX: 100 mgx3, 200 mgx2, 500 mgx 1, TFLX: 150 mgx3, 300 mgx2) with Crystal Ball 7. For S. pneumoniae, target attainment rates ofAUC/MIC; 30 were 47.18%, 75.54%, 89.16%, 93.63% and 98.63% for LVFX 100mgx3, LVFX 200mgx2, LVFX 500mgxl, TFLX 150mgx3 and TFLX 300mgx2, respectively. For H. influenzae, target attainment rates of AUC/MIC; 125 were 99.20%, 99.05%, 99.54%, 99.66% and 100% for LVFX 100mgx3, LVFX 200mgx2, LVFX 500mgxl, TFLX 150mgx3 and TFLX 300mgx2, respectively. These results suggest that administration methods might have a large impact on the efficacy of treatment with oral fluoroquinolones, and to determine administration method based on PK/PD would be important in clinical practices.
我们采用蒙特卡洛模拟法,研究了左氧氟沙星(LVFX)和妥舒沙星(TFLX)不同给药方式对岐阜县分离出的161株肺炎链球菌和309株流感嗜血杆菌的疗效。根据健康成年人血药浓度变化计算氟喹诺酮类药物的药代动力学参数。使用Crystal Ball 7对氟喹诺酮类药物(LVFX:100mg×3、200mg×2、500mg×1,TFLX:150mg×3、300mg×2)的不同给药方式进行1000次蒙特卡洛模拟,以确定AUC/MIC目标达成率。对于肺炎链球菌,LVFX 100mg×3、LVFX 200mg×2、LVFX 500mg×1、TFLX 150mg×3和TFLX 300mg×2的AUC/MIC≥30的目标达成率分别为47.18%、75.54%、89.16%、93.63%和98.63%。对于流感嗜血杆菌,LVFX 100mg×3、LVFX 200mg×2、LVFX 500mg×1、TFLX 150mg×3和TFLX 300mg×2的AUC/MIC≥125的目标达成率分别为99.20%、99.05%、99.54%、99.66%和100%。这些结果表明,给药方式可能对口服氟喹诺酮类药物的治疗效果有很大影响,在临床实践中基于PK/PD确定给药方式很重要。