Respiratory Center, Asahikawa Medical College, 2-1-1-1 Midorigaoka Higashi, Asahikawa, Hokkaido 078-8510, Japan.
Int J Antimicrob Agents. 2010 Jun;35(6):603-5. doi: 10.1016/j.ijantimicag.2010.01.020. Epub 2010 Mar 6.
The pharmacokinetics of the new oral des-fluoroquinolone antimicrobial garenoxacin (GRNX) was investigated in elderly patients with respiratory tract infections. Patients were treated with GRNX (200 mg or 400 mg) once daily for 7 days. Plasma GRNX concentrations were determined and pharmacokinetic parameters were estimated by Bayesian predictions using reported population pharmacokinetic parameters. At each dose, the maximum plasma concentration (C(max)) and the area under the concentration-time curve (AUC) were comparable with those reported in young subjects, except that the estimated C(max) and AUC values in one patient receiving the 200 mg dose whose body weight and creatinine clearance rate (CL(Cr)) were 38 kg and 17 mL/min, respectively, were higher than those of the other patients given 200 mg GRNX and were comparable with those of patients who received the 400mg dose. These results suggest that the recommended dose of GRNX should be 400 mg for most elderly and young patients, but only 200 mg in patients whose body weight and CL(Cr) are < 40 kg and < 30 mL/min, respectively.
新的口服去氟喹诺酮类抗菌药加替沙星(GRNX)的药代动力学在患有呼吸道感染的老年患者中进行了研究。患者接受 GRNX(200mg 或 400mg)每日一次,共 7 天。通过报告的群体药代动力学参数的贝叶斯预测来确定血浆 GRNX 浓度,并估算药代动力学参数。在每个剂量下,最大血浆浓度(C(max))和浓度-时间曲线下面积(AUC)与年轻受试者报告的结果相当,除了接受 200mg 剂量的一位患者的估计 C(max)和 AUC 值,其体重和肌酐清除率(CL(Cr))分别为 38kg 和 17mL/min,高于接受 200mg GRNX 的其他患者,与接受 400mg 剂量的患者相当。这些结果表明,对于大多数老年和年轻患者,GRNX 的推荐剂量应为 400mg,但对于体重和 CL(Cr)分别<40kg 和<30mL/min 的患者,剂量应为 200mg。