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依诺沙星在皮肤及皮肤结构感染和骨髓炎中的组织渗透及临床疗效综述。

Review of tissue penetration and clinical efficacy of enoxacin in skin and skin structure infections and in osteomyelitis.

作者信息

Pankey G A

机构信息

Department of Infectious Diseases, Ochsner Clinic, New Orleans, Louisiana.

出版信息

Clin Pharmacokinet. 1989;16 Suppl 1:46-51. doi: 10.2165/00003088-198900161-00008.

Abstract

Enoxacin achieves a high penetration into skin tissue and blister fluid, reaching a maximum serum concentration (Cmax) of 3.7 mg/L at a time to reach maximum concentration (tmax) of 1.9 hours and a blister-fluid Cmax of 2.9 mg/L at a tmax of 3.7 hours after an oral dose of 600 mg. The half-life of enoxacin is 6.2 hours in serum and 7.2 hours in blister fluid. In a multicentre, open, non-comparative trial, clinical cure or improvement in skin or skin structure infections was achieved after oral administration of enoxacin 200 to 600 mg twice daily in 88% of 196 evaluable patients. Overall satisfactory bacteriological response was obtained in 76% of patients. In a multicentre, randomised, double-blind trial comparing oral enoxacin 400 mg twice daily with cephalexin 500 mg twice daily, satisfactory clinical outcome was achieved in 92% of 73 evaluable patients receiving enoxacin and in 99% of 72 evaluable patients receiving cephalexin. Furthermore, there was no statistically significant difference between the bacteriological efficacy of the 2 agents. In 3 single-centre trials, satisfactory clinical results were achieved in 75 to 100% of patients, and satisfactory bacteriological results occurred in 47 to 76% of patients after administration of oral enoxacin 400 mg twice daily for 7 to 14 days. In vitro uptake of enoxacin in bone leads to a concentration of 300 micrograms/g, with 83% being retained by bone after 3 washings with saline at pH 7.2. Clinical trials involving oral enoxacin in osteomyelitis are currently under way.

摘要

依诺沙星在皮肤组织和水疱液中有较高的渗透率,口服600毫克后,达峰时间(tmax)为1.9小时时血清最大浓度(Cmax)为3.7毫克/升,达峰时间为3.7小时时水疱液Cmax为2.9毫克/升。依诺沙星在血清中的半衰期为6.2小时,在水疱液中为7.2小时。在一项多中心、开放、非对照试验中,196例可评估患者中,88%在每日两次口服200至600毫克依诺沙星后,皮肤或皮肤结构感染获得临床治愈或改善。76%的患者获得总体满意的细菌学反应。在一项多中心、随机、双盲试验中,将每日两次口服400毫克依诺沙星与每日两次口服500毫克头孢氨苄进行比较,73例接受依诺沙星治疗的可评估患者中有92%获得满意的临床结果,72例接受头孢氨苄治疗的可评估患者中有99%获得满意的临床结果。此外,两种药物的细菌学疗效之间无统计学显著差异。在3项单中心试验中,每日两次口服400毫克依诺沙星,连续7至14天,75%至100%的患者获得满意的临床结果,47%至76%的患者获得满意的细菌学结果。依诺沙星在骨中的体外摄取导致浓度达到300微克/克,用pH 7.2的盐水洗涤3次后,骨中保留83%。目前正在进行依诺沙星口服治疗骨髓炎的临床试验。

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