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氧氟沙星的临床药代动力学。

Ofloxacin clinical pharmacokinetics.

作者信息

Lamp K C, Bailey E M, Rybak M J

机构信息

Department of Pharmacy Practice, College of Pharmacy and Allied Health Professions, School of Medicine, Wayne State University, Detroit, Michigan.

出版信息

Clin Pharmacokinet. 1992 Jan;22(1):32-46. doi: 10.2165/00003088-199222010-00004.

Abstract

Ofloxacin is a new fluoroquinolone with a spectrum of activity similar to other fluoroquinolones with activity which includes Chlamydia trachomatis, Mycobacterium spp., Mycoplasma spp. and Legionella pneumophila. Through its additional mechanisms of action, ofloxacin may be less susceptible to the development of resistance from Staphylococcus aureus commonly seen with currently available fluoroquinolones. The impact of these findings cannot be evaluated without further clinical experience. The pharmacokinetics of ofloxacin are characterised by almost complete bioavailability (95 to 100%), peak serum concentrations in the range of 2 to 3 mg/L after a 400mg oral dose and an average half-life of 5 to 8h. In comparison with other available quinolones, elimination is more highly dependent on renal clearance, which may lead to more frequent dosage adjustments in patients with impaired renal function. Ofloxacin appears less likely to affect the pharmacokinetics of drugs (e.g. theophylline) which commonly interact with fluoroquinolones such as ciprofloxacin and enoxacin. The properties of ofloxacin make it a therapeutic alternative to currently available fluoroquinolones.

摘要

氧氟沙星是一种新型氟喹诺酮类药物,其抗菌谱与其他氟喹诺酮类药物相似,抗菌活性包括沙眼衣原体、分枝杆菌属、支原体属和嗜肺军团菌。通过其额外的作用机制,氧氟沙星可能不太容易像目前可用的氟喹诺酮类药物那样容易出现对金黄色葡萄球菌耐药性的产生。如果没有进一步的临床经验,这些发现的影响就无法评估。氧氟沙星的药代动力学特征为生物利用度几乎完全(95%至100%),口服400mg剂量后血清峰值浓度在2至3mg/L范围内,平均半衰期为5至8小时。与其他可用的喹诺酮类药物相比,其消除更高度依赖于肾脏清除率,这可能导致肾功能受损患者需要更频繁地调整剂量。氧氟沙星似乎不太可能影响通常与氟喹诺酮类药物(如环丙沙星和依诺沙星)相互作用的药物(如茶碱)的药代动力学。氧氟沙星的这些特性使其成为目前可用氟喹诺酮类药物的一种治疗替代药物。

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