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洛美沙星的临床药代动力学。

Lomefloxacin clinical pharmacokinetics.

作者信息

Freeman C D, Nicolau D P, Belliveau P P, Nightingale C H

机构信息

Department of Pharmacy, Hartford Hospital, Connecticut.

出版信息

Clin Pharmacokinet. 1993 Jul;25(1):6-19. doi: 10.2165/00003088-199325010-00002.

Abstract

Lomefloxacin is a quinolone antibiotic with chemical and microbiological properties similar to most commercially available agents of this class. There are differences, however, between lomefloxacin and other quinolones in activity against specific micro-organisms, a situation that is typical of most antibiotic classes. The pharmacokinetics of lomefloxacin support once- or twice-daily dosage, depending on the pathogen or site of infection. This is a result of its relatively high serum concentrations and long half-life. The outstanding pharmacokinetic features of lomefloxacin are its high degree of tissue distribution, lack of significant metabolism (and, therefore, no competitive drug interactions with other metabolised drugs showing a common metabolic pathway), and good oral absorption. Like most fluoroquinolones, lomefloxacin can chelate with heavy metals. However, this interaction can be eliminated by administering lomefloxacin 2h before the cation-containing products. Dosage adjustments are required in patients with renal dysfunction. However, patients with liver disease do not require alterations in lomefloxacin dosage regimens. The safety profile, lack of significant drug interactions and convenience of administration make lomefloxacin a useful agent in specific clinical settings.

摘要

洛美沙星是一种喹诺酮类抗生素,其化学和微生物学特性与该类大多数市售药物相似。然而,洛美沙星与其他喹诺酮类药物在对特定微生物的活性方面存在差异,这种情况在大多数抗生素类别中都很典型。洛美沙星的药代动力学支持每日一次或两次给药,具体取决于病原体或感染部位。这是其相对较高的血清浓度和较长半衰期的结果。洛美沙星突出的药代动力学特征是其高度的组织分布、缺乏显著的代谢(因此,与其他通过共同代谢途径代谢的药物无竞争性药物相互作用)以及良好的口服吸收。与大多数氟喹诺酮类药物一样,洛美沙星可与重金属螯合。然而,这种相互作用可通过在含阳离子产品给药前2小时给予洛美沙星来消除。肾功能不全患者需要调整剂量。然而,肝病患者不需要改变洛美沙星的给药方案。其安全性、缺乏显著的药物相互作用以及给药便利性使洛美沙星在特定临床环境中成为一种有用的药物。

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