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氟喹诺酮类抗生素:该类及各药物的特性

Fluoroquinolone antibiotics: properties of the class and individual agents.

作者信息

Stratton C

机构信息

Department of Pathology, Vanderbilt University Medical Center, Nashville, Tennessee.

出版信息

Clin Ther. 1992 May-Jun;14(3):348-75; discussion 347.

PMID:1638577
Abstract

The broad spectrum of activity and bactericidal nature of the fluoroquinolones, together with their excellent absorption, rapid distribution, and high tissue concentration, make them excellent therapeutic agents for the management of a number of complicated community-acquired and nosocomial infections of the urinary tract, bone and soft tissue, gastrointestinal tract, and prostate, as well as some respiratory tract infections and sexually transmitted diseases. Data are presented and reviewed concerning the in vitro activity, pharmacology, and clinical use of ciprofloxacin, norfloxacin, and ofloxacin, which have been available for some time, and lomefloxacin and temafloxacin, which are recently approved agents. The comparable qualities and differences in activity and clinical applications of these agents are considered. For many infections in selected patients, quinolones are excellent substitutes for parenteral agents. In general, adverse effects have been infrequent and rarely require drug discontinuation. Significant interactions, such as with theophylline and caffeine, have occurred but are quinolone dependent. Antacids can markedly impair the absorption of all quinolones. Because emerging resistance to Pseudomonas and Staphylococcus species have been observed, the improper use of the quinolones must be avoided, and the clinician must be aware that an unfavorable response may signal resistance. The development of future agents with better gram-positive activity, improved gram-negative coverage, and activity against unusual pathogens such as Chlamydia species and Mycobacterium species, will make these oral agents invaluable. Assessing the usefulness and safety of these antibiotics in children is an ongoing challenge.

摘要

氟喹诺酮类药物具有广泛的抗菌活性和杀菌特性,再加上其吸收良好、分布迅速且组织浓度高,使其成为治疗多种复杂的社区获得性和医院内感染的理想药物,这些感染包括泌尿系统、骨骼和软组织、胃肠道、前列腺感染,以及一些呼吸道感染和性传播疾病。本文展示并综述了环丙沙星、诺氟沙星和氧氟沙星(已上市一段时间)以及洛美沙星和替马沙星(最近获批的药物)的体外活性、药理学和临床应用数据。文中还考虑了这些药物在活性和临床应用方面的相似之处和差异。对于特定患者的许多感染,喹诺酮类药物是胃肠外用药的理想替代品。总体而言,不良反应并不常见,很少需要停药。虽然已经出现了与茶碱和咖啡因等药物的显著相互作用,但这取决于喹诺酮类药物的种类。抗酸剂会显著损害所有喹诺酮类药物的吸收。由于已观察到对铜绿假单胞菌和葡萄球菌属出现新的耐药性,必须避免喹诺酮类药物的不当使用,临床医生必须意识到不良反应可能表明出现了耐药性。开发具有更好的革兰氏阳性菌活性、更强的革兰氏阴性菌覆盖范围以及对衣原体属和分枝杆菌属等不常见病原体有活性的新型药物,将使这些口服药物具有极高的价值。评估这些抗生素在儿童中的有效性和安全性仍然是一项持续的挑战。

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