Martin S J, Meyer J M, Chuck S K, Jung R, Messick C R, Pendland S L
Department of Pharmacy Practice, College of Pharmacy, University of Toledo, OH 43606, USA.
Ann Pharmacother. 1998 Mar;32(3):320-36. doi: 10.1345/aph.17178.
To discuss the pharmacology, pharmacokinetics, spectrum of activity, clinical trials, and adverse effects of levofloxacin and sparfloxacin, two new fluoroquinolone antibiotics.
Literature was identified by a MEDLINE search from January 1985 to September 1997. Abstracts and presentations were identified by review of program abstracts from the Interscience Conference on Antimicrobial Agents and Chemotherapy from 1988 to 1996.
Randomized, controlled clinical studies were selected for evaluation; however, uncontrolled studies were included when data were limited for indications approved by the Food and Drug Administration (FDA). In vitro data were selected from comparison trials whenever available. Only in vitro trials that provided data on the minimum inhibitory concentrations required to inhibit 90% of isolates were used. Data from North American studies were selected whenever available.
Data were evaluated with respect to in vitro activity, study design, clinical and microbiologic outcomes, and adverse drug reactions.
Levofloxacin and sparfloxacin are active against pathogens frequently involved in community-acquired upper and lower respiratory tract infections, including Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Mycoplasma pneumoniae, Legionella pneumophila, and Chlamydia pneumoniae. Both compounds have enhanced activity compared with ciprofloxacin against most gram-positive bacteria, including enterococci, streptococci, and staphylococci, and retain good activity against most Enterobacteriaceae and Pseudomonas aeruginosa. Sparfloxacin has greater anaerobic activity than levofloxacin, which is more active than ciprofloxacin or ofloxacin. Although many clinical studies are available only in abstract form, the clinical data demonstrate that these new quinolones are effective for most community-acquired upper and lower respiratory tract infections, urinary tract infections, gonococcal and nongonococcal urethritis, and skin and skin structure infections. FDA-approved indications are limited for both compounds to date.
Levofloxacin and sparfloxacin have improved gram-positive activity compared with that of older fluoroquinolones, and are administered once daily. Sparfloxacin-associated photosensitivity may limit its therapeutic usefulness. Clinical trials confirm that these agents are as effective as traditional therapies for the management of community-acquired pneumonia, acute exacerbations of chronic bronchitis, sinusitis, urinary tract infections, acute gonococcal and nongonococcal urethritis, and skin and skin structure infections.
探讨两种新型氟喹诺酮类抗生素左氧氟沙星和司帕沙星的药理学、药代动力学、活性谱、临床试验及不良反应。
通过检索1985年1月至1997年9月的MEDLINE数据库获取文献。通过查阅1988年至1996年抗菌药物和化疗跨学科会议的会议摘要确定摘要和报告。
选择随机对照临床研究进行评估;然而,当食品药品监督管理局(FDA)批准的适应证数据有限时,纳入非对照研究。如有可用数据,从比较试验中选择体外数据。仅使用提供抑制90%分离株所需最低抑菌浓度数据的体外试验。如有可用数据,选择北美研究的数据。
对数据的体外活性、研究设计、临床和微生物学结果以及药物不良反应进行评估。
左氧氟沙星和司帕沙星对社区获得性上、下呼吸道感染常见病原体具有活性,包括肺炎链球菌、流感嗜血杆菌、卡他莫拉菌、肺炎支原体、嗜肺军团菌和肺炎衣原体。与环丙沙星相比,这两种化合物对大多数革兰氏阳性菌(包括肠球菌、链球菌和葡萄球菌)的活性增强,对大多数肠杆菌科细菌和铜绿假单胞菌仍保持良好活性。司帕沙星的厌氧活性比左氧氟沙星更强,左氧氟沙星比环丙沙星或氧氟沙星更具活性。尽管许多临床研究仅有摘要形式,但临床数据表明,这些新型喹诺酮类药物对大多数社区获得性上、下呼吸道感染、尿路感染、淋菌性和非淋菌性尿道炎以及皮肤和皮肤结构感染有效。迄今为止,这两种化合物的FDA批准适应证均有限。
与较老的氟喹诺酮类药物相比,左氧氟沙星和司帕沙星的革兰氏阳性菌活性有所提高,且每日给药一次。司帕沙星相关的光敏反应可能会限制其治疗用途。临床试验证实,这些药物在治疗社区获得性肺炎、慢性支气管炎急性加重、鼻窦炎、尿路感染、急性淋菌性和非淋菌性尿道炎以及皮肤和皮肤结构感染方面与传统疗法一样有效。