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依诺沙星。对其抗菌活性、药代动力学特性及治疗用途的综述。

Enoxacin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

作者信息

Henwood J M, Monk J P

机构信息

ADIS Drug Information Services, Manchester, England.

出版信息

Drugs. 1988 Jul;36(1):32-66. doi: 10.2165/00003495-198836010-00004.

DOI:10.2165/00003495-198836010-00004
PMID:3063494
Abstract

Enoxacin is a new addition to the class of 4-quinolone antibacterial drugs. It has a broad spectrum of in vitro antibacterial activity, and is particularly potent against Gram-negative organisms and staphylococci. The pharmacokinetic profile of enoxacin is similar to that of ofloxacin, achieving higher plasma and tissue concentrations and possessing a longer half-life than norfloxacin or ciprofloxacin. In comparative studies, clinical and/or bacteriological efficacy was comparable or (in studies which statistically analysed the results) not significantly different between enoxacin and amoxycillin in acute cystitis, acute Gram-negative exacerbations of chronic bronchitis and acute or chronic otitis media, between enoxacin and cephalexin in skin, skin structure and soft tissue infections, between enoxacin and trimethoprim in acute cystitis, between enoxacin and co-trimoxazole in complicated urinary tract infection and between enoxacin and pipemidic acid in suppurative otitis media. Significantly (p less than 0.01) more clinical and/or bacteriological cures were effected by enoxacin than pipemidic acid in acute cystitis and complicated urinary tract infection. In uncomplicated gonococcal infections single oral doses of enoxacin were effective in over 90% of patients. Enoxacin is a well-tolerated, orally active broad spectrum antibacterial drug which should prove a worthwhile alternative to currently available antibacterial therapy.

摘要

依诺沙星是4-喹诺酮类抗菌药物中的新成员。它具有广泛的体外抗菌活性,对革兰氏阴性菌和葡萄球菌尤其有效。依诺沙星的药代动力学特征与氧氟沙星相似,血浆和组织浓度更高,半衰期比诺氟沙星或环丙沙星更长。在比较研究中,在急性膀胱炎、慢性支气管炎急性革兰氏阴性菌加重以及急性或慢性中耳炎方面,依诺沙星与阿莫西林的临床和/或细菌学疗效相当或(在对结果进行统计分析的研究中)无显著差异;在皮肤、皮肤结构和软组织感染方面,依诺沙星与头孢氨苄相当;在急性膀胱炎方面,依诺沙星与甲氧苄啶相当;在复杂性尿路感染方面,依诺沙星与复方新诺明相当;在化脓性中耳炎方面,依诺沙星与吡哌酸相当。在急性膀胱炎和复杂性尿路感染中,依诺沙星实现的临床和/或细菌学治愈显著(p小于0.01)多于吡哌酸。在单纯性淋菌感染中,单次口服依诺沙星对超过90%的患者有效。依诺沙星是一种耐受性良好、口服有效的广谱抗菌药物,应该会被证明是现有抗菌治疗的一个有价值的替代药物。

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Comparative in vitro activities of ten antimicrobial agents against bacterial enteropathogens.十种抗菌剂对细菌性肠道病原体的体外活性比较
Antimicrob Agents Chemother. 1983 Oct;24(4):509-13. doi: 10.1128/AAC.24.4.509.
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Serum and sputum concentrations of enoxacin after single oral dosing in a clinical and bacteriological study.在一项临床和细菌学研究中单次口服给药后依诺沙星的血清和痰液浓度。
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3
The activity of enoxacin against clinical bacterial isolates in comparison with that of five other agents, and factors affecting that activity.
揭示治疗潜力:针对牙髓感染中[具体细菌名称]的脂多糖生物合成进行计算机模拟筛选研究
Int J Mol Sci. 2024 Apr 11;25(8):4239. doi: 10.3390/ijms25084239.
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Modulating microRNA Processing: Enoxacin, the Progenitor of a New Class of Drugs.调节 microRNA 加工:依诺沙星,一类新药的前体。
J Med Chem. 2020 Nov 12;63(21):12275-12289. doi: 10.1021/acs.jmedchem.0c00510. Epub 2020 Jul 30.
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Vacuolar H-ATPases (V-ATPases) as therapeutic targets: a brief review and recent developments.液泡型H⁺-ATP酶(V-ATP酶)作为治疗靶点:简要综述与最新进展
Biotarget. 2017 Dec;1. doi: 10.21037/biotarget.2017.12.01. Epub 2017 Dec 13.
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Oral Bioavailability and Plasma Disposition of Pefloxacin in Healthy Broiler Chickens.培氟沙星在健康肉鸡中的口服生物利用度及血浆处置情况
Front Vet Sci. 2017 May 24;4:77. doi: 10.3389/fvets.2017.00077. eCollection 2017.
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Rational identification of enoxacin as a novel V-ATPase-directed osteoclast inhibitor.合理鉴定依诺沙星为新型 V-ATPase 靶向性破骨细胞抑制剂。
Curr Protein Pept Sci. 2012 Mar;13(2):180-91. doi: 10.2174/138920312800493151.
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Enoxacin: a reappraisal of its clinical efficacy in the treatment of genitourinary tract infections.依诺沙星:对其治疗泌尿生殖道感染临床疗效的重新评估。
Drugs. 1996 Jan;51(1):137-60. doi: 10.2165/00003495-199651010-00009.
9
Enoxacin relieves symptoms of recurrent urinary infections more rapidly than cefuroxime axetil.依诺沙星比头孢呋辛酯更迅速地缓解复发性尿路感染的症状。
Antimicrob Agents Chemother. 1993 Jul;37(7):1558-9. doi: 10.1128/AAC.37.7.1558.
10
Fluoroquinolone antibiotics. Microbiology, pharmacokinetics and clinical use.氟喹诺酮类抗生素。微生物学、药代动力学及临床应用。
Drugs. 1988 Aug;36(2):193-228. doi: 10.2165/00003495-198836020-00004.
J Antimicrob Chemother. 1984 Sep;14 Suppl C:7-17. doi: 10.1093/jac/14.suppl_c.7.
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Diffusion of enoxacin into the cerebrospinal fluid in dogs with healthy meninges and with experimental meningitis.
J Antimicrob Chemother. 1984 Sep;14 Suppl C:57-62. doi: 10.1093/jac/14.suppl_c.57.
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Enoxacin: worldwide in-vitro activity against 22451 clinical isolates.
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In vitro activities of enoxacin and 17 other antimicrobial agents against multiply resistant, gram-negative bacteria.依诺沙星及其他17种抗菌剂对多重耐药革兰氏阴性菌的体外活性
Antimicrob Agents Chemother. 1984 Jul;26(1):97-100. doi: 10.1128/AAC.26.1.97.
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In-vitro activity of enoxacin (CL-919), a new quinoline derivative, compared with that of other antimicrobial agents.新喹啉衍生物依诺沙星(CL-919)的体外活性与其他抗菌剂的比较。
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A double blind study comparing two dosages of enoxacin for the treatment of uncomplicated urogenital gonorrhoea.一项比较两种剂量依诺沙星治疗单纯性泌尿生殖系统淋病的双盲研究。
J Antimicrob Chemother. 1984 Sep;14 Suppl C:91-4. doi: 10.1093/jac/14.suppl_c.91.