In vitro activity of sparfloxacin compared with those of five other quinolones

Cantón, Emilia; Pemán, Javier; Jimenez, M T; Ramon, M S; Gobernado, M

doi:10.1128/aac.36.3.558

Cited by 64 publications

(37 citation statements)

References 15 publications

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“…Widely-used fluoroquinolones, such as ciprofloxacin and ofloxacin, have excellent activity against Gram-negative pulmonary pathogens, but they have only marginal activity against S. pneumoniae with the minimal concentration required to produce 90% inhibition (MIC90s) ranging 1-4 mg·L -1 compared to MIC90s of <0.5 mg·L -1 for most of the Gram-negative pathogens [1,2,6]. Clinical studies have shown ciprofloxacin and ofloxacin to have good clinical efficacy in the treatment of bronchopulmonary infections due to S. pneumoniae [35], but other investigators have reported low clinical success rates with a high rate of persistence of S. pneumoniae after therapy [36].…”

Section: Discussionmentioning

confidence: 99%

“…Excellent in vitro activity, improved pharmacokinetic properties, the possibility of single daily dosing and the increased half-life of sparfloxacin as compared with the fluoroquinolones available at present makes it a suitable candidate for the treatment of lower respiratory tract infections [1,47,48]. However, the indication for treatment with sparfloxacin will have to be decided with care, because of some toxicological problems, such as photosensivity and Qtc interval prolongation [49].…”

Section: Discussionmentioning

confidence: 99%

“…However, they are less potent against some common respiratory pathogens, particularly Streptococcus pneumoniae, Mycoplasma pneumoniae and some intracellular organisms. Sparfloxacin is a novel quinolone derivative with comparable activity to ciprofloxacin and ofloxacin against gram-negative organisms, but it possesses greater activity than these quinolones against Gram-positive cocci (including S. pneumoniae), Mycoplasma spp., Chlamydia spp., Mycobacteria spp., and some anaerobes [1][2][3][4][5][6][7][8][9][10]. The pharmacokinetics of sparfloxacin are characterized by: good absorption after oral administration; good penetration into many tissues and body fluids; and a long plasma elimination half-life, ranging 16-24 h [11][12][13][14].…”

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Penetration of sparfloxacin and ciprofloxacin into alveolar macrophages, epithelial lining fluid, and polymorphonuclear leucocytes

Schüler¹,

Zemper²,

Börner³

et al. 1997

Eur Respir J

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Sparfloxacin (SPX), a novel fluoroquinolone with a broad spectrum of antibacterial activity, has been shown, in vitro, to be more effective against common pulmonary pathogens, particularly Streptococcus pneumoniae, Mycoplasma pneumoniae and some intracellular organisms, than ciprofloxacin (CPX).The objective of this open, comparative, randomized study in two parallel groups was to assess the serum concentrations and penetration of SPX and CPX into alveolar macrophages (AMs), epithelial lining fluid (ELF), and peripheral polymorphonuclear leucocytes (PMNs). Patients received either a single oral dose of SPX, 400 mg (16 patients), or CPX, 500 mg (15 patients), at various times before a routine diagnostic bronchoscopy was performed. Antibiotic concentrations were determined by using a microbiological assay.The median serum elimination half-lives were 17.3 h for SPX and 5.3 h for CPX. Peak levels (median±68% confidence range) of CPX were attained in AMs (7.6±1.7 mg·L -1 ) at 5 h after admission, and in both ELF (2.13±0.91 mg·L -1 ) and PMNs (9.1±6.2 mg·L -1 ) at 2.5 h after administration. SPX achieved comparable peak levels in PMNs (median±68% range, 9.4±1.1 mg·L -1 at 5 h), but peak concentrations attained in AMs and ELF (35.1±15.4 and 32.2±28.2 mg·L -1 , respectively, at 24 h) were several times higher than those of CPX. SPX demonstrated substantially greater accumulation in all three sites than did CPX (peak site to serum ratios of 11.0±4.3, 65.5±28.4 and 63.0±66 versus 4.94±0.64, 10.6±3.7 and 10.6±3.7 for PMNs, AMs and ELF, respectively).The results indicate, that sparfloxacin has a long elimination half-life and that it achieves higher concentrations in alveolar macrophages and epithelial lining fluid than ciprofloxacin. Site concentrations of sparfloxacin greatly exceeded the minimal inhibitory concentrations of common respiratory pathogens.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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confidence: 99%

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Penetration of sparfloxacin and ciprofloxacin into alveolar macrophages, epithelial lining fluid, and polymorphonuclear leucocytes

Schüler¹,

Zemper²,

Börner³

et al. 1997

Eur Respir J

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“…The increasing resistance of X. maltophilia to the commercially available quinolones is worrisome and requires further investigation (3, 4, 10, 12, 16, 17, 21-23, 30, 33). Although the investigational quinolones show good in vitro activity compared with that of ciprofloxacin and other quinolones (3,13,17,19,21,22,29,30,32,33), their clinical usefulness needs to VOL. 38,1994 on be determined after further in vitro investigation of, for example, their stability to selection of resistant strains.…”

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A changing pattern of susceptibility of Xanthomonas maltophilia to antimicrobial agents: implications for therapy

Vartivarian

Anaissie

Bodey

et al. 1994

Antimicrob Agents Chemother

179

110

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The in vitro susceptibilities of 130 Xanthomonas maltophilia isolates to 12 antibiotics-trimethoprimsulfamethoxazole, minocycline, ticarcillin-clavulanate, ceftazidime, cefoperazone, cefoperazone-sulbactam, imipenem, ciprofloxacin, and the investigational quinolones PD 117558, PD 117596, PD 127391, and sparfloxacin-were determined by a microtiter broth dilution technique. Other than the investigational quinolones, the most active antibiotics were minocycline, trimethoprim-sulfamethoxazole, and ticarcillinclavulanate, in order. However, the first two were not bactericidal, while about half of the isolates exhibited intermediate susceptibility to ticarcillin-clavulanate. Patterns of susceptibility to trimethoprim-sulfamethoxazole and ciprofloxacin relative to the years of isolation of these strains reflected the development of resistance to the antibiotic prophylaxis practices in the hospital. We recommend that a combination of antibiotics, such as trimethoprim-sulfamethoxazole, minocycline, and ticarcillin-clavulanate, at or close to the maximum tolerated doses be used in the treatment of serious X. maltophilia infections.Xanthomonas maltophilia has emerged as a significant cause of morbidity and mortality in cancer patients (5,6,18). This organism is capable of causing life-threatening infections (5, 25) and is usually resistant to multiple antimicrobial agents, particularly to those of the beta-lactam class (25). The standard therapy for infections by this organism is trimethoprimsulfamethoxazole. The newly developed quinolones, which have broad antimicrobial activity, are now being used in both prophylaxis and therapy of infections in cancer patients. However, at The University of Texas M. D. Anderson Cancer Center, we have cared for patients with serious X maltophilia infections that developed during quinolone prophylaxis. Because of our concern for the emergence of resistance of X. maltophilia to quinolones and the limited therapeutic options available to treat this potentially life-threatening infection, we studied the in vitro activities of various antimicrobial agents, including quinolones, against 130 clinical isolates of X. maltophilia.The strains of X maltophilia used in this study were single patient isolates from the clinical microbiology laboratory at M. D. Anderson Cancer Center. Eighty-nine of the cultures were isolated from patients' bloodstreams, 24 were from urine, 12 were from sputum or the throat, and 5 were from miscellaneous sources. These isolates had been collected in the infectious disease laboratories since 1981 for their clinical significance. The bacteria were identified as X. maltophilia by various biochemical tests using the API 20C system (Analytab Products, Plainview, N.Y.). Organisms were stored in the laboratory at -70°C.All antimicrobial agents were obtained in the form of standard laboratory powders and were stored at -70°C before use. The drugs tested were trimethoprim-sulfamethoxazole (Hoffmann-La Roche, Montclair, N.J.); minocycline (Lederle, Pearl River, N.Y.); ciprofloxac...

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“…DU-6859a (DU) is a new fluoroquinolone antimicrobial agent with the chemical structure 7-[(7S)-7-amino-5-azaspiro [2,4]heptan-5-yl]-8-chloro-6-fluoro-1-[(lR,2S)-2-fluoro-1-cyclopropyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid sesquihydrate (25). Since the presently available fluoroquinolone agents possess only moderate activities against many gram-positive bacteria, recent efforts have been directed toward the synthesis of compounds which have greater activities against these organisms, such as tosufloxacin (1), sparfloxacin (1,3,9), CI-934 (4), WIN 57273 (7,15,17), PD 117596 (5), PD 127391 (CI-960) (5,9,20), PD 131628 (9), T-3761 (10), OPC-17116 (14), AM-1155 (13), E-4497 (11), CP-74667 (16), and CP-99219 (6). DU appears to be one of the most active of these agents (25).…”

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Comparative in vitro activity of DU-6859a, a new fluoroquinolone agent, against gram-positive cocci

Korten¹,

Tomayko²,

Murray³

1994

Antimicrob Agents Chemother

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The in vitro activity of DU-6859a (DU), a new fluoroquinolone agent, was evaluated against 233 gram-positive cocci and was compared with those of ciprofloxacin, vancomycin, nafcillin, and ampicillin. The MICs of DU for 90% of the staphylococci tested were <0.06 ,ug/ml. All of the groups A and B and viridans group streptococci were inhibited by sO.125 ,ug of DU per ml, which was 32-fold more active than ciprofloxacin. On T-3761 (10), OPC-17116 (14), AM-1155 (13), E-4497 (11), CP-74667 (16), and CP-99219 (6). DU appears to be one of the most active of these agents (25). In the present study, the antibacterial activity of DU was investigated and compared with the activities of ciprofloxacin, vancomycin, nafcillin, and ampicillin against gram-positive cocci representing a broad range of antimicrobial resistance patterns. DU in powder form was provided by Daiichi Pharmaceutical Co., Tokyo, Japan; ciprofloxacin was provided by Miles Pharmaceuticals, West Haven, Conn.; and vancomycin, nafcillin, and ampicillin were purchased from Sigma Chemical Co., St. Louis, Mo. All staphylococci and streptococci were collected from hospitals in Houston, Tex., between 1989 and The bactericidal activity of DU against 7 E. faecalis and 3 E. faecium isolates was determined. Overnight cultures were diluted to yield a final inoculum of _107 CFU/ml in flasks containing brain heart infusion broth. The concentration of DU (2 ,ug/ml) used in the time-kill assays was recommended by the manufacturer to represent levels achievable in human serum. Samples (100 ,ul each) were withdrawn from flasks following 0, 4, and 24 h of incubation at 37°C with agitation. Undiluted and serially diluted samples were plated onto brain heart infusion agar plates. The lowest detectable number of organisms was 10 CFU/ml. The agar plates were incubated at 37°C for 24 h before CFU were counted. Bactericidal activity was defined as a reduction in CFU of >3 loglo. A drug carryover effect was excluded by showing that there was less than 5% difference in colony counts when 100 ,ul of 103 to 104 CFU/ml was plated onto antibiotic-free plates in the absence or presence of DU (2 ,ug/ml).The results of susceptibility testing with DU and a comparison of these results with the results of testing with other antibiotics are shown in Table 1. Fifty percent of the staphylococcal isolates tested were inhibited by .0.03 ,ug of DU per ml, and 90% were inhibited by .0.06 ,ug/ml (Table 1). The MICs for 90% of strains tested (MIC90s) were higher for the methicillin-resistant subgroups of S. aureus and coagulasenegative staphylococci than for the methicillin-susceptible sub-

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In vitro activity of sparfloxacin compared with those of five other quinolones

Cited by 64 publications

References 15 publications

Penetration of sparfloxacin and ciprofloxacin into alveolar macrophages, epithelial lining fluid, and polymorphonuclear leucocytes

Penetration of sparfloxacin and ciprofloxacin into alveolar macrophages, epithelial lining fluid, and polymorphonuclear leucocytes

A changing pattern of susceptibility of Xanthomonas maltophilia to antimicrobial agents: implications for therapy

Comparative in vitro activity of DU-6859a, a new fluoroquinolone agent, against gram-positive cocci

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