Susceptibility of &lt;i&gt;Salmonella typhi&lt;/i&gt; and Brucella melitensis to the New Fluoroquinolone Rufloxacin (MF 934)

Qadri, S. M. Hussain; Ayub, A.; Ueno, Yoshio; Saldin, Hishama

doi:10.1159/000239142

Chemotherapy

1993

DOI: 10.1159/000239142

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Susceptibility of <i>Salmonella typhi</i> and Brucella melitensis to the New Fluoroquinolone Rufloxacin (MF 934)

S. M. Hussain Qadri¹,

A. Ayub²,

Yoshio Ueno³

et al.

Abstract: The antimicrobial activity of the new fluoroquinolone rufloxacin (MF 934) was evaluated by a standardized agar dilution method against recent clinical isolates of Salmonella typhi (67 strains) and Brucella melitensis (108 isolates). The results were compared with 5 other commercially available or investigational fluoroquinolones. All the isolates of S. typhi were inhibited by 1.0 mg/l of rufloxacin as compared to 4-8 mg/l for B. melitensis. Minimum inhibitory concentrations of rufloxacin against both S. typhi … Show more

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“…The results of the current study indicate that clinafloxacin yielded the greatest overall activity against B. melitensis compared with the five other quinolones tested. This study confirms the activity of clinafloxacin and PD 131628 against B. melitensis reported by other workers (2,(11)(12)(13). In view of the excellent in vitro activity of clinafloxacin against B. melitensis, this new fluoroquinolone and the structurally related PD 117596 and PD 131628 represent additional drugs that could be useful in treatment of infections caused by B. melitensis.…”

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confidence: 93%

Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones

Garcı́a-Rodrı́guez

Sánchez

Trujillano

et al. 1995

Antimicrob Agents Chemother

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The susceptibilities of 120 clinical isolates of Brucella melitensis and 3 reference strains of the same species to six fluoroquinolones (clinafloxacin, PD 117596, PD 131628, PD 138312, PD 140248, and ciprofloxacin) were examined by agar dilution MIC methodology. Clinafloxacin was the most active compound tested (MIC at which 50% of strains tested were inhibited [MIC 50 ] and MIC 90 of 0.06 g/ml). Its level of activity was slightly higher than that of PD 117596 (MIC 50 and MIC 90 of 0.12 g/ml). PD 131628 and ciprofloxacin were less active than clinafloxacin, with MIC 50 s ranging from 0.12 to 0.25 g/ml and MIC 90 s of between 0.25 and 0.5 g/ml for the two compounds. The activity levels of PD 138312 and PD 140248, with MIC 50 s ranging from 1 to 2 g/ml and MIC 90 s of 4 to 8 g/ml, were lower than those of the other fluoroquinolones tested.Brucellosis remains a public health problem in several areas, such as Mediterranean countries. The treatment of brucellosis requires combined regimens of antibiotics and is conditioned by the fact that Brucella species are intracellular pathogens; thus, agents with a good capacity to penetrate macrophages are required for successful treatment. Current treatment of acute brucellosis combining tetracyclines and streptomycin or rifampin usually achieves excellent clinical and microbiological results. Nevertheless, variable percentages of failures and recurrences, ranging from 4 to 41% depending on the therapeutic regimens, are reported (1). In addition, these therapeutic regimens pose difficulties in patients' compliance because of their duration; moreover, tetracyclines are contraindicated for children of less than 8 years old and for pregnant women. Furthermore, since the incidence of tuberculosis in some areas of the world is increasing, the use of rifampin for nontuberculous patients in these areas should be avoided. Thus, it is felt that new antibiotics overcoming these problems would represent a significant therapeutic advancement in the treatment of brucellosis.Oral bioavailability of fluoroquinolones, high concentrations in tissues, evidence of intracellular penetration (leukocytes and macrophages) (5), and in vitro activity against Brucella spp. (7, 9) make these antimicrobial agents attractive for use against infections caused by intracellular bacteria such as Brucella spp. However, agents currently available in clinical practice (ciprofloxacin, ofloxacin, lomefloxacin, fleroxacin, and sparfloxacin) have moderate activity and lack effective bactericidal activity under intracellular conditions (pH 5) (7-9). Moreover, therapeutic failures caused by the development of resistance to these agents by Brucella melitensis have also been reported (3). Therefore, these fluoroquinolones should not be considered for primary treatment of brucellosis. Thus, it is important to evaluate new fluoroquinolones with higher intrinsic activity levels that might overcome these problems. Clinafloxacin The MICs of the antimicrobial agents were determined by the agar dilution method by using prev...

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supporting

confidence: 93%

Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones

Garcı́a-Rodrı́guez

Sánchez

Trujillano

et al. 1995

Antimicrob Agents Chemother

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Antibrucella Activity of Quinolone Sparfloxacin

et al. 1995

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Background: Sparfloxacin is a new fluoroquinolone with excellent in vitro activity against a variety of Gram-positive and Gram-negative bacteria. Methods: In vitro antibacterial activity of this new drug was tested against 139 strains of Brucella melitensis. These strains were isolated from 138 patients at a major tertiary care referral center in Riyadh, Saudi Arabia. Results: Seven percent of the strains were inhibited by 0.06 mg per L and 99% by 0.12 mg per L of sparfloxacin. Of the five other fluoroquinolones tested, ciprofloxacin, norfloxacin, pefloxacin, and fleroxacin exhibited comparable or slightly higher minimal inhibitory concentrations values. They inhibited the growth of 138 of the 139 isolates at 0.25-0.5 mg per L. Rufloxacin required 2-8 mg per L to inhibit 138 of the 139 strains tested. One of the isolates, which had previously developed resistance to ciprofloxacin during therapy with this drug, with a rise in MIC from 0.06 mg per L to >5.0 mg per L, exhibited cross-resistance to sparfloxacin and other fluoroquinolones. Conclusion: Sparfloxacin exhibited excellent in vitro activity against clinical isolates of Brucella. Clinical trials are warranted to determine its potential in the treatment of brucellosis.

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Quinolones for Treatment of Human Brucellosis: Critical Review of the Evidence from Microbiological and Clinical Studies

Falagas

Bliziotis

2006

Antimicrob Agents Chemother

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3Brucellosis is a zoonotic disease with worldwide distribution that is endemic in the Mediterranean region, the Middle East, Central Asia, and parts of Africa and Latin America. Worldwide, brucellosis remains a major cause of morbidity in humans and domesticated animals. In animals, bovine brucellosis, caused mainly by Brucella abortus, is still the most widespread form. In humans, ovine/caprine brucellosis caused by Brucella melitensis is by far the most common type of disease. The disease has a wide spectrum of clinical manifestations and can affect a variety of organs and systems. Localized and complicated forms of brucellosis cause important morbidity and require prolonged medical treatment. Fortunately, mortality is relatively low and is related mainly to cardiovascular and central nervous system complications of the disease.Although several studies have been conducted over the past 2 decades, there is no conclusive evidence on the optimum antibiotic therapy for brucellosis. Disease relapse still represents one of the most important therapeutic problems. The last recommendation by the World Health Organization (WHO) for the treatment of acute brucellosis in adults was published in 1986 and suggested 600 to 900 mg rifampin and 200 mg doxycycline daily for a minimum of 6 weeks (8). Alternatively, the WHO suggested that rifampin could be replaced with 15 mg/kg of streptomycin, administered intramuscularly for only 2 weeks. However, a meta-analysis, as well as a prospective randomized trial, both performed by Solera et al., showed that the "good old" combination regimen of streptomycin with an oral tetracycline results in fewer relapses than the doxycycline-rifampin combination (57, 58). Controlled clinical trials with other antibiotics, including trimethoprim-sulfomethoxazole, new macrolides, and ␤-lactams, have shown inferior results or involved too few patients for a proper evaluation. Thus, the most widely used regimens are the two aforementioned combinations that were recommended by the WHO. In addition, rifampin monotherapy is the main option for brucellosis during pregnancy, whereas its combination with trimethoprim-sulfomethoxazole is the suggested treatment for childhood brucellosis (5, 34).Certain focal forms of brucellosis are difficult to treat, and surgery should be considered for patients with endocarditis or cerebral, epidural, splenic, or other abscesses (20, 41). Regarding medical treatment, although the antibiotics used are essentially the same, prolonged therapy, up to six or more months, may be needed for patients with osteoarticular forms of the disease, and especially spondylitis (18,56,65). Also, tripleantibiotic combinations were found to be of value in some case series of brucellar endocarditis, spondylitis, and meningitis (2, 41, 65). Relapse of the disease also represents a major therapeutic problem for its focal forms.Since the mid 1980s, laboratory researchers and clinicians have performed several microbiological and clinical studies of the possible use of quinolones in the treatmen...

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Susceptibility of <i>Salmonella typhi</i> and Brucella melitensis to the New Fluoroquinolone Rufloxacin (MF 934)

Cited by 3 publications

References 10 publications

Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones

Susceptibilities of Brucella melitensis isolates to clinafloxacin and four other new fluoroquinolones

Antibrucella Activity of Quinolone Sparfloxacin

Quinolones for Treatment of Human Brucellosis: Critical Review of the Evidence from Microbiological and Clinical Studies

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