• Title, Summary, Keyword: fluoroquinolones

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Effect of Ophthalmic Fluoroquinolones on Bacterial Conjunctivitis: Systematic Review (세균성결막염에 대한 안과용 플루오로퀴놀론계 항균제의 효과: 체계적문헌고찰)

  • Sohn, Hyun-Soon
    • YAKHAK HOEJI
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    • v.55 no.1
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    • pp.22-31
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    • 2011
  • This systematic review was conducted to assess the clinical effect of ocular fluoroquinolones used for the treatment of bacterial conjunctivitis. A literature search for randomized controlled clinical trials registered up to January 2010 based on PubMed database, using the following search terms: conjunctivitis and fluoroquinolones (besifloxacin, moxifloxacin, gatifloxacin, levofloxacin, lomefloxacin, ciprofloxacin and ofloxacin) were performed. Pooled data on the clinical resolution and bacterial eradication rates derived from selected 16 studies were reported as the relative risk (RR) and 95% confidence interval (95% CI) compared with placebo. Early clinical resolution and microbiological eradication rates in placebo were 28% and 62% respectively. Fluoroquinolones were significantly effective comparing to placebo: early RR 1.94 (95% CI 1.60~2.34) and late RR 1.30 (1.19~1.43) in clinical resolution rates, and early RR 1.75 (1.58~1.94) and late RR 1.28 (1.18~1.39) in microbiological eradication rates. Besifloxacin, ciprofloaxain and moxifloxacin in clinical resolution, and besifloxacin and levofloxacin in microbiological eradication showed higher RRs than pooled overall fluoroquinolones' RRs. New quinolones had higher antibacterial potencies for all pathogens isolated from bacterial conjunctivitis and resistant isolates than old generation quinolones. In conclusion, ocular 7 fluoroquinolones were all effective than placebo for bacterial conjunctivitis and there were differences between quinolones in early and late clinical resolutions and microbiological eradications, and no differences in safety comparing to placebo.

Systemic use of fluoroquinolone in children

  • Choi, Soo-Han;Kim, Eun Young;Kim, Yae-Jean
    • Clinical and Experimental Pediatrics
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    • v.56 no.5
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    • pp.196-201
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    • 2013
  • Fluoroquinolones are an important class of antibiotics that are widely used in adult patients because of their broad spectrum of activity, good tissue penetration, and oral bioavailability. However, fluoroquinolone use in children is limited because juvenile animals developed arthropathy in previous experiments on fluoroquinolone use. Indications for fluoroquinolone use in patients younger than 18 years, as stated by the U.S. Food and Drug Administration, include treatment of complicated urinary tract infections and postexposure treatment for inhalation anthrax. In Korea, the systemic use of fluoroquinolones has not been approved in children younger than 18 years. Although concerns remain regarding the adverse musculoskeletal effects of fluoroquinolones in children, their use in the pediatric population has increased in many circumstances. While pediatricians should be aware of the indications and adverse effects of fluoroquinolones, recent studies have shown that the risk for musculoskeletal complications in children did not significantly increase following fluoroquinolone treatment. In addition, fluoroquinolones may be particularly helpful in treating multidrug-resistant infections that have not responded to standard antibiotic therapy in immunocompromised patients. In the present article, we provide an updated review on the safety and current recommendations for using fluoroquinolones in children.

Bifidobacterium infantis OFR-525 Strain Resistant to Rifampicin and Fluoroquinolones (리팜피신과 플로로퀴놀론계 항균제에 내성인 Bifidobacterium infantis OFR-525 균주)

  • 장현아;권애란;오태권;김동현;최응칠
    • YAKHAK HOEJI
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    • v.43 no.1
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    • pp.124-127
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    • 1999
  • Bifidobacterium infantis K-525 isolated from healthy Korean was susceptible to rifampicin and fluoroquinolones and resistant to other antituberculosis agents. When the preparation of this strain is taken as a therapeutics for human intestinal disorders with rifampicin or fluoroquinolones, its therapeutic effect can not be expected. So, B, infantis RFR-525 resistant to rifampicin was obtained by treating the parent B. infantis 525 with N-methyl-N'-nitro-N-nitrosoguanidine. B. infantis OFR-525 was produced by serial passage of B. infantis RFR-525 on agar with 2-fold minimal inhibitory concentration of ofloxacin. B. infantis OFR-525 was resistant to antituberculosis agents and fluoroquinolones up to 4∼128 fold higher than that for the original strain. The resistance of B. infantis OFR-525 against rifampicin and ofloxacin was maintained in vivo and in vitro. Conclusively, B. infantis OFR-525 can be regarded as a promising strain which can be developed as the preparation for the treatment of the intestinal disorders of the tuberculosis patients under rifampicin and ofloxacin therapy.

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Development of Enterococcus faecalis Strains Resistant to Rifampicin and Ofloxacin (리팜피신과 오플로삭신에 내성인 Enterococcus faecalis 균주의 개발)

  • Lee, Soo-Hwa;Kim, Sook-Kyung;Chung, Young-Ja;Shim, Mi-Ja;Kim, Byong-Kak;Choi, Eung-Chil
    • YAKHAK HOEJI
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    • v.40 no.3
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    • pp.351-356
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    • 1996
  • The preparation of Enterococcus faecalis RSI is used as a therapeutics for human intestinal disorders. However, the microbe in this preparation is usually very sensitive to rifampicin and fluoroquinolones. If this preparation is taken with rifampicin or fluoroquinolones, its therapeutic effect can not be expected. E. faecalis RFR11, containing resistance to rifampicin was obtained by MNNG mutation method. Serial passage of E. faecalis RFR11 produced E. feacalis OFR16 on agar with 2-fold minimal inhibitory concentration of ofloxacin produced. E. feacalis OFR16 was resistant to fluoroquinolones up to 8-256 fold higher than that for the original strain. E. faecalis OFR16 also exhibited identical characteristics with the parent strain when they were tested for lactic acid formation and growth inhibition of E. coli MB4-5737 and Shigella sonnei MB4-10411. From in vitro test, it was identified that rifampicin and ofloxacin is not inactivated by certain factors of E. faecalis OFR16. Conclusively. E. faecalis OFR16, rifampicin and fluoroquinolones resistant mutant, is an efficient strain that has insensitivity against rifampicin and fluoroquinolones and original biochemical characteristics of the parent strain.

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The use of fluoroquinolone in children (소아에서 fluoroquinolone 사용)

  • Hur, Jae Kyun
    • Clinical and Experimental Pediatrics
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    • v.51 no.10
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    • pp.1042-1046
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    • 2008
  • The fluoroquinolones are an important group of antibiotics widely used in the treatment of various infectious diseases in adults, as a result of an excellent spectrum of activity, good tissue penetration and convenient ways of administration. In recent decades, there has been extensive development, clinical investigation, licensure and use of fluoroquinolone antibiotics. However, the use of fluoroquinolones in children has been limited because of their potential to induce arthropathy in juvenile animals. Despite class label warnings against use in children, prescriptions for quinolone antibiotics to treat infections in children have become increasingly prevalent. The main use of fluoroquinolones in pediatrics should be, understandably, in serious life-threatening infections for which other antibiotics therapies are not effective or available. While most of the published studies failed to detect an increased rate of articular adverse effects in children treated with fluoroquinolones, an increase in the use of these compounds, particularly in community-acquired lower respiratory infections, could accelerate the emergence of multidrug-resistant (including fluoroquinolone) pneumococcal strains. This review will discus the main issues related to the use of fluoroquinolones in children, the major problems of resistance developing among these compounds, with special emphasis on the potential side effects and skilled use of these alternative potent drugs in pediatric infection.

The Use of Fluoroquinolones in Children: Recent Advances (소아에서의 Fluoroquinolones 사용: 최근 경향을 중심으로)

  • Choi, Kyong Min
    • Pediatric Infection and Vaccine
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    • v.15 no.2
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    • pp.93-99
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    • 2008
  • Fluoroquinolones have been widely used since the development of nalidixic acid because of the excellent spectrum of activity, superior tissue penetration, and convenient route of administration. Despite such advantages, the usage in children is limited by concerns of toxicity to cartilage, damage to joints in animal studies, and an increase in antibiotic resistance. However, pediatric use has been increasing under certain circumstances with no report of such adverse effects. Further study is required prior to recommendation for general use of fluoroquinolones in children. The careful administration of fluoroquinolones is recommended only in limited circumstances, such as failure of primary antibiotics and lack of alternative antibiotics.

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Development of Bifidobacterium bifidum Strains Resistant to Rifampicin and Ofloxacin (Rifampicin과 Ofloxacin에 내성인 Bifidobacterium bifidum 균주의 개발)

  • Chung, Young-Ja;Jeon, Myoung-In;Kang, Chang-Youl;Kim, Byoung-Kak;Choi, Eung-Chil
    • YAKHAK HOEJI
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    • v.38 no.6
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    • pp.763-769
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    • 1994
  • Bifidobacterium bifidum, one strain of medical preparation being on the market for human intestinal disorders, was sensitive to rifampicin and fluoroquinolones. If this preparation is taken with rifampicin and fluoroquinolones, its therapeutic effect can't be expected. Serial passage of B. bifidum RFR61, which was obtained by MNNG mutation method, on agar with 2-fold minimal inhibitory concentration of ofloxacin produced B. bifidum OFR9 with minimal inhibitory contentrations of fluoroquinolones up to $4{\sim}256-fold$ higher than that for the original strain. B. bifidum OFR9 produced almost the same amount of organic acid as parental strain. This strain showed growth inhibitory activity against E. coli NM522, Shigella dysenteriae ATCC9752 and E. coli 078. No inactivations of rifampicin and ofloxacin by this resistant mutant strain were found.

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Establishment of an Analytical Method of Fluoroquinolones in Milk by HPLC (HPLC를 이용한 우유에서의 fluoroquinolones 시험법 확립)

  • Kim, Jong-Hwa;Hong, Se-Lyung;Kang, Tae-Beom;Lee, Hyun-Kyung;Lee, Soon-Ho
    • Korean Journal of Food Science and Technology
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    • v.42 no.5
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    • pp.521-526
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    • 2010
  • A high-performance liquid chromatography (HPLC) method was established for the determination of fluoroquinolones in milk. Protein was removed by using trichloroacetic acid in order to increase a mean recovery of milk. The extracts were using $Strata^{TM}$-X solid-phase extraction cartridge. The analytes were detected by HPLC on a $C_{18}$ column. HPLC method with fluorescence detection system (Ex: 278 nm, Em: 456 nm) provided a high degree of sensitivity in detecting fluoroquinolones. The limits of quantitation (LOQ) and mean recoveries of fluoroquinolones were 40 ${\mu}g$/kg and 73.6-95.2% (ofloxacin), 10 ${\mu}g$/kg and 77.3-91.9% (norfloxacin), 20 ${\mu}g$/kg and 91.6-94.3% (ciprofloxacin), 10 ${\mu}g$/kg and 81.0-87.8% (enrofloxacin), 10 ${\mu}g$/kg and 71.3-81.0% (sarafloxacin), 10 ${\mu}g$/kg and 89.4-90.8% (orbifloxacin), 2 ${\mu}g$/kg and 69.4-85.5% (danofloxacin).

A study on the residues of fluoroquinolones in hen's eggs consumed in Incheon Metropolitan city (인천광역시에서 유통되는 계란의 플루오로퀴놀론계 항균물질 잔류 실태 조사)

  • Park, Eun-Jeong;Lim, Ji-Huen;Lee, Sung-Mo;Im, Jeong-Soo;Oh, Dae-Kyu
    • Korean Journal of Veterinary Service
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    • v.31 no.3
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    • pp.385-395
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    • 2008
  • This study was carried out to investigate the residue level of fluoroquinolones in hen's general eggs and specific eggs by microbiological assay method and high performance liquid chromatography (HPLC) method. HPLC separation was carried out by reversed phase chromatography on a Symmetry $C_{18}$ (250${\times}$4.6 mm, $5{\mu}m$ particle size) with a phase composed of distilled water (containing 0.4% triethylamine and phosphoric acid) : Methanol (780 : 220, v/v), pumped isocratically at a flow rate of 1.0ml/min. A fluorescence detector was utilized with an excitation wavelength of 278nm and an emission wavelength of 456nm. The calibration curves were linear $({\gamma}^2{\geq}0.999)$ over a concentration range of $0.025{\sim}0.4{\mu}g/ml$. Average recoveries of the five fluoroquinolones in whole eggs at fortified levels of $0.05{\sim}0.2{\mu}g/g$ were ranged mean $78.1{\sim}91.7%$ and low coefficient of variation was less than 10% for all analysed samples. The limits of detection and limits of quantification for whole eggs were $1.2{\sim}6.0ng/g$ and $2.3{\sim}9.1ng/g$, respectively. Only one hen's general eggfrom chicken farm in Incheon was detected with the residual fluoroquinolones (Microbiological assay method; 1 of 47 general eggs) ; the range of residual concentration enrofloxacin was 0.12ppm. Those in food stores were detected with the residual fluoroquinolones (Microbiological assay method; 4 of 88 general eggs) ; the ranges of residual concentration enrofloxacin were $0.15{\sim}2.2 ppm$, ciprofloxacin $0.01{\sim}0.06ppm$, and hen's specific eggs (40) in food stores were not detected. For the microbiological assay method of fluoroquinolones in hen's eggs, as the results of comparative analysis, the disc diffusion method with E coli may be a little highly detected for the residual fluoroquinolones.

Antibacterial and Pharmacological Evaluation of Fluoroquinolones: A Chemoinformatics Approach

  • Sood, Damini;Kumar, Neeraj;Singh, Aarushi;Sakharkar, Meena Kishore;Tomar, Vartika;Chandra, Ramesh
    • Genomics & Informatics
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    • v.16 no.3
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    • pp.44-51
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    • 2018
  • Fluoroquinolone (FQ) antibiotics are an important class of synthetic antibacterial agents. These are the most extensively used drugs for treating bacterial infections in the field of both human and veterinary medicine. Herein, the antibacterial and pharmacological properties of four fluoroquinolones: lomefloxacin, norfloxacin, ciprofloxacin, and ofloxacin have been studied. The objective of this study was to analyze the antibacterial characteristics of the different fluoroquinolones. Also, the pharmacological properties of the compounds including the Lipinski rule of five, absorption, distribution, metabolism, and excretion, LD50, drug likeliness, and toxicity were evaluated. We found that among all four FQ molecules, ofloxacin showed the highest antibacterial activity through in silico assays with a strong interaction (-38.52 kJ/mol) with the antibacterial target protein (topoisomerase-II DNA gyrase enzyme). The pharmacological and pharmacokinetic analysis also showed that the compounds ciprofloxacin, ofloxacin, lomefloxacin and norfloxacin have good pharmacological properties. Notably, ofloxacin was found to possess an IGC50 (concentration needed to inhibit 50% growth) value of $0.286{\mu}g/L$ against the Tetrahymena pyriformis protozoa. It also tested negative for the Ames toxicity test, showing its non-carcinogenic character.