• 약학회지
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• 제40권3호
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• pp.343-346
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• 1996

The influence of LB20304a, a new fluoroquinolone antibiotic agent, on microflora of caecum in mice was compared with those of ciprofloxacin and piperacillin after administration of drugs for 5 days. Selective medium (CCFMA) was used for the isolation of Clostridium difficile from the specimens of mouse caecum. The emergence of C. difficile in mouse caecum induced by LB20304a was lower than that by ciprofloxacin or piperacillin at day 1 and day 7 after completing administration of drugs.

• 대한미생물학회지
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• 제35권5_6호
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• pp.337-339
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• 2000

MRSA, erythromycin-resistant S. pyogenes, penicillin non-susceptible pneumococci, PPNG, ESBL-producing E. coli and K. pneumoniae, class C ${\beta}$-lactamase-producing E. coli, fluoroquinolone-resistant E. coli, aminoglycoside-resistant A. baumannii and P. aeruginosa are all prevalent in Korea, which suggest the presence of high levels of antimicrobial selective pressure and nosocomial spread of resistant bacteria. Rapid increase of VRE and emergence of fluoroquinolone-resistant gonococci and VIM-2 metallo-${\beta}$-lactamase-producing P. aeruginosa are recently observed new threats in Korea.

• 약학회지
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• 제31권2호
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• pp.98-104
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• 1987

The compounds synthesized by authors were evaluated for their antimicrobial activities against. Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris and Pseudomonas aeraginosa New compounds[1, 10] possess striking potency against a wide range of microorganisms, especially the Gram negative aerobes and has spectacular activity against Enterobacteriaces, S. aureus and Ps. aeruginosa. Most of new compounds are very active in vitro against most strains of Enter- bacteriaceae and Gram positive aerobes, but moderately active against Ps. aeruginosa.

• 약학회지
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• 제43권1호
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• pp.131-133
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• 1999

The bactericidal activities of DW-116, a new fluoroquinolone was estimated by comparing the minimal bactericidal concentrations (MBCs) of it against some Gram-positive and -negative bacterial strains with the minimal inhibitory concentrations (MICs). The MBCs against the test organisms were equal to or two times higher than MICs. The results support that the antibacterial activity of DW-116 is bactericidal.

• Archives of Pharmacal Research
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• 제20권4호
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• pp.358-362
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• 1997

Metabolite identification and urinary and biliary excretion of the new fluoroquinolone antibacterial agent DW116 [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1 -piperazinyl)-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid, hydrochloride] after oral administration have been studied in Sprague-Dawley rats. The excretion kinetics were monoexponential. Most of the drug was eliminated via the hepatic and renal routes. Mean renal clearance of DW116 was 73.4 ml/hr/kg and mean biliary clearance was 83.8 ml/hr/kg. The major metabolite excreted in the bile was identified as the glucuronide ester of the parent drug using base-hydrolysis of the conjugate metabolite followed by co-HPLC with standard compound, $^{19}$ F-NMR and LC-MS methods. The glucuronide conjugate was also found in urine. The mean urinary recoveries of free and total (free plus glucuronide ester) DW116 were $28.6{\pm}2.7% $and $36.4{\pm}1.8%$ of the administered dose and the corresponding biliary recoveries were $14.4{\pm} 5.5%$ and $37.0{\pm}7.6%$, respectively.

• Pediatric Infection and Vaccine
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• 제15권2호
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• pp.93-99
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• 2008

Fluoroquinolone은 Nalidixic acid가 개발된 이래로 광범위한 항균효과, 조직 내로의 우수한 침투성, 투여의 편이성 등으로 널리 사용되고 있다. 이러한 장점에도 불구하고 소아의 경우 동물연구에서 보인 연골 및 관절의 손상과 항생제 내성 증가의 우려 등으로 인해 그 사용이 제한되어 왔다. 그러나, 최근 몇몇 질환을 대상으로 소아에서 그 사용이 증가하고 있다. 반면 아직까지 이에 따른 연골 및 관절의 손상은 뚜렷한 연관성을 보이지 않고 있다. 그러나, 소아에서의 일반적 사용을 위해서는 추가적인 연구가 필요한 상태이다. 소아의 경우 fluoroquinolone 투여는 일차 항생제의 치료 실패 및 대체 가능한 항생제가 없는 경우에 한해 조심스럽게 투여하는 것이 바람직한 것으로 사료된다.

• 약학회지
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• 제55권1호
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• pp.11-15
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• 2011

Zabofloxacin is a novel broad spectrum fluoroquinolone with excellent anti-pneumococcal activity. We investigated the in vitro activity of zabofloxacin against clinical isolates of gram-positive bacteria and the in vivo activity against systemic infection in mice. Zabofloxacin was very active against gram-positive bacteria except QRSA (Quinolone-resistant S. aureus) and VRE(Vancomycin-resistant Enterococci). Especially, zabofloxacin was extremely potent against clinical isolates of Streptococci. Zabofloxacin was as active as gemifloxacin against systemic infection in mice. In view of its improved antibacterial activities against gram-positive bacteria and good pharmacokinetic profiles in animals, the clinical usefulness of zabofloxacin should be established by further studies.

• Clinical and Experimental Pediatrics
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• 제64권9호
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• pp.459-467
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• 2021

Mycoplasma pneumoniae (MP) is the most common cause of childhood bacterial pneumonia. Although macrolide is known to be effective as a first-line therapy, the proportion of macrolide resistance in MP pneumonia has strikingly increased during recent 2 decades in East Asia. This is challenging to physicians since they have to decide more often whether to use secondary treatment. Diagnostic methods to detect macrolide-resistance of MP are currently not available in Korean hospitals. Even in the diagnosis of MP infection, both serologic and molecular test have limitation: inability to differentiate current illness from carriage or asymptomatic infection. Combining these 2 diagnostic methods and excluding infection caused by other respiratory pathogens allow a more reliable diagnosis. This effort is even more demanding in recent years to keep children from unnecessary exposure to secondary antibiotics. Although several observational studies have reported that tetracycline and fluoroquinolone, which are considered in the treatment of refractory MP pneumonia, have efficacy of shortening the duration of fever and respiratory symptoms, those findings need to be proven by well-designed prospective studies. The use of tetracycline and fluoroquinolone in children is generally tolerable, as supported by many observational data. However, since concerns about side effects still remain, careful consideration about benefits and risks is needed to decide their use.

• Asian Pacific Journal of Cancer Prevention
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• 제17권1호
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• pp.285-287
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• 2016

Background: The efficacy of standard treatment of Helicobacter pylori (H. pylori) is declining because of antibiotic resistance. Clarithromycin resistance is also increasing in many Asian countries. The aim of this study was to determine the antibiotic susceptibility patterns of H. pylori infection and clinical association in Laos. Materials and Methods: A total of 329 Lao dyspeptic patients who underwent gastroscopy at Mahosot Hospital, Vientiane, Laos during December 2010-March 2012 were enrolled in this study. During gastroscopy, 4 biopsies were collected (2 each from the antrum and body) for CLO-test and histopathology. Only the positive CLO-test gastric tissues was stored at $-80^{\circ}C$ in a freezer until DNA was extracted and a GenoType$^{(R)}$HelicoDR test was conducted for detecting mutations in the rrl gene encoding 23S rRNA (clarithromycin resistance) and mutations in gyrA gene (fluoroquinolone resistance). Results: Of the total, 119 Lao patients (36.2%) were infected with H. pylori including 59 males (49.6%) and 60 females (50.4%) with a mean age of 46 years. Clarithromycin and fluoroquinolone resistance of H. pylori infection was demonstrated in 15 (12.6%) and 16 strains (13.4%) respectively. In clarithromycin resistance, the number of patients who had education above primary school and $BMI{\geq}25kg/m^2$ were significantly higher than those who had education below primary school and BMI<$25kg/m^2$ (23.1% vs 7.5%, P-value= 0.036 and 20.5% vs 8%, P-value= 0.048, respectively). In fluoroquinolone resistance, the number of lowland Lao was significantly higher than those of non-lowland (highland and midland) Lao ethnic groups (16.7% vs 0%, P-value= 0.039). Conclusions: H. pylori infections remain common in Laos. Clarithromycin and fluoroquinolone resistance with H. pylori infection are growing problems. Education above primary school and $BMI{\geq}25kg/m^2$ might be predictors for clarithromycin resistance and lowland Lao ethnicity might be predictors for fluoroquinolone resistance with H. pylori infection in Laos.

• 대한임상검사과학회지
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• 제53권3호
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• pp.217-224
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• 2021

전 세계적으로 fluoroquinolone (FQ) 내성 그람음성균이 출현하고 있는 가운데, 최근 우리나라에서 FQ 내성 E. coli의 증가 추세는 심각한 우려를 낳고 있다. 이에 본 연구에서는 2018년 6월부터 12월까지 대전지역의 3차 병원에서 분리된 ciprofloxacin 내성 E. coli 56균주를 대상으로, 역학관계와 FQ 내성 결정인자의 양상을 조사하였다. 역학관계를 확인하기 위해 multilocus sequence typing (MLST)을 실시하였다. PCR과 염기서열 분석은 gyrA, gyrB, parC, parE 유전자의 QRDR에서 염색체상의 돌연변이와 aac(6)-Ib-cr, qepA, qnrA, qnrB, qnrC, qnrD 및 qnrS와 같은 PMQR 유전자의 빈도를 확인하였다. MLST 분석 결과, 12개의 ST를 확인하였으며, 이 중 가장 우세한 ST는 ST131 (31/56, 55.4%)이었고, 순차적으로 ST1193 (13/56, 23.2%), ST405 (3/56, 5.4%)의 결과를 보였다. ciprofloxacin 내성 E. coli 56균주 중 gyrA 유전자에서 83번째 아미노산인 serine (S)이 leucine (L)으로, 87번째 아미노산인 aspartic acid (D)가 asparagine (N)으로 치환되고, parC 유전자에서 80번째 아미노산인 serine (S)이 isoleucine (I)으로, 84번째 아미노산인 glutamic acid (E)가 valine (V)으로 치환된 결과(29/56, 51.8%)가 가장 빈번하게 확인되었고, aac(6)-Ib-cr (19/56, 33.9%)은 가장 흔한 PMQR 유전자로 확인되었다. 이러한 FQ 내성 결정인자의 결과는 다른 클론과 비교하여 ST131에서 더 빈번하게 확인되었다. ciprofloxacin 내성 E. coli 균주에 대한 역학적 특성의 지속적인 모니터링과 FQ 내성 결정인자에 대한 추가 연구가 필요할 것으로 사료된다.