• Tuberculosis and Respiratory Diseases
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• 제80권2호
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• pp.143-152
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• 2017

Background: Fluoroquinolones are considered important substitutes for the treatment of tuberculosis. This study investigates the current status of fluoroquinolone for the treatment of tuberculosis. Methods: In 2009, a retrospective analysis was performed at one tertiary referral center for 953 patients diagnosed with tuberculosis. Results: A total of 226 patients (23.6%), who received fluoroquinolone at any time during treatment for tuberculosis, were enrolled in this study. The most common reasons for fluoroquinolone use were adverse events due to other anti-tuberculosis drugs (52.7%), drug resistance (23.5%), and underlying diseases (16.8%). Moxifloxacin (54.0%, 122/226) was the most commonly administered fluoroquinolone, followed by levofloxacin (36.3%, 82/226) and ofloxacin (9.7%, 22/226). The frequency of total adverse events from fluoroquinolone-containing anti-tuberculosis medication was 22.6%, whereas fluoroquinolone-related adverse events were estimated to be 2.2% (5/226). The most common fluoroquinolone-related adverse events were gastrointestinal problems (3.5%, 8/226). There were no significant differences in the treatment success rate between the fluoroquinolone and fluoroquinolone-$na{\ddot{i}}ve$ groups (78.3% vs. 78.4%, respectively). Conclusion: At our institution, fluoroquinolones are commonly used for the treatment of both multidrug-resistant tuberculosis and susceptible tuberculosis, especially as a substitute for adverse event-related drugs. Considering the low adverse event rates and the comparable treatment success rates, fluoroquinolones seem to be an invaluable drug for the treatment of tuberculosis.

• Clinical and Experimental Pediatrics
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• 제51권10호
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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.

• Clinical and Experimental Pediatrics
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• 제56권5호
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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.

• 약학회지
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• 제47권6호
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• pp.365-368
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• 2003

The bactericidal activities of DW286, a new fluoroquinolone were investigated by comparing the minimal bactericidal concentrations (MBCs) and the time-kill curve of it against some Gram-positive and Gram-negative bacterial strains. The MBCs of DW286 for the strains tested were either equal to or two-fold higher than the MICs, as were observed for the other fluoroquinolones. And DW286 exhibited rapid killing curves against the strains. Accordingly, it could be said that DW286 has bactericidal activity comparable to other fluoroquinolones.

• 대한임상검사과학회지
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• 제48권2호
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• pp.74-81
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• 2016

Fluoroquinolone 계 항생제의 광범위한 사용으로 인해 이 약제에 대한 내성 Ureaplasma 종의 분리 비율이 높아지고 있다. Fluoroquinolone 계 항생제 내성은 주로 DNA gyrase와 topoisomerase IV 유전자의 돌연변이로 인해 발생하는 것으로 알려져 있다. DNA gyrase는 A와 B 2개의 소단위로 이루어져 있으며, gyrA와 gyrB 유전자에 의해 암호화되어 있고, Topoisomerase IV는 parC와 parE 유전자에 의해 암호화되어 있다. 본 연구가 진행된 서울의 1개 3차 병원에서 2012년부터 2013년까지 1년동안 Ureaplasma 종의 fluoroquinolone 계 항생제인 OFL과 CIP의 항생제검사 감수성 결과를 분석한 결과 내성과 중등도를 합산할 경우 66.08%, 92.69%로 매우 높은 내성 비율을 보였다. 이에 Ureaplasma 종을 OFL과 CIP에 대한 감수성을 기준으로 4개 그룹으로 분류하여 gyrA, gyrB, parC, parE 유전자의 돌연변이 여부를 검사하여 항생제 내성과의 관련성을 밝히고자 하였다. 그 중 parC 유전자의 돌연변이 빈도가 높아 topoisomerase IV의 돌연변이가 fluoroquinolone 계 약제에 대한 내성과 밀접한 관련이 있음을 확인할 수 있었다. 본 연구를 통해 GyrB의 Asn481Ser, ParC의 Phe149Leu, Asp150Met, Asp151Ile, Ser152Val, ParE의 Pro446Ser, Arg448Lys을 추가로 발견할 수 있었다. 최근 fluoroquinolone 계 항생제의 사용이 증가하고 있기 때문에 추후 Ureaplasma 종의 fluoroquinolone 계 항생제 내성에 대한 지속적인 모니터링이 필수적일 것으로 사료되며, 이와 관련한 유전자의 돌연변이 양상과의 상관관계를 분석하여 기존 배양검사의 단점을 보완할 수 있는 분자 진단학적 검사법의 추가적인 분석이 필요할 것으로 사료된다.

• 대한임상검사과학회지
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• 제49권4호
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• pp.427-434
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• 2017

Acinetobacter calcoaceticus-baumannii (Acb) complex에 속한 종들은 빈번하게 병원감염 및 기회감염을 일으킨다. 또한 다제내성인 경우가 많아 이 균들의 감염증 치료를 위한 항균제 선택이 매우 제한적이다. 본 연구에서는 ciprofloxacin 내성 Acinetobacter species 53균주를 대상으로 fluoroquinolone 내성기전을 조사했다. 항균제 감수성 양상을 조사하기 위해 디스크확산법이 시행되었다. Fluoroquinolone 내성과 관련된 유전자 및 돌연변이 검출을 위해 PCR과 염기서열분석이 이루어졌다. 본 연구에서 수집된 53균주의 ciprofloxacin 내성 Acinetobacter 중 47균주가 gyrA 유전자의 83번째 serine 아미노산 잔기와 parC 유전자의 80번째 serine 아미노산 잔기가 leucine 잔기로 치환된 sense mutations 가지고 있는 것으로 나타났다. gyrA와 parC 유전자에 sense mutations을 가지고 있는 47균주 중 44균주가 A. baumannii 였고 3균주는 A. pittii였다. 본 연구에서 조사대상이 되었던 Acb complex 균주들 중 plasmid-mediated quinolone resistance (PMQR) determinants를 가지고 있는 균주는 한나도 없었다. 46 균주의 ciprofloxacin 내성 A. baumannii 는 A, B, 또는 F형의 banding pattern을 보였는데 이는 충청지역에 위치한 일개의 병원에 ciprofloxacin 내성 A. baumannii가 수평확산 되어 있음을 의미한다. Fluoroquinolone 내성 Acb complex 균주의 집락화 및 확산을 막기 위해서 다제내성 균주들을 대상으로 항균제 내성인자들을 지속적으로 조사하고 모니터링할 필요가 있을 것으로 사료된다.

• 한국동물위생학회지
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• 제40권1호
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• pp.41-46
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• 2017

The purpose of this study was to investigated the fluoroquinolone (FQ) resistance and presence of gyrA and grlA gene in 87 Staphylococcus pseudintermedius isolates obtained from clinical samples of dogs and cats. Also, the profiles of FQ resistance compared with methicillin resistant S. pseudintermedius (MRSP) isolates. FQ resistance was observed for enrofloxacin (41.4%), ciprofloxacin (39.1%), norfloxacin (36.8%), ofloxacin and levofloxacin (32.2%, respectively), and moxifloxacin (31.0%). Thirty-eight (43.7%) of 87 S. pseudintermedius isolates were resistant to more than one FQ. Twenty-six (64.5%) of 38 FQ resistant isolates were resistant to all the six FQ tested. Of 38 FQ resistant isolates, gyrA gene was detected in all isolates but grlA gene was not found. Moreover, 19 MRSP isolates were resistant to enrofloxacin (63.2%), ciprofloxacin (57.9%), norfloxacin (52.6%), and ofloxacin, levofloxacin and moxifloxacin (47.4%, respectively). FQ resistance were highly prevalence in S. pseudintermedius isolates from dogs and cats. Our results emphasize the prudent use of antimicrobial agents to companion animals is necessary for prevent antimicrobial resistance.

• 전기화학회지
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• 제13권1호
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• pp.63-69
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• 2010

플루오로퀴놀론 계 항생제들의 전기화학적 거동을 카본 페이스트 전극 (carbon paste electrode ; CPE)을 사용하여 순환 전압전류법 (cyclic voltammetry)과 네모파 흡착 벗김 전압전류법 (square wave adsorptive stripping voltammetry)으로 연구하였다. Enrofloxacin (ENR), Norfloxacin (NOR), Ciprofloxacin (CIP), Ofloxacin (OFL), Levofloxacin (LEV) 등 5가지 플루오로퀴놀론 계 항생제에 대한 전기화학적 분석을 수행하였다. pH 4.5인 아세트산 완충 용액 (acetate buffer) 에서 플루오로퀴놀론 계 항생제의 산화 전위는 Ag/AgCl 기준 전극에 대하여 각각 ENR : 0.952V, NOR : 1.052 V, CIP : 1.055 V, OFL : 0.983 V, LEV : 0.990 V 의 값을 나타내었으며, 네모파 흡착 벗김 전압전류법에 의한 산화 전류는 $0.2\;{\mu}M$에서 $1\;{\mu}M$ 사이의 농도영역에서 각 항생제의 농도와 선형을 나타내었다.

• Archives of Pharmacal Research
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• 제19권4호
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• pp.317-320
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• 1996

The time-kill curves of LB20304, a novel fluoroquinolone that has potent antibacterial activity against gram-positve and gram-negative bacteria, were calculated at the concentrations of 1/4-, 1/2-, 1-, 2- and 4-times the MIC against Staphylococcus aureus 77, Escherichia coli 3739E, Pseudomonas aeruginosa 1912E. The bactericidal activity of LB20304 for these strains was very rapid and comparable to that of ciprofloxacin. LB20304 produced a decrease in the $log_10$ CFU per milliliter of${\geq}$3 within 2 h at 4-times the MIC for all strains and consitently prevented regrowth of bacteria after 24 h of incubation. The MBCs (Minimal Bactericidal Concentration) of LB20304 against test organisms were equal to or at most four-times higher than the MICs.

• Archives of Pharmacal Research
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• 제21권2호
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• pp.106-112
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• 1998

Structure-activity relationship of 20 fluoroquinolones was studied using the susceptible and 4 resistant Escherichia coli which were developed against 4 fluoroquinolones [ciprofloxacin (1), KR-10755 (6), norfloxacin (2), and ofloxacin (3)] in our laboratory. The C-7 and C-8 substituents of fluoroquinolone were important in various functions such as the inhibitory activity on DNA gyrase, permeability, and efflux. Among 20 fluoroquinolones, compounds with a 3-methyl-3,7-diazabicyclo[3.3.0]octan-1(5)-ene-7-yl substituent at the C-7 position or a chlorine substituent at the C-8 position showed a good inhibitory activity on DNA gyrase (especially a mutated DNA gyrase). Compounds with a 3,7-diazabicyclo [3.3.0]octan-1(5)-ene-7-yl substituent at the C-7 position showed good permeability in the susceptible and resistant strains, while compounds with a fluorine substituent at the C-8 position were less eff luxed from cells.