• Tuberculosis and Respiratory Diseases
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• v.68 no.6
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• pp.334-344
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• 2010

Background: Based on the known immunoregulatory functions of moxifloxacin on phagocytes, the therapeutic effect of moxifloxacin on oleic acid (OA)-induced acute lung injury (ALI) was investigated. Methods: Moxifloxacin (10 mg/kg) was given to male Sprague-Dawley rats that had been given oleic acid (OA, $30{\mu}L$) intravenously. Five hours after OA injection, parameters demonstrating ALI were assessed to measure the effects of moxifloxacin on acute lung injury. Results: The pathological findings of OA-induced ALI's was diminished by moxifloxacin. Through ultrastructural and $CeCl_3$ EM histochemistry, moxifloxacin was confirmed to be effective in decreasing oxidative stress in the lung as well. Indices of ALI, such as lung weight/body weight ratio, protein content in bronchoalveolar lavage fluid, and lung myeloperoxidase were decreased by moxifloxacin. In diaminobenzidine immunohistochemistry, fluorescent immunohistochemistry, and Western blotting of the lung, moxifloxacin had decreased the enhanced expression of secretory phospholipase $A_2$ ($sPLA_2$) by OA. Conclusion: We concluded that moxifloxacin was effective in lessening acute inflammatory pulmonary edema caused by OA, by inhibiting the neutrophilic respiratory burst, which was initiated by the activation of $sPLA_2$.

• Tuberculosis and Respiratory Diseases
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• v.57 no.5
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• pp.405-410
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• 2004

Background : Moxifloxacin is an 8-methoxyquinolone compound which has been shown to have the best activity of the quinolones against M. tuberculosis but there is no literature showing the rate of cross-resistance between moxifloxacin and the other quinolones such as ofloxacin. Therefore, we tested the activity of moxifloxacin against ofloxacin resistant M. tuberculosis by a study of cross-resistance. Methods : We tested MIC's of moxifloxacin and ofloxacin by proportion method against 34 M. tuberculosis isolates showing resistance against ofloxacin at $2.5{\mu}g/m{\ell}$ concentration and 13 ofloxacin susceptible isolates from specimens submitted to clinical laboratory of National Masan Hospital from March 2003 to March 2004. Results : For ofloxacin susceptible isolates, $MIC_{50}$ and $MIC_{90}$ of ofloxacin were all $1.25{\mu}g/m{\ell}$, and $MIC_{50}$ and $MIC_{90}$ of moxifloxacin were $0.31{\mu}g/m{\ell}$ and $0.63{\mu}g/m{\ell}$ respectively. For ofloxacin resistant isolates, $MIC_{50}$ of ofloxacin was over $10{\mu}g/m{\ell}$ and $MIC_{50}$ of moxifloxacin was $5{\mu}g/m{\ell}$, $MIC_{90}$ of ofloxacin and moxifloxacin were all over $10{\mu}g/m{\ell}$. The rate of cross-resistance between the two was 67.6%(23/34) at $2.5{\mu}g/m{\ell}$ concentration. Conclusions : Moxifloxacin showed activity against 82.4%(28/34) of ofloxacin resistant M. tuberculosis at $10{\mu}g/m{\ell}$, but more studies are needed so that moxifloxacin will be used for patient with multi-drug resistant tuberculosis including oflokacin resistance.

• Tuberculosis and Respiratory Diseases
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• v.49 no.6
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• pp.740-751
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• 2000

Background : Moxifloxacin is a newly developed drug which is more potent and safe compared to previous fluoroquinolones. This drug effectively eradicates organisms such as beta-lactamase-producing or other resistant bacteria. Moxifloxacin is known to be effective in treating respiratory infections such as Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Chlamydia pneumoniaeme, Legionella spp. and Mycoplasma pneumoniae. Methods : In a multicenter, randomized, open, comparative study, the efficacy and safety of oral moxifloxacin taken 400 mg once a day and clarithromycin taken 500 mg twice daily for 7 days were compared for the treatment of Korean patients with acute exacerbations of chronic bronchitis. Results : A total of 170 patients were enrolled, and they were divided into two groups: 87 in the moxifloxacin group and 83 in the clarithromycin group. Of those enrolled, 76 (35 for bacteriologic efficacy) in the moxifloxacin group and 77 (31 for bacteriologic efficacy) in the clarithromycin group were included in the efficacy analysis. All were included in the safety analysis. Clinical success was noted in 70 (92.1%) of 76 moxifloxacin-treated patients and 71 (92.2%) of 77 clarithromycin-treated patients. Bacteriologic success rate seemed to be higher in moxifloxacin group (73.5%) than in clarithromycin group (54.8%), but statistically insignificant (p=0.098). Drug susceptibility among organisms initially isolated was higher in moxifloxacin group on Streptococcus pneumoniae, Pseudomonas aeruginosa, Klebsiella pneumoniae (p<0.001). Adverse events were reported by 12.8% of 86 patients receiving moxifloxacin and 21.7% of 83 patients receiving clarithromycin. Headache (4.7% vs 4.8%, moxifloxacin group vs clarithromycin group, respectively) and indigestion (2.3% vs 6.0%, moxifloxacin group vs clarithromycin group, respectively) were the most frequent side effects in the two groups. Conclusion : This study demonstrated that for the treatment of acute exacerbations of chronic bronchitis a 7-day course of moxifloxacin 400 mg od was clinically equivalent and microbiologically superior to clarithromycin 500 mg bid.

• Tuberculosis and Respiratory Diseases
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• v.71 no.2
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• pp.97-105
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• 2011

Background: It was hypothesized that the immunomodulating effects of moxifloxacin contribute to ameliorate oleic acid (OA)-induced acute lung injury (ALI) by suppression of cytosolic phospholipase A2 (cPLA2). This was based on observations from experiments on rats associated with neutrophilic respiratory burst, cPLA2 activity, and expressions of cPLA2, $TNF{\alpha}$, and COX-II in the lung. Methods: ALI was induced by intravenous injection of OA in male Sprague-Dawley rats. Five hours after OA injection, protein content in bronchoalveolar lavage (BAL), lung myeloperoxidase (MPO) activity, and numbers of BAL neutrophils were measured. As an index of oxidative stress-induced lung injury, the content of malondialdehyde (MDA) in lung tissues was also determined. Lung histology, immunohistochemistry and determination of activity of cPLA2 in lung tissues were carried out. In addition, Western blotting of $TNF{\alpha}$ and COX-II in lung tissues was performed. Results: The accumulation of neutrophils in the lungs was observed after OA injection. BAL protein was increased along with neutrophilic infiltration and migration by OA. Moxifloxacin decreased all of these parameters of ALI and ameliorated ALI histologically. The increased malondialdehyde (MDA) in the lung by OA was also decreased by moxifloxacin. Moxifloxacin not only suppressed cPLA2 expression in the lungs and neutrophils but also decreased cPLA2 activity in lung tissues of rats given OA. The enhanced expressions of $TNF{\alpha}$ and COX-2 in the lung tissues of rats given OA were also suppressed by moxifloxacin. Conclusion: Moxifloxacin inhibited cPLA2 and down-regulated $TNF{\alpha}$ and COX-2 in the lungs of rats given OA, which resulted in the attenuation of inflammatory lung injury.

• Journal of Life Science
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• v.21 no.8
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• pp.1100-1108
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• 2011

The immunomodulating effects of moxifloxacin seem to be effective in downregulating inflammatory reactions. This presumed effect was tested in endotoxin (ETX)-induced acute lung injury (ALI) in rats. After moxifloxacin treatment (10 mg/kg) of ETX-given rats, lung myeloperoxidase (MPO) activity, bronchoalveolar-lavage (BAL) protein, and the number of neutrophils in the BAL cells were measured. Light and electron microscopic structures were also examined. Electron microscopic $CeCl_3$ histochemistry for the detection of hydrogen peroxide in the lungs and immunohistochemistry of cytosolic phospholipase A2 (cPLA2) in the lung tissues and BAL cells were performed. To examine the expression of TNF${\alpha}$ in the lungs, western blotting was carried out with the lung tissues. ETX had accumulated neutrophils in the lungs, which was followed by lung leak. Oxidative stress occurred, and increased expression of cPLA2 in the lung tissues and BAL cells was observed in the ETX-given rats. Simultaneously, the expression of TNF${\alpha}$ was enhanced by ETX. Moxifloxacin, however, decreased all these parameters, indicating that ALI may have been ameliorated. Moxifloxacin appears to ameliorate ETX-induced ALI partially through the suppression of cPLA2 in the lungs of rats.

• Korean Journal of Clinical Pharmacy
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• v.21 no.4
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• pp.394-399
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• 2011

이 증례는 알코올 중독증을 앓은 병력을 가졌으나 간 기능에 특이한 증후가 없던 환자가, 지역 사회 획득성 폐렴으로부터 유발된 중증 패혈증 치료를 받기 위해서 linezolid, moxifloxacin 과 함께 aztreonam을 초회 정맥주사 맞은 후, 아주 높은 수치의 alanine aminotransferase (ALT), aspartate aminotransferase (AST) 혈중 농도가 검출된 경우이다. 후속 치료에서 상기 3가지 항생제 대신 vancomycin과 ceftazidime을 주사했더니, ALT/AST가 빠르게 정상화됨이 관찰되었다. 이 증례 보고는 linzolid, moxifloxacin과 aztreonam을 함께 사용할 경우, 각별한 주의 관찰이 필요하며, 알코올 중독증을 앓은 병력을 가진 환자에게 투여 시 특별한 주의와 함께 AST/ALT혈중 수치를 검사토록 권하기 위한 것이다.

• The Korean Journal of Physiology and Pharmacology
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• v.19 no.2
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• pp.99-104
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• 2015

The aim of this study is to develop a physiologically based pharmacokinetic (PBPK) model in intra-abdominal infected rats, and extrapolate it to human to predict moxifloxacin pharmacokinetics profiles in various tissues in intra-abdominal infected human. 12 male rats with intra- abdominal infections, induced by Escherichia coli, received a single dose of 40 mg/kg body weight of moxifloxacin. Blood plasma was collected at 5, 10, 20, 30, 60, 120, 240, 480, 1440 min after drug injection. A PBPK model was developed in rats and extrapolated to human using GastroPlus software. The predictions were assessed by comparing predictions and observations. In the plasma concentration versus time profile of moxifloxcinin rats, $C_{max}$ was $11.151{\mu}g/mL$ at 5 min after the intravenous injection and $t_{1/2}$ was 2.936 h. Plasma concentration and kinetics in human were predicted and compared with observed datas. Moxifloxacin penetrated and accumulated with high concentrations in redmarrow, lung, skin, heart, liver, kidney, spleen, muscle tissues in human with intra-abdominal infection. The predicted tissue to plasma concentration ratios in abdominal viscera were between 1.1 and 2.2. When rat plasma concentrations were known, extrapolation of a PBPK model was a method to predict drug pharmacokinetics and penetration in human. Moxifloxacin has a good penetration into liver, kidney, spleen, as well as other tissues in intra-abdominal infected human. Close monitoring are necessary when using moxifloxacin due to its high concentration distribution. This pathological model extrapolation may provide reference to the PK/PD study of antibacterial agents.

• Korean Journal of Clinical Pharmacy
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• v.15 no.2
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• pp.75-81
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• 2005

Community acquired pneumonia (CAP) remains a prevalent and potentially life threatening illness. American Thoracic Society and Infectious Disease Society America recommend combination therapies with ${\beta}-lactam$ plus a macrolide or a fluoroquinolone monotherapy for the empirical treatment of CAP. The aim of this study was to compare moxifloxacin monotherapy with cephalosporin plus azithromycin combination therapies. From January 2004 to March 2005, 18 patients in the moxifloxacin group(MG) and 21 patients in the cefuroxime or ceftriaxone plus azithromycin group(CAG) with CAP were retrospectively reviewed with regard to clinical, laboratory and microbiological data. Each patient was stratified into mild (risk class I-II), moderate (risk class III) and severe (risk class VI, V) group according to and PSI (Pneumonia Severity Index) score. Each group was compared for microbiological eradication, clinical assessment, the length of hospital stay. As results, Total 39 patients with CAP were reviewed. The appropriateness of admission was 83.3% in MC vs. 76.2% in CAC. The mean length of the hospital day was for 8.31 days vs. 7.39 days, days switching parenteral to oral antibiotics in 5.19 days vs. 5.28 days, clinical improvement in 2.43 days vs. 2.61 days in MG vs. CAC. Radiological improvement required 3.75 days vs 3.63 days in MG vs. CAG and bacteriological eradication rate at discharge was the same in the both groups. Mortality rate was 11.1% (2 of 18) vs 14.3% (3 of 21) in MG vs. CAG (p=0.77). Drug cost of the mean 5 hospital days requiring parenteral antibiotics was the most inexpensive in moxifloxacin group for the 147,045 won, and ceftriaxone 1g-azithromycin group for the 170,285 won, cefuroxime bid-azithromycin group for the 207,800 won, ceftriaxone 2g-azithromycin group far the 220,570 won, cefuroxime tid-azithromycin group for the 251,700 won. There was no significant statistical difference in clinical, bacterial, radiological cure and hospital days, and switch to oral days. In conclusion, that i.v. moxifloxacin monotherapy was as effective as azithromycin plus cefuroxime or ceftriaxone combination therapies fur the treatment of CAP. In drug cost analysis, moxifloxacin is less expensive than CAG.

• Korean Journal of Clinical Pharmacy
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• v.22 no.1
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• pp.55-64
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• 2012

The quinolones are broad-spectrum antibiotics and enhanced antimicrobial activity has extended the use of the quinolones beyond the traditional indications for quinolone antibiotics in the treatment of urinary tract infections. The quinolones are effective in a wider variety of infectious diseases, including skin and respiratory infections. Because of their excellent safety and tolerability, they have become popular alternatives to penicillin and cephalosporin derivatives in the treatment of various infections. A retrospective study was performed to evaluate efficacy and safety of IV quinolones for inpatient use. Total 117 patients who administerd quinolones for longer than 3 continuous days at community hospital from October 1st, 2008 to December 31st, 2008 were reviewed. The criterias for drug evaluation were included the validation of indication, outcome, dosage and side effects. In the results, ciprofloxacin 13 (total 93), levofloxacin 3 (total 59) and moxifloxacin 2 (total 19) cases were not met the criterias based on the culture results. Major indications were pneumonia (ciprofloxacin 16.3%, levofloxacin 67.8%, moxifloxacin 84.2%), urinary tract infection (ciprofloxacin 44.1%), skin infection (ciprofloxacin 7.5%, levofloxacin 20.3%, moxifloxacin 10.5%), intra-abdominal infection (ciprofloxacin 10.8%, moxifloxacin 5.3%), etc.. In the results of quinolone monotherapy, the frequencies were each ciprofloxacin 74.2%, levofloxacin 50.8% and moxifloxacin 47.4%. In the results of dosage validation, the validities were each ciprofloxacin 54.8%, levofloxacin 94.9% and moxifloxacin 100.0%. In the results of duration validation, the validities were each ciprofloxacin 59.1%, levofloxacin 78.0% and moxifloxacin 89.5%. Adverse drug reactions were reported for total 49 cases and those were gastrointestinal tract effects including nausea, vomiting, diarrhea and central nervous system effects including headache, dizziness. In summary, the quinolones appropriately used for hospitalized patients based on this study. A focused approach emphasizing "correct use of quinolones" may reduce development of antimicrobial resistance and maximize class efficacy. Consequently, correct use of antibiotics will contribute to decrease medical expenses for person and community.

• Tuberculosis and Respiratory Diseases
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• v.69 no.4
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• pp.256-264
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• 2010

Background: According to the notion of the immunoregulatory functions of moxifloxacin (MFX), the effect of MFX on the neutrophilic respiratory burst in conjunction with the expression of cytosolic phospholipase $A_2$ ($cPLA_2$) was investigated. Methods: The effects and possible mechanisms of MFX on neutrophilic respiratory burst in oleic acid (OA)-induced acutely injured rats lung and OA-stimulated, isolated murine neutrophils were probed, associated with the expression of cytosolic phospholipase $A_2$ in vivo and in vitro. Results: In the OA-induced acutely-injured lungs, neutrophils were accumulated, which was attenuated by MFX. The parameters denoting a neutrophilic respiratory burst, such as nitro blue tetrazolium reaction, cytochrome-c reduction, neutrophil aggregation, $H_2O_2$ production in neutrophils revealed increased neutrophilic respiratory burst by OA, and MFX decreased all of these parameters. In addition, the enhanced expression of $cPLA_2$ in the lung and isolated murine neutrophils by OA were decreased by MFX. Conclusion: MFX suppresses the OA-induced neutrophilic respiratory burst by the suppression of $cPLA_2$ in neutrophils.