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Jinghua Wang, Haiyang Xu, Dunwei Wang, Mingxian Li
OBJECTIVE: A large number of population in both developing and developed countries are affected by bronchitis, among all the factors, bacterial infection was considered as a critical cause of acute exacerbations of chronic bronchitis. Although several anti-bacterial agents were proved to have the effect of alleviating bronchitis, their relative efficacies and potential side effects remained not clear. We are keen to compare the pathogen eradication rate and safety of anti-bacterial agents for bronchitis...
February 23, 2017: Journal of Cellular Biochemistry
Hee-Soo Park, Sang-Hun Oh, Hye-Shin Kim, Dong-Rack Choi, Jin-Hwan Kwak
Zabofloxacin is a novel fluoroquinolone agent that has potent activity against gram-positive pathogens. In this study, we confirmed that zabofloxacin showed the most potent in vitro and in vivo activities against drug-resistant Streptococcus pneumoniae. Among the fluoroquinolone compounds, zabofloxacin showed the most potent in vitro activity against clinical isolates of penicillin-sensitive S. pneumoniae (minimum inhibitory concentration, MIC90: 0.03 mg/L) and penicillin-resistant S. pneumoniae (MIC90: 0.03 mg/L)...
November 17, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Muhammad Ashfaq, Khujasta Nawaz Khan, Muhammad Saif Ur Rehman, Ghulam Mustafa, Muhammad Faizan Nazar, Qian Sun, Javed Iqbal, Sikandar I Mulla, Chang-Ping Yu
The pharmaceutical industry of Pakistan is growing with an annual growth rate of 10%. Besides this growth, this industry is not complying with environmental standards, and discharging its effluent into domestic wastewater network. Only limited information is available about the occurrence of pharmaceutical compounds (PCs) in the environmental matrices of Pakistan that has motivated us to aim at the occurrence and ecological risk assessment of 11 PCs of different therapeutic classes in the wastewater of pharmaceutical industry and in its receiving environmental matrices such as sludge, solid waste and soil samples near the pharmaceutical formulation units along Shiekhupura road, Lahore, Pakistan...
February 2017: Ecotoxicology and Environmental Safety
Muhammad Umair, Aqeel Javeed, Aamir Ghafoor, Muhammad Ashraf
OBJECTIVES: Gemifloxacin is a broad spectrum antibiotic and has shown excellent coverage against a wide variety of microorganisms. In this study, an attempt was made to evaluate the immunomodulatory potential of gemifloxacin in male swiss albino mice in vivo. MATERIALS AND METHODS: Three doses of gemifloxacin 25 mg/kg, 50 mg/kg and 75 mg/kg were used intraperitoneally (IP) for the evaluation of immune responses in mice. Delayed type hypersensitivity (DTH), heamagglutination assay, jerne hemolytic plaque formation assay and cyclophosphamide induced neutropenia assay were performed to evaluate the effect of gemifloxacin on immune responses...
September 2016: Iranian Journal of Basic Medical Sciences
Laleh Mahmoudi, Shohreh Farshad, Mehrdad Seddigh, Paria Mahmoudi, Fardad Ejtehadi, Ramin Niknam
BACKGROUND: Helicobacter pylori (H pylori) is a common gastric pathogen which is associated with chronic gastritis, peptic ulcer, and gastric cancer. It has worldwide distribution with higher incidence in developing countries. Gemifloxacin is a fluoroquinolone antibiotic with documented in vitro activity against H pylori. Considering that there is no clinical data to verify gemifloxacin efficacy in H pylori eradication, this pilot clinical trial was designed. METHODS: This prospective pilot study was performed during February 2014 to February 2015...
October 2016: Medicine (Baltimore)
Meltem Erdem, Ceyhun Küçük, Ender Büyükgüzel, Kemal Büyükgüzel
Gemifloxacin mesylate (GEM) is a synthetic, fourth-generation fluoroquinolone antibacterial antibiotic that has a broad spectrum of activity against bacteria. GEM inhibits DNA synthesis by inhibiting DNA gyrase and topoisomerase IV activities. Recent research into insect nutrition and mass-rearing programs, in which antibiotics are incorporated into the culture media to maintain diet quality, raised a question of whether clinical antibiotics influence the health or biological performance of the insects that ingest these compounds...
December 2016: Archives of Insect Biochemistry and Physiology
Andreana Marino, Anna Rita Blanco, Giovanna Ginestra, Antonia Nostro, Giuseppe Bisignano
In recent years, the emergence of methicillin-resistant Staphylococcus aureus (MRSA) strains has been observed in ocular infections. Resistance of MRSA to second- and third-generation fluoroquinolones has increased interest in the fourth-generation fluoroquinolones. In this study, the antibacterial activity of gemifloxacin against MRSA ocular isolates in vitro and in a modified ex vivo rabbit keratitis model was investigated. In vitro susceptibility test results indicated that the minimum inhibitory concentrations (MICs) of gemifloxacin were lower than the MICs of other fluoroquinolones, including moxifloxacin (MIC50 range, 0...
October 2016: International Journal of Antimicrobial Agents
Muhammad Ashfaq, Khujasta Nawaz Khan, Sana Rasool, Ghulam Mustafa, Muhammad Saif-Ur-Rehman, Muhammad Faizan Nazar, Qian Sun, Chang-Ping Yu
In the present study, wastewater and sludge samples of two major hospitals of Lahore, Pakistan were analyzed by developing an HPLC-UV method for the possible occurrence of five frequently used fluoroquinolone antibiotics i.e. ofloxacin, ciprofloxacin, sparfloxacin, moxifloxacin and gemifloxacin. The highest detected concentration was for moxifloxacin in both wastewater (224 μg/L) and sludge samples (219 μg/kg. The highest concentration of ofloxacin, ciprofloxacin, sparfloxacin and gemifloxacin were found to be 66, 18, 58 and 0...
March 2016: Environmental Toxicology and Pharmacology
Rasha M Arabyat, Dennis W Raisch, June M McKoy, Charles L Bennett
OBJECTIVE: To review and summarize reports of tendon rupture associated with each fluoroquinolone (FQ) currently marketed in the United States (US), as reported to the FDA's Adverse Event Reporting System (FAERS). METHODS: FAERS data were reviewed for reports of tendon rupture associated with each FQ from their respective approval date through September 2012. Disproportional reporting signal detection was estimated using empirical Bayes geometric mean (EBGM) with 95% confidence intervals (CI)...
2015: Expert Opinion on Drug Safety
Clésio Soldateli Paim, Fernanda Führ, Magda Targa Martins, Simone Gnoatto, Lisiane Bajerski, Cássia Virginia Garcia, Martin Steppe, Elfrides Eva Scherman Schapoval
Gemifloxacin mesylate (GFM), chemically (R,S)-7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid methanesulfonate, is a synthetic broad-spectrum antibacterial agent. Although many papers have been published in the literature describing the stability of fluorquinolones, little is known about the degradation products of GFM. Forced degradation studies of GFM were performed using radiation (UV-A), acid (1 mol L(-1) HCl) and alkaline conditions (0...
March 2016: Biomedical Chromatography: BMC
Nuha Fathi Ali Dsugi, Abdalla A Elbashir, Fakhr Eldin Osman Suliman
The solid inclusion complex of gemifloxacin (GFX) and hydroxyl propyl β-cyclodextrin (HPβ-CD) was prepared and examined by UV-visible, FTIR, NMR, electrospray ionization mass spectrometry (ESI-MS) and fluorescence spectroscopy. The formation of inclusion complex has been confirmed on the basis of changes of spectroscopic properties. Further the interaction between GFX and HPβ-CD was studied using molecular modeling approaches. The results showed that HPβCD reacted with GFX to form a 1:1 host-guest inclusion complex...
2015: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Mohsen Masoodi, Mahshid Talebi-Taher, Khadijeh Tabatabaie, Siamak Khaleghi, Amir-Hossein Faghihi, Shahram Agah, Reyhaneh Asadi
BACKGROUND Eradication of Helicobacter pylori infection plays a crucial role in the treatment of peptic ulcer. Clarithromycin resistance is a major cause of treatment failure. This randomized clinical trial aimed at evaluating the efficacy of a clarithromycin versus gemifloxacin containing quadruple therapy regimen in eradication of H.pylori infection. METHODS In this randomized double blind clinical trial (RCT 2012102011054N2), a total of 120 patients were randomized to two groups of 60 patients each. Patients with proven H...
April 2015: Middle East Journal of Digestive Diseases
Olcay Sagirli, Seda Demirci, Armağan Önal
A high-performance liquid chromatographic method with fluorescence detection was developed and validated for the determination of gemifloxacin in human breast milk. The proposed method allows the determination of gemifloxacin in breast milk samples without complex sample preparation. The samples were mixed with a mobile phase and filtered with a 0.45 µm polytetrafluoroethylene filter before analysis. Chromatographic separation was carried out on a C18 column (150 × 4.6 mm, 5 µm I.D.) using methanol:50 mM ortho-phosphoric acid solution (40:60) as the mobile phase with a 1...
December 2015: Luminescence: the Journal of Biological and Chemical Luminescence
J M Blondeau, S D Shebelski, C K Hesje
Streptococcus pneumoniae continues to be a significant respiratory pathogen, and increasing antimicrobial resistance compromises the use of β-lactam and macrolide antibiotics. Bacterial eradication impacts clinical outcome, and bacterial loads at the site of infection may fluctuate. Killing of two macrolide- and quinolone-susceptible clinical S. pneumoniae isolates by azithromycin, clarithromycin, erythromycin, telithromycin and gemifloxacin against varying bacterial densities was determined using the measured minimum inhibitory concentration (MIC) and mutant prevention concentration (MPC)...
June 2015: International Journal of Antimicrobial Agents
Yulie Xu, Yancheng Liu, Jianfeng Zhao, Haixia Li, Peng Zhang, Wenfeng Wang
The photochemical properties of gemifloxacin (GEFX), a fluoroquinolone antibacterial drug that exhibits phototoxicity toward biological substrates, were studied in aqueous solutions by laser flash photolysis (LFP) and pulse radiolysis. GEFX triplet state ((3)GEFX(∗)) absorption spectra showed maximum absorption at 510nm. (3)GEFX(∗) was quenched by naproxen (NAP) via energy transfer with a rate constant of 1.2×10(8)dm(3)mol(-1)s(-1). The energy of (3)GEFX(∗) was 266kJmol(-1) and the transient absorption spectra showed direct evidence of electron transfer from 2'-deoxyguanosine-5'-monophosphate, N,N,N',N'-tetramethyl-p-phenylenediamine, and tryptophan to (3)GEFX(∗) with bimolecular reaction rate constants of 4...
February 2015: Journal of Photochemistry and Photobiology. B, Biology
Daichi Kazamori, Hiroshi Aoi, Kaori Sugimoto, Taichi Ueshima, Hirotaka Amano, Kenji Itoh, Yasuhiro Kuramoto, Akira Yazaki
The aim of this study was to examine the in vitro antibacterial activity of WQ-3810, a new fluoroquinolone, against clinically relevant pathogens such as Acinetobacter baumannii, Escherichia coli and Streptococcus pneumoniae, including multidrug-resistant (MDR) and fluoroquinolone-resistant (FQR) isolates, compared with those of ciprofloxacin, levofloxacin, moxifloxacin and gemifloxacin. WQ-3810 demonstrated the most potent activity against the antimicrobial-resistant pathogens tested. Against A. baumannii, including MDR isolates, the potency of WQ-3810 [minimum inhibitory concentration for 90% of the organisms (MIC(90))=1 mg/L] was more than eight-fold higher than that of ciprofloxacin (64 mg/L) and levofloxacin (8 mg/L)...
November 2014: International Journal of Antimicrobial Agents
Syed Saeedul Hassan, Uzma Hayat, Imran Tariq, Irshad Ahmad, Muhammad Munawar Hayat, Muhammad Uzair, Muhammad Tayyab Ansari
A spectrophotometric method for the determination of Gemifloxacin mesylate (GFX) is developed and validated according to ICH guidelines. GFX is a fluoroquinolone that is used in the treatment of pneumonia. The analysis of the pure drug was carried out at its λmax 270 nm. The method was linear from 0.5-5μg/mL, r(2) 0.999 and equation is 0.102-0.000. The % RSD for inter-day (0.969%) and intra-day (0.714%) assuring a good precision and accuracy was close to 100%. Limit of detection and Limit of quantification were 0...
September 2014: Pakistan Journal of Pharmaceutical Sciences
Ju-Young Shin, Mi Hee Kim, Sun Mi Shin, Shin Haeng Lee, Byung-Joo Park
PURPOSE: This study was performed to evaluate the change of prescribing patterns after the regulatory action regarding fluoroquinolones in pediatric patients. METHODS: We conducted a time series analysis using the Korea Health Insurance Review and Assessment Service National Patients Sample database. Study subjects consisted of pediatric patients under 18 years of age who were prescribed antibiotics at least once (ATC code, J01) before (January 2009-December 2009) and after implementation (January 2010-December 2011) of the regulation...
December 2014: Pharmacoepidemiology and Drug Safety
W M El-Koussi, N N Atia, A M Mahmoud, S R El-Shabouri
Novel, simple and sensitive high performance thin-layer chromatography (HPTLC) with fluorescence detection has been successfully developed and validated for determination of gemifloxacin mesylate (GFX) in plasma samples without prior pretreatment. Montelukast (MK) was used as internal standard. GFX and MK in plasma samples were separated using a mobile phase consisting of a mixture of ethyl acetate:methanol:25% ammonia, (8:4.5:3, v/v/v). The emission intensity was measured using optical filter K400 after excitation at 342 nm...
September 15, 2014: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Robert D Kirkcaldy, Hillard S Weinstock, Page C Moore, Susan S Philip, Harold C Wiesenfeld, John R Papp, Peter R Kerndt, Shacondra Johnson, Khalil G Ghanem, Edward W Hook
BACKGROUND: Ceftriaxone is the foundation of currently recommended gonorrhea treatment. There is an urgent need for backup treatment options for patients with cephalosporin allergy or infections due to suspected cephalosporin-resistant Neisseria gonorrhoeae. We evaluated the efficacy and tolerability of 2 combinations of existing noncephalosporin antimicrobials for treatment of patients with urogenital gonorrhea. METHODS: We conducted a randomized, multisite, open-label, noncomparative trial in 5 outpatient sexually transmitted disease clinic sites in Alabama, California, Maryland, and Pennsylvania...
October 15, 2014: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
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